New Hippolide Derivatives with Protein Tyrosine Phosphatase 1B Inhibitory Activity from the Marine Sponge Hippospongia lachne

Marine Drugs

Shu-Juan Piao²  Wei-Hua Jiao¹  Fan Yang¹  Yang-Hua Yi²  Ying-Tong Di³  Bing-Nan Han¹ 

[1] Key Laboratory for Marine Drugs, Department of Pharmacy, Renji Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200127, China; E-Mails:;Laboratory of Marine Drugs, Department of Pharmacy, Changzheng Hospital, Second Military Medical University, Shanghai 200003, China; E-Mails:;Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, Yunnan, China; E-Mail:

关键词: marine sponge;    Hippospongia lachne;    sesterterpenoids;    absolute configuration;    PTP1B;   

DOI  :  10.3390/md12074096

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.