Showing papers on "Stigmasterol published in 2022"

Bioactive Constituents and Toxicological Evaluation of Selected Antidiabetic Medicinal Plants of Saudi Arabia

Abstract: The purpose of this review is to summarize the available antidiabetic medicinal plants in the Kingdom of Saudi Arabia with its phytoconstituents and toxicological findings supporting by the latest literature. Required data about medicinal plants having antidiabetic activities and growing in the Kingdom of Saudi Arabia were searched/collected from the online databases including Wiley, Google, PubMed, Google Scholar, ScienceDirect, and Scopus. Keywords used in search are in vivo antidiabetic activities, flora of Saudi Arabia, active ingredients, toxicological evaluations, and medicinal plants. A total of 50 plant species belonging to 27 families were found in the flora of Saudi Arabia. Dominant family was found Lamiaceae with 5 species (highest) followed by Moraceae with 4 species. β-Amyrin, β-sitosterol, stigmasterol, oleanolic acid, ursolic acid, rutin, chlorogenic acid, quercetin, and kaempferol are the very common bioactive constituents of these selected plant species. This paper has presented a list of antidiabetic plants used in the treatment of diabetes mellitus. Bioactive antidiabetic phytoconstituents which showed that these plants have hypoglycemic effects and highly recommended for further pharmacological purposes and to isolate/identify antidiabetes mellitus (anti-DM) active agents also need to investigate the side effects of active ingredients.

Health Benefits and Pharmacological Properties of Stigmasterol

Abstract: Stigmasterol is an unsaturated phytosterol belonging to the class of tetracyclic triterpenes. It is one of the most common plant sterols, found in a variety of natural sources, including vegetable fats or oils from many plants. Currently, stigmasterol has been examined via in vitro and in vivo assays and molecular docking for its various biological activities on different metabolic disorders. The findings indicate potent pharmacological effects such as anticancer, anti-osteoarthritis, anti-inflammatory, anti-diabetic, immunomodulatory, antiparasitic, antifungal, antibacterial, antioxidant, and neuroprotective properties. Indeed, stigmasterol from plants and algae is a promising molecule in the development of drugs for cancer therapy by triggering intracellular signaling pathways in numerous cancers. It acts on the Akt/mTOR and JAK/STAT pathways in ovarian and gastric cancers. In addition, stigmasterol markedly disrupted angiogenesis in human cholangiocarcinoma by tumor necrosis factor-α (TNF-α) and vascular endothelial growth factor receptor-2 (VEGFR-2) signaling down-regulation. The association of stigmasterol and sorafenib promoted caspase-3 activity and down-regulated levels of the anti-apoptotic protein Bcl-2 in breast cancer. Antioxidant activities ensuring lipid peroxidation and DNA damage lowering conferred to stigmasterol chemoprotective activities in skin cancer. Reactive oxygen species (ROS) regulation also contributes to the neuroprotective effects of stigmasterol, as well as dopamine depletion and acetylcholinesterase inhibition. The anti-inflammatory properties of phytosterols involve the production of anti-inflammatory cytokines, the decrease in inflammatory mediator release, and the inhibition of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). Stigmasterol exerts anti-diabetic effects by reducing fasting glucose, serum insulin levels, and oral glucose tolerance. Other findings showed the antiparasitic activities of this molecule against certain strains of parasites such as Trypanosoma congolense (in vivo) and on promastigotes and amastigotes of the Leishmania major (in vitro). Some stigmasterol-rich plants were able to inhibit Candida albicans, virusei, and tropicalis at low doses. Accordingly, this review outlines key insights into the pharmacological abilities of stigmasterol and the specific mechanisms of action underlying some of these effects. Additionally, further investigation regarding pharmacodynamics, pharmacokinetics, and toxicology is recommended.

A Comprehensive Review on Therapeutic Perspectives of Phytosterols in Insulin Resistance: A Mechanistic Approach

Abstract: Natural products in the form of functional foods have become increasingly popular due to their protective effects against life-threatening diseases, low risk of adverse effects, affordability, and accessibility. Plant components such as phytosterol, in particular, have drawn a lot of press recently due to a link between their consumption and a modest incidence of global problems, such as Type 2 Diabetes mellitus (T2DM), cancer, and cardiovascular disease. In the management of diet-related metabolic diseases, such as T2DM and cardiovascular disorders, these plant-based functional foods and nutritional supplements have unquestionably led the market in terms of cost-effectiveness, therapeutic efficacy, and safety. Diabetes mellitus is a metabolic disorder categoriszed by high blood sugar and insulin resistance, which influence major metabolic organs, such as the liver, adipose tissue, and skeletal muscle. These chronic hyperglycemia fallouts result in decreased glucose consumption by body cells, increased fat mobilisation from fat storage cells, and protein depletion in human tissues, keeping the tissues in a state of crisis. In addition, functional foods such as phytosterols improve the body’s healing process from these crises by promoting a proper physiological metabolism and cellular activities. They are plant-derived steroid molecules having structure and function similar to cholesterol, which is found in vegetables, grains, nuts, olive oil, wood pulp, legumes, cereals, and leaves, and are abundant in nature, along with phytosterol derivatives. The most copious phytosterols seen in the human diet are sitosterol, stigmasterol, and campesterol, which can be found in free form, as fatty acid/cinnamic acid esters or as glycosides processed by pancreatic enzymes. Accumulating evidence reveals that phytosterols and diets enriched with them can control glucose and lipid metabolism, as well as insulin resistance. Despite this, few studies on the advantages of sterol control in diabetes care have been published. As a basis, the primary objective of this review is to convey extensive updated information on the possibility of managing diabetes and associated complications with sterol-rich foods in molecular aspects.

Effect of Ethylene and Abscisic Acid on Steroid and Triterpenoid Synthesis in Calendula officinalis Hairy Roots and Saponin Release to the Culture Medium

Abstract: Phytohormones (plant growth regulators) can be applied as efficient elicitors to enhance the productivity of plant in vitro cultures, due to their significance in regulating the plant metabolism and strong influence on plant defense responses. In the present study, the effects of exogenous ethylene (ETY, applied in the form of ethephon as an ethylene-generating agent) and abscisic acid (ABA) on the synthesis of triterpenoids and steroids in Calendula officinalis hairy roots were investigated. ABA appeared to be an efficient elicitor of the biosynthesis of triterpenoid oleanolic acid (almost two-fold) and the release of its glycosides (saponins) to the culture medium (up to 6.6-fold). ETY had only a slight effect on triterpenoid metabolism; instead, it strongly influenced steroid metabolism, leading to profound modifications of the quantitative profiles of these compounds, particularly the ratio of stigmasterol to sitosterol. Both the applied phytohormones influenced the interplay between steroid and triterpenoid biosynthetic pathways, revealing the symptoms of their competition.

Variations in Physicochemical Characteristics of Olive Oil (cv ‘Moroccan Picholine’) According to Extraction Technology as Revealed by Multivariate Analysis

Abstract: Olive oil is an important component of Mediterranean diet widely, consumed thanks to its numerous health-healing properties. Its quality is dependent upon a set of factors (genotypic, environmental, agronomic practices, ripening, etc). These are well documented, but little is known about the impact of extraction technology on ‘Moroccan Picholine’ olive oil quality. In this paper, physicochemical traits of olive oil (cv ‘Moroccan Picholine’) were investigated according to extraction technology namely super pressure (SP), 2-phase (2P), and 3-phase (3P) systems as well as traditionally extracted oil (Alwana Oil, AO). The obtained results revealed significant differences (p < 0.05) in terms of the studied physicochemical traits. The investigated oil samples were classified as extra-virgin olive oil. Oil samples from super pressure and AO marked by high records of peroxide value, acidity, K270, fatty acids and trans fatty acids likely due to partial oxidation during extraction. AO was marked by high MUFA, stigmasterol, brassicosterol, 2P displayed high SFA and β-sitosterol, and 3P had high PUFA, SFA, ∆7-avenasterol, and ∆7-stigmasterol. These results were confirmed by principal component analysis, cluster analysis and artificial neural networks. In conclusion, continuous systems (2- and 3-phase) produced olive oil of better quality as compared to super-pressure and traditionally extracted oil.

Phytoconstituents of traditional Himalayan Herbs as potential inhibitors of Human Papillomavirus (HPV-18) for cervical cancer treatment: An In silico Approach

Abstract: Human papillomavirus (HPV) induced cervical cancer is becoming a major cause of mortality in women. The present research aimed to identify the natural inhibitors of HPV-18 E1 protein (1R9W) from Himalayan herbs with lesser toxicity and higher potency. In this study, one hundred nineteen phytoconstituents of twenty important traditional medicinal plants of Northwest Himalayas were selected for molecular docking with the target protein 1R9W of HPV-18 E1 Molecular docking was performed by AutoDock vina software. ADME/T screening of the bioactive phytoconstituents was done by SwissADME, admetSAR, and Protox II. A couple of best protein-ligand complexes were selected for 100 ns MD simulation. Molecular docking results revealed that among all the selected phytoconstituents only thirty-five phytoconstituents showed the binding affinity similar or more than the standard anti-cancer drugs viz. imiquimod (-6.1 kJ/mol) and podofilox (-6.9 kJ/mol). Among all the selected thirty-five phytoconstituents, eriodictyol-7-glucuronide, stigmasterol, clicoemodin and thalirugidine showed the best interactions with a docking score of -9.1, -8.7, -8.4, and -8.4 kJ/mol. Based on the ADME screening, only two phytoconstituents namely stigmasterol and clicoemodin selected as the best inhibitor of HPV protein. MD simulation study also revealed that stigmasterol and clicoemodin were stable inside the binding pocket of 1R9W, Stigmasterol and clicoemodin can be used as a potential investigational drug to cure HPV infections.

Supercritical fluid extraction of phytosterols from sugarcane bagasse: Evaluation of extraction parameters

Abstract: Sugarcane bagasse, is one of the largest agriculture residues in the world and its chemical composition is interesting for several areas. Among one of the lipid components was found phytosterols. These are structurally and functionally similar to cholesterol, they are contributing to the reduction of cholesterol in the blood when consumed. Phytosterols were extracted with supercritical CO2 from sugarcane bagasse. In this work was evaluated the effect of temperature (40–80 °C), flowrate (6–10 ml min−1), pressure (200–400 bar) and co-solvent (0–10% ethanol) on extraction yield and phytosterols (β-sitosterol, campesterol and stigmasterol) concentration. The addition of co-solvent improves total phytosterols concentration at low pressure, but has no effect at high pressure. At optimal extraction conditions the yield was 0.92% and 0.300 mg total phytosterol g−1 dry material. The extract obtained presented a lipidic composition with possible cardiovascular health benefits due to phytosterols, policosanols and unsaturated fatty acids found.

The inhibitory role of stigmasterol on tumor growth by inducing apoptosis in Balb/c mouse with spontaneous breast tumor (SMMT)

Abstract: Abstract Background Breast cancer is one of the most common types of cancer in women worldwide. Anti-apoptotic activity of cancer cells is considered the main reason for drug resistance in BC which reduces the 5-year survival rate of patients and is still considered the main obstacle for cancer therapy. Stigmasterol (SS) is natural phytosterols compound in the plant which has been proved to play an important role to lower cholesterol and inducing anti-inflammatory, and anticancer properties. Methods In this, study, we aimed to evaluate the effect of SS on the expression of anti-apoptotic genes (Bcl-2 and BCL-XL), and also evaluate its effects on cell apoptosis and cell viability using MCF-7 cell line as well as evaluating its effect on tumor growth of spontaneous breast tumor (SMMT) in vivo. Result SS significantly decreased the expression of Bcl-2 and BCL-XL genes (* P < 0.05), induced apoptosis, and reduced cell proliferation in MCF-7 cell lines. Our in vivo study also indicated that SS could inhibit tumor size after treatment with (0, 10, 20 µM) compared to the normal control. Conclusion SS can be suggested as a potential agent in BC cancer treatment or as an adjuvant based on its ability to decrease the expression of Bcl-2 and BCL-XL genes and induce apoptosis.

The inhibitory role of stigmasterol on tumor growth by inducing apoptosis in Balb/c mouse with spontaneous breast tumor (SMMT)

Abstract: Abstract Background Breast cancer is one of the most common types of cancer in women worldwide. Anti-apoptotic activity of cancer cells is considered the main reason for drug resistance in BC which reduces the 5-year survival rate of patients and is still considered the main obstacle for cancer therapy. Stigmasterol (SS) is natural phytosterols compound in the plant which has been proved to play an important role to lower cholesterol and inducing anti-inflammatory, and anticancer properties. Methods In this, study, we aimed to evaluate the effect of SS on the expression of anti-apoptotic genes (Bcl-2 and BCL-XL), and also evaluate its effects on cell apoptosis and cell viability using MCF-7 cell line as well as evaluating its effect on tumor growth of spontaneous breast tumor (SMMT) in vivo. Result SS significantly decreased the expression of Bcl-2 and BCL-XL genes (* P < 0.05), induced apoptosis, and reduced cell proliferation in MCF-7 cell lines. Our in vivo study also indicated that SS could inhibit tumor size after treatment with (0, 10, 20 µM) compared to the normal control. Conclusion SS can be suggested as a potential agent in BC cancer treatment or as an adjuvant based on its ability to decrease the expression of Bcl-2 and BCL-XL genes and induce apoptosis.

Modulation of Steroid and Triterpenoid Metabolism in Calendula officinalis Plants and Hairy Root Cultures Exposed to Cadmium Stress

Abstract: The present study investigated the changes in the content of steroids and triterpenoids in C. officinalis hairy root cultures and plants exposed to cadmium stress. The observed effects included the content and composition of analyzed groups of compounds, particularly the proportions among individual sterols (e.g., stigmasterol-to-sitosterol ratio), their ester and glycoside conjugates. The total sterol content increased in roots (by 30%) and hairy root culture (by 44%), whereas it decreased in shoots (by 15%); moreover, these effects were inversely correlated with Cd-induced growth suppression. Metabolic alterations of sterols and their forms seemed to play a greater role in the response to Cd stress in roots than in shoots. The symptoms of the competition between general metabolites (sterols) and specialized metabolites (triterpenoids) were also observed, i.e., the increase of the sterol biosynthesis parallel to the decrease of the triterpenoid content in C. officinalis plant roots and hairy root culture, and the inverse phenomenon in shoots. The similarity of the metabolic modifications observed in the present study on C. officinalis plant roots and hairy roots confirmed the possibility of application of plant in vitro cultures in initial studies for physiological research on plant response to environmental stresses.

Isolation, Characterization and Pharmacological Investigations of a New Phenolic Compound along with Four Others Firstly Reported Phytochemicals from Glycosmis cyanocarpa (Blume) Spreng

Abstract: Plants are serving the mankind with important bioactive phytochemicals from the very ancient ages to develop novel therapeutics against different disease states. Glycosmis cyanocarpa (Blume) Spreng is a plant from the Rutaceae family and a very less explored species from the Glycosmis genus. Thus, this present study was intended to present the chemical and biological investigation of Glycosmis cyanocarpa (Blume) Spreng. The chemical investigation resulted in the isolation of one new phenolic compound to the best of our knowledge which is (4-(3-hydroxy-2-methylpropyl)-2-methoxyphenol) (1) along with four known compounds that are isolated for the first time from this species- 3-methyl-1H-indole (2), Tri-transpoly-cis prenol-12 (3), Stigmasterol (4) and β-sitosterol (5). Their chemical structures were elucidated based on extensive spectroscopic methods, including 1D and 2D NMR, and comparison with the available literature data. Isolated phytochemicals were further investigated to unveil their antioxidant properties with IC50 values (ranged from 9.97–75.48 µg/mL), cytotoxicity with LC50 values (ranged from 1.02–1.92 µg/mL), and antibacterial properties against some selected Gram (+) ve and Gram (−) ve bacteria. Among the compounds, 3-methyl-1H-indole (2) was found to be the most active against Staphylococcus aureus. Moreover, the phenolic compound (1) and the alkaloid (2) revealed the highest antioxidant (9.97 µg/mL) and cytotoxic activities (1.02 µg/mL), respectively. Thus, the isolation of these bioactive phytochemicals from the plant revealed a new perception in the study arena of drug discovery and the findings may ease the development and discovery of novel therapeutics. Further investigations are still recommended to understand their exact molecular mechanism and toxicological impact.

Phytochemical, Cytotoxic, and Antimicrobial Evaluation of Tribulus terrestris L., Typha domingensis Pers., and Ricinus communis L.: Scientific Evidences for Folkloric Uses

Abstract: Many medicinal plants have been utilized for centuries despite the lack of scientific evidence of their therapeutic effects. This study evaluated the phytochemical and dual biological profiling, namely, antibacterial and cytotoxic properties, of three plant species, namely, Tribulus terrestris L., Typha domingensis Pers., and Ricinus communis L., in order to explore potential relationships (if any) with their ethnopharmacological uses. GC-MS was used to achieve phytochemical screening of two plant extracts (T. terrestris and T. domingensis). The primary chemicals detected in varying amounts in both extracts were siloxane derivatives, fatty acid esters, diisooctyl phthalate, phytosterol, and aromatic acid esters. According to the findings, the major component detected in both extracts was 1,2-benzenedicarboxylic acid and diisooctyl ester (antibacterial and antifungal). T. domingensis contained a low level of benzoic acid, methyl ester (antibacterial). Both extracts included stigmasterol and sitosterol, as well as six different forms of fatty acid esters. Antimicrobial, antioxidant, anticancer, thyroid inhibitor, and anti-inflammatory properties have all been described. Human breast adenocarcinoma (MCF7), human ovary adenocarcinoma (A2780), and human colon adenocarcinoma (HT29), as well as normal human fetal lung fibroblasts (MRC5), all showed cytotoxic activity. The most potent activity against A2780 cells was seen in T. terrestris and T. domingensis extracts (IC50: 3.69 and 5.87 g/mL, respectively). R. communis was more active against MCF7 cells (1.52 μg/mL) followed by A2780 and HT29 cells, respectively. R. communis showed a dose-dependent clonogenic effect against MCF7 cells. The antibacterial activity of all three plant extracts was tested against three standard Gram-positive, four standard Gram-negative, and two clinical bacterial strains. Among the three extracts examined, T. terrestris was the most effective, followed by R. communis, and finally, T. domingensis plant extract was effective against various isolated bacteria. This study, interestingly, sheds light on the bioactive components found in plant extracts that can be utilized for cytotoxic and antibacterial purposes.

GC–MS profiling and antibacterial activity of Solanum khasianum leaf and root extracts

Abstract: Abstract Background Solanum khasianum is an important medicinal herb of the Solanaceae family. The present study was focused to determine the bioactive compounds in S. khasianum leaf and root extract by GC–MS analysis and their antibacterial activity by agar well diffusion method. Results Sixteen bioactive compounds were detected in leaf extract and thirty-two compounds in root methanolic extract by GC–MS. The major potent compounds identified in leaf and root extracts were heptadecane 9-hexyl (43.65%) and stigmasterol (23.18%). The root extract showed increased antibacterial activity than leaf extract. Conclusion These extracts possessed significant antibacterial activity against the tested bacterial isolates in dose-dependent manner. This study provides the phytoconstituents, antibacterial property and scientific evidence for the traditional claim and use of S. khasianum.

GC–MS profiling and antibacterial activity of Solanum khasianum leaf and root extracts

Abstract: Abstract Background Solanum khasianum is an important medicinal herb of the Solanaceae family. The present study was focused to determine the bioactive compounds in S. khasianum leaf and root extract by GC–MS analysis and their antibacterial activity by agar well diffusion method. Results Sixteen bioactive compounds were detected in leaf extract and thirty-two compounds in root methanolic extract by GC–MS. The major potent compounds identified in leaf and root extracts were heptadecane 9-hexyl (43.65%) and stigmasterol (23.18%). The root extract showed increased antibacterial activity than leaf extract. Conclusion These extracts possessed significant antibacterial activity against the tested bacterial isolates in dose-dependent manner. This study provides the phytoconstituents, antibacterial property and scientific evidence for the traditional claim and use of S. khasianum.

Metabolic Modifications in Terpenoid and Steroid Pathways Triggered by Methyl Jasmonate in Taxus × media Hairy Roots

Abstract: The in vitro cultures of Taxus spp. were one of the first plant in vitro systems proved to exert the positive effect of elicitation with methyl jasmonate (MeJA) on the biosynthesis of specialized metabolites. The main aim of the present study is to examine the effect of MeJA treatment on the steroid and triterpenoid content of two genetically different hairy root lines of Taxus × media, KT and ATMA. The results revealed that the two lines differed in the total content of steroids and triterpenoids (in the ATMA root line, their amounts were lower than those in the KT line by 43% and 30%, respectively), but not in the composition of these compounds. The metabolic response to elicitation with MeJA was different: in the KT root line, the content of steroids decreased by 18%, whereas it increased by 38% in the ATMA line. Several metabolic features were common, including the characteristic changes in the ratio of sitosterol to stigmasterol content, caused by the very sharp boost in stigmasterol levels, the increase in the amount of glycoside forms of sterols, as well as in triterpenoid and total phenolic content. It is the first report on modifications of the terpenoid biosynthetic pathway in Taxus hairy root cultures triggered by MeJA, concerning steroids and triterpenoids.

Comparative analysis of the seasonal influence on polyphenolic content, antioxidant capacity, identification of bioactive constituents and hepatoprotective biomarkers by in silico docking analysis in Premna integrifolia L.

Abstract: The present study reports the effect of different seasons on polyphenol content and antioxidant potential of ethanolic, methanolic, ethyl acetate, and aqueous extracts of leaves, stems, and roots of Premna integrifolia. Ethyl acetate extract of leaves (EAEPI) collected in the rainy season showed potent antioxidant activity with highest total phenol (74.33 ± 2.26 µg/mg, gallic acid equivalent), and flavonoid (98.83 ± 0.26 µg/mg, rutin equivalent) content. Therefore, EAEPI extract was subjected to characterization by UHPLC-Q-TOF-MS/MS and GC–MS analysis for the identification of active constituents. UHPLC-Q-TOF-MS/MS analysis in + ve ion mode revealed the presence of eight polyphenolic compounds namely quercetin-3-D-xyloside, kaempferol-3,7-O-bis-alpha-L-rhamnoside, isorhamnetin-3-Oglucoside, luteolin-3′,7-di-O-glucoside, eriodictyol-7-O-glucoside, syringetin-3-O-galactoside, petunidin-3-O-beta-glucopyranoside and vitexin-2″-O-rhamnoside. GC–MS analysis confirmed the presence of 26 compounds with six major compounds viz; citronellol, phytol acetate, campesterol, squalene, stigmasterol, and hexadecanoic acid. These compounds are reported for the first time from P. integrifolia except phytol and stigmasterol. Our previous study validates the hepatoprotective potential of P. integrifolia but there was no idea about the bioactive compound responsible for the activity. So, in present work, the major compounds identified in spectrometry analysis were subjected to in silico docking against an important liver enzyme alanine amino transaminase to confirm its hepatoprotective properties. Docking analysis validates the presence of two hepatoprotective lead compounds stigmasterol, and campesterol, which satisfy the drug-likeness criteria with good absorption, distribution, metabolism, and toxicity properties. Thus, present work gives a clear insight about the influence of season on the total polyphenolic constituent in different plant parts of P. integrifolia, their antioxidant potential and preclinical evaluation of hepatoprotective lead compounds.

GhCYP710A1 Participates in Cotton Resistance to Verticillium Wilt by Regulating Stigmasterol Synthesis and Plasma Membrane Stability

Abstract: Cotton is an important economic crop. Cotton Verticillium wilt caused by Verticillium dahliae seriously damages production. Phytosterols play roles in plant-pathogen interaction. To explore the function and related mechanism of phytosterols in the interaction between Verticillium dahliae and cotton plants, and the resistance to Verticillium wilt, in this study, we analyzed the changes of sterol composition and content in cotton roots infected by Verticillium dahliae, and identified the sterol C22-desaturase gene GhCYP710A1 from upland cotton. Through overexpressing and silencing the gene in cotton plant, and ectopically expressing the gene in Arabidopsis, we characterized the changes of sterol composition and the resistance to Verticillium wilt in transgenic plants. The infection of Verticillium dahliae resulted in the content of total sterol and each sterol category decreasing in cotton root. The ratio of stigmasterol to sitosterol (St/Si) increased, indicating that the conversion of sitosterol to stigmasterol was activated. Consistently, the expression level of GhCYP710A1 was upregulated after infection. The GhCYP710A1 has the conservative domain that is essential for sterol C22-desaturase in plant and is highly expressed in root and stem, and its subcellular location is in the endoplasmic reticulum. The ectopic expression of GhCYP710A1 gene promoted the synthesis of stigmasterol in Arabidopsis. The St/Si value is dose-dependent with the expression level of GhCYP710A1 gene. Meanwhile, the resistance to Verticillium wilt of transgenic Arabidopsis increased and the permeability of cell membrane decreased, and the content of ROS decreased after V991 (a strain of Verticillium dahliae) infection. Consistently, the resistance to Verticillium wilt significantly increased in the transgenic cotton plants overexpressing GhCYP710A1. The membrane permeability and the colonization of V991 strain in transgenic roots were decreased. On the contrary, silencing GhCYP710A1 resulted in the resistance to Verticillium wilt being decreased. The membrane permeability and the colonization of V991 were increased in cotton roots. The expression change of GhCYP710A1 and the content alteration of stigmasterol lead to changes in JA signal transduction, hypersensitivity and ROS metabolism in cotton, which might be a cause for regulating the Verticillium wilt resistance of cotton plant. These results indicated that GhCYP710A1 might be a target gene in cotton resistance breeding.

Comparative analysis of the seasonal influence on polyphenolic content, antioxidant capacity, identification of bioactive constituents and hepatoprotective biomarkers by in silico docking analysis in Premna integrifolia L.

Abstract: The present study reports the effect of different seasons on polyphenol content and antioxidant potential of ethanolic, methanolic, ethyl acetate, and aqueous extracts of leaves, stems, and roots of Premna integrifolia. Ethyl acetate extract of leaves (EAEPI) collected in the rainy season showed potent antioxidant activity with highest total phenol (74.33 ± 2.26 µg/mg, gallic acid equivalent), and flavonoid (98.83 ± 0.26 µg/mg, rutin equivalent) content. Therefore, EAEPI extract was subjected to characterization by UHPLC-Q-TOF-MS/MS and GC–MS analysis for the identification of active constituents. UHPLC-Q-TOF-MS/MS analysis in + ve ion mode revealed the presence of eight polyphenolic compounds namely quercetin-3-D-xyloside, kaempferol-3,7-O-bis-alpha-L-rhamnoside, isorhamnetin-3-Oglucoside, luteolin-3′,7-di-O-glucoside, eriodictyol-7-O-glucoside, syringetin-3-O-galactoside, petunidin-3-O-beta-glucopyranoside and vitexin-2″-O-rhamnoside. GC–MS analysis confirmed the presence of 26 compounds with six major compounds viz; citronellol, phytol acetate, campesterol, squalene, stigmasterol, and hexadecanoic acid. These compounds are reported for the first time from P. integrifolia except phytol and stigmasterol. Our previous study validates the hepatoprotective potential of P. integrifolia but there was no idea about the bioactive compound responsible for the activity. So, in present work, the major compounds identified in spectrometry analysis were subjected to in silico docking against an important liver enzyme alanine amino transaminase to confirm its hepatoprotective properties. Docking analysis validates the presence of two hepatoprotective lead compounds stigmasterol, and campesterol, which satisfy the drug-likeness criteria with good absorption, distribution, metabolism, and toxicity properties. Thus, present work gives a clear insight about the influence of season on the total polyphenolic constituent in different plant parts of P. integrifolia, their antioxidant potential and preclinical evaluation of hepatoprotective lead compounds.

Polyphenols, Saponins and Phytosterols in Lentils and Their Health Benefits: An Overview

Abstract: The lentil (Lens culinaris L.) is one of the most important legumes (family, Fabaceae). It is a natural functional food rich in many bioactive compounds, such as polyphenols, saponins and phytosterols. Several studies have demonstrated that the consumption of lentils is potentially important in reducing the incidence of a number of chronic diseases, due to their bioactive compounds. The most common polyphenols in lentils include phenolic acids, flavan-3-ol, flavonols, anthocyanidins, proanthocyanidins or condensed tannins, and anthocyanins, which play an important role in the prevention of several degenerative diseases in humans, due to their antioxidant activity. Furthermore, lentil polyphenols are reported to have antidiabetic, cardioprotective and anticancer activities. Lentil saponins are triterpene glycosides, mainly soyasaponins I and βg. These saponins have a plasma cholesterol-lowering effect in humans and are important in reducing the risk of many chronic diseases. Moreover, high levels of phytosterols have been reported in lentils, especially in the seed coat, and β-sitosterol, campesterol, and stigmasterol are the most abundant. Beyond their hypocholesterolemic effect, phytosterols in lentils are known for their anti-inflammatory activity. In this review, the current information on the nutritional composition, bioactive compounds including polyphenols, saponins and phytosterols, and their associated health-promoting effects are discussed.

Chemical Constituents and Antiproliferative Activity of Eleusine indica (L.) Gaertn.

Abstract: Eleusine indica, locally known as ‘rumput sambau’ is widely used by traditional practitioners in many parts of the world to treat various ailments including sprained muscle, asthma, black jaundice, stomach pain, diarrhea, convulsions, and those related to infection such as malaria, influenza, dysentery as well as pneumonia. The plant has been reported to possess a wide array of biological activities, which were antioxidant, anti-inflammatory, antimicrobial, antidiabetic, antipyretic, antiplasmodial, antiviral, hepatoprotective, and urolithiasis. Despite all the reported traditional uses and biological activities, not many chemical constituents have been isolated from the plant. In this work, E. indica methanolic and hexane extracts were assessed for their anti-proliferative activities against human liver cancer (HepG2) and African green monkey kidney epithelial normal (Vero) cell lines through 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. Although both extracts were considered to be not active on both cell lines with an IC50 of 91.02 ± 5.74 and 85.30 ± 3.03 µg/mL, and CC50 of >1000 and 639.39 ± 13.97 µg/mL, they were nevertheless more selective towards HepG2 cancer cells compared to the Vero normal cells with selectivity indexes (SI) of 10.99 and 7.50, respectively. Chemical profiling of the extracts on ultra-high performance liquid chromatography (UHPLC) coupled with a diode array detector showed a mixture of different complexity and polarities of compounds. Further isolation and purification on the hexane extract afforded β-sitosterol and stigmasterol, while the methanolic extract yielded loliolide, a benzofuran type of compound. Loliolide has been previously reported to exhibit antitumor activity, which could correlate to the higher antiproliferative selectivity against HepG2 cancer cell line of the methanolic compared to the hexane extracts. This is the first report on the isolation of β-sitosterol, stigmasterol, and loliolide from E. indica.

Phytochemicals As a Potential Inhibitor of COVID-19: An In-Silico Perspective

Abstract: The current research has centered on the use of pharmacological and binding affinity methods to test the 36 compounds as bioactive constituents’ inhibitors for COVID-19. Six compounds out of 36 phytoconstituents (rutin, quercetin, catechin gallate, rhamnetin, campesterol and stigmasterol) have demonstrated outstanding molecular docking and drug-like properties as HIV inhibitors Lopinavir and Indinavir. Interestingly, the lowest binding energies (LBE) and the inhibition constant (Ki) have showed that these compounds are able to bind to the P-glycoprotein substrate of 3CLpro and Nsp15. Interestingly, rutin has been found to be an excellent potential inhibitor for COVID-19 proteins because it has the best LBE score and Ki value than those of other compounds, and of its ability to form strong H-bonds with COVID-19 proteins. The compounds that come next to the rutin compound are stigmasterol and campesterol. As a result, these compounds are considered possible novel inhibitors of COVID-19. In order to validate the computational results, more in vitro and in vivo investigations are required to support the findings of this research.