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.
Highlights
Protein tyrosine phosphatase 1B (PTP1B), as a therapeutic target for the treatment of Type-II diabetes and obesity, has been the subject of intense study over the past decade [1,2,3,4,5]
Further investigation of crude fractions with PTP1B inhibitory activity from the same sample led to the isolation of a series of new hippolides-related sesterterpenes, compounds
We have evaluated the cytotoxicity of compounds 1–5 against A549, HeLa, and HCT-116 cancer cell lines, only compound 1 exhibited weak activity against HCT-116 cell line with an IC50 value of 11.6 μM and no activity was observed for other compounds
Summary
Protein tyrosine phosphatase 1B (PTP1B), as a therapeutic target for the treatment of Type-II diabetes and obesity, has been the subject of intense study over the past decade [1,2,3,4,5]. 300 new or known natural products with PTP1B inhibitory activity, have been isolated and identified from various natural resources, many of which are of marine origin [2]. Marine sponges of the genus Hippospongia (family Spongiidae, order Dictyoceratida) have attracted a great deal of attention as they contain bioactive sesquiterpenes [8,9,10,11], sesterterpenes and sulfates [12,13,14], furanoterpenes [15], triterpenoic acids [16], and polyketides [17]. Further investigation of crude fractions with PTP1B inhibitory activity from the same sample led to the isolation of a series of new hippolides-related sesterterpenes, compounds. We report the isolation, structure elucidation, and bioactivity of these compounds
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