New antimalarial norterpene cyclic peroxides from Xisha Islands sponge Diacarnus megaspinorhabdosa. Issue 8 (15th April 2016)

• Record Type: Journal Article
• Authors: Yang, Fan; Wang, Ru-Ping; Xu, Bin; Yu, Hao-Bing; Ma, Guo-Yi; Wang, Guang-Fei; Dai, Shu-Wen; Zhang, Wei; Jiao, Wei-Hua; Song, Shao-Jiang; Lin, Hou-Wen
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 8(2016)
• Page Start: 2084
• Page End: 2087
• Publication Date: 2016-04-15
• Subjects: Diacarnus megaspinorhabdosa -- Norterpene cyclic peroxide -- Antimalarial; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.02.070
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Seven norterpene cyclic peroxides including four new ones have been isolated from Xisha Islands sponge Diacarnus megaspinorhabdosa in the South China Sea. The structures of the compounds were elucidated on the basis of spectroscopic analyses. All the norterpene cyclic peroxides displayed antimalarial activity against Plasmodium falciparum (D6 and W2 clones) with the IC50 values in the range of 1.6–8.6 μM. Especially, the new compound3 showed significant antimalarial activity with the IC50 values of 1.6 (W2) and 2.2 (D6) μM. Abstract: Four new norterpene cyclic peroxides (1 –4 ), together with three known norterpene cyclic peroxides were isolated from the Xisha Islands Sponge Diacarnus megaspinorhabdosa . Their structures were elucidated on the basis of spectroscopic analyses and comparison with the related model compounds. The compounds (1 –7 ) were evaluated for the inhibitory activity against the malaria parasite Plasmodium falciparum, all of them showed significant antimalarial activity with IC50 values in the range of 1.6–8.6 μM.