深海沉积物来源真菌中的潜在 -葡萄糖苷酶抑制剂

Potential -Glucosidase Inhibitors from the Deep-Sea Sediment-Derived Fungus .

机构信息

Beijing Key Laboratory for Separation and Analysis in Biomedicine and Pharmaceuticals, School of Life Science, Beijing Institute of Technology, Beijing 100081, China.

Hainan Provincial Key Laboratory for Functional Components Research and Utilization of Marine Bio-Resources, Institute of Tropical Bioscience and Biotechnology, Chinese Academy of Tropical Agricultural Sciences & Key Laboratory for Biology and Genetic Resources of Tropical Crops of Hainan Province, Hainan Institute for Tropical Agricultural Resources, Haikou 571101, China.

出版信息

Mar Drugs. 2023 Feb 26;21(3):157. doi: 10.3390/md21030157.

DOI:10.3390/md21030157

PMID:36976206

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10056930/

Abstract

Three new phenolic compounds, epicocconigrones C-D (-) and flavimycin C (), together with six known phenolic compounds: epicocconigrone A (); 2-(10-formyl-11,13-dihydroxy-12-methoxy-14-methyl)-6,7-dihydroxy-5-methyl-4-benzofurancarboxaldehyde (); epicoccolide B (); eleganketal A (); 1,3-dihydro-5-methoxy-7-methylisobenzofuran (); and 2,3,4-trihydroxy-6-(hydroxymethyl)-5-methylbenzyl-alcohol (), were isolated from fermentation cultures of a deep-sea sediment-derived fungus, . Their planar structures were elucidated based on the 1D and 2D NMR spectra and HRESIMS data. The absolute configurations of compounds - were determined by ECD calculations. Compound represented a rare fully symmetrical isobenzofuran dimer. All compounds were evaluated for their -glucosidase inhibitory activity, and compounds , -, and exhibited more potent -glucosidase inhibitory effect with IC values ranging from 17.04 to 292.47 μM than positive control acarbose with IC value of 822.97 μM, indicating that these phenolic compounds could be promising lead compounds of new hypoglycemic drugs.

摘要

从深海沉积物来源的真菌中分离得到三种新的酚类化合物，即 epicocconigrones C-D (-) 和 flavimycin C ( )，以及六种已知的酚类化合物：epicocconigrone A (); 2-(10-甲酰基-11,13-二羟基-12-甲氧基-14-甲基)-6,7-二羟基-5-甲基-4-苯并呋喃甲酰醛 (); epicoccolide B (); eleganketal A (); 1,3-二氢-5-甲氧基-7-甲基异苯并呋喃 (); 和 2,3,4-三羟基-6-(羟甲基)-5-甲基苄醇 ( )。它们的平面结构是根据 1D 和 2D NMR 光谱和 HRESIMS 数据确定的。通过 ECD 计算确定了化合物 - 的绝对构型。化合物代表了一种罕见的完全对称的异苯并呋喃二聚体。所有化合物均进行了 -葡萄糖苷酶抑制活性评价，化合物、、和对 -葡萄糖苷酶的抑制活性强于阳性对照阿卡波糖（IC 值为 822.97 μM），IC 值范围为 17.04 至 292.47 μM，表明这些酚类化合物可能是新型降血糖药物的有前途的先导化合物。