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进一步从西沙软珊瑚 Sinularia polydactyla 中得到的作为 PTP1B 抑制剂的新二萜。

Further New Diterpenoids as PTP1B Inhibitors from the Xisha Soft Coral Sinularia polydactyla.

机构信息

State Key Laboratory of Drug Research, Shanghai Institute of MateriaMedica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Zhangjiang Hi-Tech Park, Shanghai 201203, China.

University of Chinese Academy of Sciences, No. 19A Yuquan Road, Beijing 100049, China.

出版信息

Mar Drugs. 2018 Mar 25;16(4):103. doi: 10.3390/md16040103.

Abstract

A new prenyleudesmane type diterpene, sinupol (), and a new capnosane type diterpenoid, sinulacetate (), were isolated from the Xisha soft coral along with five known related diterpenes (- and ). Their structures, including absolute configurations, were determined by extensive spectroscopic analysis, the comparison of their NMR data with those of related compounds, and time-dependent density functional theory electronic circular dichroism (TDDFT ECD) calculations. Both new compounds ( and ) exhibited promising inhibitory activity against protein tyrosine phosphatase 1B (PTP1B), a potential drug target for the treatment of type II diabetes and obesity.

摘要

从西沙软珊瑚中分离得到了一种新的prenyleudesmane 型二萜化合物 sinupol()和一种新的 capnosane 型二萜类化合物 sinulacetate(),以及五种已知的相关二萜类化合物 (- 和 )。通过广泛的光谱分析、与相关化合物的 NMR 数据比较以及时变密度泛函理论电子圆二色性(TDDFT ECD)计算,确定了它们的结构,包括绝对构型。这两个新化合物(和)对蛋白酪氨酸磷酸酶 1B(PTP1B)表现出了有希望的抑制活性,PTP1B 是治疗 II 型糖尿病和肥胖症的潜在药物靶点。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0b79/5923390/ff8fcfd6c841/marinedrugs-16-00103-g001.jpg

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