Otshudi A Longanga, Apers S, Pieters L, Claeys M, Pannecouque C, De Clercq E, Van Zeebroeck A, Lauwers S, Frédérich M, Foriers A
Department of Pharmaceutical Sciences, Laboratory of Pharmacognosy and Phytochemistry, Vrije Universiteit Brussel (VUB), Laarbeeklaan 103, B-1090 Brussels, Belgium.
J Ethnopharmacol. 2005 Oct 31;102(1):89-94. doi: 10.1016/j.jep.2005.05.021.
Methanol and water extracts of the root of Epinetrum villosum (Exell) Troupin (Menispermaceae) were found to exhibit antimicrobial and antiplasmodial activities. Investigation of the active methanol fraction led to the isolation of four bisbenzylisoquinoline alkaloids, i.e., cycleanine, cycleanine N-oxide, isochondodendrine and cocsoline. Structures were established by spectroscopic methods. Cocsoline displayed antibacterial and antifungal activities (MIC values of 1000-15.62 and 31.25 microg/ml, respectively). Isochondodendrine was found to have the most potent antiplasmodial activity (IC50 = 0.10 microg/ml), whereas the IC50 on HCT-116 human colon carcinoma cells was 17.5 microg/ml (selectivity index 175). Cycleanine acted against HIV-2 (EC50=1.83 microg/ml) but was at least 10-fold less active against HIV-1. Cycleanine N-oxide showed no activity towards all tested microorganisms.
绒毛千金藤(防己科)根的甲醇提取物和水提取物具有抗菌和抗疟活性。对活性甲醇部位的研究导致分离出四种双苄基异喹啉生物碱,即轮环藤宁碱、轮环藤宁碱氮氧化物、异谷树碱和考索林。通过光谱方法确定了其结构。考索林具有抗菌和抗真菌活性(MIC值分别为1000 - 15.62和31.25微克/毫升)。发现异谷树碱具有最强的抗疟活性(IC50 = 0.10微克/毫升),而对HCT - 116人结肠癌细胞的IC50为17.5微克/毫升(选择性指数175)。轮环藤宁碱对HIV - 2有作用(EC50 = 1.83微克/毫升),但对HIV - 1的活性至少低10倍。轮环藤宁碱氮氧化物对所有测试微生物均无活性。