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Abstract
Since the middle of this century and especially since the 1960s and 1970s. Chinese scientists have put considerable effort and resources into the search for new antimalarial compounds extracted from Chinese traditional herbs. Archaeological findings indicate that qinghao (Artemisia annua L.) has been used as a traditional remedy in China for over two thousand years. Its antimalarial principle was finally isolated in 1971 and named artemisinin or qinghaosu (meaning the principle of qinghao in Chinese). Its rapid action, low toxicity and powerful effect against falciparum malaria made it a favored subject for research. In 1976, the unique structure of the molecule, characterized by an endoperoxide and an alternative O-C-O-C segment, was identified. The specific lactone reduction discovered during the determination of the structure opened the way for the synthesis of qinghaosu derivatives, and thereafter a series of more active and more oil- or water-soluble derivatives was developed. Subsequent studies of the structure/activity relationship led to the discovery of dihydroartemisinin, artemether and artesunate. Now qinghaosu and these three derivatives are being used around the world as effective new antimalarial drugs in the fight against falciparum malaria, including multi-drug-resistant Plasmodium falciparum. At the present time new qinghaosu analogues or derivatives are being developed and studies of their structure/activity relationships, their antimalarial mechanisms, their interaction with ferrous ions and the DNA damage associated with these processes are being actively pursued. In addition, recent studies also indicate that some qinghaosu derivatives have other bioactivities, including antiparasitic (against Schistosoma japonicum, Toxoplasma gondii and so on) and anticancer activities. Research into qinghaosu and its derivatives has already produced and will no doubt continue to produce results of the utmost importance in the fight against malaria and other diseases.
... Les médicaments incriminés sont multiples comme les anesthésiants, les anti-inflammatoires non stéroïdiens (AINS), les neuroleptiques, la buprénorphine, le chloroforme, le piroxicam et le paracétamol dans un contexte d'éthylisme chronique [5]. L'artemether est un dérivé de l'artémisinine utilisé dans le traitement curatif du paludisme à Plasmodium falciparum [6][7][8][9]. Son métabolisme est essentiellement hépatique et son élimination est urinaire [7,10]. En cas de paludisme simple avec des vomissements, il est administré par voie intramusculaire à raison de 3,2 mg/kg le 1 er jour, 1,6 mg/kg du 2 e au 5 e jour, soit pour un adulte de 50 kg, une dose totale de 480 mg repartie en 5 jours [8]. ...
... L'artemether est un dérivé de l'artémisinine utilisé dans le traitement curatif du paludisme à Plasmodium falciparum [6][7][8][9]. Son métabolisme est essentiellement hépatique et son élimination est urinaire [7,10]. En cas de paludisme simple avec des vomissements, il est administré par voie intramusculaire à raison de 3,2 mg/kg le 1 er jour, 1,6 mg/kg du 2 e au 5 e jour, soit pour un adulte de 50 kg, une dose totale de 480 mg repartie en 5 jours [8]. ...
... En cas de paludisme simple avec des vomissements, il est administré par voie intramusculaire à raison de 3,2 mg/kg le 1 er jour, 1,6 mg/kg du 2 e au 5 e jour, soit pour un adulte de 50 kg, une dose totale de 480 mg repartie en 5 jours [8]. Lorsque l'artemether est administré selon les recommandations chez un adulte sans antécédents particuliers, aucune toxicité hépatique ni rénale n'a été rapportée [5][6][7][8]. Par contre, l'hépatotoxicité de la combinaison artésunate-amodiaquine en association avec l'éfavirenz a été documentée chez les personnes vivant avec le VIH (PV-VIH) et serait peut-être due à l'inhibition du métabolisme de l'amodiaquine CYP2C8 médiée par l'éfavirenz [1]. Il n'existe aucun cas rapporté de toxicité hépatorénale liée à l'utilisation de l'artemether. ...
We report on a case of acute hepatonephritisthat occurred during a treatment with artemether in a patient with HIV and hepatitis B. The patient suffered from cholestatic and cytolytic jaundice associated with oliguric acute renal failure after the intramuscular administration of a cumulative dose of 480 mg of artemether in 72 hours. The patient was successfullytreated with hemodialysis. We wish to draw the attention of physicians regarding the conditions of artemether drug use under special clinical situations.
... Результаты. В процессе исследования надземной части полыни в 1972 году был идентифицирован сесквитерпеновый лактон -артемизинин (1) (huanghuahaosu или ошибочно -qinghaosu) -источник противомалярийной активности полыни однолетней [1,2]. ...
... Results. While studying the aboveground of Artemisia annua in 1972 sesquiterpene lactone of artemisinin (1) was identified (huanghuahaosu or wrong -qinghaosu) -the source of anti-malaria activity of Artemisia annua [1,2]. ...
... К Structure c was the most preferable at the certain stage of the researches because of the close peroxy lactones [5,6]. Real structure and relative configuration (2) were finally proved by x-ray crystal analysis, and absolute configuration was obtained with abnormal diffraction x-ray crystal analysis [7]. ...
Artemisia annua is an herblike annual plant which has been used in Chinese folk medicine for more than 2,000 years. In 1970-s sesquiterpene lactones of artemisinin was isolated from the aboveground part of this plant. Today it is the most efficient known natural and synthetic compound for malaria treatment.The purpose of the study was the review of the information from the open sources about the study for sesquiterpene lactones of Artemisia annua referring to its pharmacological activity.Methods. The study was carried out using informational and search engines (PubMed, ScholarGoogle), library databases (eLibrary, Cyberleninca), and the results of our own researches.Results. It was established that apart from the essential oil and phenolic compounds, aboveground part of Artemisia annua, it contains a significant amount of sesquiterpene lactones. Qualitative content and quantitative composition of sesquiterpene lactones varies depending on the ecological and geographic factors, plants growing phase, cultivation technology, drying methods etc. Well-known pharmacological studies of the extracts from Artemisia annua herb with sesquiterpene lactones, as well as individual compounds of this group characterize this type of raw materials as a perspective source for more profound research.Conclusion. Our analysis of the open materials on the sesquiterpene lactones of Artemisia annua, including phytochemical and pharmacological ones, allows characterization of the Artemisia annua herb as a perspective source for new drugs working out.
... Artemether (ART), C 16 H 26 O 5, molecular weight 298 g/mol, is a safe, stable, lipid-soluble compound, which has shown higher antimalarial activity when compared to other artemisinin derivatives. 5 Current marketed oral formulations include tablet and dispersible formulations, which have similar pharmacokinetic properties. 6 For the treatment of uncomplicated malaria caused by P falciparum, ART in combination with LUM improved efficacy, with the dose of each drug depending on the patient's weight. ...
... ART is a semisynthetic derivative of a sesquiterpene, known as artemisinin. 3,5,6 Terpenes act as permeation enhancers that encourage the diffusion of compounds across the skin because of their structural characteristics. [58][59][60] The terpenes are classified as monoterpenes (C 10 ), which contain 2 units of isoprene, sesquiterpenes (C 15 ), which contain 3 units of isoprene, and diterpenes (C 20 ), which contain 4 units of isoprene. ...
According to the most recent World Health Organization statistics, malaria infected approximately 219 million people in 2017, with an estimate of 435,000 deaths (World Health Organization, 2018). Communities isolated from cities are the most deprived of access to the necessary hospital facilities. Herein we report the development of a transdermal bioadhesive containing artemether (ART), an alternative, potentially lifesaving, treatment regimen for malaria in low-resource settings. Bioadhesives were prepared from an aqueous blend of hydroxyethylcellulose (4.5% w/w), ART, propoxylated-ethoxylated-cetyl-alcohol, polysorbate 80, propyleneglycol, glycerine, mineral oil, and oleic acid. In this study, the average pore size of bioadhesive 5.5b was 52.6 ± 15.31 μm. Differential scanning calorimetry and thermogravimetric analyses confirm the thermal stability of ART bioadhesives at room temperature. Tensile tests indicated good mechanical properties for bioadhesive 5.5b, when compared to 5.5a, where 5.5b showed elastic modulus 0.19 MPa, elongation at break 204%, tensile stress 0.31 MPa, tensile strength at break 0.23 MPa. Bioadhesion assays suggested that formulations containing surfactants had higher detachment forces. Permeation studies demonstrated that the best outcome was achieved with a bioadhesive containing 25 mg ART (5.5b) that after 24 h released 6971 ± 125 μg, which represents approximately 28% of drug permeation. Data reported presents a promising candidate for a new antimalarial transdermal formulation.
... Полынь однолетняя получила широкую известность благодаря выделению из её надземной части сесквитерпенового лактона -артемизинина -наиболее активного среди всех природных и синтетических противомалярийных соединений [4,5]. 5 октября 2015 года китаянка Юю Ту получила Нобелевскую премию по медицине за открытие лекарства от малярии, ежегодно убивающей 400-500 ...
... Artemisia annua gained wide popularity owing to the secretion of a sesquiterpenic lactone artemisinin from its aboveground part. It is the most active substance among all natural and synthetic antimalarial compounds [4,5]. ...
Artemisia annua is a herblike annual plant which has been used in Chinese folk medicine for more than 2,000 years. In 1970-s sesquiterpenic lactone of artemisinin was isolated from the above-ground part of this plant. Today it is the most efficient known natural and synthetic compound for malaria treatment. The purpose of the study was to review the data from the open sources about a component composition of Artemisia annua essential oil in the spectrum of its pharmacological activity. Methods. The study was carried out using information and searching sources (PubMed, ScholarGoogle), library data bases (eLibrary, Cyberleninca), as well as the results of our studies. Results. We have established that aboveground part of Artemisia annua have a significant amount of essential oil apart from the sesquiterpene lactones. Essential oil contains more than 120 components, which belong to different classes of natural compounds. The study for dynamics of the essential oil accumulation in the Artemisia annua herb showed that the amount of oil in the herb rises significantly during budding, reaching maximum value in blossom. Qualitative composition and quantitative content of certain components varies depending on ecological and geographical factors, plant growing phase, cultivation technology, drying methods etc. Well-known pharmacological studies of essential oil of the Artemisia annua characterize it as a prospective source for the development of new antimicrobial medicinal drugs. Besides, as the studies shown, it can be related to the 6 class according to K. Sidorov’s classification – “relatively non-hazardous substances”. Conclusion. The analysis of the open sources on the study of essential oil of Artemisia annua made by us, as well as the results of our own studies, including phytochemical studies allow characterizing the essential oil of Artemisia annua as a prospective source for the working out of new antimicrobial drugs.
... Other medicines, including spiramycin, azithromycin, trimethoprim plus sulfamethoxazole (TMP-SMX), are also commonly used. Traditional Chinese medicine (TCM) formulae containing herbs Astragalus membranaceus, Scutellaria baicalensis, Artemisia annua, Ginkgo biloba etc are also used in the treatment of T. gondii infections [8][9][10]. Spiramycin has minimal foetal toxicity and can be effectively absorbed after oral administration, spreading quickly to tissues to kill the tachyzoites and reduce the parasite or prevent the parasite from spreading through the placenta to the foetus [11]. ...
... Artemisia annua was shown to reduce the number or density of T. gondii tachyzoites in host cells in vitro and in vivo [8,26,27]. Other herbs, including Phellodendron chinense, Hedyotis diffusa, rhizoma Anemarrhenae asphodeloides, radix Sophorae flavescentis, fructus Amomum tsaoko, radix Astragalus membranaceus, Semen arecae, cortex Moutan radicis Poria cocos, Glycyrrhiza uralensis, Rheum palmatum were reported to be able to kill T. gondii tachyzoites and tissue cyst bradyzoites in different combination in host cells and in mice [28][29][30][31][32][33][34]. ...
No effective drug and definitive "gold standard" treatment for Toxoplasma gondii (T. gondii) infection has been available so far, though some medicines have been commonly used in the treatment of T. gondii infection, such as spiramycin, azithromycin, traditional Chinese medicine (TCM), pyrimethamine- sulfadiazine (P-S), trimethoprim-sulfamethoxazole (TMP-SMX), and pyrimethamine-clindamycin (P-C). A systematic review and meta-analysis were performed to compare the efficacies of these conventional medicines in the treatment. Cohort studies for the treatment of acute T. gondii infection were searched from PubMed, Google Scholar, ect. All the cases number for different group extracted from each included literature were input to meta-analysis 3.13 software to calculate the pooled negative conversion rate (NCR), cure rate (CR) or vertical transmission rate based on their sample size and weight. The pooled NCR with 95% confidence intervals (CI) was used to evaluate the overall rate of a diagnosis positive result conversion to a negative result after treatment, which of spiramycin, azithromycin and TCM were 83.4% (95%CI, 72.1%-90.8%), 82.5% (95%CI, 75.9%-87.6%), and 85.5% (95%CI, 71.3%-93.3%) respectively, with no statistical difference between them. The pooled CR with 95% CI was used to evaluate the overall rate of complete disappearance of clinical symptoms for toxoplasmic encephalitis after therapy, which of P-S, TMP-SMX, and P-C were 49.8% (95%CI, 38. 8% -60.8%), 59.9% (95%CI, 48.9%-70.0%), and 47.6% (95%CI, 24.8%-71.4%) respectively, with no statistical difference between them. Primary T. gondii infection in pregnancy was treated mainly with spiramycin alone or combined with other drugs, and the pooled rate of vertical transmission was about 9.9% (95%CI, 5.9%-16.2%) after therapy. Toxoplasmic encephalitis in AIDS patients was usually treated with sulfonamides combined with other drugs and the pooled CR was 49.4% (95%CI, 37.9%-60.9%).
... Although progress has been made in metabolic engineering of artemisinin biosynthesis in A. annua L., more needs to be done in order to further increase artemisinin production to a level of practical application through metabolic regulation. Chinese authorities; DHA was approved in 1991 (Li and Wu, 1998). Their outstanding antimalarial efficacy has also been confirmed in clinical trials around the world. ...
Chronic inflammation is involved in many pathological conditions such as rheumatoid arthritis, atherosclerosis, type 2 diabetes, asthma, obesity, inflammatory bowel diseases, neurodegenerative diseases, and cancer. Currently, there is a demand for effective anti-inflammatory drugs with low toxicity and reduced side effects. In this context, A. annua appears to be a promising source of anti-inflammatory compounds, as numerous studies on different models of inflammation certify. Further research is needed in order to understand the underlying mechanism of action for each compound. The anti-inflammatory activity of extracts is also promising, considering the fact they have been demonstrated to be more efficient than isolated compounds, although they raise the problem of reproducibility and standardization. In addition, no clinical trials were yet undertaken to assert the anti-inflammatory effect of A. annua in the human body.
... At a dose level of 6.00 mg/kg artesunate, the 1.50 mg/kg folic acid administered could not bring down the serum iron concentration. The high dose of the drug might have destroyed the megaloblasts and the iron in them liberated into the peripheral blood circulation from where the iron shunt back into the serum and plasma thus increasing the iron level at the expense of tissues and organs, a condition referred to as megaloblastic anemia (Liy and Wu, 1998) . ...
The effects of oral administration of artesunate alone and with folic acid on the liver and on the serum levels of iron were assessed in eighty-one male wistar rats with a mean weight of 180 g (172-188 g). Thirty-six rats received artesunate of graded doses ; another thirty-six rats received a combination of artesunate and folic acid; while normal saline was administered to the remaining nine rats which served as the negative control group. Comparison of means of results was done with the student's t-test at a 95% level of significance. The results showed that in rats treated with 6.00 mg/kg of artesunate alone, there was a significant decrease in liver weight from 3.25±0.55 to 2.64±0.12g. Necrosis of the hepatocytes as revealed by liver histology also occurred. The serum iron level rose significantly from 784±11.49 mol/L to 1773±11.32 mol/L. It was also found that folic acid reversed metabolic and tissue disorder associated with lower doses of artesunate but offered partial relief to the same disorders associated with higher doses of the drug. This is evident by the decrease in serum iron and the the healthy cytoarchitecture of the liver .
... Several new editions and numerous translations of the Compendium have been made throughout the centuries. In modern times the herb qinghao has been used as an antimalarial in the countryside of Southeast China[8].During the wars in neighbouring Cambodia and Vietnam in the late 1960s, the Chinese Government began a systematic examination of plants used in traditional Chinese medicine with the aim of finding a new antimalarial agent. In 1971, the pharmacologist Tu Youyou from the Institute of Chinese Materia Medica, ...
Every year 880,000 people are killed by malaria, mostof them children in impoverished regions of the worldlacking adequate medical care. While many preventativemeasures, such as mosquito nets have decreased theincidence of malaria, once the disease is contracted,it must be treated. Many plasmodial species havedeveloped a frightening resistance to antimalarial agents,making the search for new, effective antimalarial agentsan urgent priority of global importance.
... Youyou Tu's own remarks [15] at the Fourth Meeting of the WHO Scientific Working Group on the Chemotherapy of Malaria, held in Beijing 1981, provided further details of the new drug. The landmark work carried out under her direction [21] constituted a break-through for malaria therapy and led to the development of artemisinin-based combination therapy (ACT) that has since revolutionized the care of malaria patients [22] eventually leading to Youyou Tu being awarded the Nobel prize in Medicine for 2015, together with Campbell and ¯ Omura for ivermectin [23,24]. However, the story does not end there since, amazingly, it was found that the artemisinin do not only affect the malaria parasites, but are also active against juvenile schistosomes, which was first shown by Chen et al. [25] at the end of the golden decade of antiparasitic drug discovery in the 1970s. ...
The stumbling block for the continued, single-drug use of praziquantel (PZQ) against schistosomiasis is less justified by the risk of drug resistance than by the fact that this drug is inactive against juvenal parasites, which will mature and start egg production after chemotherapy. Artemisinin derivatives, currently used against malaria in the form of artemisinin-based combination therapy (ACT), provide an opportunity as these drugs are not only active against malaria plasmodia, but surprisingly also against juvenile schistosomes. An artemisinin/PZQ combination would be complimentary, and potentially additive, as it would kill two schistosome life cycle stages and thus confer a transmission-blocking modality to current chemotherapy. We focus here on single versus combined regimens in endemic settings. Although the risk of artemisinin resistance, already emerging with respect to malaria therapy in Southeast Asia, prevents use in countries where ACT is needed for malaria care, an artemisinin-enforced praziquantel treatment (APT) should be acceptable in North Africa (including Egypt), the Middle East, China, and Brazil, as these countries are not endemic for malaria. Thanks to recent progress with respect to high-resolution diagnostics, based on circulating schistosome antigens in humans and molecular approaches for snail surveys, it should be possible to keep areas scheduled for schistosomiasis elimination under surveillance, bringing rapid response to bear on problems arising. The next steps would be to investigate where and for how long APT should be applied to make a lasting impact. A large-scale field trial in an area with modest transmission should tell how apt this approach is.
... Furthermore, it was also reported that the sensitivity to artemisinin action was related to the expression level of proapoptotic (Bax) and antiapoptotic (Bcl2) genes [112]. Also, artemisinin role in the inhibition of cancer is postulated to be associated with direct DNA damage [113] or indirectly in tumor cells involving a cascade of signaling pathways in many hallmarks of cancer [114]. Taken together, these results could explain the apoptotic pathway induction by artemisinin on tested cancer cells [101,102,115,116]. ...
... La información de los ensayos clínicos y la experiencia postautorización no indican que exista un aumento del riesgo de padecer neoplasias sólidas para la exposición a fármacos biológicos. El riesgo puede variar según el agente biológico y la patología (11,12). Los fármacos biológicos no presentan toxicidad acumulada que limite, según ficha técnica, su uso de forma continuada y a largo plazo. ...
... Furthermore, it was also reported that the sensitivity to artemisinin action was related to the expression level of proapoptotic (Bax) and antiapoptotic (Bcl2) genes [112]. Also, artemisinin role in the inhibition of cancer is postulated to be associated with direct DNA damage [113] or indirectly in tumor cells involving a cascade of signaling pathways in many hallmarks of cancer [114]. Taken together, these results could explain the apoptotic pathway induction by artemisinin on tested cancer cells [101,102,115,116]. ...
... Several new editions and numerous translations of the Compendium have been made throughout the centuries. In modern times the herb qinghao has been used as an antimalarial in the countryside of Southeast China[8].During the wars in neighbouring Cambodia and Vietnam in the late 1960s, the Chinese Government began a systematic examination of plants used in traditional Chinese medicine with the aim of finding a new antimalarial agent. In 1971, the pharmacologist Tu Youyou from the Institute of Chinese Materia Medica, ...
... Several new editions and numerous translations of the Compendium have been made throughout the centuries. In modern times the herb qinghao has been used as an antimalarial in the countryside of Southeast China[8].During the wars in neighbouring Cambodia and Vietnam in the late 1960s, the Chinese Government began a systematic examination of plants used in traditional Chinese medicine with the aim of finding a new antimalarial agent. In 1971, the pharmacologist Tu Youyou from the Institute of Chinese Materia Medica, ...
... Furthermore, it was also reported that the sensitivity to artemisinin action was related to the expression level of proapoptotic (Bax) and antiapoptotic (Bcl2) genes(Karnak & Xu, 2010). Also, artemisinin's role in the inhibition of cancer is postulated to be associated with direct DNA damage(Li & Wu, 1998) or indirectly in tumor cells involving a cascade of signaling pathways in many hallmarks of cancer(O'neill, Barton, & Ward, 2010). Moreover, artemisinin has been described to suppress proinflammatory cytokines such as TNF-α(Xu et al., 2007), inhibiting the activation of factor hypoxia-inducible factor 1α(He et al., 2011;Huang, Ma, Zhang, Lu, & Wei, 2007). ...
Artemisinin is one of the most widely prescribed drugs against malaria and has recently received increased attention because of its other potential biological effects. The aim of this review is to summarize recent discoveries of the pharmaceutical effects of artemisinin in basic science along with its mechanistic action, as well as the intriguing results of recent clinical studies, with a focus on its antitumor activity. Scientific evidence indicates that artemisinin exerts its biological activity by generating reactive oxygen species that damage the DNA, mitochondrial depolarization, and cell death. In the present article review, scientific evidence suggests that artemisinin is a potential therapeutic agent for various diseases. Thus, this review is expected to encourage interested scientists to conduct further preclinical and clinical studies to evaluate these biological activities.
... They are originated from the active ingredient of the Chinese herb named qinghao (Artemisia annua). This group of compounds, which are applied traditionally for treating fevers, has been increasingly used for treating this disease over the past decades [10][11][12]. Although inexpensive by international standards, artemisinin derivatives are significantly more expensive than traditional antimalarials such as chloroquine and sulphadoxine/pyrimethamine. ...
Malaria has been known as one of the major causes of morbidity and mortality on a large scale in tropical countries until now. In the past decades, many scientific groups have focused their attention on looking for ideal drugs to this disease. So far, this research area is still a hot topic. In the present study, the antimalarial activity of 1, 4- naphthoquinonyl derivatives was modeled by linear and nonlinear statistical methods, that is to say, by forward stepwise multilinear regression (MLR) and radial basis function neural networks (RBFNN). The derived QSAR models have been statistically validated both internally - by means of the Leave One Out (LOO) and Leave Many Out (LMO) crossvalidation, and Y-scrambling techniques, as well as externally (by means of an external test set). The statistical parameters provided by the MLR model were R2 =0.7876, LOOq2 =0.7068, RMS =0.3377, R0 2 =0.7876, k =1.0000 for the training set, and R2 =0.7648, q2 ext =0.7597, RMS=0.2556, R0 2=0.7598, k=1.0417 for the external test set. The RBFNN model gave the following statistical results, namely: R2=0.8338, LOOq2=0.5869, RMS=0.2781, R0 2 = 0.8335, k=1.0000 for the training set, and R2 =0.7586, q2 ext =0.7189, RMS=0.2788, R0 2=0.7129, k=1.0284 for the external test set. Overall, these results suggest that the QSAR MLR-based model is a simple, reliable, credible and fast tool for the prediction and virtual screening of 1, 4-naphoquinone derivatives with high antimalarial activity. In addition, the energies of the highest occupied molecular orbital were found to have high correlation with the activity.
... 87.7/min 117.8 mmHg 64.9 mmHg [60][61][62][63][64][65][66][67][68][69][70]17.0/min 15.0 78.4 cm [70][71][72][73][74][75][76][77][78][79][80][81][82][83][84]62.2 kg [51][52][53][54][55][56][57][58][59][60][61][62][63][64][65][66][67][68][69][70]168.1 cm [161][162][163][164][165][166][167][168][169][170][171][172][173][174][175]22.4 kg/m 2 [19.124.2] 37.3°C [36.5-38.0] ...
... The earliest documentation of such efforts can be evidenced in the form of mosquito nets that were used by the pharaohs and garlic as a mosquito repellent by the pyramid builders. The use of artemisinin compounds can be traced back to as early as the ancient Chinese civilizations, where Qing-hao (Artemisia annua) was being used to treat malarial fever (Hsu, 2006;Li and Wu, 1998). Till the middle ages, the treatment of malaria, commonly, had revolved around unscientific measures like bloodletting, induced vomiting, trepanning and sorcery. ...
One peek into the history of malaria, shows us that despite many attempts by mankind to counter the development and propagation of malaria, it has always risen back like a 'phoenix from its ashes'. This has been possible by virtue of the singular ability of the malarial parasite to mutate and evade the actions of various anti-malarial drugs. The emergence of drug resistant malarial parasites by virtue of the various molecular mechanisms, has put the authorities under the cosh and forced the scientists to start generating newer and better anti-malarial drugs. In this review, we have dwelt upon the various molecular mechanisms which have allowed the malaria parasite to develop resistance, as it can serve to educate the scientists in their effort to generate newer anti-malarials.
... This proves that the medicinal plants are a natural source of new antimalarials that still need to be explored. 3 Other herbs that are proven to have antimalarial activities are Nigella sativa 4 , Vernonia staehelinoides 5 , Acalypha fruticosa, Azadirachta indica and Dendrosicyos socotrana 6 , Arcangelisia flava, Fibraurea tinctoria, Harrisonia perforated, Irvingia malayana, Elaeocarpus kontumensis and Anneslea fragrans 7 , Andrographis paniculata, Hedyotis corymbosa8, Enicostemma littorale 9 and Quassia amara. 10 In Madagascar it is estimated that about 80% of the population is still dependent on traditional medicine, which essentially involves the use of plants. ...
Malaria is one of the three deadly dangerous infectious diseases and is successfully treated with medicinal plants in endemic regions. This work was carried out with the aim to investigate the phytochemical screening and antiplasmodial activities of Mundulea antanossarum seeds extract using two standardized parasites strains (Plasmodium falciparum FcM29-Cameroon and P. yoelii subsp nigeriensis) as model systems. The in vitro antiplasmodial activity of the plant extracts was evaluated by isotopic micro-test, while the in vivo anti-malarial activity was determined by the classical 4-day suppressive test. Qualitative chemical screening was carried out using standard methods of analysis. The ethanolic crude extract and Dichloromethane fraction of the seeds of Mundulea antanossarum showed interesting in vitro antiplasmodial activity against Plasmodium falciparum with the IC50 values of 1.08 ± 0.072 μg/mL and 0.215 ± 0.008 μg/mL respectively. The in vivo bioassay revealed also that ethanol and dichloromethane soluble extracts have interesting bioactivity with the ED50 values of 5.020 ± 0.563 and 2.500 ± 0.462 mg/kg.bw/day, respectively. The phytochemical screening analysis of Mundulea antanossarum seeds extract revealed the presence of flavonoids, terpenoids, saponins, tannins, and total phenols. However, alkaloids were absent. The present findings validated the ethno-medical claim that the extract of Mundulea antanossarum could be useful in treating malaria and fever. For the best of our knowledge, this is the first report on the antimalarial activity of this plant species in the literature.
... Our observation that control mice given oral administration of eupatilin (10 mg/kg) appeared healthy also suggests that cell toxicity is not associated with eupatilin. Artemisia herb extracts have been safely used for many inflammatory diseases like gastritis or malaria over a few thousand years (Li and Wu, 1998). Osteoporosis is an aging-associated disease. ...
Osteoporosis is an aging-associated diseases requiring better therapeutic modality. Eupatilin is a major flavonoid from Artemisia plants such as Artemisia princeps and Artemisia argyi which has been reported to possess various beneficial biological effects including anti-inflammation, anti-tumor, anti-cancer, anti-allergy, and anti-oxidation activity. Complete blockade of RANK-dependent osteoclastogenesis was accomplished upon stimulation prior to the receptor activator of nuclear factor κB (RANK)-ligand (RANKL) treatment or post-stimulation of bone marrow macrophages (BMCs) in the presence of RANKL with eupatilin. This blockade was accompanied by inhibition of rapid phosphorylation of Akt, GSK3β, ERK and IκB as well as downregulation of c-Fos and NFATc1 at protein, suggesting that transcriptional suppression is a key mechanism for anti-osteoclastogenesis. Transient reporter assays or gain of function assays confirmed that eupatilin was a potent transcriptional inhibitor in osteoclasts (OC). Surprisingly, when mature osteoclasts were cultured on bone scaffolds in the presence of eupatilin, bone resorption activity was also completely blocked by dismantling the actin rings, suggesting that another major acting site of eupatilin is cytoskeletal rearrangement. The eupatilin-treated mature osteoclasts revealed a shrunken cytoplasm and accumulation of multi-nuclei, eventually becoming fibroblast-like cells. No apoptosis occurred. Inhibition of phosphorylation of cofilin by eupatilin suggests that actin may play an important role in the morphological change of multinucleated cells (MNCs). Human OC similarly responded to eupatilin. However, eupatilin has no effects on osteoblast differentiation and shows cytotoxicity on osteoblast in the concentration of 50μM. When eupatilin was administered to LPS-induced osteoporotic mice after manifestation of osteoporosis, it prevented bone loss. Ovariectomized (OVX) mice remarkably exhibited bone protection effects. Taken together, eupatilin is an effective versatile therapeutic intervention for osteoporosis via; 1) transcriptional suppression of c-Fos and NFATc1 of differentiating OC and 2) inhibition of actin rearrangement of pathogenic MNCs.
... Natural products have long been used to develop drugs to combat disease and improve human health. One example is the antimalarial drug artemisinin, which is naturally produced by a plant, Artemisia annua and has been used for a long time in traditional Chinese medicine (1,2). However, due to the long production time and usually low titre of these products in the original hosts, the imbalance between supply and demand inevitably drives the price of these drugs to a very high level. ...
It is a routine task in metabolic engineering to introduce multicomponent pathways into a heterologous host for production of metabolites. However, this process sometimes may take weeks to months due to the lack of standardized genetic tools. Here, we present a method for the design and construction of biological parts based on the native genes and regulatory elements in Saccharomyces cerevisiae. We have developed highly efficient protocols (termed YeastFab Assembly) to synthesize these genetic elements as standardized biological parts, which can be used to assemble transcriptional units in a single-tube reaction. In addition, standardized characterization assays are developed using reporter constructs to calibrate the function of promoters. Furthermore, the assembled transcription units can be either assayed individually or applied to construct multi-gene metabolic pathways, which targets a genomic locus or a receiving plasmid effectively, through a simple in vitro reaction. Finally, using β-carotene biosynthesis pathway as an example, we demonstrate that our method allows us not only to construct and test a metabolic pathway in several days, but also to optimize the production through combinatorial assembly of a pathway using hundreds of regulatory biological parts.
© The Author(s) 2015. Published by Oxford University Press on behalf of Nucleic Acids Research.
... Many more plants might have antimalarial potential. (Ying and Yu-Lin, 1998). The research study reports on the active compounds present in Terminalia catappa. ...
The leaves of Terminalia catappa were air dried, grounded and soaked with ethanol. The extracts obtained (47.23g, TC1) was fractionated sequentially using aqueous methanol with petroleum ether, chloroform and ethyl acetate respectively. The residue of ethanol extract (marc) was extracted with 5M HCl, basified and extracted with chloroform. These were labeled as TC1-01–TC1-05 for the plant. Each of these fractions was phytochemically screened to detect the class of secondary metabolite present. The fractions obtained from the plant were found to be selectively active against brine shrimp larvae. These fractions were also subjected to antimalaria parasites bioassay. Fractions TC1, TC1-02 and TC1-05 were found to be active against tested organisms, with TC1-02 being the most active. TC1-02 was further subjected to activity guided column chromatography that led to the isolation of two pure compounds TC1-02-1 and TC1-02-64. Compound TC1-02-64 was found to be active against the malaria parasite. This was further purified and subjected to qualitative and quantitative analysis.
Key Words: Fractionation, Antimalaria, Ethanol, Column Chromatography, Terminalia catappa.
... Artemisinin, the endoperoxide sesquiterpene lactone is the active constituent of the plant Artemisia annua which is a common weed in Southern China. Since the isolation of artemisinin in 1971, a water soluble ester called artesunate and two oil soluble preparations artemether and arteether have been developed, (Hsu, 2006; Liao, 2009; Tu, 2004; Liy and Wy, 1998). Inhibition of protein synthesis (Hong and Meshnick, 1994) in Plasmodium and generation of organic free radicals are the basic mechanisms of action of artemisinin. ...
Background: Previous studies in animal have shown that high doses of artemisinin caused injury to liver cells.
Presently artemisinin and its derivatives such as artesunate (ART), and it’s combination therapy (ACT) has been
adopted as the frontline drug for treatment of uncomplicated malaria in Nigeria without considering the effect it has
on some major organs of the body.
Objective: The objective of this study was to evaluate the effect of ART when administered as a monotherapeutic
agent and in combination as ACT on the plasma levels of aspartate aminotransferase (AST), alanine aminotransferase
(ALT) and bilirubin (BIL) and the effect of concomitant administration of a hepatotonic phospholipid (PL) on such
effects.
Methodology: The prepared plasma samples were analyzed using the end point calorimetric method for each
parameter as explained in the Randox kits manual.
Results: Co-administration of ART with amodiaquine (AMQ), mefloquine (MFQ) and sulphadoxine/pyremethamine
(SP) respectively, on the 4th day of the studies increased the mean plasma concentration of AST to 80.70%, 108.0%
and 75.0% against 59% for ART alone; ALT increased to 104%, 33.0% and 43.30% against 25.05% for ART alone;
total bilirubin (TBIL) increased to 80.0%, 78.88% and 98.91% against 17.6% for ART alone. The co-administration
and post-administration of ART and the ACTs with 900mg and 1800mg daily dose of PL respectively reduced the
levels of the AST, ALT and BIL by 65.0% and 97.0% of the increased values respectively on 4th day.
Discussion: The results suggest that ART as a monotherapeutic agent has injurious effect on the liver, and this effect
is aggravated when ART is used in ACTs, however, the co-administration with phospholipids cushions the adverse
effects.
... They noted the antimalarial qualities of Artemisia in 1971, developed an effective extraction process, and identified artemisinin as the active ingredient in 1972 (Klayman 1985(Klayman , p. 1049Anonymous 1992;Hien and White 1993;NA 2004, p. 133;Zamiska and McKay 2007;White 2008, p. 330;Ye 2008. Also see Li and Wu 1998, Jansen and Yin 2002, Hsu 2006b, Zhang 2006). ...
The key ingredient in the leading treatment for malaria in Africa -artemisinin -comes not from high-tech research, but is an extract of an ancient medicinal plant, Artemisia annua, commonly known as Artemisia. Chloroquine and replacement drugs have lost effectiveness with the development of resistance and have increasingly been replaced by derivatives of artemisinin combined with other drugs. Known as artemisinin–based combination therapies (ACTs), they provide the most effective treatment at present. This has led to efforts to increase cultivated production of Artemisia in the short run and to develop, through biological and chemical research, synthetic substitutes in the longer run. The resulting juxtaposition of activities and players provides both opportunities and challenges for society. While individual components have been examined, there is little in the way of comprehensive analysis. This paper attempts to weave the many complex and dynamic components -historical, scientific, technical, economic -together in order to aid understanding of the issues and facilitate development of informed public/private policies and actions. Although focused on Africa, the main components and issues are global in nature and resolution and relate to more general issues in infectious disease control and economic development., I have continued work on the paper as a personal effort and may be contacted at dana.dalrymple@verizon.net. The views expressed are my own and not necessarily those of USAID. Mention of commercial firms and products does not imply endorsement. This is a revision and update of he December 10, 2009 version of the paper which was posted on the Medicines for Malaria Venture website [www.mmv.org/research-development/optimizing-artemisinin-production/related-publications].
... In questo testo si illustravano le proprietà curative degli estratti e degli infusi di A. annua contro la malaria (Sumner, 2000). Ad inizio anni '70, sotto il governo di Mao (Li & Wu, 1998), si diede ordine a tutti i settori delle scienze sinniche, di indagare approfonditamente sulle proprietà curative reali di svariate piante note dalla tradizione cinese e tra queste anche le numerose specie del genere Artemisia. Dallo screening (che oggi ammonta ad oltre 130 specie congeneri indagate) ne risultò che A. annua possedeva effettivamente una potente azione antimalarica e pertanto si pervenne alla prima identificazione ufficiale di azione anti-Plasmodium alternativa agli antibiotici ed al chinino: il qinghaosu poi ribattezzato in occidente artemisinina (vedi: http://www.sviluppoumano.it/stopmalaria/). ...
See also these papers about Artemisia phytoextracts.
PLATYZOA ► https://www.researchgate.net/publication/263714074
NEMATODA ► https://www.researchgate.net/publication/235331332
DIPTERA ► https://www.researchgate.net/publication/235675253
MOLLUSCA ► https://www.researchgate.net/publication/235791811
ALLELOPATHY ► https://www.researchgate.net/publication/235675272
VIRUS & PROCARIOTA ► http://www.researchgate.net/publication/259822587
PROTISTA ► http://www.researchgate.net/publication/264344623
GLOBAL REVIEW ►✉◀ https://www.researchgate.net/publication/235331350
Natural compounds of CoAlTa species
➽STEVIA-- https://www.researchgate.net/publication/264200766
➽ASPIDISTRA-- https://www.researchgate.net/publication/256443888
➽MYRTUS-- https://www.researchgate.net/publication/256444098
➽PITTOSPORUM-- https://www.researchgate.net/publication/256484932
➽KENAF-- https://www.researchgate.net/publication/256475476
➽ASPHODELUS-- https://www.researchgate.net/publication/256484895
➽AUCUBA-- https://www.researchgate.net/publication/264161671
➽ETHNOBOTANY-- https://www.researchgate.net/publication/256453477
____________________________________________
#ABSTRACT.-- The main aim of this contribute was to review the biological activity of phyto-extracts of Artemisia against Viruses, Bacteria, Micota, Protista, helmints (Platyzoa and Nematoda) and Diptera (Culicidae, Calliphoridae, Drosophilidae, Muscidae). The main phyto-extracts recognized are as follows: aesculetine, arcapilline, artemisinine, artesunate, beta-arteannuine, beta-sitosterol, dehidro-artemisinine, deoxy-artemisinine, isorhamnetine, stigmasterol (antiviral); artemisinine, artesunate (cito-toxics and anti-helmintic); cineol (antimammal); alfa-terpinene, alfa-tujone and beta-tujone, beta-isobornil-acetate, beta-pinene, bornil-acetate, camphor, capillin, cineol, iso-borneol and borneol, limonene, linalol, mircene, nonanone-3, terpinene-4-ol (anti-Diptera).
... Some drugs are prepared from excretory plant products such as gum, resins, and latex. Commonly used spices, herbs, and herbal Figure 4: Styles of Chinese herbal medicine (CHM) in the global market (see also [62] of quasi-chemical model and [63][64][65] of full-chemical model). formulae are utilized for therapeutic interventions in about 28 kinds of chronic diseases in humans [89]. ...
In recent years, increasing numbers of people have been choosing herbal medicines or products to improve their health conditions, either alone or in combination with others. Herbs are staging a comeback and herbal "renaissance" occurs all over the world. According to the World Health Organization, 75% of the world's populations are using herbs for basic healthcare needs. Since the dawn of mankind, in fact, the use of herbs/plants has offered an effective medicine for the treatment of illnesses. Moreover, many conventional/pharmaceutical drugs are derived directly from both nature and traditional remedies distributed around the world. Up to now, the practice of herbal medicine entails the use of more than 53,000 species, and a number of these are facing the threat of extinction due to overexploitation. This paper aims to provide a review of the history and status quo of Chinese, Indian, and Arabic herbal medicines in terms of their significant contribution to the health promotion in present-day over-populated and aging societies. Attention will be focused on the depletion of plant resources on earth in meeting the increasing demand for herbs.
... Similarly to salicylic acid, artemisinin is naturally produced by a plant, Artemisia annua, which has a long history of use in traditional Chinese medicine. The antimalarial properties of A. annua extracts were re-discovered by Chinese scientists in the 1970s, and the active compound was identified as artemisinin; this was followed shortly afterwards by the elucidation of its chemical structure 5 . Although artemisinin derivatives were designated first-line antimalarial drugs by the WHO in 2002 (REF. ...
Recent developments in synthetic biology, combined with continued progress in systems biology and metabolic engineering, have enabled the engineering of microorganisms to produce heterologous molecules in a manner that was previously unfeasible. The successful synthesis and recent entry of semi-synthetic artemisinin into commercial production is the first demonstration of the potential of synthetic biology for the development and production of pharmaceutical agents. In this Review, we describe the metabolic engineering and synthetic biology approaches that were used to develop this important antimalarial drug precursor. This not only demonstrates the incredible potential of the available technologies but also illuminates how lessons learned from this work could be applied to the production of other pharmaceutical agents.
... For example is the discovery of new antimalarial artemisinin and its derivatives from Artemisia annua that has been used in China for centuries traditionally. This proves that the medicinal plants is a natural source of new antimalarials that still need to be explored (Li and Wu, 1998). Other herbs that are proven to have antimalarial activities such as Nigella sativa (Abdulelah and Zainal-Abidin, 2007) Vernonia staehelinoides Harv. ...
A series of studies has been conducted to prove the Eurycoma longifolia Jack. root as an antimalarial. However, the in vivo antiplasmodial activity of E. longifolia Jack. root standardized extract and its lethal dose 50% (LD50) values is unknown. In vivo antiplasmodial activity was conducted on Plasmodium berghei infected Swiss mice as malaria model with 4-day suppression methods. Sixty mice were divided into 6 groups. Five groups as treatment groups received test material with 5 various doses and one group was given distilled water as control group. Parasite growth inhibition was calculated by comparing the parasitemia at treatment groups to control group. Effective dose that could inhibit parasite growth by 50% (ED50) was calculated by probit analysis based on the relationship between dose and the percentage of parasite growth inhibition. The results showed that E. longifolia Jack. root standardized extract have in vivo antiplasmodial activity in P. berghei infected Swiss mice with ED50 value of 28.78 mg kg −1 . Acute toxicity testing was conducted on 60 mice, divided into 6 groups. Five groups received test materials with 5 various doses as a single dose orally. One other group was given distilled water as control group. Each animal was observed for the first 24 h and observation was continued for 14 days. The lethal dose 50% (LD50) was calculated by probit analysis based on the number of animal deaths that occurred within 24 h after the administration of the test material. The results showed that the LD50 value of E. longifolia Jack. root standardized extract was 6128.71 mg kg −1 . Therapeutic Index was calculated as ratio of the LD50 and ED50 with results 212.95. It showed high therapeutic index which indicated that E. longifolia Jack. root standardized extract has low toxicity.
... Artemisia annua L. (sweet or annual wormwood) is an annual herb endemic to the northern parts of Chahar and Suiyuan provinces in China, where it is known as 'quinghao' and has been used as a remedy for chills and fevers for more than 2000 years [1,2]. Traditionally, the plant is used to prepare a drink, as indicated in the Compendium of Treatments (Ben Cao Gang Mu), written in 1596 AD by Li Shizhen: "take a handful of qinghao, soak it in a sheng (liter) of water, and squeeze out the juice and drink it all" [3,4]. Nowadays the (daily) dose of A. annua given in the Chinese Pharmacopoeia for the treatment of various fevers, including malaria, is 4.5-9 g of dried plant material, extracted by heating with water [5,6]. ...
Artemisia annua L. is a promising and potent antimalarial drug. This activity has been ascribed to its content of artemisinin, a sesquiterpene lactone that is stage specific and very effective against drug-resistant Plasmodium species and which has low toxicity. The in vitro antiplasmodial activity of artemisinin is enhanced by the flavonoids of the extract, as recently proposed by the authors. Different extracts (tinctures, infusions and decoctions), obtained from a cultivar selected by the University of Campinas (0.52% artemisinin), were analyzed in order to prove the selectivity of the solvents to obtain high yields of both artemisinin and flavonoids. Tinctures 40 and 60% v/v showed a greater power of extraction in comparison with infusions and decoctions. The best performance was obtained using 60% v/v tincture. The extraction efficiency for artemisinin was 40% and for flavonoids was 29.5%. Among aqueous extracts, the best results were obtained by preparing an infusion with boiling water, left to cool for 15 minutes before filtration. The extraction efficiency for artemisinin was 57.5% and for flavonoids was 8.2%. If leaves are boiled for several minutes the artemisinin concentration is decreased, probably due to the heat instability of this constituent. Also microwave could represent a valid alternative method to extract the phytocomplex, the extraction efficiency for artemisinin was 41.0% and that for flavonoids was 7.7%.
... Reduction of the lactone in dihydroartemisinin and artemether has led to increased oil solubility, whereas the acidic moiety lends water solubility to artesunate [88,89]. Consequently, artemisinin derivatives, such as dihydroartemisinin, artemether, and artesunate, are developed and being used around the world as effective antimalarial drugs, including those targeted against multidrug-resistant Plasmodium falciparum [90]. These derivatives appear to be more potent than the parent compound and the most rapidly acting among all other antimalarial agents [91]. ...
With tens of thousands of plant species on earth, we are endowed with an enormous wealth of medicinal remedies from Mother Nature. Natural products and their derivatives represent more than 50% of all the drugs in modern therapeutics. Because of the low success rate and huge capital investment need, the research and development of conventional drugs are very costly and difficult. Over the past few decades, researchers have focused on drug discovery from herbal medicines or botanical sources, an important group of complementary and alternative medicine (CAM) therapy. With a long history of herbal usage for the clinical management of a variety of diseases in indigenous cultures, the success rate of developing a new drug from herbal medicinal preparations should, in theory, be higher than that from chemical synthesis. While the endeavor for drug discovery from herbal medicines is "experience driven," the search for a therapeutically useful synthetic drug, like "looking for a needle in a haystack," is a daunting task. In this paper, we first illustrated various approaches of drug discovery from herbal medicines. Typical examples of successful drug discovery from botanical sources were given. In addition, problems in drug discovery from herbal medicines were described and possible solutions were proposed. The prospect of drug discovery from herbal medicines in the postgenomic era was made with the provision of future directions in this area of drug development.
... In recent years, studies have demonstrated that artemisinin and its derivatives had a significant cytotoxic effects toward cancer cells and could reverse multiple drug resistance of tumors8910. Artemisinin was first isolated from leaves of Artemisia annua, a Chinese traditional herb, by Chinese pharmacists in 1971 [11]. Artemether, the methyl ether derivative of artemisinin, is widely used in the therapy of malaria [12]. ...
Artemether is the derivative extracted from Chinese traditional herb and originally used for malaria. Artemether also has potential therapeutic effects against tumors. Vascular cell adhesion molecule-1 (VCAM-1) is an important cell surface adhesion molecule associated with malignancy of gliomas. In this work, we investigated the role and mechanism of artemether combined with shRNA interference of VCAM-1 (shRNA-VCAM-1) on the migration, invasion and apoptosis of glioma cells. U87 human glioma cells were treated with artemether at various concentrations and shRNA interfering technology was employed to silence the expression of VCAM-1. Cell viability, migration, invasiveness and apoptosis were assessed with MTT, wound healing, Transwell and Annexin V-FITC/PI staining. The expression of matrix metalloproteinase-2 (MMP-2), matrix metalloproteinase-9 (MMP-9) and phosphorylated Akt (p-Akt) was checked by Western blot assay. Results showed that artemether and shRNA-VCAM-1 not only significantly inhibited the migration, invasiveness and expression of MMP-2/9 and p-Akt, but also promoted the apoptosis of U87 cells. Combined treatment of both displayed the maximum inhibitory effects on the malignant biological behavior of glioma cells. Our work revealed the potential therapeutic effects of artemether and antiVCAM-1 in the treatments of gliomas.
... In 2001, the World Health Organization (WHO) recommended artemisinin (ART)-based combination therapies (ACTs) as first-line treatment for uncomplicated P. falciparum malaria, and during the past decade most malaria endemic countries have shifted their national treatment policies to ACTs (WHO, 2010a). ART and its derivatives are the most potent and rapidly acting antimalarial drugs (see reviews byCumming et al. (1997),Gera and Khalil (1997),Li and Wu (1998), Meshnick (1998), White (1998b),Balint (2001), Haynes andKrishna (2004), Olliaro and Taylor (2004),Bray et al. (2005), Nosten and White (2007) andDing et al. (2010). These drugs act on all asexual stages of the parasite and are able to reduce parasite biomass by up to 10,000-fold per cycle (White, 1997), thus providing rapid relief of symptoms. ...
Artemisinin (ART) based combination therapy (ACT) is used as the first line treatment of uncomplicated falciparum malaria in over 100 countries and is the cornerstone of malaria control and elimination programs in these areas. However, despite the high potency and rapid parasite killing action of ART derivatives there is a high rate of recrudescence associated with ART monotherapy and recrudescence is not uncommon even when ACT is used. Compounding this problem are reports that some parasites in Cambodia, a known foci of drug resistance, have decreased in vivo sensitivity to ART. This raises serious concerns for the development of ART resistance in the field even though no major phenotypic and genotypic changes have yet been identified in these parasites. In this article we review available data on the characteristics of ART, its effects on Plasmodium falciparum parasites and present a hypothesis to explain the high rate of recrudescence associated with this potent class of drugs and the current enigma surrounding ART resistance.
... on artemisinina e derivati , sono i seguenti : ascite di Ehrlich ( Woerdenbag et al . , 1993 ; Li & Wu , 2003 ) cancro cavità orale ( Nam et al . , 2007 ) cancro cervello ( Lai et al . , 2005 ) cancro cervice uterina ( Lee et al . , 2005 ) cancro collo ( Keltner et al . , 2007 ) cancro endometrio ( Keltner et al . , 2007 ) cancro naso - faringeo ( Li & Wu , 2003 ) cancro osseo ( Beekman et al . , 1998 ) cancro ovarico ( Jiao et al . , 2007 ) cancro pancreas ( Keltner et al . , 2007 ) cancro polmone ( Mu et al . , 2008 ) cancro sistema nervoso ( Efferth et al . , 2001 , 2003 ) carcinoma cavità boccale " squamoso " ( Yamachika et al . , 2004 ) carcinoma colo - rettale ( Li et al . , 2007a ) carcinoma gastrico ( Keltner et al . , 2007 ) ...
-- See also these papers about Artemisia phytoextracts.
PLATYZOA ► https://www.researchgate.net/publication/263714074
NEMATODA ► https://www.researchgate.net/publication/235331332
DIPTERA ► https://www.researchgate.net/publication/235675253
MOLLUSCA ► https://www.researchgate.net/publication/235791811
ALLELOPATHY ► https://www.researchgate.net/publication/235675272
VIRUS & PROCARIOTA ► http://www.researchgate.net/publication/259822587
PROTISTA ► http://www.researchgate.net/publication/264344623
Natural compounds of CoAlTa species ► https://www.researchgate.net/publication/264161671
_______________________________________________________
Phyto-extracts of Artemisia species (Asteraceae) are employed as natural bio-cides (anti-insects, anti-helminthes, and anti-biotics) from many century.
The main aim of this review was to summarized the toxic effects of chemical extracts from Artemisia on not human targets. Toxic effects was reported for the taxa as follows.
Virus species. - human flou virus, DEN/2, FIV, HBV, HCMV, HIV, HPV, HSV/1, HSV/2, JUNV, ToMV. Quercetin have antiviral effects on the following viruses: bird-myeloblastosis; encephalo-myocardites (Col, SK, MM, Mengo-M/L); HSV/1; Murine-leukemia of Maloney; human polio-virus; Rous-virus associate/II; stomovesciculite-virus.
Procariote genera. - Acinetobacter, Agrobacterium, Aeromonas, Alcaligenes, Bacillus, Beneckea, Bordetella, Brevibacterium, Bronchotrix, Citrobacter, Corynebacterium, Cryptococcus, Enterococcus, Enterobacter, Erwinia, Escherichia, Haemophilus, Helicobacter, Klebsiella, Listeria, Mycobacterium, Mycoplasma, Neisseria, Nocardia, Oersokovia, Proteus, Pseudomonas, Ralstonia, Salmonella, Sarcinea, Serratia, Shigella, Staphylococcus, Streptococcus, other Mycobacteria.
Mycote genera. - Acremonium, Alternaria, Aspergillus, Botrytis, Candida, Cladosporium, Colletotrichum, Epidermophyton, Erysiphe, Fonsecaea, Fusarium, Gaeumannomyces, Geotrichum, Gerlachia, Gibberella, Helminthosporum, Malassezia, Microsporum, Mucora, Nannizzia, Penicillium, Phialophora, Phytophtora, Piedraia, Pleurotus, Pneumocystis, Puccinia, Pyricularia, Pythium, Rhizoctonia, Rhizopus, Rhodotorula, Saccharomyces, Sclerotinia, Sporotrichum, Tiarosporella, Trichoderma, Trichophyton, Trichosporon, Verticillium, Zygorrynchus).
Other not-autotrophic Protista genera. - Acanthamoeba, Babesia (caballi, equii, microti), Balantidium, Cryptosporidium, Eimeria (acervulina, tenella; limited effects also versus maxima, necatrix), Entamoeba, Giardia, Haemoproteus, Leishmania (amazonensis, braziliensis, donovani, infantum, major, mexicana, tropica), Naegleria, Neospora, Plasmodium (berghei, chabaudi, cynomolgi, falciparum, inui, knowlesi, nigeriensis, ovale, petteri, vinckei, vivax, yoelii), Theileria, Toxoplasma, Trichomonas, Trypanosoma (brucei, cruzi, evansi, rhodesiense). Toxic effects were due also to quercetin versus Cryptosporidium, Encephalitozoon, Leishmania, Plasmodium, Toxoplasma.
Human tumoral cells. - bone; brain; breast; cervice, colorectal; Ehrlich ascites tumor; endometre, fibrosarcoma; gastric, glioma; hepatoma; Kaposi sarcome; laryngeoma; leukemia; lung; multiple myeloma; myelo-leukemia; nasopharyngeal; neck, neuvous system; oral; ovarian; pancreas, pituitary-macroadenoma; promyelocytic-leukemia; prostate; renal; thyroid, uveal-melanoma, via several effects as cyto-toxicity, apoptosys, anti-angiogenesys, anti-metastatic and inhibition of nuclear KB-factor for the carcinocyte progression.
Anti-helminth effects on the following Platyzoa genera. - Clonorchis, Dipylidium, Echinostoma, Fasciola, Moniezia, Opisthorchis, Schistosoma, Taenia.
Anti-helminth effects on the following Nematoda genera. - Ascaridia, Ascaris, Bunostomum, Caenorhabditis, Dictyocaulus, Dirofilaria, Ditylenchus, Enterobius, Gnathostoma, Haemonchus, Helicotylenchus, Meloidogyne, Nematodirus, Neoascaris, Pratylenchus, Protostrongylus, Rotylenchulus, Strongyloides, Toxocara, Trichinella, Trichostrongylus.
Mollusca taxa. - Deroceras (Agriolimacidae); Biomphalaria, Planorbella (Planorbidae); Pomacea (Ampullariidae).
Anellida Clitellata. - Pheretima (Megascolecidae).
Mammals Marsupiales. - Trichosurus.
Arthropoda belonging to the following taxa:
- Acari (Psoroptidae; Sarcoptidae, Tetranychidae; Ixodidae);
- Anoplura (Pediculidae);
- Coleoptera (Bostrichidae, Bruchidae, Chrysomelidae, Coccinellidae, Curculionidae, Tenebrionidae);
- Diptera (Culicidae, Calliphoridae, Drosophilidae, Muscidae, Tephritidae);
- Dyctioptera (Blattellidae, Blattidae);
- Heteroptera (Pyrrhocoridae);
- Homoptera (Aleurodidae, Aphididae, Coccidae, Delphacidae, Pseudococcidae);
- Hymenoptera (Formicidae);
- Isoptera (Rhinotermitidae);
- Lepidoptera (Noctuidae, Pieridae, Plutellidae, Pyralidae, Tineidae, Tortricidae);
- Orthoptera (Acrididae);
- Siphonaptera (Pulicidae);
- Thisanoptera (Thripidae).
Allelopathy Artemisia-induced has been showed in 15 species (A. annua most interesting ones) on about 56 plant genera, as follows: Amaranthaceae 3 genera; Apiaceae 3; Asteraceae 8; Brassicaeceae 4; Graminaceae 3; Papilionaceae 5; Poaceae 17; Solanaceae 2; 1 genus per Araceae, Cistaceae, Cucurbitaceae, Linaceae, Malvaceae, Onagraceae, Pinaceae, Plantaginaceae, Polygonaceae, Portulacaceae, Violaceae. Allelopathic effects Artemisia-induced have due to aqueous or alcoholic extracts, epigeal or ipogeal plant organs or from soil. Allelopathic effects influence seed germination and plant productivity. Main allelochemicals recognized are absinthine, arteannuine-B, arteannuate, artemine, artemisinin and 9 semi-sinthetics derivatives, arteannuate, arteannuine-B, artesunate, arteether, dehidro-artemisinin, deoxy-artemisinin, tauremisine, taurine (sesquiterpens), capillene (alchin-idrocarbure), and some essential oil components, alpha-pinene, beta-pinene, canfor, 1,8-cineol, CH3-jasmoate, eucalyptol.
The Artemisia species used for bio-essay were as follows: A. abrotanum, A. absinthium, A. afra, A. annua, A. anomala, A. arborescens, A. argyi, A. asiatica, A. aucheri, A. austriaca, A. biennis, A. borealis, A. brevifolia, A. caerulescens, A. californica, A. capillaris, A. caruifolia, A. changaica, A. cana, A. cina, A. copa, A. diffusa, A. douglasiana, A. dracunculus, A. feddei, A. filifolia, A. frigida, A. gilvescens, A. giraldi, A. glutinosa, A. herba-alba, A. inculta, A. indica, A. iwayomogi, A. japonica, A. judaica, A. kopetdaghensis, A. kurrmensis, A. lavandulaefolia, A. lerchiana, A. lobelii, A. longifolia, A. ludoviciana, A. maritima, A. mexicana, A. molinieri, A. mongolica, A. monogyna, A. monosperma, A. montana, A. moorcroftiana, A. nilagirica, A. nova, A. pallens, A. parviflorum, A. pectinata, A. persica, A. pontica, A. princeps, A. saissanica, A. santonicum, A. scoparia, selengenesis, A. sieberi, A. sieversiana, A. spicigera, A. stolonifera, A. sublessingiana, A. sylvatica, A. transiliensis, A. tridentata, A. verlotorum, A. vestita, A. vulgaris.
Bio-actives chemicals recognized from bio-assay, were as follows: 1,2,4-trioxanes, 1,2,4-trioxolanes, 1,2,4-trioxolanes-monospiro, 1,2,4-trioxolanes-dispiro, 1,2,4,5,7-pentoxocanes, 1,2,4,5,7,8-exaoxocanes, 1-2-6-7-tetraxaspiro[7.11]-nonadecane, 1,8-cineol, 1-Alpha-4-Alpha-dihydroxybishopsolicepolide, 1-desoxy-1-Alpha-peroxy-rupicolin-A-8-O-acetate, 1-phenil-2-4-hexadiyne (= capillene), 1-phenil-2-4-pentadiyne, 2-6-dimethoxiphenol, 3-4-dimetoxy-benzan-ol, 3-butylisocoumarins, 3alpha-4alpha-epoxirupicoline-C, 3alpha-4alpha-epoxirupicoline-D, 3alpha-4alpha-epoxirupicoline-E, 3-CH3-3-phenil-1,4-pentadyne, 3-methoxi-tanapartolide, 4,6,7-trihidroxy-3,5-dimethoxy-flavone, 5,5-dihidroxy-3,4,8-trimethoxy-flavone, 5,6,3,5-tetrametoxy-7,4-OH-flavone, 5-phenil-1,3-pentadyne, 7-methoxyacacetin, Absinthine, Acacetin, Acetophenone, AIP1-polysaccharide complex, Alpha-artether, Alpha-copene, Alpha-phellandrene, Alpha-pinene, Alpha-terpinene, Alpha-terpineol, Alpha-terpinol, Alpha-thujone, Alkyl-deoxoartemisinin, Anhidro-dihidro-artemisinine, Ar-curcumene, Arteannuina-B, Arteflene, Arteinculton, Artelinic acid, Artemether (alpha and beta), Artemifone, Artemine, Artemisia-ketone, Artemisinate, Artemisinin (artemisinin-dimers, trioxan-dimers, ethylsulfon-artemisinin-dimers, ethylsulfid-artemisinin-dimers, artemisinin-trimers, deoxy-artemisinin-trimers, artemisinin-tetramers), Artemisinine-CH3-ether, Artemisinin-1-propyl-ether, Artemisinin-1-buthyl-ether, Artemisinin-cyanoarylmethyle, Artemisolide, arteminolide-B, arteminolide-D, Artemisitene (epoxy-artemisitene, deoxy-artemisitene, ethyl-peroxy-artemisitene, hydro-peroxy-artemisitene), Artesunate and Glicosyl-artesunate, Artether, Ascaridol, B-arteannuine, Beta-artether, Belencamidin, Beta-Artelinate, Beta-carophyllene, Beta-isobornil-acetate, Beta-phellandrene, Beta-pinene, Beta-sitosterol, Beta-thujone, Borneol, Bornil-acetato, Buthyl-azide-artemisinin, Caffeic-acid, Canphor, Capillin, Capillarin, Capillarisin, Cariophyllene-oxide, Casticin, CH3-artemisinin, CH3-diperoxy-artemisinin, CH3-eugenol, Chamazulene, Chrysanthenil, Chrysosplenol-D, Chrysoplenetin, Cineol, Cinnamyl-aldeid, Cis-o-cymene, Clorogenic-acid, Colletotric acid, Coumarin, Cyano-artemisinin, Davanone, deacetyl-laurenobiolide, Dehidro-leucodin, Deoxy-artelinate, Difluoro-methylen-artemisinin, Dihydro-arteannuin, Dis-piro-1,2,4,5-tetraoxanes, Epi-deoxy-dihidroartemisinine, Eugenol, Eupatilin, Exiguaflavone-A, Exiguaflavone-B, Fenozan50F, Friedelin, Genkwanin, Geranil-acetate, Germacrene-D, Hexene-1-ol, Hispidulin, Iso-borneol, Jaceosidin, Konokiol, Limonene, Linalol, Linalooloxide, Magnolol, Menthol, Myrcene, moxartenolide, Myrtenil-acetate, N-N-N-3p-coumaroil-spermidina, Nonanone-3, OH-artemisinin, Paracymene, Peroxy-homoditerpenes, Pinitol, Piperitone, Quebrachitol, Quercetin and derivatives, Ridentin, Rupicolin-A-8-O-acetate, Sabinene, Santonin, Santolynol, Scopoletin, Seco-tanapartholide-A, Seco-tanapartholide-B, Selin-11-en-4alpha-ol, Spinacetin, Steroidal-tetraoxanes, Stigmasterol, Tauremisine, Taurin, Terpinene-4-olo, Thiocarbamate-artemisinin, Thujenol, Thujilol, Thymol, Tehranolide, Trans-ethyl-cinnamate, Trifluoromethyl-idroartemisinin, Trioxaquines, Trioxaquines-DU1302, Triquinanes (7alpha-silphiperfol-5-ene, silphiperfol-5-ene, pethybrene, alpha-isocomene, beta-isocomene), Umbelliferone, Vulgarone-B, Z-hepoxy-o-cimene, and 3 endo-peroxydes without name.
Ethnobotanic use of Artemisia species in Campania (A. absinthium, A. alba, A. annua, A. arborescens, A. campestris, A. variabilis, A. verlotum, A. vulgaris) were reported for A. absinthium only, and were as follows: anti-pyretic (Caserta Province); anti-hypercolesterolemic, anti-hyperglycemic, biliar calculosis, dyspepsia, hepatic stimulating, parotitis, skin-cicatrizing (Napoli-Salerno Province).
The main molecular-cellular mechanisms recognized in Artemisia phytoextracts cyto-toxicity were as follows:
alkylation with heme and protein with heme as prostetic group (hemoglobin; cytochrome; mithocondrial complexes I-IV; mithocondrial ABC cassettes) forming a carbo-centric radical highly reactive versus proteins;
extensive damages and loss of mithocondrial membranes physiology;
alkylation of endo-membrane proteins (SERCA pump; TCTP), with disruption of Ca cyto-homeostasis/metabolism and cytoskeletal disorders;
alkylation of proteins with Fe prostetic group (NADH-dehydrogenase; transferrins) with disruption of mithocondrial membrane functions;
alkylation of IKK at CYS/179 and of NF-KB at CYS/38, with inhibition of NF-KB pro-inflammatory sequence;
alkylation of bacterial efflux pumps, with disruption of detoxificant functions of procariote in presence of antibiotic chemicals.
Data on biological functions of Artemisia extracts are very interesting for a potential widespread use in bio-medicine and agro-ecology. Artemisinin is the new molecular platform for the development of a complete molecular library with potential application as follows:
-) cancer chemotherapy and inflammatory-immunological disorders;
-) inflammatory pathology and immunological disorders;
-) biological control of Arthropoda, Gastropoda, Nematoda, Mycota in agro-environments;
-) treatment of helminth (Platyzoa and Nematoda) and micro-parasites (Virus, Bacteria, Protista) of bio-medical and economic interest for humans and animals.
Besides the clinically proven superior antimalarial activity, artemisinins (ARTs) are also associated with anticancer properties, albeit at much lower potency. Iron and heme have been proposed as possible activators of ARTs against cancer cells. Here we show that zinc protoporphyrin-9 (ZnPPIX), a heme homolog and a natural metabolite for heme synthesis during iron insufficiency, greatly enhanced the anticancer activity of dihydroartemisinin (DHA) in multiple cell lines. Using melanoma B16 and breast cancer 4T1 cells, we demonstrated ZnPPIX dramatically elevated intracellular free heme levels, accompanied by heightened reactive oxidative species (ROS) production. The tumor-suppression activity of ZnPPIX and DHA is mitigated by antioxidant vitamin E or membrane oxidation protectant ferrostatin. In vivo xenograft animal models confirmed that ZnPPIX significantly potentiated the tumor-inhibition capability of DHA while posing no apparent toxicity to the mice. The proliferating index and growth of tumors after the combinatory treatment of DHA and ZnPPIX were evidently reduced. Considering the clinical safety profiles of both DHA and ZnPPIX, their action synergy offers a promising strategy to improve the application of ARTs in our fight against cancer.
Natural products (NPs) and their structural analogs represent a major source of novel drug development for disease prevention and treatment. The development of new drugs from NPs includes two crucial aspects. One is the discovery of NPs from medicinal plants/microorganisms, and the other is the evaluation of the NPs in vivo at various physiological and pathological states. The heterogeneous spatial distribution of NPs in medicinal plants/microorganisms or in vivo can provide valuable information for drug development. However, few molecular imaging technologies can detect thousands of compounds simultaneously on a label-free basis. Over the last two decades, mass spectrometry imaging (MSI) methods have progressively improved and diversified, thereby allowing for the development of various applications of NPs in plants/microorganisms and in vivo NP research. Because MSI allows for the spatial mapping of the production and distribution of numerous molecules in situ without labeling, it provides a visualization tool for NP research. Therefore, we have focused this mini-review on summarizing the applications of MSI technology in discovering NPs from medicinal plants and evaluating NPs in preclinical studies from the perspective of new drug research and development (R&D). Additionally, we briefly reviewed the factors that should be carefully considered to obtain the desired MSI results. Finally, the future development of MSI in new drug R&D is proposed.
For the first time in Uzbekistan, an anatomical and histological study of the vegetative organs of Artemisia annua was carried out. When treated with a solution of methylene blue and safranine, drops of yellow essential oil are found in palisade spongy cells. Also, in the primary crust, parenchymal cells are filled with biologically active substances. The results obtained made it possible to determine a number of morphological, anatomical, histological and characteristic diagnostic signs for this species. These identified diagnostic signs can serve in the identification of plant materials.
Artemisinin is an antimalarial lactone derived from qinghao. Clinically, artemisinin is mainly used to treat malaria symptoms, malignant cerebral malaria, uncomplicated malaria, and severe malaria. Combined with different antimalarial can delay and prevent resistance of malaria parasites. Artemisinin combination therapies (ACT) have been recommended by the WHO as the first-line therapy for P. falciparum malaria worldwide. The discovery of artemisinin has completely changed the treatment of malaria. With the widespread use of artemisinin and its derivatives, the resistance of Plasmodium to these drugs has emerged, which pose a new challenge to the treatment of malaria. Therefore, a new generation of artemisinin drugs should have a broader application prospects.
Despite the incessant efforts to decrease exorbitant number of daily deaths, malaria remains a major threat to the public health in many countries. Transmitted by Anopheles mosquitoes, it is caused by infection with Plasmodium parasites that have become resistant to many antimalarial drugs. In this context, series of metal-based compounds have been screened for optimal activity against different Plasmodium species and strains. This chapter briefly reviews current and potential uses of metal complexes (such as iron, cobalt, nickel, gallium, copper, gold, and silver), metal chelators, and organometallic compounds, as interesting medicinal agents that greatly benefits the fight against malaria.
Medicinal plants are widely used in traditional medicine in both underdeveloped and developing countries in the word until now. Some secondary metabolites isolated from medicinal plants have been developed as modern drugs. New antimalarial artemisinin is an example of modern medicine that developed from Artemisia annua L, a plant used in China since 4,000 years ago. Indonesia is endowed with a rich natural resource. The biodiversity comprises thousands plant species. Therefore, Indonesian flora and fauna are a remarkable opportunity for the development of secondary metabolites for pharmaceutical industry. The Indonesian National Agency for Drug and Food Control, Republic of Indonesia (Badan Pengawas Obat dan Makanan, Republik Indonesia = BPOM RI) classifies traditional medicine into three classes, namely jamu (Indonesian indigenous traditional medicine), standardized herbal medicine and phytopharmaca based on its scientific evidences. The BPOM also determined 9 medicinal plants for focusing research for drug development. This paper discusses some secondary metabolites and their pharmacological activities of the following 9 selected Indonesian medicinal plants namely Piper retrofractum Vahl, Andrographis paniculata Ness, Curcuma xanthorrhiza, Psidium guajava L, Syzigium polyanthi, Morinda citrifolia, Guazuma ulmifolia Lamk, Zingiber officinale, and Curcuma domestica collected from various publications. Furthermore, several modern drugs derived from medicinal plants are also discussed.
La autora relata la historia de Tu Youyou, quien buscando entre la medicina tradicional china encontró que el extracto de la Artemisia annua, planta usada por más de dos mil años como tratamiento contra la fiebre, era potencialmente útil contra la malaria. Aislada la artemisina, fue probada en ensayos clínicos demostrándose su eficacia, especialmente contra el Plasmodium falciparum.
Clinical Oncology strives for complete remission of patients with cancer, but still crusades against multidrug resistance of various cancers. Scientists and clinicians have been challenged to identify new potent anticancer compounds with new targeting strategies. Traditional Chinese Medicine (TCM) provides a large spectrum of medicinal plants containing many biocompounds that possess anticancer activities. These represent a source of molecules that may have antiproliferative effects on a variety of cancers.
Our interest on natural products from TCM was raised in the 1990s by sesquiterpene lactones of the artemisinin type from Artemisia annua L., which exert antimalarial and profound anticancer activity.
Besides novel preclinical developments, we review and discuss the benefit of adjuvant therapies with artemisinin in combination with known chemotherapeutics. Moreover, we depict new biotechnological production methods for meeting the worldwide increasing demand of artemisinin since the WHO officially recommends it for the treatment of malaria.
Some attempts to employ the singlet oxygen generated from molybdate-catalyzed decomposition of hydrogen peroxide are presented. Reduction of ascaridole with diimide is also described, along with the preliminary results of the cleavage study using Fe-cysteinate as a simple model for FeS type redox species. There were strong indications that S-alkylation occurred as observed in similar cleavage of the potent antimalarial qinghaosu.
Abstract Malaria continues to be a major global public health problem with 3.3 billion people at risk in 106 endemic countries. Globally, over 1000 plants have been used as potential antimalarials in resource-poor settings due to fragile health-care systems and lack of accessibility and affordability of artemisinin-based combination therapies (ACTs). Although many believe that the use of medicinal plants that have folklore reputations for antimalarial properties is relatively safe, many herbs may be potentially toxic due to their intrinsic adverse side effects. Therefore, herbal-derived remedies require powerful and deep assessment of their pharmacological qualities to establish their mode of action, safety, quality, and efficacy. In addition, the evolution of drug resistance also demands new antimalarial agents. This can be achieved by forming a vibrant antimalarial discovery pipeline among all stakeholders, including traditional healers, ethnobotanists, scientists, entomologists, pharmacists, and research institutions, for the isolation and characterization of the bioactive compounds with the ultimate objective of finding novel modes of action antimalarial compounds that can be used to fight against drug-resistant malarial parasites.
More than half of the world's population live in areas with appreciable risk of malaria infection. During last years, the situation has worsened in many ways, mainly due to malarial parasites becoming increasingly resistant to several antimalarial drugs. The knowledge of the genomic structure of Plasmodium falciparum (Pf) may offer new perspectives for malaria therapy and control. The efflux pumps serve both as natural defense mechanisms and influence the bioavailability and disposition of drugs. Such mechanism was suggested in Pf where RBCs infected with chloroquine (CQ) resistant parasites accumulated significantly less drug than the sensitive ones - suggesting that some factor/factors allowed a decreased intracellular concentration of drug in the resistant parasite. In this review we will concentrate our presentation mainly to experimentally supported evidence, as this represents the core of the present hypotheses on mechanisms of drug resistance in Plasmodium.
The heat capacities of artemisinin in crystal form were measured in the temperature range from 80 to 363K by an adiabatic calorimeter. Three thermal anomalies were observed at 198, 240, and 312K. Thermogravimetry and differential thermal analysis from 300 to 700K showed melting at 420K, loss of formic acid at 480K, and further decomposition above 480K.
The constant-volume energy of combustion of crystalline artemisinin and its two derivatives, artemether and artesunate, in oxygen at T = 298.15 K was determined to be {-(7546.53 +/- 3.24), -(7582.28 +/- 3.09), and -(8150.75 +/- 4.24)} kJ.mol(-1) using combustion calorimetry, respectively. The derived standard molar enthalpies of formation of the three compounds in crystalline states at T = 298.15 K were {-(1492.81 +/- 7.62), -(2419.75 +/- 7.52), and -(3320.12 +/- 9.90)} kJ.mol(-1), respectively. The thermal stabilities of the three compounds were also investigated by thermal analysis combined with an FT-IR method.
Objective:
To investigate the possible mechanism through which Artemisinin induced apoptosis in pancreatic cell line.
Methods:
Column chromatography, thin layer chromatography (TLC) and proton NMR spectroscopy were used to purify Artemisinin. The flowcytometry was employed to detect apoptosis and reactive oxygen species (ROS).
Results:
The results indicated that 50% inhibiting concentration (IC50 value) for pancreatic cell line (RIN) was 45 μmol/L of Artemisinin. Artemisinin had no cytotoxic effect on the growth of peripheral blood lymphocytes. The mechanism of apoptosis was evaluated by measuring intracellular ROS. It was shown that Artemisinin-induced apoptosis occurred independently of the binding of CD95L to CD95 receptor in the RIN cells. Moreover, Artemisinin, in a dose-dependent manner, could significantly increase the level of ROS.
Conclusion:
Artemisinin can induce apoptosis in the RIN cells via the generation of ROS and triggering the intrinsic pathway of cell death.
This paper is a bibliographical review on toxic effects on molluscan species by phytoextracts of Artemisia species, particularly Vulgarone-B extract from A. douglasiana.
➽➽See also these papers about Artemisia phytoextracts.
PLATYZOA ► https://www.researchgate.net/publication/263714074
NEMATODA ► https://www.researchgate.net/publication/235331332
DIPTERA ► https://www.researchgate.net/publication/235675253
MOLLUSCA ► https://www.researchgate.net/publication/235791811
ALLELOPATHY ► https://www.researchgate.net/publication/235675272
VIRUS & PROCARIOTA ► http://www.researchgate.net/publication/259822587
PROTISTA ► http://www.researchgate.net/publication/264344623
GLOBAL REVIEW ►✉◀ https://www.researchgate.net/publication/235331350
Natural compounds of CoAlTa species ► https://www.researchgate.net/publication/264161671
ResearchGate has not been able to resolve any references for this publication.