天然和半合成吖啶烷和木兰烷二萜的抗结核活性。
Antituberculosis activity of natural and semisynthetic azorellane and mulinane diterpenoids.
机构信息
Grupo de Química Orgánica, Unidad de Biotecnología, Centro de Investigación Científica de Yucatán, Calle 43 No 130, Colonia Chuburná, Mérida, Yucatán 97200, Mexico.
出版信息
Fitoterapia. 2010 Jan;81(1):50-4. doi: 10.1016/j.fitote.2009.07.005. Epub 2009 Jul 24.
The antituberculosis activity of 14 natural azorellane and mulinane diterpenoids isolated from Azorella compacta, Azorella madreporica, Mulinum crassifolium, and Laretia acaulis, together with eight semisynthetic derivatives, was evaluated against two Mycobacterium tuberculosis strains. The natural azorellanes azorellanol (3) and 17-acetoxy-13-alpha-hydroxyazorellane (6), and the semisynthetic mulinanes 13-hydroxy-mulin-11-en-20-oic-acid methyl ester (13) and mulinenic acid methyl ester (23), showed the strongest activity, with MIC values of 12.5 microg/mL against both strains. The methylated derivatives 13-hydroxy-mulin-11-en-20-oic-acid methyl ester (13), mulin-11,13-dien-20-oic acid methyl ester (15) and mulinenic acid methyl ester (23) proved to be more active than the parent compounds.
从 Azorella compacta、Azorella madreporica、Mulinum crassifolium 和 Laretia acaulis 中分离得到的 14 种天然偶氮雷兰烷和木兰烷二萜类化合物及其 8 种半合成衍生物对两种结核分枝杆菌菌株的抗结核活性进行了评价。天然偶氮雷兰烷类化合物 azorellanol（3）和 17-乙酰氧基-13-α-羟基偶氮雷兰烷（6）以及半合成木兰烷类化合物 13-羟基木兰-11-烯-20-酸甲酯（13）和木兰酸甲酯（23）表现出最强的活性，对两种菌株的 MIC 值均为 12.5μg/mL。甲基化衍生物 13-羟基木兰-11-烯-20-酸甲酯（13）、木兰-11,13-二烯-20-酸甲酯（15）和木兰酸甲酯（23）比母体化合物更具活性。
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