Salacinol and related analogs: new leads for type 2 diabetes therapeutic candidates from the Thai traditional natural medicine Salacia chinensis

Nutrients
Toshio MorikawaOsamu Muraoka

Abstract

The antidiabetic effect of a hot water extract of stems of Salacia chinensis (SCE) was evaluated in vivo in KK-Ay mice, a typical type 2 diabetes mellitus mice model. Administration of CE-2 dietary feed containing 0.25 and/or 0.50% of SCE for three weeks to KK-Ay mice significantly suppressed the elevation of both blood glucose and HbA1c levels without significant changes in body weight or food intake. Glucose tolerance was improved by administration to KK-Ay mice for 27 days of AIN93M purified dietary feed containing 0.12% of SCE. No suppressive effect with respect to HbA1c level was observed when AIN93M/Glc dietary feed in which all digestible glucides were replaced with glucose was administered with SCE. Thus, α-glucosidase inhibitory activity approved as the mechanism of action of the antidiabetic effect of SCE by in vitro investigation was reconfirmed also in in vivo studies. Evaluation of the α-glucosidase inhibitory activity of the active constituents, salacinol (1), kotalanol (3), and neokotalanol (4), by employing human α-glucosidases revealed that these compounds inhibited them as potently (IC50 = 3.9-4.9 μM for maltase) as they inhibited rat small intestinal α-glucosidase. The principal sulfonium constituents (1-4) w...Continue Reading

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Citations

Jun 3, 2015·Phytotherapy Research : PTR·Sidney J Stohs, Sidhartha Ray
Jul 5, 2016·Chemical & Pharmaceutical Bulletin·Kiyofumi NinomiyaToshio Morikawa
Dec 14, 2017·Journal of Natural Medicines·Toshio MorikawaKiyofumi Ninomiya
Jul 2, 2019·Chemical & Pharmaceutical Bulletin·Toshio MorikawaOsamu Muraoka
Aug 30, 2020·Pharmaceuticals·Francesca MangiavacchiLuca Sancineto
Mar 18, 2021·Natural Product Research·Nhan T NguyenMai T T Nguyen
Dec 1, 2017·The Journal of Organic Chemistry·Fumihiro IshikawaGenzoh Tanabe

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Methods Mentioned

BETA
pharmacotherapy

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