来自钝叶大戟乳汁的具有抑制哺乳动物线粒体呼吸链活性的大戟烷二萜类化合物。
Tigliane diterpenes from the latex of Euphorbia obtusifolia with inhibitory activity on the mammalian mitochondrial respiratory chain.
作者信息
Betancur-Galvis Liliana, Palomares Emilio, Marco J Alberto, Estornell Ernesto
机构信息
Grupo de Reproducción, Universidad de Antioquia, A.A. 1226, Medellín, Colombia.
出版信息
J Ethnopharmacol. 2003 Apr;85(2-3):279-82. doi: 10.1016/s0378-8741(03)00010-2.
Six diterpenes isolated from the latex of Euphorbia obtusifolia Poir. (Euphorbiaceae) were evaluated for their inhibition of the NADH oxidase activity in submitochondrial particles from beef heart. 4,20-Dideoxyphorbol-12,13-bis(isobutyrate) was the most potent inhibitor and showed an inhibitory concentration with IC(50) value of 2.6+/-0.3mM. In the present study, some structure-activity trends are suggested for the inhibitory activity of the mammalian mitochondrial respiratory chain of these natural product derivatives of 4-deoxyphorbol esters.
对从钝叶大戟（大戟科）乳胶中分离出的六种二萜类化合物进行了评估，以研究它们对牛心亚线粒体颗粒中NADH氧化酶活性的抑制作用。4,20-二脱氧佛波醇-12,13-双（异丁酸酯）是最有效的抑制剂，其抑制浓度的IC(50)值为2.6±0.3mM。在本研究中，针对这些4-脱氧佛波醇酯天然产物衍生物对哺乳动物线粒体呼吸链的抑制活性，提出了一些构效关系趋势。
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