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具有α-葡萄糖苷酶抑制活性的色酮衍生物来自海洋真菌 梅雷。

Chromone Derivatives with α-Glucosidase Inhibitory Activity from the Marine Fungus Maire.

机构信息

School of Pharmacy, Henan University, Kaifeng 475004, China.

Key Laboratory of Marine Biogenetic Resources, Third Institute of Oceanography, Ministry of Natural Resources, Xiamen 361005, China.

出版信息

Molecules. 2021 Aug 31;26(17):5273. doi: 10.3390/molecules26175273.

Abstract

The fungal strain YPGA3 was isolated from the sediments of the Yap Trench and identified as . Eight new chromone derivatives, named penithochromones M-T (-), along with two known analogues, and were isolated from the strain. The structures were established by detailed analyses of the spectroscopic data. The absolute configuration of the only chiral center in compound was tentatively determined by comparing the experimental and the calculated specific rotations. Compounds and represent the first examples of chromone derivatives featuring a 5,7-dioxygenated chromone moiety with a 9-carbon side chain. Bioassay study revealed that compounds - exhibited remarkable inhibition against α-glucosidase with IC values ranging from 268 to 1017 μM, which are more active than the positive control acarbose (1.3 mmol).

摘要

真菌菌株 YPGA3 从 Yap 海沟的沉积物中分离出来,并被鉴定为. 从该菌株中分离得到了八个新的色酮衍生物,命名为 penithochromones M-T(-),以及两个已知类似物 和. 通过详细分析光谱数据确定了结构。通过比较实验和计算的比旋光度,暂定确定了化合物 中唯一手性中心的绝对构型。化合物 和 代表了具有 5,7-二氧代色酮部分和 9 碳侧链的色酮衍生物的首例。生物测定研究表明,化合物 - 对 α-葡萄糖苷酶具有显著的抑制作用,IC 值范围为 268 至 1017 μM,比阳性对照阿卡波糖(1.3 mmol)更具活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/93ab/8434415/6044a7b79670/molecules-26-05273-g001.jpg

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