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从西沙群岛海绵大刺肉球海绵中分离得到的新型抗疟诺萜类环状过氧化物。

New antimalarial norterpene cyclic peroxides from Xisha Islands sponge Diacarnus megaspinorhabdosa.

作者信息

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

机构信息

Research Center for Marine Drugs, State Key Laboratory of Oncogenes and Related Genes, Department of Pharmacy, Ren Ji Hospital, School of Medicine, Shanghai Jiao Tong University, Shanghai 200127, China.

Research Center for Marine Drugs, State Key Laboratory of Oncogenes and Related Genes, Department of Pharmacy, Ren Ji Hospital, School of Medicine, Shanghai Jiao Tong University, Shanghai 200127, China; School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, China.

出版信息

Bioorg Med Chem Lett. 2016 Apr 15;26(8):2084-7. doi: 10.1016/j.bmcl.2016.02.070. Epub 2016 Feb 23.

DOI:10.1016/j.bmcl.2016.02.070
PMID:26965857
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.

摘要

从西沙群岛海绵巨刺肉海绵中分离得到4个新的降萜环过氧化物(1-4),以及3个已知的降萜环过氧化物。通过光谱分析并与相关模型化合物对比确定了它们的结构。对化合物(1-7)进行了抗疟原虫恶性疟原虫的抑制活性评价,所有化合物均表现出显著的抗疟活性,IC50值在1.6-8.6 μM范围内。

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