International Journal of Phytomedicine
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    Mechanism of action of a bioassay-guided aqueous fraction of Pterocarpus marsupium Roxb hardwood on glucose-dependent insulin secretion

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    We previously demonstrated that a high molecular weight aqueous fraction of Pterocarpus marsupium Roxb. (PM) hardwood has insulinotrophic properties. However, the pharmacological mechanisms by which this fraction modulates insulin secretion remained unknown. The present study therefore isolated the insulinotrophic activity enriched fraction (AEF) from aqueous extract of PM and examined its pharmacological mechanisms. A bioassay method utilizing insulin secretion from mouse pancreas in vitro, was used to fractionate the insulinotrophic activity of PM and to delineate its pharmacological mechanisms. In addition, the effect of AEF on glucose clearance in normoglycemic, non-diabetic sheep in vivo was examined. The AEF mimicked the effect of sulphonylureas on insulin secretory pathways and modulated insulin biosynthesis. However, unlike tolbutamide, AEF-induced insulin secretion is glucose-dependent. Furthermore, three daily intravenous administrations of AEF had prolonged effects on glucose responsiveness in non-diabetic normal sheep. The use of AEF to combat the adverse effects of hyperglycemia appears to be beneficial by enhancing and sustaining the glucose-dependent insulin secretion processes in pancreas. Of note, the insulinotrophic effect of AEF is prolonged by many hours to days, unlike the numerous conventional insulin secretagogus which over stimulate the β-cells or pose a risk of hypoglycemia

    Evaluation of the estrogenic properties of aqueous extracts of Tragia benthamii Baker (Euphorbiaceae) and Graptophyllum pictum (Acanthaceae) and their ability to alleviate some menopausal symptoms induced by ovariectomy in Wistar rats

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    Tragia benthamii Baker (Euphorbiaceae) and Graptophyllum pictum Linn (Acanthaceae) are two Cameroonian medicinal plants traditionally used against female reproductive tract disorders, during and after the reproductive period, and as an abortifacient. Since there were no scientific data supporting the above claims and pharmacological studies characterizing their estrogenic properties, we therefore aimed to evaluate their ability to induce estrogen-like effects on primary estrogens targets, uterine, vagina and mammary gland; as well as their ability to alleviate hot flushes in ovariectomized adult rats. For this purpose, we applied a 3-day uterotrophic assay to determine the estrogenic effects of each extract and the mixture of both plants as used by traditional practitioners. The extracts were administered orally for 3 days to the 10 to 12 weeks aged ovariectomized rats. The results obtained showed that the aqueous extract of T. benthamii at the dose of 500 mg / kg BW, the aqueous extract of G. pictum at all the tested doses as well as the aqueous extract of the mixture at 275 mg / kg body weight induced a significant increase (p ˂ 0.01) of the uterine epithelium thickness. In addition, the aqueous extract of T. benthamii at the dose of 500 mg / kg BW, as well as the aqueous extract of the mixture at the doses of 50 and 275 mg / kg induced acinar development and eosinophil secretions. These results are proof of estrogen-like effects of T. benthamii and G. pictum and therefore justify the traditional use of these plants. This suggests the presence in these plants, of secondary metabolites with estrogenic properties, can induce cell proliferation, and to correct disorders of post-oophorectomy œstrogénopénia in the Wistar rats and therefore menopausal disorders

    HPLC-UV profile of Genista ulicina Spach. (Fabaceae) extracts and in vitro antioxidant activity

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    To perform a qualitative and quantitative analysis of the phenolic and flavonoid contents and evaluate the antioxidant activity of ethyl acetate (EtOAc) and n-butanol (n-BuOH) extracts of the aerial parts of Genista ulicina Spach. from Algeria. The qualitative analysis of plant extracts was carried out by RP-HPLC using UV detector, whereas the quantification of total phenolic and flavonoid contents was completed according to the Folin-Ciocalteu procedure and aluminium chloride colorimetric method respectively. To evaluate the extract\u27s antioxidant activity, Two in vitro antioxidant tests were employed: DPPH and β-carotene bleaching assay. The HPLC/DAD chromatogram showed several peaks indicating the presence of phenolic acids, flavonoids and isoflavonoids in both extracts. The total phenolic content (TPC) ranged from 62.56 and 50.45 mgGAE/g extract, while the total flavonoids content varied between 53.1 and 48.4 mgQE/g extract for EtOAC and n-BuOH respectively. EtOAc extract showed a maximum inhibition value (78.15%) at 150µg/mL using DPPH test and highest antioxidative power (82.42%) using β-carotene bleaching assay comparing with standards. The HPLC-UV analysis showed the richeness of both extracts in phenolic and flavonoid contents. The EtOAc extract exhibited good antioxidant activities comparing to the n-BuOH extract. Thus Genista ulicina could be indicated as a plant of phytopharmaceutical importance

    In-vitro scavenging activity and acute toxicity study of methanol leaves extract and fractions of Lophira lanceolata Tiegh. Ex Keay (Ochnaceae) in rats.

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    The present study aims at comparing in-vitro scavenging activities of methanol extract and fractions of Lophira lanceolata leaves, and also to study the oral acute toxicity of the ethyl acetate fraction. Petroleum ether, dichloromethane, ethyl acetate, butanol and water fractions were prepared from the methanol extract of the plant. The scavenging activity of DPPH (2, 2-Diphenyl-1-picrylhydrazyl), the total phenolic (TPC) and total flavonoid (TFC) contents of the extract and fractions were determined by spectrophotometrical methods using gallic acid (GA) and quercetin (Qu) as reference antioxidant. The fifty percent inhibitory concentration (IC50), fifty percent effective concentration (EC50) and the antiradical power (ARP) were determined for all extract and fractions. An acute toxicity study using a single oral dose of 5000 mg/kg of the ethyl acetate fraction of the plant was conducted in female Albino rats following the OECD (420) Guidelines. Blood samples were collected for hematological and biochemical analysis. Histopathological examinations of the heart, kidney and liver were performed. The results showed that the ethyl acetate fraction of L. lanceolata had the highest free radical scavenging activity of DPPH (IC50=1,43; EC50= 0.07 and ARP = 14,28) and also contain the highest amount of total phenols (14,4±0,02 mg of GA equivalent/g of plant fraction) and total flavonoids (93,3±0,04 mg of Qu equivalent/g of plant fraction) as compared to other fractions and ascorbic acid (IC50=5,82; EC50= 3.44; ARP=3,44). The hematological parameters and the lipid profile didn’t show any major change compared to the control group. However, a significant increase of aspartate aminotransferase (AST, p<0.001) and alanine aminotransferase (ALT, p<0.001) showed that the ethyl acetate fraction of the methanol extract of L. lanceolata leaves might not totally be safe for consumption, in the conditions of our experiment

    Phytochemical analysis and DPPH scavenging activity of Combretum punctatum var. squamosum (Combretaceae), an ethnomedicinal plant of Mizoram.

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    The main objective of the study is to determine the phytochemical constituents and the DPPH scavenging activity of the aqueous extract of Combretum punctatum var. squamosum. The phytochemical screening revealed that the crude aqueous extract contained phenols, flavonoids, phytosterols and diterpenes while alkaloids, glycosides, tannins, carbohydrates, proteins and amino acids were found to be absent. The total phenol and flavonoid content in the crude aqueous extract was found to be comparatively high, i.e. 111 mg/g GAE and 120.99 mg/g QE respectively. It was also found that the % DPPH scavenging activity was very high and comparable to the standard used. The IC50 value of the aqueous extract was found to be 1.76 mg/ml which is lower but comparable to the IC50 value of the standard

    In silico investigations revealed four potential colon cancer drugs from phytochemicals in Zingiber officinale

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    Cancer is a difficult disease to treat, and few effective drugs are available. Hence, it is of great importance to develop effective anti-cancer therapeutic agents with well-defined pharmacokinetic properties. Although, ginger (Zingiber officinale) has a number of proven pharmacological activities, its effect on colon cancer has not received much attention. This study therefore investigated the potential colon cancer drug of compounds found in ginger. Dihydropyrimidine dehydrogenase was modeled using comparative homology modeling and virtual screening was performed locally on a Linux platform using AutoDock Vina®. The results showed that human dihydropyrimidine dehydrogenase is a homolog of pig dihydropyrimidine dehydrogenase. The leads of potential colon cancer drugs were beta-sitosterol, 6-Shogoal, Alloaromadedrene, and Zingiberol. They had similar binding site with levamisole for tumor necrosis factor ligand superfamily member 6 with His 148 and Tyr 192 common at their binding site whereas they had different binding sites from 5-fluorouracil for dihydropyrimidine dehydrogenase. The leads had better bioactivities compared with reference drugs (5-flourouracil and Levamisole) approved clinically for the treatment of colon cancer. In vitro, ex vivo and/or in vivo validations of the leads against colon cancer are recommended

    Phytochemical analysis, anti-oxidant and anti-microbial activity of Acalypha indica leaf extracts in different organic solvents

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    The herb Acalypha indica which belongs to Euphorbiaceae family has multiple medicinal properties which include anti-oxidant, anti-bacterial, anti-fungal, anti-inflammatory, antiulcer, anti-helmintic, anti-cancerous, anti-venom, and neuro-protective activity. The present study was designed to evaluate the phytochemical, antimicrobial and anti-oxidant activity of Acalypha indica leaves extracts in different solvent extractions like methanol, hexane, ethyl acetate and petroleum ether. Fresh leaves of the plant were collected and shade dried. Dried leaves were milled to obtain powder. Powder was subjected to soxhlet extraction using solvents and extracts were successively obtained. Phytochemical analysis was conducted following standard methods. Phytochemical analysis showed the presence of Alkaloids, Phenols, Saponins, Flavanoids and Amino acids. Leaf extract of methonal have shown the highest anti-oxidation capacity than hexane, ethyl acetate and petroleum ether. Anti-microbial activity has been performed on microbes like Bacillus sps, E.coli, Psuedomonas sps and Streptococcus sps. A highest value of zone of inhibition was found in methanol extract against E.coli. These results provide evidence that Acalypha indica leaf extract possesses vital phytochemicals, antimicrobial and antioxidant properties. Hence this plant can be studied further for drug analysis for finding potent medicines for diseases

    Cognitive antihyperlipidemic and antioxidant activities of bitter leaf (Vernonia amygdalina) and Scent leaf (Ocimum gratissimum)

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    Oxidative stress manifests an imbalance in the production and the detoxification of free radicals. Free radicals cause oxidative degradation of biomolecules like lipids, proteins, nucleic acids, and carbohydrate molecules, thereby compromising cell integrity and function and leading to health deterioration from a range of metabolic anomalies that cause diseases and ailments including cardiovascular diseases (CVD), hypertension, stroke and cancer. Both bitter leaf (VA) and Scent leaf (OG) have been medicinally useful in the cure of diseases in different cultures.The addition of scent leaf as additive in preparation of delicacies in Nigeria has prompted this study to determine the cognitive activities of both plants to repair the damages caused by high fat diet present, by evaluating the antidyslipidemic activitiesas well as their antioxidant potentials. The results obtained revealed that both plants have antioxidant abilities when subjected to standard antioxidant evaluations although VA was significantly higher (p˂0.05) when compared with OG, however the cognitive effects showed that the antioxidant potentials of VA was depressed on the addition of OG. The results obtained from the modulation of lipid in albino rats challenged with hyperlipidemia showed that both VA and OG have a positive effect to lower LDL-C, TAG, TCHOL and increase HDL-C thus potentiating their antidyslipidemic ability and protective role against dyslipidemic disorders. Similarly, the cognitive effect showed reduction in the activities of VA while the activity of OG was boosted. The high phospholipid contents of the selected tissues upon treatments with the leaf extracts also showed that both VA and OG can have ameliorating effects on coronary heart disease, inflammation or cancer by enhancing membrane integrity. It is noteworthy that both VA and OG have good potential in the ability to reverse induced dyslipidemia and in spontaneous cellular lipid, while the addition causes a reduction in the activities of VA

    Evaluation of central nervous system depressant activity of methanolic and petroleum ether extract of Manilkara zapota leaves (in vivo)

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    The purpose of this study was to examine the central nervous system (CNS) -depressant activity of methanolic and petroleum ether extracts of leaves obtained from Manilkara zapota (Sapotaceae) in vivo. CNS-depressant action was evaluated by observing the effects of plant extracts on both exploratory and spontaneous locomotor activity in mice using open field and hole cross tests respectively. The extracts were found to exhibit CNS-depressant activity in a dose-dependent manner. In the open field test, both the methanolic and petroleum ether extracts reduced the exploratory behavior of mice significantly (p<0.05). Although the extracts reduced locomotor activity in the hole cross test, the results were found to be insignificant. Overall, these findings indicate that both types of extracts derived from M. zapota leaves possess CNS-depressant activity

    Neuroprotective effects of sea buckthorn leaf extract against hypobaric hypoxia and post-hypoxic reoxygenation induced hippocampal damage in rats.

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    Exposure to hypobaric hypoxia (HBH) and reoxygenation (H/R) causes hippocampal neuronal damage leading to memory dysfunction and mood state alteration. The present study aimed at investigating the potential neuroprotective effect of seabuckthorn leaf extract ((SBTLE)) against HBH and reoxygenation induced neuronal injury in brain. Six groups of male sprague dawley rats were taken and exposed to simulated HBH equivalent at an altitude of 7600m in an animal decompression chamber for 7 days followed by reoxygenation. Rats were supplemented with SBTLE (100mg/kgBW) 20 days prior and during hypoxic exposure. Recovery from injuries following HBH exposure and subsequent reoxygenation was carried out in separate group of animals. Our study revealed that exposure to reoxygenation stress following hypoxia enhanced hypoxia induced oxidative stress in hippocampal neurons which was reversed with SBTLE supplementation. SBTLE restored Hypoxia/Reoxygenation(H/R) induced downregulation of γ-glutamylcysteine synthetase (GCLC) enzymes responsible for glutathione biosynthesis. Post hypoxic supplementation of SBTLE decreased the reoxygenation induced enhanced oxidative markers, however, administration of SBTLE in conjunction with the inhibitor of GCLC resulted in slow recovery from H/R injuries. These results provide the first evidence of SBTLE induced increase in glutathione biosynthesis by upregulating GCLC enzyme expression and hence can be used as a promising drug to cure H/R induced neuronal damages

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    International Journal of Phytomedicine
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