A novel sesquiterpene quinone from Hainan sponge Dysidea villosa.
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 IC(50) value of 6.70microM and 6 had significant cytotoxic activity against Hela cell line with an IC(50) value of 5.45microM. New compound 5 showed moderate PTP1B inhibitory activity and cytotoxicity with IC(50) values of 39.50 and 19.45microM, respectively.
Li
Yan
Y
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Zhangjiang Hi-Tech Park, Shanghai 201203, PR China.
Zhang
Yu
Y
Shen
Xu
X
Guo
Yue-Wei
YW
D000818:Animals; D004353:Drug Evaluation, Preclinical; D006367:HeLa Cells; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D011161:Porifera / Q000737:chemistry*; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors; D011809:Quinones / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D012717:Sesquiterpenes / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology
D011809:Quinones; D012717:Sesquiterpenes; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1