Discovery Phytomedicine Journal
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Evaluation of the anti-diarrheal activity of 80% methanol extracts and the solvent fraction of the leaves of Withania somnifera (L.) Dunal (Solanaceae) in mice
No full textBackground: The leaf of Withania somnifera has been used for the treatment of diarrhea without evaluation of its efficacy. This study was aimed to evaluate the antidiarrheal activity of 80% methanol extract and the solvent fraction of Withania somnifera leaf in mice.Materials and Methods: The extraction was done using a cold maceration technique. The antidiarrheal activity was investigated on the castor oil-induced diarrhea, castor oil-induced gastrointestinal transit tests, and castor oil-induced enteropooling models. The mice were randomly grouped into negative control received 10ml/kg 2% tween-80 in distilled water, positive control received 3mg/kg loperamide, and group III - V received 100 mg/kg, 200 mg/kg, and 400mg/kg of the extract orally.Result: The crude extract, aqueous, and n-butanol fractions significantly delayed the onset of diarrhea at 200mg/kg and 400mg/kg doses. All three doses of the crude extract showed significant activity on the three models (castor oil induced diarrhea, castor oil induced gastro-intestinal motility, and castor oil-induced enteropooling test), whereas the aqueous and n-butanol fractions revealed a significant result at 200mg/kg and 400mg/kg. The phytochemical screening showed that flavonoids, tannins, alkaloid, phenols, saponin, terpenoids, and steroid were presented in the crude, flavonoid, phenol, tannin, saponin, alkaloid, and steroid were possessed in aquas fraction, while the n-butanol fraction contained flavonoid, tannins, phenols, alkaloid and terpenoids, the chloroform fraction showed the presences of flavonoids, steroids and terpenoids. The acute oral toxicity test revealed that the crude extract was safe at 2000 mg/kg.Conclusion: This study demonstrated that the crude and fractions of Withania somnifera leaf has antidiarrheal activity and supports the folklore use of the plan for the treatment of diarrhea.
Molecular Docking Studies on the Interaction of Four Malagasy Cytotoxic Compounds with Angiogenesis Target Protein HIF-1α and Human Androgen Receptor and Their ADMET properties
No full textBackground and objectives: Cancer is a significant public health problem worldwide and constitutes the second leading cause of death after cardiovascular disease. This study was thus designed to identify new natural compounds from Malagasy medicinal plants traditionally used to treat cancer.Methodology: In silico analyses by molecular docking to model ligand-protein interactions, and by SwissADME and ADMET webservers to establish the pharmacokinetic profile of the four investigated compounds in interaction with the angiogenesis target protein HIF-1α/breast cancer (PDB ID: 3KCX) and human androgen receptor/prostate cancer (PDB ID: 1E3G) were performed.Results: The docking results show that the HIF-1α receptor has the best binding energy when it interacts with compound 1 (1’,4-dihydroxy-2,3’-dimethyl-1,2’-binapthyl-5,5’,8,8’-tetraone: -8.49 kcal/mol) followed by compound 3 ((E)-5,6-dimethyl-2-(2-methyl-3-(prop-1-enyl)phenyl)-2H-chromene: -8.43 kcal/mol), compound 2 (6’-ethoxy-1’3’-dihydroxy-4,6-dimethyl-1,2’-binaphthyl-2,5’,8,8’-tetraone: -7.80 kcal/mol) and compound 4 (methyl 10-hydroxy-2,4a,6a,9,12b,14a-hexamethyl-11-oxo-1,2,3,4,4a,5,6,6a,11,12b,13,14,14a,14b-tetradecahydropicene-2- carboxylate : -7.63 kcal/mol). The receptor 1E3G displayed poor binding affinity energy to all tested compounds with energy value above -11.99 Kcal/mol (co-crystal). Based on the H-bonding interaction, ligands 1 and 2 displayed good pharmacophore profile to both protein targets 3KCX and 1E3G. The ligand 3 does not interact with the selected receptors via hydrogen bonds. The pharmacokinetic profile of these phyto-compounds revealed that they are orally active and safe. They were isolated and their chemical structures were elucidated previously by our teamusingchromatographic and spectroscopic techniques(LC/MS/NMR).Conclusion: The ligands 1 and 2 can be considered as hits since they are non-carcinogenic and non-hepatotoxic, and could thus be useful as alternative therapy in breast than in prostate cancer.Â
Glucose oxidase as a model enzyme for antidiabetic activity evaluation of medicinal plants: In vitro and in silico evidences
No full textBackground and objectives: Diabetes mellitus is a major public health problem in the world. In Africa, more than 80% of patients use plants for their treatment. However, the methods of validation of endogenous knowledge usually used are costly. The alternative method we propose aims at creating hyperglycemia in vitro and exploiting the metabolic pathway involving glucose oxidase for UV-visible spectrophotometric screening of the antidiabetic activity of medicinal plants.Methodology: The evolution of glucose oxidation as a function of drug concentration is followed by UV-visible spectrophotometry. The formation of the stable complex between the enzyme and the inhibitor is studied by molecular docking.Results: Drugs used (Gliben and plant extracts) displayed an in vitro hypoglycemic effect by exponentially reducing the level of free glucose in vitro. L. multiflora is more active than V. amygdalina (IC50: 1.36 ± 0.09 mg/mL Vs IC50: 3.00 ± 0.54 mg/mL). Gliben (0.5 mg/mL) and L. multiflora (2 mg/mL) reduced both the rate of oxidation of glucose by glucose oxidase (catalytic power Vmax: 0.84 ± 0.11 mg*mL-1*min-1 for Gliben and 1.72 ± 0.13 mg*mL-1*min-1 for L. multiflora) and the affinity of this enzyme for its substrate-glucose (KM: 15.11 ± 2.72 mg*mL-1 for Gliben and 9.17 ± 1.56 mg*mL-1 for L. multiflora) when compared to enzyme catalysis in the  absence of inhibitor (Vmax: 2.86 ± 0.44 mg*mL-1*min-1; KM: 8.07 ± 1.96 mg*mL-1). The binding of GOX (1GAL) to selected phyto-compounds derived from L. multiflora was confirmed by molecular docking. The best stability complexes were obtained for four compounds 8 (-10.3 Kcal/mol), 9 (-9.7 Kcal/mol), 6 (-9.7 Kcal/mol) and 3 (-9.5 Kcal/mol). Among these compounds, compounds 8 et 6 formed their complexes through  hydrogen bonds: the compound 8 form 04 hydrogen bond (ALA 292, GLY 290, SER 291, TYR 80) while the compound 6 form 03 hydrogen bonds (SER 103, THR 110, TYR 515). However, none H-bonding interaction occurs in the complex that involves ligands 9 and 3 despite their high binding energy (-9.7 Kcal/mol and -9.5 Kcal/mol respectively).Conclusion: Glucose oxidase can serve as a marker enzyme for in vitro antidiabetic activity evaluation of medicinal plants
Characterization of phytochemicals and determination of antioxidant, antimicrobial and cytotoxic properties of the medicinal plant Ardisia solanacea
No full textThe present study was conducted to detect possible phytochemicals and evaluate antioxidant, antimicrobial and cytotoxic activities of the extract of Ardisia solanacea. Phytochemical screening was carried out using the standard test methods of different chemical group. For investigating the antioxidant activity, two complementary test methods namely DPPH free radical scavenging assay and total phenolic content determination were carried out. For the evaluation of in vitro antimicrobial activity, disc diffusion method was used. Evaluation of cytotoxic activity was done using the brine shrimp lethality bioassay. In DPPH free radical scavenging test, the petroleum ether soluble fraction showed the highest free radical scavenging activity with IC50 value 40.04 ?g/ml. while compared to that of the reference standards ascorbic acid. Ardisia solanacea was also found as a good source of total phenolic contents. Moreover, the extracts revealed moderate antimicrobial activity at the concentration of 400 ?g/disc. In cytotoxic activity test, the petroleum ether soluble fraction showed significant cytotoxic potential (LC50 value of 0.703 ?g/ml) among all the fractions comparing with that of standard vincristine (0.544 ?g/ml). Therefore, further studies are suggested to determine the active compounds responsible for the pharmacological activities of the plant extracts.
In vitro cytotoxic, thrombolytic, anthelmintic and antioxidant activities of Litsea monopetala: a medicinal plant
No full textThe present study was conducted to assess the cytotoxicity, thrombolytic, anthelmintic and antioxidant activity of mehanolic extract of Litsea monopetala (Family: Lauraceae) leaves in laboratory using in vitro methods. Cytotoxicity test was done by brine shrimp lethality bioassay where the extract concentration was 400, 200, 100, 50, 25, 12.5, 6.25, 3.125, 1.5625, 0.78125 (µg/ml). In vitro thrombolytic activity of Litsea monopetala was performed by clot lysis method using extract concentration 2.5, 5, 10 and 20 (mg/mL) in saline water. Anthelmintic activity test was done by using adult earthworms where 10, 20, 40, 60, 80 (mg/ml) extract concentration were used. Finally antioxidant activity was determined by total phenolic content determination using Folin-Ciocalteu reagent. The Litsea monopetala extract showed cytotoxic activity against brine shrimp nauplii and LC50 value was 41.05(µg/ml) and the investigated thrombolytic activity in our research was 9.52, 9.49, 13.64 and 17.50 % respectively as % of clot lysis. The paralysis time were at 76.75 min, 60 min, 51.75 min, 44.5 min and 64.5 min and death were at 90.50min, 63.75min, 55.50min, 44.75min and 71min. respectively. The Litsea monopetala extract displayed significant antioxidant activity which was 20.75 (mg of GAE / gm) of extracts. The activities observed could be attributed to presence of some of the phytochemicals which have been related with cytotoxic, thrombolytic, anthelmintic and antioxidant property.
Plants secondary metabolites and antiviral properties
No full textThere are between three and five million viral infections annually. And normally viral infections are being managed therapeutically through available antiviral regimens with unsatisfactory clinical outcomes. So chemically synthesized drugs can be replaced by secondary metabolites from medicinal plants, which are healthier, safer, and cheaper alternatives. Phytomolecules have been employed as antiviral medicines against a variety of viruses since they can inhibit them directly through blocking their entry or throughout the replication phases, in addition to their use as adjuvant treatments in respiratory infections. For instance, the newly emerged COVID-19 is causing one of the most disruptive pandemics in this century. Thus, phytomolecules offer a ray of hope for human health amid pandemics such as COVID-19. This review provides updated data on the secondary metabolites with different antiviral activities
In vitro analysis of phytoconstituents and bioactivities of Senna alata L. leaf extracts
No full textSenna alata L. is a widely distributed medicinal plant mainly used to treat fungal infections. The objectives of the present study were to investigate the phytochemical constituents, antioxidants, thrombolytic, anticoagulant and anthelmintic potentials of the aqueous (AE) and ethanolic (EE) extracts of Senna alata leaves. The major phytochemical classes were checked through qualitative screening. Quantitative assays were employed to determine the total phenolic, flavonoid, flavonol, tannin, and protein contents. Antioxidant potential was revealed through the DPPH scavenging assay. The extracts were applied to dissolve blood clots to evaluate the thrombolytic potential. Prothrombin time (PT) and activated partial thromboplastin time (aPTT) tests indicated the potential anticoagulant activity. The anthelmintic potential was evaluated by using aquarium worms (Tubifex tubifex). The presence of 9 different classes of phytochemicals indicated the chemical diversity of the extract. In the quantitative determination, EE was found to contain higher quantities of phytochemicals than AE. The highest DPPH scavenging activity (89.44%) was displayed by the EE at its 800 µg/mL concentration. The IC50 values of EE and AE were 61.02 µg/mL and 142.42 µg/mL, respectively. During the thrombolytic potential evaluation of EE and AE, 37% and 27% clot lysis abilities were observed respectively. EE paralyzed the aquarium worms at 4 min and killed them at 6 min. The leaves of Senna alata have the potentials for being utilized for medicinal purposes other than their traditional use as an antifungal agent. These findings can pave the way for the exploration of herbal remedies with better efficacy
Insight in the Phytochemistry of Wild Vegetable Vitex grandifolia Gürke with its Biological and Nutritional Importance – A Review
No full textVitex grandifolia belongs to genus Vitex, which is the largest in the family Lamiaceae, the species is distributed worldwide. The young leaves of V. grandifolia is culturally used as vegetables and for medicinal purposes. Vitex grandifolia is considered an underutilized and indigenous vegetable (UIV) because its importance and usefulness are greatly undervalued. Micro and macro-deficiency which is one of the main cause of health problems and high incidence of death in most children in sub-Sahara Africa. This has necessitated much research towards underutilized and indigenous vegetables (UIVs) because the populace in the remote places outside the commercial route mostly depends on food gathering from the wild and this could contribute greatly to their food system. Various publications’ sites, dissertation search engines, search engines were queried employing keywords as “Vitex grandifolia†and “biological activity of Vitex grandifoliaâ€. This study reports the untapped huge benefits this plant presents and further climaxes with up-to-date knowledge of its chemistry. Only about five compounds have been isolated so far, these compounds are mainly flavonoids and iridoids. The various in vitro and in vivo biological studies of these constituents and extracts were reported. Furthermore, the contradiction about the plant’s toxicity was explained in detail. The indications of its enormous traditional uses are large but the pharmacological facts are unsatisfying because they are few. It is quite relieving that its nutritional evidence is great though much is still needed. This review tends to create a foundation for further studies on its use as a vegetable
Silver hull buckwheat (Fagopyrum esculentum Moench) is a part of nature that offers best health and honour
No full textThe gluten-free pseudocereal Fagopyrum esculentum Moench (Silver hull buckwheat) belongs to the Polygonaceae family, which has a long history of both edible and medicinal use. It's a highly nutritious food ingredient that's been shown to have a variety of health benefits. Plasma cholesterol levels are lowered, neuroprotection is given, anticancer, anti-inflammatory, antidiabetic effects are provided, and hypertension conditions are improved thanks to Silver hull buckwheat. It has also been stated to have prebiotic and antioxidant properties. The aim of this review was to include an up-to-date and detailed study of F. esculentum. Furthermore, the potential for future research was addressed. Flavonoids, phenolics, fagopyritols, triterpenoids, hormones, and fatty acids are among the various compounds derived from F. esculentum. The main active ingredients were believed to be flavonoids and phenolic compounds. All of the information presented leads us to believe that Silver hull buckwheat has a strong medicinal potential. However, further research is needed to better understand its bioactive constituents, their structural functions, and molecular mechanisms underlying
Mini-review on the Phyto-chemistry, Pharmacology and Toxicology of Cola nitida (Vent.) Schott & Endl. (Malvaceae): A medically interesting bio-resource of multiple purposes in Africa
No full textThe aim of the present mini-review was to document knowledge on the phytochemistry, pharmacology and toxicity of Cola nitida, a medicinal plant species traditionally used in Africa for its multiple purposes. A non-exhaustive literature review for relevant articles published online was conducted in January 2021 using various electronic databases like Science Direct, PubMed, Web of Science, Scopus, Google Scholar and SciELO. The scientific name of this plant was used as keyword, along with the terms phytochemistry, pharmacology and toxicology. The chemical structures of compounds isolates from this plant were drawn using ChemBioDraw Ultra 12.0 software package. Literature surveys have revealed that C. nitida is highly appreciated by African populations in various cultures, especially in West Africa. Phytochemical analyses showed that  C. nitida contains mainly catechin, caffeine, epicatechin, polyphenols, alkaloids, tannins, saponins, bromelain, cardenolides, proanthocyanidins, triterpenes, glycosides, flavonoids, anthraquinones, steroids, anthocyanins, glycosides, alkaloids, etc. The presence of these phyto-compounds in the investigated plant species justify it’s used as anti-microbial, anti-malarial, anti-inflammatory, anti-diabetic, anti-coagulant agent. Thus, C. nitida could be as raw material for manufacturing efficient medication against various diseases including Sickle cell disease.Â