Lee Sang-Myung, Park Jin-Gyu, Lee You-Hee, Lee Cheal-Gyu, Min Byung-Sun, Kim Jung-Hee, Lee Hyeong-Kyu
KT&G Central Research Institute, Yuseong, Daejeon, Korea.
Biol Pharm Bull. 2004 Nov;27(11):1883-6. doi: 10.1248/bpb.27.1883.
In order to determine on the anti-complement activity of triterpenes, following eleven triterpenoides were isolated from the fruits of the Zizyphus jujuba MILL: ceanothane-type triterpenes: colubrinic acid (1), zizyberenalic acid (11); lupane-type triterpenes: alphitolic acid (2), 3-O-cis-p-coumaroyl alphitolic acid (3), 3-O-trans-p-coumaroyl alphitolic acid (4), betulinic acid (7), betulonic acid (9); and oleanane-type triterpenes: 3-O-cis-p-coumaroyl maslinic acid (5), 3-O-trans-p-coumaroyl maslinic acid (6), oleanolic acid (8), oleanonic acid (10). These compounds were examined for their anti-complement activity against the classical pathway of the complement system. Among them, compounds 5, 6, and 8 exhibited significant anti-complement activity with IC(50) values of 101.4, 143.9, and 163.4 microM, respectively, whereas the ceanothane-type and the lupane-type triterpenes were inactive. This suggests that the oleanane-structure plays an important role in inhibiting the hemolytic activity of human serum against erythrocytes.
为了测定三萜类化合物的抗补体活性，从酸枣果实中分离出以下11种三萜类化合物：ceanothane型三萜类化合物：蛇麻脂酸（1）、酸枣仁烯酸（11）；羽扇豆烷型三萜类化合物：α-香树脂醇酸（2）、3-O-顺式对香豆酰基α-香树脂醇酸（3）、3-O-反式对香豆酰基α-香树脂醇酸（4）、桦木酸（7）、桦木酮酸（9）；以及齐墩果烷型三萜类化合物：3-O-顺式对香豆酰基山楂酸（5）、3-O-反式对香豆酰基山楂酸（6）、齐墩果酸（8）、齐墩果酮酸（10）。检测了这些化合物对补体系统经典途径的抗补体活性。其中，化合物5、6和8表现出显著的抗补体活性，IC50值分别为101.4、143.9和163.4微摩尔，而ceanothane型和羽扇豆烷型三萜类化合物无活性。这表明齐墩果烷结构在抑制人血清对红细胞的溶血活性中起重要作用。
