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Since ancient times Chrysopogon zizanioides have been utilized as a traditional medicinal 27 plant for the treatment of numerous ailments, but neither its plant extract form nor its phytoconstit-28 uents have been explored much. With this in mind, the present research was designed to isolate and 29 structurally characterize one of its chemical cons...
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... MTT assay mainly employs MTT dye, which is converted to purple formazan by mitochondrial dehydrogenase enzymes of viable cells (Figure 7) that turns the solution purple in color with the addition of DMSO, acidified isopropranolol, etc. The colored solution is spectrophotometrically measured indicating the effect produced by the test and standard sample to provide the result in the form of IC50. ...
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... Finally, β-elemene, junipene, β-caryophyllene, and caryophyllene oxide describe earthy and grassy notes. β-elemene exhibits good activity on specific cancer types [25], and junipene possesses cytotoxic potential against prostate and oral cancer cell lines with minor toxicity in healthy cells [26]. Also, β-caryophyllene promotes plant growth, induces defence genes and is active against specific plant pathogenic bacteria and fungi [27]. ...
Mexican Coccoloba uvifera fruit contains polyphenols, flavonoids, and anthocyanins, while in the leaves, lupeol, α- and β-amyrin have been previously identified by HPLC. However, the low resolution by HPLC of pentacyclic triterpenes (PTs) is a limitation. Moreover, the volatile profile of C. uvifera fruit is still unknown. Therefore, this study aimed to identify PTs in C. uvifera leaf and fruit extracts by CG-MS analysis and to determine the volatile profile of C. uvifera pulp by headspace solid-phase microextraction. The results showed trimethylsilylated compounds of standards lupeol, α- and β-amyrin, indicating that the silylation reaction was suitable. These trimethylsilylated compounds were identified in leaf and fruit extracts. The fruit volatile profile revealed the presence of 278 esters, 20 terpenes, 9 aldehydes, 5 alcohols, and 4 ketones. The fruit showed a high content of esters and terpenes. Due to their flavour properties, esters are essential for the food, cosmetics, and pharmaceutics industries. Moreover, terpenes in the fruit, such as menthone, β-elemene, junipene, and β-caryophyllene have the potential as anticancer and phytopathogen agents. The results indicated that GC-MS is an alternative to HPLC approaches for identifying PTs. Besides, identifying volatile compounds in the fruit will increase the value of this plant and expand its application. Identifying PTs and volatile compounds in Mexican C. uvifera leads to a better understanding of the potential benefits of this plant. This would increase the consumption of Mexican C. uvifera fresh or as functional ingredients in nutraceutical or pharmaceutical products.
... Chinese specialists advise treating patients with 500 mg of chloroquine twice day for ten days if they have been diagnosed with mild, moderate, or severe instances of COVID-19 pneumonia and do not have any contraindications to the medication. Longifolene is a bicyclic compound that falls under the sesquiterpene category [8]. Numerous plant essential oils contain a broad family of chemical molecules called sesquiterpenes. ...
The goal of the current study is to find an alternative to hydroxychloroquine that is an antimalarial and has in vitro activity against SARS-CoV-2. The crystal structure of the COVID-19 main protease in complex with an inhibitor N3 (6LU7) was used for molecular docking analysis with hydroxychloroquine and phytochemicals with medicinal properties. The novel corona virus (2019-nCoV), family Coronaviridae, genus Beta coronavirus, is thought to be one of the most dangerous pathogenic RNA viruses that causes severe acute respiratory syndrome and is thought to be a threat to humanity. Our research has led to the discovery of two useful phytochemicals that can be obtained from the annual flowering plant Nigella sativa, which is native to the Indian Subcontinent and West Asia. These phytochemicals, longifolene and thymohydroquinone, are suitable alternatives to hydroxychloroquine in the treatment of malaria and COVID-19.
... Therefore, E. ingens ethyl acetate fraction seems to be a potential source for prospecting chemotherapeutic agent against PCa. The inhibitory effect of E. ingens ethyl acetate on DU-145 was more potent when compared to that reported for longifolene isolated from Chrysopogon zizanioides (IC 50 of 78.64 µg/mL) on the same DU-145 cells [22]. In prior studies, the stem and leaf parts of E. ingens were inactive against human colon adenocarcinoma (CACO2), human hepatoma (HepG2), and human breast adenocarcinoma (MCF-7) cell lines [10]. ...
... Cancer is the most confounding illness of the 21st century and is growing enormously without any discernment based on cell type, age, or gender [1]. Although incredible advancements in cancer treatment have been achieved, the prevalence and mortality rates are still the highest across the world. ...
The limitations associated with the conventional treatment of cancer have necessitated the design and development of novel drug delivery systems based mainly on nanotechnology. These novel drug delivery systems include various kinds of nanoparticles, such as polymeric nanoparticles, solid lipid nanoparticles, nanostructured lipid carriers, hydrogels, and polymeric micelles. Among the various kinds of novel drug delivery systems, chitosan-based nanoparticles have attracted the attention of researchers to treat cancer. Chitosan is a polycationic polymer generated from chitin with various characteristics such as biocompatibility, biodegradability, non-toxicity, and mucoadhesiveness, making it an ideal polymer to fabricate drug delivery systems. However, chitosan is poorly soluble in water and soluble in acidic aqueous solutions. Furthermore, owing to the presence of reactive amino groups, chitosan can be chemically modified to improve its physiochemical properties. Chitosan and its modified derivatives can be employed to fabricate nanoparticles, which are used most frequently in the pharmaceutical sector due to their possession of various characteristics such as nanosize, appropriate pharmacokinetic and pharmacodynamic properties, non-immunogenicity, improved stability, and improved drug loading capacity. Furthermore, it is capable of delivering nucleic acids, chemotherapeutic medicines, and bioactives using modified chitosan. Chitosan and its modified derivative-based nanoparticles can be targeted to specific cancer sites via active and passive mechanisms. Based on chitosan drug delivery systems, many anticancer drugs now have better effectiveness, potency, cytotoxicity, or biocompatibility. The characteristics of chitosan and its chemically tailored derivatives, as well as their use in cancer therapy, will be examined in this review.
... Studies have reported that these have antitumor properties. Furthermore, menthol also acts as an antibacterial, antifungal, antipruritic, and analgesic agent [80][81][82]. ...
Horseradish is a globally well-known and appreciated medicinal and aromatic plant. The health benefits of this plant have been appreciated in traditional European medicine since ancient times. Various studies have investigated the remarkable phytotherapeutic properties of horseradish and its aromatic profile. However, relatively few studies have been conducted on Romanian horseradish, and they mainly refer to the ethnomedicinal or dietary uses of the plant. This study reports the first complete low-molecular-weight metabolite profile of Romanian wild-grown horseradish. A total of ninety metabolites were identified in mass spectra (MS)-positive mode from nine secondary metabolite categories (glucosilates, fatty acids, isothiocyanates, amino acids, phenolic acids, flavonoids, terpenoids, coumarins, and miscellaneous). In addition, the biological activity of each class of phytoconstituents was discussed. Furthermore, the development of a simple target phyto-carrier system that collectively exploits the bioactive properties of horseradish and kaolinite is reported. An extensive characterization (FT-IR, XRD, DLS, SEM, EDS, and zeta potential) was performed to investigate the morpho-structural properties of this new phyto-carrier system. The antioxidant activity was evaluated using a combination of three in vitro, non-competitive methods (total phenolic assay, 2,2-Diphenyl-1-picrylhydrazyl (DPPH) radical-scavenging assay, and phosphomolybdate (total antioxidant capacity)). The antioxidant assessment indicated the stronger antioxidant properties of the new phyto-carrier system compared with its components (horseradish and kaolinite). The collective results are relevant to the theoretical development of novel antioxidant agent fields with potential applications on antitumoral therapeutic platforms.
... Therefore, E. ingens has significant potential for further studies as a potential chemotherapeutic agent. The inhibitory effects of E. ingens ethyl acetate on DU-145 is better when compared to that reported for longifolene isolated from Chrysopogon zizanioides (IC50 of 78.64 µg/mL) on the same DU-145 cells [25]. Meanwhile, El-Hawary et al. [26] found E. ingens to be inactive when tested against human colon adenocarcinoma (CACO2), human hepatoma (HepG2) and human breast adenocarcinoma (MCF-7) cell lines. ...
Euphorbia ingens is traditionally used to treat and manage cancer in Ambeere community of Embu County in Kenya. Whilst research has demonstrated the bioactivities of E. ingens including antimicrobial, antitubercular and antifungal activities, scientific validation of its anticancer properties is limited. This study evaluated the antiproliferative potentials of E. ingens on human prostate cancer cell line (DU-145). The 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide assay was used to assess the antiproliferative activity, chemical constituents were analysed by qualitative colour method and Gas Chromatography-Mass Spectrometry analysis. At the same time, the investigation of putative molecular targets and mechanisms of action of E. ingens was done through network pharmacological analysis. Reverse transcription-quantitative polymerase chain reaction (RT-qPCR) was carried out to validate the network predictions of putative targets. Our result showed E. ingens ethyl acetate inhibited DU-145 growth (IC50 of 9.71 ± 0.4 µg/ml) with a high selectivity index of 8.26. There was the presence of phenols, terpenoids, flavonoids, tannins, sterols, and saponins; additional 18 compounds were identified by the GC-MS approach. ESR1, IL6, MMP9, CDK2, MAP2K1, AR, PRKCD, CDK1, CDC25B, and JAK2 were indicated as key targets of E. ingens against prostate cancer with the PI3K-AKT, MAPK, and p53 signalling pathways identified as the most probable mechanisms of action. There was significant downregulation of AR and BCL2, and upregulation of p53 and caspase-3 in E. ingens-treated DU-145 cells compared to 0.2 % DMSO negative control. Our results suggest that E. ingens has phytochemical compounds efficacious at inhibiting the proliferation of DU-145 cells; therefore, the plant can be considered a potential source of compounds that may be used to manage and treat prostate cancer; however, further in vivo evaluations are needed.
... Despite remarkable progress in treatment of cancer, the prevalence and fatality rates are highest throughout the world [1]. According to a report generated by International Agency for Research on Cancer (IARC) in 2020, approximately 19.3 million new cases and 10 million deaths due to cancer were reported across the world, whilst the new cases and deaths due to cancer in India were 1.32 million and 0.8 million, respectively [2]. ...
Anticancer drugs in monotherapy are ineffective to treat various kinds of cancer due to the heterogeneous nature of cancer. Moreover, available anticancer drugs possessed various hurdles, such as drug resistance, insensitivity of cancer cells to drugs, adverse effects and patient inconveniences. Hence, plant-based phytochemicals could be a better substitute for conventional chemotherapy for treatment of cancer due to various properties: lesser adverse effects, action via multiple pathways, economical, etc. Various preclinical studies have demonstrated that a combination of phytochemicals with conventional anticancer drugs is more efficacious than phytochemicals individually to treat cancer because plant-derived compounds have lower anticancer efficacy than conventional anticancer drugs. Moreover, phytochemicals suffer from poor aqueous solubility and reduced bioavailability, which must be resolved for efficacious treatment of cancer. Therefore, nanotechnology-based novel carriers are employed for codelivery of phytochemicals and conventional anticancer drugs for better treatment of cancer. These novel carriers include nanoemulsion, nanosuspension, nanostructured lipid carriers, solid lipid nanoparticles, polymeric nanoparticles, polymeric micelles, dendrimers, metallic nanoparticles, carbon nanotubes that provide various benefits of improved solubility, reduced adverse effects, higher efficacy, reduced dose, improved dosing frequency, reduced drug resistance, improved bioavailability and higher patient compliance. This review summarizes various phytochemicals employed in treatment of cancer, combination therapy of phytochemicals with anticancer drugs and various nanotechnology-based carriers to deliver the combination therapy in treatment of cancer.
Nigella sativa L. (black seed or black cumin) belonging to the Ranunculaceae family is an annual flowering plant native to southwest Asia. It has been widely used in traditional medicinal systems and practices such as Siddha, Unani, Ayurveda, and folk medicine for its remarkable medicinal value in treating liver disorders and other illnesses. Especially, the seeds of N. sativa (NS) are rich in essential oils and other phytoconstituents which results in significant pharmacological activities such as antimicrobial, antioxidant, antihypertensive, anti-inflammatory, anticancer, antidiabetic hepatoprotective, immunomodulatory, and neuroprotective properties. Recent pieces of evidence report that the exploration of the phytoconstituents of N. sativa seeds will tremendously improve the significance of herbal and alternative medicine to the existing therapies. In this chapter, we have focused on the compilation of Nigella sativa oil’s (NSO) phytoconstituents, extraction and isolation strategies, various pharmacological activities, and their toxic properties. In addition, thymoquinone was discussed in detail for its significant medicinal properties. Furthermore, we have also discussed the commercially available Nigella sativa L. products and their manufacturers with market value. Exploration of NSO will lead to the identification of valuable pharmaceutically important compounds in near future.
Syzygium aromaticum seed from the family of Myrtaceae is a highly priced natural spice used in preparation of food which have been acclaimed and reported by previous researchers to have anticancer activities potentials. Due to the rising burden of cancer worldwide its severity and fatality coupled with side effects of synthetic drugs calls for an alternative treatment solution. Hence the current research studied the phytocompounds from the seed by extracting and screening the compounds using solvent maceration method and gas chromatography coupled to mass selective detector respectively to extract, identify and quantify the component phytochemicals present in the seed. Site directed multi-ligand docking of the identified compounds was performance on progesterone receptor protein responsible for breast cancer development using the compounds from GCMS results and compared with four standard breast cancer drugs by molecular docking method. The result showed that the alpha cubebene (-7 kcal/mol), Velerena -4, 7- (II) diene (-7.1 kcal/mol), caryophyllene (-7.4 kcal/mol), caryophyllene oxide (-7.4 kcal/mol), dibutyl phthalate have binding affinity close to the standard breast cancer drugs Abemaciclib (-8.3), Anastrozole (-7.2 kcal/mol) and Paclitaxel (-8.8 kcal/mol) and they have better binding affinity than the drug Cyclophasphamide (-5.6 kcal/mol). The result also revealed that some compounds from the GC-MS were found to have a binding affinity closer tothat of thecocrystallized ligand (-10.7 kcal/mol). Other compounds from clove seed showed favourable docking scores in comparison with the drugs as many of the compounds have docking scores of more than (-6 kcal/mol) suggesting that the compounds have anti breast cancer activities since their amino acids showed hydrogen bonding corresponding to that on the binding site
