Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 2, Pages 390-392Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.11.068
Keywords
Dysidea villosa; Sesquiterpene quinone; PTP1B inhibitory activity
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Funding
- National Marine 863 Projects [2006AA09Z447, 2006AA09Z412, 2007AA09Z447]
- Natural Science Foundation of China [30730108, 20721003, 20772136]
- STCSM Project [07XD14036]
- CAS Key Project [KSCX2-YW-R-18]
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A new sesquiterpene quinone, 21-dehydroxybolinaquinone (5), together with two known related analogues, bolinaquinone (6) and dysidine (7), had been isolated from the Hainan sponge Dysidea villosa. The structure of the new compound 5 was elucidated on the basis of detailed analysis of spectroscopic data and by comparison with related model compounds. Compounds 5-7 were evaluated for the inhibitory activity against hPTP1B, a potential drug target for treatment of type-II diabetes and obesity, and cytotoxic activity against Hela cell line. The results showed that dysidine (7) had the strongest hPTP1B inhibitory activity with an IC50 value of 6.70 mu M and 6 had significant cytotoxic activity against Hela cell line with an IC50 value of 5.45 mu M. New compound 5 showed moderate PTP1B inhibitory activity and cytotoxicity with IC50 values of 39.50 and 19.45 mu M, respectively. (C) 2008 Elsevier Ltd. All rights reserved.
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