Microbial transformation of the antimalarial sesquiterpene endoperoxide dihydroartemisinin

被引:9
作者
Han, Fubo
Lee, Ik-Soo [1 ]
机构
[1] Chonnam Natl Univ, Coll Pharm, Gwangju, South Korea
基金
新加坡国家研究基金会;
关键词
Dihydroartemisinin; microbial transformation; Absidia coerulea; Penicillium chrysogenum; IN-VIVO; ARTEMISININ; METABOLISM; DRUG; DERIVATIVES; ARTESUNATE; ARTEMETHER;
D O I
10.1080/14786419.2016.1250092
中图分类号
O69 [应用化学];
学科分类号
081704 ;
摘要
Dihydroartemisinin (DHA, 1), a sesquiterpene endoperoxide derived from artemisinin, has shown potent antimalarial and anticancer activities. Microbial transformation of DHA by Absidia coerulea and Penicillium chrysogenum yielded one new (3) and four known metabolites (2, 4-6). The chemical structures of these compounds were identified as deoxydihydroartemisinin (2), 8-hydroxydeoxyartemisinin (3), deoxyartemisinin (4), 9-hydroxyartemethin-I (5) and 3-hydroxydeoxydihydroartemisinin (6) using spectroscopic analyses. Among them, compounds 3 and 4 are artemisinin analogues, which were achieved by unusual oxidation at C-12 position. Biotransformation of DHA by microorganisms was an effective approach to obtain new derivatives of DHA.
引用
收藏
页码:883 / 889
页数:7
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