Abstract
Four new phenanthrene derivatives, gastrobellinols A-D (1–4), were isolated from the methanolic extract of Gastrochilus bellinus (Rchb.f.) Kuntze, along with eleven known phenolic compounds including agrostophyllin (5), agrostophyllidin (6), coniferyl aldehyde (7), 4-hydroxybenzaldehyde (8), agrostophyllone (9), gigantol (10), 4-(methoxylmethyl)phenol (11), syringaldehyde (12), 1-(4′-hydroxybenzyl)-imbricartin (13), 6-methoxycoelonin (14), and imbricatin (15). Their structures were determined by spectroscopic methods. Each isolate was evaluated for α-glucosidase inhibitory activity. Compounds 1, 2, 3, 7, 9, 13, and 15 showed higher activity than the drug acarbose. Gastrobellinol C (3) exhibited the strongest α-glucosidase inhibition with an IC50 value of 45.92 μM. A kinetic study of 3 showed competitive inhibition on the α-glucosidase enzyme. This is the first report on the phytochemical constituents and α-glucosidase inhibitory activity of G. bellinus.
Highlights
Diabetes mellitus (DM), one of the most common metabolic diseases, is characterized by high blood glucose levels due to a deficiency of insulin in the body or insufficient insulin sensitivity [1]. α-Glucosidase inhibitors (AGIs), for example, acarbose and voglibose, are the drugs of choice for treating type II DM patients owing to their minimal side effects
As part of our continuing studies on bioactive compounds from orchids [10,11,12], we investigated the chemical constituents of G. bellinus and their α-glucosidase inhibitory potential
This study is the first report on the secondary metabolites of Gastrochilus bellinus
Summary
Α-Glucosidase inhibitors (AGIs), for example, acarbose and voglibose, are the drugs of choice for treating type II DM patients owing to their minimal side effects. These AGI drugs still have shortcomings, involving the high cost of production and the need for sugar-like unit(s) in their core structure, and this has motivated researchers to find alternative sources of AGIs [2]. As part of our continuing studies on bioactive compounds from orchids [10,11,12], we investigated the chemical constituents of G. bellinus and their α-glucosidase inhibitory potential. The butanol and aqueous extracts were found to be devoid of activity (less than 10% inhibition)
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