Scalarane sesterterpenes from the South China Sea sponge Hyrtios erecta and their PTP1B inhibitory activity

被引:2
|
作者
Sun, Li-Li [1 ]
Shen, Yi-Ran [1 ]
Li, Jia [1 ,2 ]
Wang, Jian-Rong [1 ]
Li, Xu-Wen [1 ,2 ]
Guo, Yue-Wei [1 ,2 ]
机构
[1] Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zu Chong Zhi Rd,Zhangjiang Hitech Pk, Shanghai 201203, Peoples R China
[2] Bohai Rim Adv Res Inst Drug Discovery, Drug Discovery Shandong Lab, Yantai 264117, Shandong, Peoples R China
基金
中国国家自然科学基金;
关键词
Sponge; Hyrtios erecta; Scalarane-type sesterterpene; Configuration; PTP1B; MARINE SPONGE; ANTINEOPLASTIC AGENTS; SESQUITERPENES;
D O I
10.1016/j.tet.2023.133388
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Three new scalarane-type sesterterpenes, namely Hyrtiosins H-J (1-3), along with thirteen known related compounds (4-16), were isolated from the South China Sea sponge Hyrtios erecta. Their struc-tures were elucidated by extensive spectroscopic analysis and by the comparison of their spectroscopic data with those reported in the literature. The stereochemistry of heteronemin (9) was determined for the first time by X-ray crystallography study using Cu Ka radiation. In bioassay, compound 5 and 10 displayed considerable inhibitory activity against human protein tyrosine phosphatase 1B (PTP1B) enzyme with IC50 values of 19.68 mM, and 8.81 mM, respectively.(c) 2023 Elsevier Ltd. All rights reserved.
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页数:5
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