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Plants with Anticancer Potential
Abstract
Plants have been utilized for health and medicinal benefits for hundreds of years due to their multiple beneficial attributes such as anticancer, antitumor, antioxidant, antimicrobial, antibacterial, anti-ulcer, anti-arthritic, etc. It has been estimated that there are altogether 250,000 species of higher plants on Earth and among them 35,000–70,000 species are being used to treat various diseases due to the presence of secondary metabolites (alkaloids, flavonoids, steroids, glycosides, saponins, etc.). Cancer is a worldwide leading cause of morbidity and mortality. To cure this at right time, herbal drugs are more beneficial than synthetic drugs, because the synthetic medicines can cause heavy damage to normal cells while destroying the tumor cells. The present work consists of a review of 149 plant families harboring 667 species reported to possess anticancer property. Moreover, other biological properties of the bioactive compounds are also covered. This work is based on reliable data collected from multifarious databases such as CAB abstract, MEDLINE, EMBASE, J GATE, ERIC, Proquest, INMEDPLAN, NATTS, The Plant List, JSTOR, Google Scholar, Springer, Elsevier, and websites such as www.sciencedirect.com, www.jstor.org, www.eflora.org, and www.pfaf.org. The complete data regarding plant names, synonyms, common names, botanical description, medicinal properties, and bioactive compounds present in the plant parts is compiled. In near future, these bioactive compounds can be deployed singly or in combination with routine chemotherapy and radiotherapy to treat various types of cancers, after proper standardization, dose optimization, and stringent clinical trials.
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Naturevolution is a term necessary to evaluate ourselves in term metabolism of natural metabolites. Our studies insist on natural products more extremely powerful treatment for cancer cures. The truth is they actually hate people using any form of natural cures for cancer. The plant based drug discovery resulted mainly in the development of anticancer agents including plants (vincristine, vinblastine, etoposide, paclitaxel, camptothecin, topotecan and irinotecan), marine organisms (citarabine, aplidine and dolastatin 10) and micro-organisms (dactinomycin, bleomycin and doxorubicin). Beside this there is numerous agents identified from fruits and vegetables can used in anticancer therapy. The plant products which are in daily useage include capsaicin (red chilli), diosgenin (fenugreek), 6-gingerol (ginger), ellagic acid (pomegranate), curcumin (turmeric), resveratrol (red grapes, peanuts and berries), genistein (soybean), diallyl sulfide (allium), S-allyl cysteine (allium), allicin (garlic), lycopene (tomato), ursolic acid (apple, pears, prunes), silymarin (milk thistle), anethol (anise, camphor, and fennel), catechins (green tea), eugenol (cloves), indole-3-carbinol (cruciferous vegetables), limonene (citrus fruits), beta carotene (carrots), and dietary fiber. In this review active principle derived from natural products are offering a great opportunity to evaluate not only totally new chemical classes of anticancer agents, but also novel lead compound and potentially relevant mechanisms of action.
Objective: The present study was carried out to evaluate the antitumor and antioxidant activities of the methanol extract of Cordia dichotoma (MECD) against EAC in Swiss albino mice. Materials and Methods: The present study evaluated the anticancer effect of the methanolic extract of C. dichotoma (MECD) bark against Ehrlich ascites carcinoma (EAC) cells induced in albino mice and against human cancer cell lines (malondialdehyde-MB-231 and MCF-7 cells). Results and Discussion: There was significant fall in the red blood cell count and hemoglobin (Hb) content, and a significant increase in white blood cell (WBC) count in the EAC control mice as compared to normal control mice. Treatment with MECD (500 mg/kg, b.w., p.o.) or 5-Fluorouracil (20 mg/kg b.w., i.p.) in EAC-cell bearing mice caused a significant (P < 0.01) increase in Hb levels while a significant (P < 0.01) decrease in WBC levels compared to EAC control rats. Furthermore, increase in the concentration of MECD dose-dependently increased the percent cytotoxicity and decreased the cell viability in both cell line types. The results with MECD were comparable to the tamoxifen. The maximum gain of body weight was observed in the EAC control group. In case of MECD and 5-Fluorouracil treated groups, the body weight was significantly (P < 0.01) reduced. The tumor volume and tumor weight were found to be significantly (P < 0.05 or P < 0.01) decreased in MECD treated animals at the doses 250 and 500 mg/kg and 5-Fluorouracil (20 mg/kg) when compared with EAC control animals. With MECD treatment, the survival of EAC bearing mice significantly (P < 0.01) increased as compared to EAC bearing control group. In treated group, mean survival time (MST) was significantly increased to 29.0 ± 1.98 (%ILS = 69.04), 34.12 ± 1.84 (%ILS = 81.25), and 36.87 ± 1.67 (%ILS = 87.79), respectively, when compared to EAC control group. Conclusion: The results of the current study propose that the antitumor activity of MECD can be inferred from the increased life span of EAC bearing mice which is due to its antioxidant activity.
Protective effect of free phenolics from Lycopus lucidus Turcz. root (FPLR) on CCl4-induced hepatotoxicity in vivo and in vitro was first evaluated. Oral administration of FPLR (100 mg/kg bw) to mice significantly reduced the CCl4-induced elevation of serum alanine aminotransferase, aspartate aminotransferase, alkaline phosphatase, triacylglycerols, total cholesterol, and total bilirubin. FPLR also increased the hepatic GSH contents and antioxidant enzyme activities of SOD and CAT and decreased the hepatic MDA level. Histopathological examinations further confirmed that the FPLR could protect the liver from CCl4-induced damage. Further research indicated that FPLR prevented the DNA fragmentation caused by CCl4 based on TUNEL assay. Moreover, immunohistochemistry staining demonstrated that pretreatment with FPLR significantly inhibited the elevation of hepatic TNF-α, IL-6, IL-8, iNOS, COX-2, and Caspase-3 in CCl4-treated mice. In vitro experiments showed that FPLR remarkably reduced BRL hepatocyte apoptosis and damage caused by CCl4 treatment. These findings indicate that FPLR could be developed as a functional food or medication for therapeutic purpose and prevention of hepatic injury.
Achyrocline satureioides, popularly known as "marcela", is a medicinal plant found in South America. This plant is rich in flavonoids, which have been reported to exert numerous biological activities. The aim of this study was to purify, identify and evaluate the mechanisms underlining anticancer activity of A. satureioides flavonoids in glioma cell lines (U87, U251 and C6) as well as their comparative toxicity in normal brain cells (primary astrocytes, neurons and organotypic hippocampal cultures). The main flavonoids present in A. satureioides are luteolin, quercetin, 3-O-methyl-quercetin and achyrobichalcone, the later a very unique metabolite present in this plant. Isolated flavonoids as well as A. satureioides extracts reduced proliferation and clonogenic survival, and induced apoptosis of glioma cell lines. In addition, A. satureioides flavonoids potentiated the cytotoxic effect and apoptosis induction by the glioma chemotherapeutic temozolomide (TMZ). Importantly, A. satureioides flavonoids were less cytotoxic to astrocytes, neuron:astrocytes co-cultures and hippocampal cultures if compared to gliomas. Investigation of 10 cancer-related pathways showed a reduced activation of MYC and the Map kinases ERK and JNK by A. satureioides flavonoid-enriched extract, an effect not observed when individual flavonoids were evaluated. Altogether, the herein presented results show that A. satureioides extract possesses a combination of flavonoids, some unique for this plant, which have synergistic anticancer activity and potential for further studies in vivo.
Caesalpinia coriaria (C. coriaria), also named cascalote, has been known traditionally in México for having cicatrizing and inflammatory properties. Phytochemical reports on Caesalpinia species have identified a high content of phenolic compounds and shown antineoplastic effects against cancer cells. The aim of this study was to isolate and identify the active compounds of a water:acetone:ethanol (WAE) extract of C. coriaria pods and characterize their cytotoxic effect and cell death induction in different cancer cell lines. The compounds isolated and identified by chromatography and spectroscopic analysis were stigmasterol, ethyl gallate and gallic acid. Cytotoxic assays on cancer cells showed different ranges of activities. A differential effect on cell cycle progression was observed by flow cytometry. In particular, ethyl gallate and tannic acid induced G2/M phase cell cycle arrest and showed interesting effect on microtubule stabilization in Hep3B cells observed by immunofluorescence. The induction of apoptosis was characterized by morphological characteristic changes, and was supported by increases in the ratio of Bax/Bcl-2 expression and activation of caspase 3/7. This work constitutes the first phytochemical and cytotoxic study of C. coriaria and showed the action of its phenolic constituents on cell cycle, cell death and microtubules organization.
The plant Lepechinia mutica (Benth.) Epling (family Lamiaceae) is endemic to Ecuador. In the present study, we report some major non-volatile secondary metabolites from the leaves and the chemistry of the essential oil distilled from the flowers. The main identified compounds were carnosol, viridiflorol, ursolic acid, oleanolic acid, chrysothol, and 5-hydroxy-4′,7-dimethoxy flavone. Their structures were determined by X-ray diffraction and NMR and MS techniques. The essential oil showed a chemical composition similar to that distilled from the leaves, but with some qualitative and quantitative differences regarding several minor compounds. The main constituents (>4%) were: δ-3-carene (24.23%), eudesm-7(11)-en-4-ol (13.02%), thujopsan-2-α-ol (11.90%), β-pinene (7.96%), valerianol (5.19%), and co-eluting limonene and β-phellandrene (4.47%). The volatile fraction was also submitted to enantioselective analysis on a β-cyclodextrin column, obtaining the separation and identification of the enantiomers for α-thujene, β-pinene, sabinene, α-phellandrene, limonene and β-phellandrene. Furthermore, the anti-fungal activity of non-volatile secondary metabolites was tested in vitro, with carnosol resulting in being very active against the “blast disease” caused by the fungus Pyricularia oryzae.
In the last few decades, phytochemicals have potentially gained as an important place in cancer research. The interests for these compounds have grown by researchers, as these compounds have natural in origin and hence, no stipulated side effects are known. Currently, thousands of natural herbs based compounds have been screened for their novel efficiency to control cancer cell proliferation. Among these, a large number of natural compounds gained high preventive and therapeutic values against cancer and most potential compounds along of the are lupeol, saponins, flavanoids, curcumin, resveratrol, geneistein, gingerol, allyl sulfide, berberine, lycopene, bromelain, indole-3-carbinol and polyphenols. The recent research on phytochemicals towards evaluating the anticancer efficacy has been accelerated by development of biophysical technologies. However, several challenges still persist in cancer research like heterogeneity, development of novel phenotypes in cancer cell by therapeutic drugs and tumour recurrence. These challenges open a new dimension for cancer research, and also give weightage to explore the uses of specific phytochemicals in therapy. This review summarizes the latest research in cancer treatment using the bioactive components from medicinal plants.
Background
Inhabitants of the Eastern Cape Province of South Africa use the roots of Dianthus thunbergii and corms of Hypoxis argentea to treat diabetes mellitus and other ailments.
Objective
The objective of this study was to analyze the phytochemical composition and antioxidant activities of the aqueous and ethanol extracts of the roots and corms of two plants.
Materials and Methods
Total phenolics, flavonoids, flavonols, proanthocyanidins, tannins, and alkaloids were determined by standard methods. The scavenging activities of the extracts against 1,1 diphenyl-2-picrylhydrazyl (DPPH), 2'-azino-bis (3-ethylbenthiazoline-6-sulfonic acid (ABTS), nitric oxide (NO), hydrogen peroxide (H2O2), and their ferric-reducing antioxidant potentials (FRAPs) were measured.
Results
The ethanol extract of H. argentea had the highest content of phenolics (66.71 ± 2.71 mg gallic acid equivalent/g) and tannins (1.18 ± 0.07 mg TAE/g), while the ethanol extract of D. thunbergii gave higher contents of flavonoids and proanthocyanidins (62.21 ± 1.75 mg Qe/g and 432.62 ± 2.43 mg Ca/g, respectively). Flavonols were the most predominant in the aqueous extract of H. argentea (25.51 ± 1.92 mg Qe/g). We observed a concentration-dependent response in the ABTS- and H2O2-scavenging activities and FRAP values of the extracts and standards (Vitamin C, butylated hydroxytoluene, and rutin). The ethanol extracts of both plants generally demonstrated better antioxidant activities against H2O2, NO, and ABTS while also possessing better reducing power than the aqueous extracts. The aqueous extract of D. thunbergii, however, showed the best DPPH scavenging activity.
Conclusion
The higher content of phytochemicals and antioxidant capacity obtained for the ethanol extracts of D. thunbergii and H. argentea may prove to be valuable information in selecting suitable extraction solvents for the medicinal applications of both plants.
SUMMARY
Ethanol extracts of Hypoxis argentea had the highest levels of phenolics and tannins
Ethanol extracts of Dianthus thunbergii had the highest levels of flavonoids and proanthocyanidins
Ethanol extracts of both plants possess better antioxidant activityagainst hydrogen peroxide, nitric oxide, and ABTS as well as higher reducingpower than the aqueous extracts
Aqueous extract of Dianthus thunbergii had the highest free radical scavenging activity as measured with DPPH.
Abbreviations used: ABTS: 2'-azino-bis (3-ethylbenthiazoline-6-sulfonic acid); BHT: Butylated hydroxytoluene; DPPH: 1,1 diphenyl-2-picrylhydrazyl; DTA: Dianthus thunbergii aqueous extract (16.6%); DTE: Dianthus thunbergii ethanol extract (2.4%); Fe³⁺-TPTZ: Ferric tripyridyltriazine; FRAP: Ferric-reducing antioxidant potentials; GAE: Gallic acid equivalent; HAA: Hypoxis argentea aqueous extract (3.2%); HAE: Hypoxis argentea ethanol extract (1.8%); Qe: Quercetin equivalence; ROS: Reactive oxygen species; TBA: Thiobarbituric acid;TCA: Trichloroacetic acid.
As a leading cause of global mortality, cancer frequently cannot be cured due to the development of drug resistance. Therefore, novel drugs are required. Naturally occurring anthraquinones are mostly present in Rumex and Rhamnus species and are of interest because of their structural similarity to anthracyclines as well established anticancer drugs. In the present study, we focused on the structural elucidation of phytochemicals from R. acetosella as well as the investigation of cytotoxicity and modes of action of the main anthraquinone aglycons (emodin, Aloe-emodin, physcion, rhein). Resazurin reduction and protease viability marker assays were conducted to test their cytotoxicity. Microarray-based gene expression profiling was performed to identify cellular pathways affected by the compounds, which was validated by qPCR analyses and functional assays. Flow cytometry was used to measure cell cycle distribution, apoptosis and necrosis, induction of reactive oxygen species (ROS) and disruption of mitochondrial membrane potential (MMP). The comet assay was used to detect DNA damage. Aloe-emodin as the most cytotoxic compound revealed IC50 values from 9.872 μM to 22.3 μM in drug-sensitive wild-type cell lines and from 11.19 μM to 33.76 μM in drug-resistant sublines, was selected to investigate its mechanism against cancer. Aloe-emodin-induced S phase arrest, ROS generation, DNA damage and apoptosis. Microarray hybridization revealed a profile of deregulated genes in Aloe-emodin-treated CCRF-CEM cells with diverse functions such as cell death and survival, cellular growth and proliferation, cellular development, gene expression, cellular function and maintenance. Aloe-emodin as well as R. acetosella deserve further investigations as possible antineoplastic drug candidates.
Objective: To explore anti-hyperalgesic properties of methanol extract of Piptadeniastrum africanum stem bark (PAME) and it possible action mechanism. Methods: PAME was tested on carrageenan induced hyperalgesia using plantar test (thermal) and analgesymeter (mechanical) in rats, on prostaglandin E2 (PGE2) induced mechanical hyperalgesia and vincristine induced neuropathic pain in rat, both with analgesymeter. Modulators of NO/ cGMP/K+ channel pathway and endogenous opioids receptor antagonists and/or agonists were used to determine the possible action mechanism of PAME. Results: PAME significantly decreased carrageenan induced thermal and mechanical hyperalgesia, as well as PGE2 induced mechanical hyperalgesia. PAME significantly protected the animals against the installation of neuropathic pain. Anti-nociception activity produced by PAME was significantly blocked in animals pre treated with all the antagonists (naloxone, NW-nitro-L-arginine methyl ester (L-NAME), methylene blue and glibenclamide). Conclusions: Results of this study reveal that, PAME administrate orally, can induce anti-hyperalgesic action against installation of inflammatory pain as well as neuropathic pain. The mechanism underlying PAME anti-hyperalgesic effect could probably be associated with an activation of opioid receptors and NO/cGMP/K+ channel pathway.
Various parts of sea buckthorn [Elaeagnus rhamnoides (L.) A. Nelson], particularly the berries, known also as seaberries, or Siberian pineapples, are characterized by a unique composition of bioactive compounds: phenolic compounds, vitamins (especially vitamin C), unsaturated fatty acids, and phytosterols such as beta-sitosterol. These berries, together with the juices, jams, and oils made from them, have a range of beneficial antioxidant, anti-inflammatory, and anticancer effects. This short review discusses whether sea buckthorn may represent a “golden mean” for the treatment of cancers: It has anti-proliferation properties and can induce apoptosis and stimulate the immune system, and sea buckthorn oil counteracts many side effects of chemotherapy by restoring kidney and liver function, increasing appetite, and keeping patients in general good health. Although the anticancer activity of sea buckthorn has been confirmed by many in vitro and animal in vivo studies, the treatment and prophylactic doses for humans are unknown. Therefore, greater attention should be paid to the development of well-controlled and high-quality clinical experiments in this area.
Objective: This study was carried out to investigate the antimigration activity of Zanthoxylum acanthopodium DC.
in the 4T1 breast cancer cell line. Methods: Zanthoxylum acanthopodium DC. fruit powder was extracted by maceration
method with n-hexane and ethylacetate solvents. Cytotoxicity and proliferation were assessed using the MTT method
and the cell cycle by flow cytometry. In addition, wound healing assays were conducted by a microscopic method,
and expression of COX-2 and VEGFR-2 were determined using qRT-PCR. Results: The IC50 of the ethylacetate
fraction (EAF) was 48.1 ± 1.06 μg/mL. The EAE at a concentration 10 μg/mL with viable cells was 62.3 ± 0.28%
after 72 h incubation, with accumulation in the G2-M phase, inhibition of cell migration in the wound healing assay,
and decrease in expression of COX-2 (0.62 ± 0.01) and VEGFR-2 (0.39 ± 0.003). Conclusion: The results reveal that
an ethylacetate fraction of Zanthoxylum acanthopodium DC. fruits provides effective antimigration effects. Further
studies are now planned to assess the potential of the ethylacetate fraction to inhibit angiogenesis in breast cancer and
determine underlying mechanisms.
Mosquito control with naturally derived herbal insecticides has gained much momentum, with the increased insecticide resistance of vectors and the multiple infectious diseases spread by them. Yet, recent studies also suggest that mosquitoes could probably transmit some cancerous cells or cancer-causing viruses from one individual to another between their blood meals. The current research thus focused on the screening and characterization of novel plants with both mosquitocidal and anticancerous properties. Accordingly, different solvent extracts of Hypericum japonicum, a key plant in Chinese medicine, were screened for its larvicidal efficacy using the fourth instar larvae of Aedes aegypti (major vector of Dengue and chikungunya). Methanolic extracts of the plant showed effective larvicidal property with LC50 7.37 ppm and LC9011.59 ppm values. The anticancerous property of the plant extract was also evaluated by in vitro cytotoxicity assay against Daltons Lymphoma Ascites (DLA) cells. The results indicated that H. japonicum plant extracts at very low concentrations of LC500.95 ppm and LC901.85 ppm were potent cytotoxic agents. To the best of our knowledge, this is the first and the foremost report of Hypericum japonicum as a potent mosquitocidal and anticancerous agent. Identification and characterization of such plant-derived bioactive plants thus could serve as a double-headed sword against the spread of infectious diseases and cancer.
Background:
Medicinal plants (MPs) used by traditional healers (THs) were investigated in Megera and adjacent subdistricts (kebeles) of Dalle District, Sidama Zone, southern Ethiopia. The objective of the study was to identify and record MPs and their traditional uses in the treatment of various human ailments with emphasis on malignancies and other most frequently reported diseases.
Methods:
Traditional medicinal knowledge held by 20 THs was investigated following standard ethnobotanical approaches. Guided field walk, free listing, rigorous individual interviews with extended discussions, and local market surveys were employed to obtain information. Preference rankings, paired comparisons, use value (UV) index, frequency of citation (FC), fidelity level (FL), and informant consensus factor (ICF) matrices were engaged to identify MPs used to treat malignancies and the other most prevalent human ailments.
Results:
Seventy-one MP species belonging to 63 genera and 46 families, used to treat 39 human ailments, were recorded. A high proportion of the species recovered was shrubs (35.2%); while 64.7% were retrieved from the wild habitat. Leaves were the main part of the MPs used (42.9%), followed by fruits/seeds (13%); all preparations were made from fresh materials and about 27.9% involved boiling. The frequent route of delivery was oral (77.9%), followed by dermal (17.6%). About 40.8% of the MPs were used for treating two or more ailments. About 19.7% of the MPs were used to treat malignancies (ICF = 0.86) among which the plant species Sideroxylon oxyacanthum was the most frequently used (FL = 70%). The species Podocarpus falcatus and Hagenia abyssinica were preferred to treat jaundice and deworm in helminthiases, respectively.
Conclusion:
The study area is very rich in plant biodiversity, and the herbal medicine is an integral part of the traditional healthcare system. The MPs are exposed to various destructive anthropogenic activities, and this situation calls for integrated conservation measures. Furthermore, the rich ethnomedicinal knowledge held by the Sidama community at large and TM practitioners, in particular, needs an in-depth study and documentation. Investigations of the MPs with high ICF, FL, and UVs to malignancies, jaundice, and helminthiases could possibly contribute to future drug development efforts.
With an increasing number of cancer patients seeking an improved quality of life, complementary and alternative therapies are becoming more common ways to achieve such improvements. The potential risks of concurrent administration are serious and must be addressed. However, comprehensive evidence for the risks and benefits of combining anticancer drugs with traditional herbs is rare. Pharmacokinetic investigations are an efficient way to understand the influence of concomitant remedies. Therefore, this study aimed to collect the results of pharmacokinetic studies relating to the concurrent use of cancer chemotherapy and complementary and alternative therapies. According to the National Health Insurance (NHI) database in Taiwan and several publications, the three most commonly prescribed formulations for cancer patients are Xiang-Sha-Liu-Jun-Zi-Tang, Jia-Wei-Xiao-Yao-San and Bu-Zhong-Yi-Qi-Tang. The three most commonly prescribed single herbs for cancer patients are Hedyotis diffusa, Scutellaria barbata, and Astragalus membranaceus. Few studies have discussed herb–drug interactions involving these herbs from a pharmacokinetics perspective. Here, we reviewed Jia-Wei-Xiao-Yao-San, Long-Dan-Xie-Gan-Tang, Curcuma longa and milk thistle to provide information based on pharmacokinetic evidence for healthcare professionals to use in educating patients about the risks of the concomitant use of various remedies.
Background: Cancer is one of the major problems affecting public health worldwide. As other cultures, the populations of the Near East rely on medicinal herbs and their preparations to fight cancer.
Methods: We compiled data derived from historical ethnopharmacological information as well as in vitro and in vivo results and clinical findings extracted from different literature databases including (PubMed, Scopus, Web of Science, and Google Scholar) during the past two decades.
Results: In this survey, we analyzed the huge amount of data available on anticancer ethnopharmacological sources used in the Near East. Medicinal herbs are the most dominant ethnopharmacological formula used among cancer’s patients in the Near East. The data obtained highlight for the first time the most commonly used medicinal plants in the Near East area for cancer treatment illustrating their importance as natural anticancer agents. The literature survey reveals that various Arum species, various Artemisia species, Calotropis procera, Citrullus colocynthis, Nigella sativa, Pulicaria crispa, various Urtica species, Withania somnifera, and others belong to the most frequently used plants among cancer patients in the Near East countries. Molecular modes of action that have been investigated for plant extracts and isolated compounds from Near East include cell cycle arrest and apoptosis induction with participation of major player in these processes such as p53 and p21, Bcl-2, Bax, cytochrome c release, poly (ADP-ribose) polymerase cleavage, activation of caspases, etc.
Conclusion: The ethnopharmacology of the Near East was influenced by Arabic and Islamic medicine and might be promising for developing new natural and safe anticancer agents. Further research is required to elucidate their cellular and molecular mechanisms and to estimate their clinical activity.
Potentilla discolor has been used in traditional Chinese medicine for the treatment of hyperglycemia. However, the potential role of Potentilla discolor against cancer and its mode of action remain to be fully elucidated. The present study explored the apoptotic effect of methanol extract of Potentilla discolor (MEPD) in human mucoepidermoid carcinoma (MEC) cell lines of salivary glands. MEPD markedly suppressed the growth and induced apoptotic cell death in MC3 and YD15 cells. MEPD treatment significantly upregulated the expression of PUMA and reduced STAT3 phosphorylation. Overexpression of STAT3 partially recovered the growth of MEC cells inhibited by MEPD. In addition, dephosphorylation of STAT3 by cryptotanshinone (a potent STAT3 inhibitor) was sufficient to inhibit the growth of MEC cells and induce apoptosis via affecting PUMA protein. These results suggest that MEPD has a potential anticancer property via the STAT3/PUMA signaling axis in human MEC cells of salivary gland.
Cancer is a multistage process resulting in an uncontrolled and abrupt division of cells and is one of the leading causes of mortality. The cases reported and the predictions for the near future are unthinkable. Food and Drug Administration data showed that 40% of the approved molecules are natural compounds or inspired by them, from which, 74% are used in anticancer therapy. In fact, natural products are viewed as more biologically friendly, that is less toxic to normal cells. In this review, the most recent and successful cases of secondary metabolites, including alkaloid, diterpene, triterpene and polyphenolic type compounds, with great anticancer potential are discussed. Focusing on the ones that are in clinical trial development or already used in anticancer therapy, therefore successful cases such as paclitaxel and homoharringtonine (in clinical use), curcumin and ingenol mebutate (in clinical trials) will be addressed. Each compound's natural source, the most important steps in their discovery, their therapeutic targets, as well as the main structural modifications that can improve anticancer properties will be discussed in order to show the role of plants as a source of effective and safe anticancer drugs.
Leaves and roots of Acanthospermum australe (Asteraceae) have been used in Brazilian folk medicine for the treatment of various ailments including diarrhea, skin diseases, blennorrhagia, dyspepsia, parasitic worms and malaria. The aim of study was to characterize the chemical profiles of the aqueous and hydroalcoholic extracts of leaves and roots of A. australe, and to evaluate their antimicrobial activities against diarrhea-inducing bacteria (Enterococcus faecalis, Shigella dysenteriae and Yersinia enterocolitica), as well as their cytotoxic properties. Aqueous leaf extracts were obtained by infusion, while aqueous root extracts were obtained by decoction. The hydroalcoholic leaf and root extracts were prepared by maceration in 90% ethanol for 3 days. Antimicrobial activity was assessed using standard techniques and cytotoxicity was evaluated using Chinese hamster ovary cells CHO-K1. Chemical analysis revealed the presence of tannins, flavonoids, saponins and phenolic compounds in the extracts. Although root extracts were not effective against E. faecalis, leaf extracts at concentrations of 20 mg/mL exhibited bactericidal activities against this microorganism. The hydroalcoholic root extract was unique in presenting a bactericidal effect against S. dysenteriae. None of the extracts showed bacteriostatic or bactericidal activities against Y. enterocolitica. The results presented herein demonstrate that the Gram-positive E. faecalis and the Gram-negative S. dysenteriae were susceptible to A. australe extracts, although bacteriostatic/bactericidal activities were only observed at concentrations considered too high for clinical application. Our results support the ethnopharmacological use of A. australe in the treatment of gastrointestinal disorders, particularly diarrhea caused by infectious bacteria, although further studies are required to determine the anti-diarrhea effects and the toxicities of the extracts in vivo.
Over the last two decades, inducing DNA damage of cancer cells by natural medicines has become a research hotspot in the field of cancer treatment. Although various natural medicines have anticancer effects, very few studies have been conducted to explore the anti-cancer effect of pine needle oil. In the present study, the role of pine needle oil in inducing G2/M arrest in HepG2 cells was investigated. The data revealed that pine needle oil could induce DNA damage in a dose-dependent manner. In the pine needle oil-treated HepG2 cells, the protein levels of phosphorylated (p)-ataxia-telangiectasia mutated (ATM), γ-H2A histone family, member X, p-p53, p-checkpoint kinase 2 and p-cell division cycle 25C were evidently increased, indicating that pine needle oil facilitated G2/M arrest in HepG2 cells through the ATM pathway. In response to the treatment with pine needle oil, ATM was activated in HepG2 cells, which subsequently phosphorylated downstream targets and induced G2/M arrest. In summary, the data of the present study indicated that pine needle oil induces G2/M arrest in HepG2 cells by facilitating ATM activation.
Cancer is a frightful disease and represents one of the biggest health-care issues for the human race and demands a proactive strategy for cure. Plants are reservoirs for novel chemical entities and provide a promising line for research on cancer. Hitherto, being effective, chemotherapy is accompanied by certain unbearable side effects. Nevertheless, plants and plant derived products is a revolutionizing field as these are Simple, safer, eco-friendly, low-cost, fast, and less toxic as compared with conventional treatment methods. Phytochemicals are selective in their functions and acts specifically on tumor cells without affecting normal cells. Carcinogenesis is complex phenomena that involves many signaling cascades. Phytochemicals are considered suitable candidates for anticancer drug development due to their pleiotropic actions on target events with multiple manners. The research is in progress for developing potential candidates (those can block or slow down the growth of cancer cells without any side effects) from these phytochemicals. Many phytochemicals and their derived analogs have been identified as potential candidates for anticancer therapy. Effort has been made through this comprehensive review to highlight the recent developments and milestones achieved in cancer therapies using phytomolecules with their mechanism of action on nuclear and cellular factors. Furthermore, drugs for cancer treatment and their limitations have also been discussed.
Background
Cancer is a leading cause of death world-wide, with approximately 17.5 million new cases and 8.7 million cancer related deaths in 2015. The problems of poor selectivity and severe side effects of the available anticancer drugs, have demanded the need for the development of safer and more effective chemotherapeutic agents. The present study was aimed at determining the cytotoxicities of 31 medicinal plants extracts, used in Nigerian ethnomedicine for the treatment of cancer.
Methods
The plant extracts were screened for cytotoxicity, using the brine shrimp lethality assay (BSLA) and MTT cytotoxicity assay. Rhabdomyosarcoma (RD) cell line, normal Vero cell line and the normal prostate (PNT2) cell line were used for the MTT assay, while Artemia salina nauplii was used for the BSLA. The phytochemical composition of the active plant extracts was determined by high performance liquid chromatography (HPLC) analysis.
Results
The extract of Eluesine indica (L.) Gaertn (Poaceae), with a LC50 value of 76.3 μg/mL, had the highest cytotoxicity on the brine shrimp larvae compared to cyclophosphamide (LC50 = 101.3 μg/mL). Two plants extracts, Macaranga barteri Mull. Arg. (Euphorbiaceae) and Calliandra portoricensis (Jacq.) Benth (Leguminosae) exhibited significant cytotoxic activity against the RD cell line and had comparable lethal activity on the brine shrimps. Further cytotoxic investigation showed that the dichloromethane fraction of Macaranga barteri (DMB) and the ethyl acetate fraction of Calliandra portoricensis (ECP), exhibited approximately 6-fold and 4-fold activity, respectively, compared to cyclophosphamide on RD cell line. Determination of selective index (SI) using Vero and PNT2 cell line indicated that DMB and ECP displayed a high degree of selectivity against the cancer cell under investigation. HPLC analysis showed that 3,5dicaffeoylquinic acid, acteoside, kampferol-7-O-glucoside and bastadin 11 were the major components of DMB while the major components of ECP were neurolenin B, nigrosporolide and trans-geranic acid.
Conclusion
The results demonstrate the cytotoxicity of Macaranga barteri and Calliandra portoricensis extracts, which are used in Nigerian folklore for cancer treatment.
Background
Research of natural products from traditionally used medicinal plants to fight against the human ailments is fetching attention of researchers worldwide. Bidens pilosa Linn. var. Radiata (Asteraceae) is well known for its folkloric medicinal use against various diseases from many decades. Mizoram, North East India, has high plant diversity and the use of this plant as herbal medicine is deep rooted in the local tribes. The present study was executed to understand the pharmacological potential of B. pilosa leaves extract. Methods
The antimicrobial potential was determined using agar well diffusion and broth microdilution method against bacterial and yeast pathogens. Cytotoxicity was evaluated using MTT and apoptotic DNA fragmentation assays. Further, the antioxidant ability of the extract was analysed using DPPH and ABTS free radical scavenging assay. Mosquitocidal activity was evaluated against third in-star larvae of C. quinquefasciatus using dose response and time response larvicidal bioassay. Additionally, the major phenolic and volatile compounds were determined using UHPLC-QqQLIT-MS/MS and GC/MS respectively. ResultsWe found that the extract showed highest antimicrobial activity against E. coli (MIC 80 μg/mL and IC50 110.04 μg/mL) and showed significant cytotoxicity against human epidermoid carcinoma (KB-3-1) cells with IC50 values of 99.56 μg/mL among the tested cancer cell lines.The IC50 values for scavenging DPPH and ABTS was 80.45 μg/mL and 171.6 μg/mL respectively. The extract also showed the high phenolics (72 μg GAE/mg extract) and flavonoids (123.3 μg Quercetin /mg extract). Lastly, five bioactive and six volatile compounds were detected using UHPLC-QqQLIT-MS/MS and GC-MS respectively which may be responsible for the plant’s bioactivities. An anticancerous compound, Paclitaxel was detected and quantified for the first time from B. pilosa leaves extract, which further showed the anticancerous potential of the tested extract. Conclusion
On the basis of the present investigation, we propose that the leaf extract of B. pilosa might be a good candidate for the search of efficient environment friendly natural bioactive agent and pharmaceutically important compounds.
Luteolin 5-O-glucoside is the major flavonoid from Korean thistle, Cirsium maackii. We previously reported the anti-inflammatory activities of luteolin 5-O-glucoside in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells. In this study, we determined the anti-inflammatory mechanisms of luteolin 5-O-glucoside through the inhibition of nitric oxide (NO) production in vitro and in vivo. Results revealed that luteolin 5-O-glucoside dosedependently inhibited NO production and expression of iNOS and COX-2 in LPS-induced RAW 264.7 cells. Luteolin 5-O-glucoside also significantly inhibited the translocation of NF-κB, the activation of MAPKs, and ROS generation in LPS-induced RAW 264.7 cells. In addition, protein expressions of Nrf-2 and HO-1 were also upregulated by luteolin 5-O-glucoside treatment. Moreover, luteolin 5-O-glucoside inhibited λ-carrageenaninduced mouse paw edema by 65.34% and 48.31% at doses of 50 and 100 mg/kg body weight, respectively. These findings indicate potential anti-inflammatory effect of luteolin 5-O-glucoside particularly by downregulating NF-κB and upregulating HO-1/Nrf-2 pathway.
Milk thistle (Silybum marianum) is a medicinal plant that has been used for thousands of years as a remedy for a variety of ailments. The main component of S. marianum fruit extract (silymarin) is a flavonolignan called silybin, which is not only the major silymarin element but is also the most active ingredient of this extract, which has been confirmed in various studies. This compound belongs to the flavonoid group known as flavonolignans. Silybin’s structure consists in two main units. The first is based on a taxifolin, the second a phenyllpropanoid unit, which in this case is conyferil alcohol. These two units are linked together into one structure by an oxeran ring. Since the 1970s, silybin has been regarded in official medicine as a substance with hepatoprotective properties. There is a large body of research that demonstrates silybin’s many other healthy properties, but there are still a lack of papers focused on its molecular structure, chemistry, metabolism, and novel form of administration. Therefore, the aim of this paper is a literature review presenting and systematizing our knowledge of the silybin molecule, with particular emphasis on its structure, chemistry, bioavailability, and metabolism.
Euclea undulata (E. undulata) is traditionally used for the treatment of body pains, chest complaints, cough, diabetes, diarrhoea, headaches, heart diseases and toothaches in southern Africa. This study was aimed at reviewing the botany, ethnopharmacology and biological activities of E. undulata in southern Africa. Results presented in this study are based on review of literature using search engines such as Science Direct, Springerlink, Scopus, PubMed, Web of Science, BioMed Central and Google Scholar. Herbal medicine is prepared from the decoctions of the roots, bark and leaves, and extracts of these plant parts have demonstrated anticholinesterase, anti-inflammatory, antimicrobial, antimycobacterial, antiplasmodial, antioxidant and hypoglycaemic activities. Multiple classes of phytochemical compounds such alkaloids, diterpenes, fatty acids, flavonoids, glycosides, naphthoquinones, phenolics, phytosterols, reducing sugars, saponins and tannins have been isolated from the species. E. undulata has a lot of potential as herbal medicine in tropical Africa, and advanced research is required aimed at correlating its medicinal uses with the phytochemistry and pharmacological properties.
Rosa laevigata is a white aromatic rose inhabitant to Southern China and Taiwan and growing offensively as invasive in the United States of America. It is herbaceous climbing shrub, growing over the other shrubs and reaching upto 5-10 metre in height. In 1780’s, it gained its English name Cherokee rose from America. This review was aimed to analyze various active secondary metabolites of Rosa laevigata with their medicinal value. The study infers that plant possess novel secondary metabolites i.e., polysaccharides, flavonoids, steroids, tannins, laevigatins E, F, G, triterpenoids, 11α-hydroxytormentic acid, 2α-methoxyursolic acid, 6-methoxy-β-glucopyranosyl ester, tormentic acid and 5α-diol 3-O-β-d-glucopyranoside with their antibacterial, anticancer, astringent, depurative and anti-inflammatory activities. A profound efforts has been done in past to address the active secondary metabolites, but still consistent struggles are required to explore the volatile compounds present in Rosa laevigata and their medicinal and therapeutic values should be investigated in future.
Background: Melanoma is a metastatic type of skin cancer that is difficult to treat and the majority of efforts are directed to the design of new drugs. Medicinal Plants have been the primary source of medicines since life on earth; more than 50% of existing cancer treatments is derived from plants. Bauhinia variegata is well-known
medicinal plant used from the ancient era to till date for their medicinal values. Scientific literatures have not
documented any evidence of the antitumour potential of Bauhinia variegata against B16F10 melanoma tumor
model in C57BL mice. The present investigation was undertaken to explore the antitumour activity of Leaf, stem
bark and flower extract of Bauhinia variegata against B16F10 melanoma tumour model in C57BL mice.
Methods: Hydro-methanolic extract prepared from the leaf, stem bark and flower of Bauhinia variegata were
assessed for their antitumor activity. The extracts at doses of 500 and 750 mg/kg b.wt. were given orally along with cyclophosphamide (chemotherapeutic drug) for 40 days for exploring antitumor activity against melanoma tumor (B16F10) in C57BL mice. Inhibition of tumor growth, increase in survival time of animal with treatment,
histopathological studies and antioxidant parameter were determined.
Results: The Present investigation showed significant effect of the B. variegata L. in preventing melanoma tumor by B16F10 cell line in C57BL/6 mice. As compared with the tumour control group, the remarkable results especially in the group which received B. variegata extract and cyclophosphamide together were obtained for all of the measured parameters. Dose dependent response was observed in tumor volume, inhibition rate, life span time and antioxidant parameter of extracts. Combination treatment of cyclophosphamide and B. variegata extracts showed more pronounced effect.
Conclusions: These findings suggest that B. variegata hydromethanolic extract may contain bioactive compoundsof potential therapeutic significance which are relatively safe from toxic effects, and can compromise the medicinal use of this plant in folk medicine.
ABSTRACT
Background: Phytochemical and Biological studies are always needed to define chemical composition, bioactivity and toxicity of plants from folk medicines before integrating them into conventional medicines.
Here we compared phytochemical composition and antihyperglycemic activity of some plants used in Kisangani to treat diabetes. Methods: The plants tested are Aloe vera (AV), Bidens pilosa (BP), Cassia alata
(CA), Cassia occidentalis (CO), Catharanthus roseus pink flower (CRp), Catharanthus roseus white flower or alba (CRw), Mangifera indica (MI), Morinda lucida (ML), Morinda morindoides (MM), Panda oleosa (PO), Terminalia catappa (TC), and Vernonia amygdalina (VA). Their content in polyphenols, saponins, alkaloids and mineral ash were compared. Hyperglycemia was induced in rabbits by oral glucose tolerance test with glibenclamide 0.2 mg/kg as reference. Blood glucose level was assayed by Folin-Wu photometric method.
The mean percentage in glucose level reduction (MPR) was calculated from control untreated animals. The relative potency of each extract (RP) was calculated from glibenclamide MPR taken as 100%. Results: Flavonoids, tannins and saponins, were the main components; alkaloids were found only in CRp, CRw, ML and MM. The water content varied from 67% to 88%; Total ashes content was lower in roots (9%) than other parts (11-16%). Glibenclamide gave MPR=56.8% and RP=100%. MPR and RP for plant extracts were, ML(29.8%; 52.4%), CA(31.9%; 56.2%), MI(46.6%; 81.9%), MM(46.6%; 81.9%), TC(47.2%; 83.1%), VA(49.4%; 86.9%),
CO(54.4%; 95.8%), CRw(57.4%; 101.0%), BP(60.8%; 107.0%), CRp(63.2%; 111.1%), AV(64.5%; 113.4%), PO(83.2%;
146.3%).Conclusion: All plants but Panda oleosa have been studied by others; the main phytochemical groups reported have been confirmed in the local species. All plants exhibited some antihyperglycem activity, differing however by their relative potency.
Conventional treatments have varying degrees of success in ameliorating cancer. But administration of chemotherapeutic drugs can often cause side effects in afflicted individuals, exacerbating the morbidity and mortality associated with this disease. Efforts are being made all over the world to develop new and better anti-cancer drugs from the vast repertoire of plant-derived phytoconstituents available in nature. At least four groups of plant-derived annti-neoplastic drugs are already available commercially. In this review, the potential of the angiospermic plant Hygrophila auriculata (Schumach.) Heine as a source of anti-cancer drug has been discussed. The crude extract of the plant has shown anti-tumour efficacy in Ehrlich ascites carcinoma and Sarcoma-180, MDA-MB-435S and hepatocarcinogenesis in male Wistar rats. Five phytoconstituents of H. auriculata have been reported to possess extensive anti-cancer potential and exhibit anti-tumour effects in many different cell lines and in many different types of cancer.
The dichloromethane extract of the roots of Jatropha dioica afforded riolozatrione (1) and a C-6 epimer of riolozatrione, 6-epi-riolozatrione (2), as a new structure and only the second reported riolozane diterpenoid. The two known diterpenoids jatrophatrione (3) and citlalitrione (4) were also isolated and characterized. Both epimers 1 and 2 are genuine plant constituents, with 2 likely being the biosynthesis precursor of 1 due to the tendency for the quantitative transformation of 2 into 1 under base catalysis. The structural characterization and distinction of the stereoisomers utilized ¹H iterative full-spin analysis, yielding complete J-correlation maps that were represented as quantum interaction and linkage tables. The absolute configuration of compounds 1–4 was established by means of vibrational circular dichroism and via X-ray diffraction analysis for 1, 2, and 4. Additionally, the cytotoxic and antiherpetic in vitro activities of the isolates were evaluated.
There is an increasing interest in natural plant products as a source of new pharmaceuticals and other biologically- active compounds. This is a timely review of the latest advances and trends in a field which is becoming a commercially significant area of investigation for the pharmaceutical industry. The pharmacological and phytochemical aspects of different preparations from vegetable sources is a truly interdisciplinary field and this book includes information on ethnopharmacology, selection, isolation and structure determination of plant-derived natural products. Many examples of different bioassyas (in vitro and in vovo test systems) and pharmacological tests are given, providing the reader with an insight into what is currently possible in the study of bioactive plant material.
From the stem bark of Dracaena draco, three new compounds, namely, draconins A-C (13), were isolated, along with 17 known compounds. The structures of the new compounds isolated were elucidated on the basis of spectroscopic data interpretation. Several of the isolated compounds showed potent cytotoxic activities measured on the human leukemia cell line HL-60 (IC50’s from 2.0 to 9.7 íM at 72 h). The mechanism by which compounds 1 and 2 display their cytostatic properties is through induction of cell death by apoptosis, as evaluated by fluorescence microscopy and DNA fragmentation.
Importance of herbs (medicinal plants) can hardly be overemphasized. They are exploited for manyfold applications, ranging from phytopharmaceuticals, to nutraceuticals, to cosmetics and many others. Keeping in view the richness of herbs and their vast potential, this book collates the most up-to-date knowledge of important herbs and herbals. The book also gives an overview of some issues causing hindrance in the promotion of herbals. This book attempts to compile the rich experience of experts working on various herbs. New age single plant species, having multiple medicinal traits worth exploiting i.e. Hippophae rhamnoides (seabuckthorn), and Morinda citrifolia (noni) also find place as full chapters in the book. © Springer Nature Singapore Pte Ltd. 2018. All rights reserved.
Nature is an attractive source of therapeutic and preventive compounds, and with such chemical diversity found in millions of species of plants, over 60% of currently used anticancer agents are derived from natural sources. Cancer Inhibitors from Chinese Natural Medicines summarizes new advancements in the experimental and clinical research of a selection of promising cancer inhibitors. It focuses on the latest scientific investigations of 238 Chinese herbs and discusses important aspects, including the types of inhibitors in the herbs, level of potency, mechanisms, and the advances in modification and formulation. Formulations from nano-particulates and immunotoxins in cancer inhibitors are also included in this comprehensive resource.
Objectives: The objective was to determine the in-vitro effect of extracts from 19 Ethiopian plant species and four pure pyrrolizidine alkaloids on bloodstream forms of Trypanosoma brucei brucei and human leukaemia HL-60 cells. Methods: Crude plant extracts were prepared using methanol and dichloromethane. The alkaloidal extracts from Solanecio angulatus flowers were prepared with and without zinc reduction using the acid-base extraction method. Cell proliferation inhibitory activity of the extracts and compounds was assessed using Alamarblue. Key findings: The most active extract was the dichloromethane extract of Solanecio angulatus flowers, with an IC50 value of 12.17 μg/ml. The best selectivity index (SI > 41.08) was obtained for the same extract determined with HL-60 cells. The reduced alkaloidal extract prepared from S. angulatus flowers and after acid-base extraction showed more antitrypanosomal activity than unreduced alkaloidal extract with an IC50 value of 14.35 μg/ml and with a selectivity index of 12.23. The second most active extract was the dichloromethane extract of Crotalaria phillipsiae twigs with an IC50 value of 12.67 μg/ml and a selectivity index of 34.35. Most of the other extracts tested showed moderate antitrypanosomal activities to variable extents. Among the four pure pyrrolizidine alkaloids tested, senecionine showed moderate antitrypanosomal activity with an IC50 value of 41.78 μg/ml. Conclusions: Solanecio angulatus (flowers) and Crotalaria phillipsiae (twigs) could serve as sources of novel trypanocidal compounds for the treatment of trypanosomiasis.
Twenty-eight naturally occurring Cephalotaxus tropone analogues, including 19 previously undescribed ones, were identified from Cephalotaxus fortunei Hook. var. alpina H. L. Li and C. lanceolata K. M. Feng. The presence of the C20 cephinoids A-E revealed that these tropones were assigned to the norditerpenoids and were perhaps derived from labdane-type diterpenoids. These norditerpenoids showed excellent cytotoxicity against human cancer cells (IC50, 20-0.1 μM) in vitro. The SAR (structure-activity relationship) analysis disclosed that the tropone moiety and the lactone ring were crucial structural features for the observed activities. Further SAR analyses led to a new candidate, cephinoid H, which demonstrated an inhibition of 49.0% by administration to zebrafish at a dose of 60.0 ng/mL, compared to cisplatin (DDP, 22.4%) at 15.0 μg/mL. These compounds might affect the NF-κB signaling pathway rather than binding to microtubules. Additionally, the isolated norditerpenoids showed almost equal anti-inflammatory activities compared to the positive control, MG132.
Objectives:
Barleria cristata (Family: Acanthaceae), commonly known as Philippine violet, is used in different ethnomedical systems for the treatment of a wide range of ailments. This review aimed to provide a scientific overview of B. cristata with reference to its ethnobotanical aspects, geographical distribution, medicinal uses, phytochemistry and pharmacological activity, and critical analyses research gaps and future research opportunities for investigations on this plant.
Key findings:
Ethnomedical uses of the plant have been observed in lungs disorders, inflammatory conditions, toothache, anaemia, snake bite, diabetes and tuberculosis. The exhaustive bibliographic research carried out on this plant revealed that the plant parts are rich in various phytochemical constituents including triterpenes, phenolic compounds, glycosides and flavonoids type phenolic compounds. Furthermore, the plant was also investigated in terms of its anti-inflammatory, antibacterial, antidiabetic, antifungal, hepatoprotective and antioxidant activity.
Conclusions:
This review confirms that B. cristata is a potential herb for the treatment of a wide range of diseases especially lung disorders and inflammatory conditions. Modern pharmacological studies have also validated many ethnobotanical uses of B. cristata, though data regarding many aspects of this plant such as mechanism of action, adverse effects of extracts and active compounds are still limited which call for additional studies.
This study investigated the effects of purple rice extract (PRE ) on inflammation-related colon carcinogenesis. Administration of PRE 1 g/kg bodyweight reduced both the number (39.05%) and size of aberrant crypt foci (ACF) (14.28%) in the colons of rats that received dimethylhydrazine (DMH) initiation with promotion by dextran sulfate sodium (DSS) (P<0.05) with the reduction of TNF-α expression in colonic epithelial cells. On the other hand, PRE could suppress the expression of both TNF-α and IL-6 in RAW 264.7 cells activated by lipopolysaccharide (LPS) at both the mRNA and protein levels. Moreover it could reduce the expression of TNF-α and IL-1β mRNA in inflamed HT-29. These findings suggested that PRE is able to modulate the inflammatory process in both activated macrophages and colon cancer cells. Therefore, PRE suppressed macrophage activation and colon cancer cell line response to inflammation and modulated of inflammation induced ACF progression in the rat colon.
The aim of the present study is to isolate bioactive compounds from the roots of Piper sarmentosum and examine the mechanism of action using human breast cancer cell line (MDA-MB-231). Bioassay guided-fractionation of methanolic extract led to the isolation of asaricin (1) and isoasarone (2). Asaricin (1) and isoasarone (2) had significant cytotoxicity towards MDA-MB-231. MCF-10A (human normal breast epithelial cells) cells are less sensitive than MDA-MB-231, but they respond to the treatment with the same unit of measurement. Both compounds increase reactive oxygen species (ROS), decrease mitochondrial membrane potential (MMP) and enhance cytochrome c release in treated MDA-MB-231 cells. Isoasarone (2) markedly elevated caspase -8 and -3/7 activities and caused a decline in nuclear NF-κB translocation, suggesting extrinsic, death receptor-linked apoptosis pathway. Quantitative PCR results of MDA-MB-231 treated with asaricin (1) and isoasarone (2) showed altered expression of Bcl-2: Bax level. The inhibitory potency of these isolates may support the therapeutic uses of these compounds in breast cancer.
Background
Melastoma malabathricum (MM) is a traditional plant used in the Borneo region. The cytotoxic effects of methanol extracts from MM leaves have been reported in a number of human cancer cell lines. However, the mode of cell death by MM has not been investigated.
Objective
We investigated the cytotoxic effects of MM in both human breast and lung cancer cell lines, MCF-7 and A549, respectively, and defined the mode of cell death.
Materials and Methods
Cell viability was measured using the 3-(4-, 5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. Annexin-V/propidium iodide (PI) and terminal deoxynucleotidyl transferase dUTP nick-end labeling (TUNEL) staining was done to determine the mode of cell death.
Results
The MTT assay revealed that MM extract had an IC50 of >400 μg/ml on both cell lines at 24 h posttreatment. Flow cytometric and fluorescence microscopy analysis of Annexin-V/PI stained MM-treated cells revealed that the majority of the cells underwent secondary necrosis/late apoptosis. TUNEL assay showed that little to no DNA nicks were present in MM-treated cells, suggesting that cells have undergone secondary necrosis, not late apoptosis, at that time point.
Conclusion
MCF-7 and A549 cells undergoes secondary necrosis 24 h post-treatment with MM extract. MM leaf extract could be a potential source for a novel anti-tumor agent for cancer therapy.
SUMMARY
Melastoma malabathricum (MM) extract was toxic on human breast and lung cancer cell lines
Majority of MM-treated cells died by either secondary necrosis or late apoptosis at 24 h post-treatment
Terminal deoxynucleotidyl transferase dUTP nick-end labeling assay confirmed that MM-treated cells underwent secondary necrosis, not late apoptosis.
Abbreviations used: DMSO: Dimethyl sulfoxide; MM: Melastoma malabathricum; MTT: 3-(4-, 5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide; PI: Propidium iodide; TUNEL: Terminal deoxynucleotidyl transferase dUTP nick-end labeling.
Aim: To investigate whether Potentilla discolor Bunge (PDB) extracts could protect islet β cells and promote cell proliferation and insulin secretion. Methods: β-cell injury model was induced by Streptozotocin. Cell viability, insulin secretion and gene expression were measured to investigate the protective effects of PDB extract on RIN-m5f β cells damaged by streptozotocin. Results: PDB extracts inhibited cell damage, improved cell viability, promoted insulin secretion, and increased protein level of p-Fox O1 in RIN-m5f β cells in a dose-dependent manner. Conclusions: PDB extracts exhibit protective role in streptozotocin induced β cell injury model. The mechanism may be related to increased phosphorylation of Fox O1, which increases the number and improves the function of β cells.