Lupenone Isolated from Diospyros melanoxylon Bark Non-competitively Inhibits alpha-amylase Activity

Mohan Krishna Durgam, Praveen Kumar Vemuri, Vijaya Lakshmi Bodiga, Sreedhar Bodiga

Abstract


Diabetes mellitus is a chronic disease that poses a serious global health problem, due to its associated effects on obesity and aging. Therapeutic strategies for targeting diabetes include the downregulation and/or inhibition of enzymes such as a-amylase and a-glucosidase, hydrolyzing the dietary carbohydrates in intestine. There is increasing interest for a-amylase inhibitors from natural sources. Our objective was to undertake the phytochemical screening of bark extracts of Diospyros melanoxylon for potential a-amylase inhibitory activity and further identification of the active principle and the underlying mechanisms of inhibition. Enzyme-assay guided fractionation of the Diospyros melanoxylon bark extract led to the isolation of a triterpene, Lupenone as a potential inhibitor of a-amylase, with a non-competitive inhibition and inhibitor constant = 30 mM. Lupenone-mediated inhibition of a-amylase responsible for the breakdown of dietary sugar may be effective in preventing postprandial hyperglycemia in the diabetic subjects.


Keywords


Diospyros melanoxylon; Ebenaceae; Triterpenoid ketone; pancreatic amylase; non-competitive inhibition

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DOI: https://doi.org/10.14421/biomedich.2023.121.171-176

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Copyright (c) 2023 Mohan Krishna Durgam, Praveen Kumar Vemuri, Vijaya Lakshmi Bodiga, Sreedhar Bodiga



Biology, Medicine, & Natural Product Chemistry
ISSN 2089-6514 (paper) - ISSN 2540-9328 (online)
Published by Sunan Kalijaga State Islamic University & Society for Indonesian Biodiversity.

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