Grupo de Química Orgánica, Unidad de Biotecnología del Centro de Investigación Científica de Yucatán, Calle 43 No 130, Colonia Chuburná, Mérida, Yucatán, 97200 México.
Fitoterapia. 2010 Apr;81(3):219-22. doi: 10.1016/j.fitote.2009.09.006. Epub 2009 Sep 23.
Natural azorellane and mulinane diterpenoids show antituberculosis activity, which is increased by methylation of their free carboxyl group. We have systematically investigated the effect of alkylation in this class of diterpenoids and found that the profile of bioactivity is relatively unaffected by the introduction of short alkyl groups, both linear and branched. In this investigation, three semisynthetic diterpenoids, 13 hydroxy-mulin-11-en-20-oic acid n-propyl ester (3) and the n-propyl (19) and n-butyl (20) esters of isomulinic acid, showed the strongest antituberculosis activity (MIC=6.25 microg/mL) against a drug-resistant strain of Mycobacterium tuberculosis.
天然偶氮雷琐烷和木兰烷二萜类化合物具有抗结核活性，其游离羧基的甲基化可增强其活性。我们系统地研究了此类二萜化合物的烷基化效应，发现短链烷基（无论是直链还是支链）的引入对生物活性的分布影响不大。在本研究中，三种半合成二萜化合物，13-羟基木兰-11-烯-20-酸正丙酯（3）和异木兰酸的正丙酯（19）和正丁酯（20），对耐多药结核分枝杆菌表现出最强的抗结核活性（MIC=6.25μg/mL）。
