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In Vitro Antidiabetic Effects of Isolated Triterpene Glycoside Fraction from Gymnema sylvestre.

ABSTRACT: A triterpene glycoside (TG) fraction isolated and purified from ethanolic extract of Gymnema sylvestre (EEGS) was investigated for blood glucose control benefit using in vitro methods. The HPLC purified active fraction TG was characterized using FTIR, LC-MS, and NMR. The purified fraction (TG) exhibited effective inhibition of yeast α-glucosidase, sucrase, maltase, and pancreatic α-amylase with IC₅₀ values 3.16 ± 0.05 μg/mL, 74.07 ± 0.51, 5.69 ± 0.02, and 1.17 ± 0.24 μg/mL, respectively, compared to control. TG was characterized to be a mixture of triterpene glycosides: gymnemic acids I, IV, and VII and gymnemagenin. In vitro studies were performed using mouse pancreatic β-cell lines (MIN6). TG did not exhibit any toxic effects on β-cell viability and showed protection against H₂O₂ induced ROS generation. There was up to 1.34-fold increase in glucose stimulated insulin secretion (p<0.05) in a dose-dependent manner relative to standard antidiabetic drug glibenclamide. Also, there was further one-fold enhancement in the expression of GLUT2 compared to commercial standard DAG (deacylgymnemic acid). Thus, the present study highlights the effective isolation and therapeutic potential of TG, making it a functional food ingredient and a safe nutraceutical candidate for management of diabetes.

SUBMITTER: Shenoy RS

PROVIDER: S-EPMC6106959 | biostudies-literature |

REPOSITORIES: biostudies-literature

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Project description:Gymnema sylvestre Wild R.Br (family: Asclepidaceae) is a valuable medicinal plant used in folk medicine to treat diabetes, obesity, asthma etc. in India for antiquity. Diabetes mellitus is a syndrome characterized immunologically by lymphocyte apoptosis and reduced cell-mediated and humoral immunity. Modulation of immune responses to alleviate diseases has been of interest, and traditional herbal medicines may play an important role in this regard. In this study, we aim to evaluate the immunomodulatory potential of methanolic extract of G. sylvestre leaf using rat model. HPLC analysis of leaf extract was carried out for gymnemic acid. The method involves the initial hydrolysis of gymnemic acids, the active ingredients, to a common aglycone followed by the quantitative estimation of gymnemagenin, using gymnemagenin as reference standard. Gymnemic acid content was 2.40% (w/w) in G. sylvestre leaf extract. In vitro immunomodulatory activity of the methanolic extract of G. sylvestre leaf (1-200μg/ml) was evaluated by gauging its effects on nitroblue tetrazolium reduction and nitrite release in rat peritoneal macrophages and on mitogen (ConA, PHA and LPS) induced splenic lymphocyte proliferation. G. sylvestre leaf extract showed significant (<0.05) enhancement in NO and ROS generation in macrophages and in proliferation of lymphocytes in dose dependent manner. EC50 value was 3.10, 3.75 and 2.68 μg/ml for NBT reduction, nitrite release and lymphoproliferation, respectively. Potential effect was observed at 100 μg/ml in NO and ROS generation in macrophages and 20 μg/ml in lymphocyte proliferation. G. sylvestre leaf extract stimulates macrophage reactivity, increasing the level of activity even higher when combined with PMA or LPS. These findings suggest the presence of active compounds, gymnemic acid, in methanolic extract of G. sylvestre leaf that stimulates both myeloid and lymphoid components of immune system, and therefore can restore the innate immune function. Through this study, the traditional knowledge of anti-diabetic property of G. sylvestre is scientifically supplemented with its immunomodulatory properties.

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In Vitro Antidiabetic Effects of Isolated Triterpene Glycoside Fraction from Gymnema sylvestre.

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