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从海洋海绵拉氏 Hippospongia lachne 中分离得到的具有蛋白酪氨酸磷酸酶1B抑制活性的新型海马内酯衍生物。

New hippolide derivatives with protein tyrosine phosphatase 1B inhibitory activity from the marine sponge Hippospongia lachne.

作者信息

Piao Shu-Juan, Jiao Wei-Hua, Yang Fan, Yi Yang-Hua, Di Ying-Tong, Han Bing-Nan, Lin Hou-Wen

机构信息

Laboratory of Marine Drugs, Department of Pharmacy, Changzheng Hospital, Second Military Medical University, Shanghai 200003, China.

Key Laboratory for Marine Drugs, Department of Pharmacy, Renji Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200127, China.

出版信息

Mar Drugs. 2014 Jul 8;12(7):4096-109. doi: 10.3390/md12074096.

Abstract

Five new sesterterpenoids, compounds 1-5, have been isolated from the sponge Hippospongia lachne off Yongxing Island in the South China Sea. The structures of compounds 1-5 were elucidated through extensive spectroscopic analysis, including HRMS, 1D, and 2D NMR experiments. The stereochemistry, including absolute configurations of these compounds, was determined by spectroscopic, chemical, and computational methods. Compounds 1 and 5 showed moderate protein tyrosine phosphatase 1B (PTP1B) inhibitory activities with IC50 values of 5.2 μM and 8.7 μM, respectively, more potent than previously reported hippolides.

摘要

从中国南海永兴岛附近的海绵希波海绵(Hippospongia lachne)中分离出了5种新的倍半萜化合物,即化合物1 - 5。通过广泛的光谱分析,包括高分辨质谱(HRMS)、一维(1D)和二维(2D)核磁共振实验,阐明了化合物1 - 5的结构。这些化合物的立体化学,包括绝对构型,通过光谱、化学和计算方法确定。化合物1和5表现出适度的蛋白酪氨酸磷酸酶1B(PTP1B)抑制活性,IC50值分别为5.2 μM和8.7 μM,比先前报道的海兔毒素更有效。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/64c8/4113817/14e22679eaf2/marinedrugs-12-04096-g001.jpg

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