丝瓜素I的合成与生物活性
Synthesis and bioactivity of Luffarin I.
作者信息
Urosa Aitor, Marcos Isidro S, Díez David, Lithgow Anna, Plata Gabriela B, Padrón José M, Basabe Pilar
机构信息
Department of Organic Chemistry, Chemistry Faculty, University of Salamanca, Plaza de los Caídos 1-5, 37008 Salamanca, Spain.
Nuclear Magnetic Resonance Service, University of Salamanca, Plaza de los Caídos 1-5, 37008 Salamanca, Spain.
出版信息
Mar Drugs. 2015 Apr 20;13(4):2407-23. doi: 10.3390/md13042407.
The first synthesis of Luffarin I, sesterterpenolide isolated from sponge Luffariella geometrica, has been accomplished from commercially available sclareol. The key strategy involved in this synthesis is the diastereoselective reduction of an intermediate ketone. Luffarin I against human solid tumor cell lines showed antiproliferative activities (GI50) in the range 12-17 μM.
从海绵状几何芋参（Luffariella geometrica）中分离得到的倍半萜内酯鲁法林I（Luffarin I）首次全合成已由市售的香紫苏醇完成。该合成过程的关键策略是中间体酮的非对映选择性还原。鲁法林I对人实体瘤细胞系显示出抗增殖活性（GI50），范围为12 - 17 μM。
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