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In vitro evaluation of the ?-glucosidase inhibitory potential of methanolic extracts of traditionally used antidiabetic plants.

ABSTRACT: BACKGROUND:Different plant parts of Roylea cinerea (D. Don) Baill. (Lamiaceae), Clematis grata Wall. (Ranunculaceae), Cornus capitata Wall. (Cornaceae) are traditionally used in the management of diabetes and various other diseases. METHOD:The air-dried plant parts from different plants were coarsely powdered and macerated in methanol to obtain their crude extracts. The crude extracts were evaluated for their ?-glucosidase inhibitory activity. On the basis of results obtained, the methanolic crude extract of Cornus capitata Wall. was further sequentially fractionated in hexane, diethyl ether, ethyl acetate, n-butanol. Fractions obtained were also evaluated for their ?-glucosidase inhibitory potential. The kinetic study was performed using Lineweaver Burk plot to evaluate the type of inhibition. Furthermore, in silico analysis was also carried with active sites of the enzyme (PDB ID: 3WY1) using Autodock4. RESULTS:Among all the plant extracts, Cornus capitata extract showed maximum inhibitory activity. Therefore its methanolic extract was further fractionated with the help of different solvents and the maximum activity was shown by the ethyl acetate fraction (IC50 50??g/mL). Kinetic analysis indicated that Vmax and Km were increased indicating a competitive type of inhibition. In docking studies, among different constituents known in this plant, betulinic acid showed minimum binding energy (-?10.21?kcal/mol). The kinetic and docking studies have strengthened the observation made in the present study regarding the ?-glucosidase inhibitory activity of Cornus capitata. CONCLUSION:The study provided partial evidence for pharmacological basis regarding clinical applications of Cornus capitata in the treatment of diabetes suggesting it to be a suitable candidate for the treatment of postprandial hyperglycemia.

SUBMITTER: Bhatia A

PROVIDER: S-EPMC6434821 | biostudies-literature | 2019 Mar

REPOSITORIES: biostudies-literature

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In vitro evaluation of the α-glucosidase inhibitory potential of methanolic extracts of traditionally used antidiabetic plants.

Bhatia Astha A Singh Balbir B Arora Rohit R Arora Saroj S

BMC complementary and alternative medicine 20190325 1

<h4>Background</h4>Different plant parts of Roylea cinerea (D. Don) Baill. (Lamiaceae), Clematis grata Wall. (Ranunculaceae), Cornus capitata Wall. (Cornaceae) are traditionally used in the management of diabetes and various other diseases.<h4>Method</h4>The air-dried plant parts from different plants were coarsely powdered and macerated in methanol to obtain their crude extracts. The crude extracts were evaluated for their α-glucosidase inhibitory activity. On the basis of results obtained, the ...[more]

PMID: 30909900

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Project description:α-glucosidase inhibitors represent an important class of type 2 antidiabetic drugs and they act by lowering postprandial hyperglycemia. Today, only three synthetic inhibitors exist on the market, and there is a need for novel, natural and more efficient molecules exhibiting this activity. In this study, we investigated the ability of Tamarix nilotica ethanolic and aqueous shoot extracts, as well as methanolic fractions prepared from aqueous crude extracts to inhibit α-glucosidase. Both, 50% ethanol and aqueous extracts inhibited α-glucosidase in a concentration-dependent manner, with IC50 values of 12.5 μg/mL and 24.8 μg/mL, respectively. Importantly, α-glucosidase inhibitory activity observed in the T. nilotica crude extracts was considerably higher than pure acarbose (IC50 = 151.1 μg/mL), the most highly prescribed α-glucosidase inhibitor on the market. When T. nilotica crude extracts were fractionated using methanol, enhanced α-glucosidase inhibitory activity was observed in general, with the highest observed α-glucosidase inhibitory activity in the 30% methanol fraction (IC50 = 5.21 μg/mL). Kinetic studies further revealed a competitive reversible mechanism of inhibition by the plant extract. The phytochemical profiles of 50% ethanol extracts, aqueous extracts, and the methanolic fractions were investigated and compared using a metabolomics approach. Statistical analysis revealed significant differences in the contents of the crude extracts and fractions and potentially identified the molecules that were most responsible for these observed variations. Higher α-glucosidase inhibitory activity was associated with an enrichment of terpenoids, fatty acids, and flavonoids. Among the identified molecules, active compounds with known α-glucosidase inhibitory activity were detected, including unsaturated fatty acids, triterpenoids, and flavonoid glycosides. These results put forward T. nilotica as a therapeutic plant for type 2 diabetes and a source of α-glucosidase inhibitors.

Project description:Hyperglycemia is the hallmark of type 2 diabetes mellitus, and its prevention will go a long way in managing the disease and its associated complications. Reduction of postprandial hyperglycemia through retarding carbohydrates digesting enzymes is one of the major therapeutic approaches used in the management of diabetes.The aim of the present study was to investigate the antidiabetic and cytotoxic effects of Cissus cornifolia extracts in vitro.The α-amylase and α-glucosidase inhibitory activities of ethanolic and aqueous extracts of C. cornifolia root and leaves were investigated when the cytotoxic effects of these extracts were analyzed using MTT assay on human embryonic kidney (HEK 293) cell lines.The root ethanolic extract showed a mild α-amylase inhibitory activity with IC50 value of 22.75 ± 1.23 μg/ml, but strong α-glucosidase inhibitory activity with IC50 value 2.81 ± 0.97 μg/ml and the aqueous root extract indicated moderate inhibition for both α-amylase and α-glucosidase with IC50 values of 33.70 ± 3.75 and 37.48 ± 2.35 μg/ml, respectively. The ethanolic root extract was found nontoxic at tested concentrations on HEK 293 cell lines as confirmed by the MTT assay with 93% cell viability at the highest concentration (200 μg/ml) tested. However, the aqueous extracts (leaf and root) were found cytotoxic at concentrations above 50 μg/ml.Data of this study suggest that the root ethanolic extracts of C. cornifolia possesses moderate α-amylase, but strong α-glucosidase inhibitory activity in vitro and did not show significant cytotoxicity with the tested concentrations.Present study was conducted to examine effects of antidiabetic and cyctotoxic effects of Cissus conrnifolia root and leaves extracts in vitro. Data of this study suggest that the root ethanolic extract of C. cornifolia possesses mild to moderated antidiabetic activity via inhibiting carbohydrate digesting enzymes when no significant toxicity was observed with tested concentrations. Abbreviations used: alex: Aqueous leaf extract; arex: Aqueous root extract; CC: Cissus cornifolia; DNS: Dinitrosalicylic acid; DMSO: Dimethylsulfoxide; elex: Ethanolic leaf extract; erex: Ethanolic root extract; IDF: International Diabetes Federation; MEM: Minimum essential medium; NIDDM: Noninsulin-dependent diabetes mellitus; pNPG: Para-nitrophenyl glucopyranoside; SD: Standard deviation; T2D: Type 2 diabetes.

Project description:A study was carried out to evaluate the acaricidal activities of crude methanolic extract of leaves of six medicinal plants, namely, Vernonia amygdalina, Calpurnia aurea, Schinus molle, Ricinus communis, Croton macrostachyus, and Nicotiana tabacum, against Rhipicephalus (Boophilus) decoloratus and Rhipicephalus pulchellus using an in vitro adult immersion test. Five graded concentrations of the crude extracts, 6.25, 12.5, 25, 50, and 100?mg/ml, were tested at different time intervals, and temporal changes in tick viability were recorded for 24 hours. Diazinon (0.1%) and distilled water were used as positive and negative controls, respectively. Standard procedures were applied to screen the phytochemical constituents of the tested plant parts. Phytochemical screening showed the presence of a condensed amount of tannins in all extracts. Starting from 30?min post exposure, the 100?mg/ml concentration of C. aurea and R. communis extracts has caused significantly higher mortality (P < 0.05) compared to the diazinon. A significant increase in tick mortality started 2?hr post exposure with diazinon and 50 and 100?mg/ml concentrations of S. molle. Vernonia amygdalina extract and diazinon showed a significant increase in tick mortality 3?hr post exposure with 100?mg/ml concentration. Similarly, a significant increase in tick mortality started 2?hr post exposure with diazinon and 100?mg/ml concentrations of C. macrostachyus and N. tabacum. At 24?hr post exposure, diazinon and 50 and 100?mg/ml concentrations of all the extracts have caused significantly higher tick mortality than the rest of the concentrations (P < 0.05). Higher concentrations of all the extracts had showed a comparable and strong acaricidal effect on Rhipicephalus (Boophilus) decoloratus and Rhipicephalus pulchellus having no significant difference with that of the positive control (P > 0.05) at 24?hr post exposure period. Tick killing activity of all evaluated plant extracts increases with increasing exposure time and concentration as well. Thus, all the tested plants could be used against Rhipicephalus (Boophilus) decoloratus and Rhipicephalus pulchellus as a potential alternative to substitute commercially available drugs. We recommend further study on fractionating each component separately and validating the materials.

Project description:Background: Cancer is a major cause of mortality worldwide with increasing numbers by the years. In North Africa, the number of cancer patients is alarming. Also shocking is that a huge number of cancer patients only have access to traditional medicines due to several factors, e.g., economic difficulties. In fact, medicinal plants are widely used for the treatment of several pathologies, including cancer. Truthfully, herbalists and botanists in North African countries prescribe several plants for cancer treatment. Despite the popularity and the potential of medicinal plants for the treatment of cancer, scientific evidence on their anticancer effects are still scarce for most of the described plants. Objective: Bearing in mind the lack of comprehensive and systematic studies, the aim of this review is to give an overview of studies, namely ethnobotanical surveys and experimental evidence of anticancer effects regarding medicinal plants used in North Africa for cancer therapy. Method: The research was conducted on several popular search engines including PubMed, Science Direct, Scopus and Web of Science. The research focused primarily on English written papers published between the years 2000 and 2016. Results: This review on plants traditionally used by herbalists in North Africa highlights that Morocco and Algeria are the countries with most surveys on the use of medicinal plants in folk medicine. Among the plethora of plants used, Nigella sativa and Trigonella foenum-graecum are the most referred ones by herbalists for the treatment of cancer. Moreover, a plethora of scientific evidence qualifies them as candidates for further drug development. Furthermore, we report on the underlying cellular and molecular mechanisms. Conclusion: Overall, this review highlights the therapeutic potential of some medicinal plants as anticancer agents. The North African flora offers a rich source of medicinal plants for a wide array of diseases, including cancer. The elucidation of their modes of action represents an indispensable condition for the rational development of new drugs for cancer treatment. Furthermore, testing the anticancer activity in vivo and in clinical trials are warranted to explore the full therapeutic potential of North African plants for cancer therapy.

Project description:The number of patients with type 2 diabetes mellitus (T2DM) has increased worldwide. Although an instant cure was achieved with the standard treatment acabose, unsatisfactory symptoms associated with cardiovascular disease after acabose administration have been reported. Therefore, it is important to explore new treatments. A Thai folk recipe has long been used for T2DM treatment, and it effectively decreases blood glucose. However, the mechanism of this recipe has never been proven. Therefore, the potential anti-T2DM effect of this recipe, which is used in Thai hospitals, was determined to involve alpha-glucosidase (AG) inhibition with a half maximal inhibitory concentration (IC50). In vitro experiments showed that crude Cinnamomum verum extract (IC50 = 0.35 ± 0.12 mg/mL) offered excellent inhibitory activity, followed by extracts from Tinospora crispa (IC50 = 0.69 ± 0.39 mg/mL), Stephania suberosa (IC50 = 1.50 ± 0.17 mg/mL), Andrographis paniculate (IC50 = 1.78 ± 0.35 mg/mL), and Thunbergia laurifolia (IC50 = 4.66 ± 0.27 mg/mL). However, the potencies of these extracts were lower than that of acabose (IC50 = 0.55 ± 0.11 mg/mL). Therefore, this study investigated and developed a formulation of this recipe using computational docking. Among 61 compounds, 7 effectively inhibited AG, including chlorogenic acid (IC50 = 819.07 pM) through 5 hydrogen bonds (HBs) and 2 hydrophobic interactions (HIs); β-sitosterol (IC50 = 4.46 nM, 6 HIs); ergosterol peroxide (IC50 = 4.18 nM, 6 HIs); borapetoside D (IC50 = 508.63 pM, 7 HBs and 2 HIs); borapetoside A (IC50 = 1.09 nM, 2 HBs and 2 His), stephasubimine (IC50 = 285.37 pM, 6 HIs); and stephasubine (IC50 = 1.09 nM, 3 HBs and 4 HIs). These compounds bind with high affinity to different binding pockets, leading to additive effects. Moreover, the pharmacokinetics of six of these seven compounds (except ergosterol peroxide) showed poor absorption in the gastrointestinal tract, which would allow for competitive binding to AG in the small intestine. These results indicate that the development of these 6 compounds into oral antidiabetic agents is promising.

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In vitro evaluation of the ?-glucosidase inhibitory potential of methanolic extracts of traditionally used antidiabetic plants.

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In vitro evaluation of the α-glucosidase inhibitory potential of methanolic extracts of traditionally used antidiabetic plants.

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