Abstract

Four new polyketides: nectriacids A–C (1–3) and 12-epicitreoisocoumarinol (4), together with three known compounds: citreoisocoumarinol (5), citreoisocoumarin (6), and macrocarpon C (7) were isolated from the culture of the endophytic fungus Nectria sp. HN001, which was isolated from a fresh branch of the mangrove plant Sonneratia ovata collected from the South China Sea. Their structures were determined by the detailed analysis of NMR and mass spectroscopic data. The absolute configuration of the stereogenic carbons for compound 4 was further assigned by Mosher’s ester method. All of the isolated compounds were tested for their α-glucosidase inhibitory activity by UV absorbance at 405 nm, and new compounds 2 and 3 exhibited potent inhibitory activity with IC50 values of 23.5 and 42.3 μM, respectively, which were more potent than positive control (acarbose, IC50, 815.3 μM).

Highlights

  • Diabetes mellitus, one of the most common chronic metabolic diseases, occurs when the pancreas produces insufficient levels of insulin or when the body cannot use the insulin effectively [1]

  • The fungal strain HN001 was isolated from the branches of the mangrove plant Sonneratia ovata collected from the South China Sea in Hainan province, China

  • The reported IC50 was the average value of two independent experiments

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Summary

Introduction

One of the most common chronic metabolic diseases, occurs when the pancreas produces insufficient levels of insulin or when the body cannot use the insulin effectively [1]. Α-Glucosidase is an important enzyme for breaking down complex carbohydrates for absorption, and α-glucosidase inhibitors such as acarbose, miglitol, and voglibose, all originating from natural products, are widely used to treat type II diabetes, indicating that natural products are an important source of anti-diabetes drugs. As part of our ongoing investigation into bioactive metabolites from mangrove endophytic fungi collected from the South. China Sea [6,7,8,9,10,11,12], a chemical investigation of the mangrove-derived fungus Nectria sp. Theresults resultsshowed showedthat thatcompounds compounds and and 33 exhibited inhibitory activity activity toward toward α-glucosidase. Details details of of the the isolation, activity against against α-glucosidase α-glucosidase of of these these compounds compounds are are described

15 H18 O4
C16 H20 O4
General
Fungal Material
In Vitro Inhibition Studies on α-Glucosidase
Conclusions
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