title: New hippolide derivatives with protein tyrosine phosphatase 1B inhibitory activity from the marine sponge Hippospongia lachne.
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.
authors.affiliation: Laboratory of Marine Drugs, Department of Pharmacy, Changzheng Hospital, Second Military Medical University, Shanghai 200003, China. piaoshujuan@163.com.
authors.forename: Shu-Juan
authors.initials: SJ
authors.lastname: Piao
authors.affiliation: Key Laboratory for Marine Drugs, Department of Pharmacy, Renji Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200127, China. jiaoweihua1982@sina.com.
authors.forename: Wei-Hua
authors.initials: WH
authors.lastname: Jiao
authors.affiliation: Key Laboratory for Marine Drugs, Department of Pharmacy, Renji Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200127, China. bill1985@126.com.
authors.forename: Fan
authors.initials: F
authors.lastname: Yang
authors.affiliation: Laboratory of Marine Drugs, Department of Pharmacy, Changzheng Hospital, Second Military Medical University, Shanghai 200003, China. yiyanghua@126.com.
authors.forename: Yang-Hua
authors.initials: YH
authors.lastname: Yi
authors.affiliation: Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, Yunnan, China. diyt@mail.kib.ac.cn.
authors.forename: Ying-Tong
authors.initials: YT
authors.lastname: Di
authors.affiliation: Key Laboratory for Marine Drugs, Department of Pharmacy, Renji Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200127, China. hanbingnan@shsmu.edu.cn.
authors.forename: Bing-Nan
authors.initials: BN
authors.lastname: Han
authors.affiliation: Laboratory of Marine Drugs, Department of Pharmacy, Changzheng Hospital, Second Military Medical University, Shanghai 200003, China. franklin67@126.com.
authors.forename: Hou-Wen
authors.initials: HW
authors.lastname: Lin
mesh_terms: D000818:Animals; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D011161:Porifera / Q000378:metabolism*; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors*; D054830:Sesterterpenes / Q000494:pharmacology*
chemical_list: D004791:Enzyme Inhibitors; D054830:Sesterterpenes; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1