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Cucurbitane-type compounds from Momordica charantia: Isolation,in vitro antidiabetic,anti-inflammatory activities and in silico modeling approaches
Affiliation:1. Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming 650500, Yunnan, People''s Republic of China;2. State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, Yunnan, People''s Republic of China;3. University of Chinese Academy of Science, Beijing 100049, People''s Republic of China
Abstract:Momordica charantia L., commonly known as bitter melon, belongs to the Cucurbitaceae family. Various in vitro and in vivo studies have indicated that extracts of bitter melons have anti-diabetic properties. However, very little is known about the specific purified compounds responsible for these antidiabetic properties. In the present study, 3β,7β,25-trihydroxycucurbita-5,23(E)-dien-19-al, charantal, charantoside XI, and 25ξ-isopropenylchole-5, 6-ene-3-O-d-glucopyranoside were isolated from bitter melon fruit. The structures of the purified compounds were elucidated by HR-ESIMS, 1D, and 2D NMR experiments. All compounds exhibited significant inhibition of α-amylase and α-glucosidase comparable to acarbose. Molecular docking studies demonstrated that purified compounds were able to bind to the active sites of proteins. Additionally, the purified compounds showed significant anti-inflammatory activity, downregulating the expression of NF-κB, iNOS, IL-6, IL-1β, TNF-α, and Cox-2 in lipopolysaccharide-activated macrophage RAW 264.7 cells. Our findings suggest that the purified compounds have potential anti-diabetic and anti-inflammatory activities and therefore hold promise for the development of plant-based management for diabetic and inflammatory conditions.
Keywords:Bitter melon  Cucurbitaceae  Triterpene aglycones  Murine macrophages  Molecular docking
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