Department of Organic Chemistry, University of Yaoundé I, P.O. Box 812 Yaoundé, Cameroon.
Phytother Res. 2010 Nov;24(11):1676-9. doi: 10.1002/ptr.3192.
The methanol extract from the stem bark of Diospyros sanza-minika as well as five norbergenin derivatives isolated from this crude extract were evaluated for their in vitro activity against Plasmodium falciparum K1 and cytotoxicity on MRC-5 cells. 4-O-(3'-methylgalloyl)norbergenin was found to be the most potent compound (IC(50) 0.6 μg/mL; CC(50) 24.7 μg/mL), followed by 4-O-galloylnorbergenin (IC(50) 3.9 μg/mL; CC(50) > 64 μg/mL) and 11-O-p-hydroxy-benzoyl-norbergenin (IC(50) 4.9 μg/mL; CC(50) > 64 μg/mL). Norbergenin and 4-O-syringoylnorbergenin were inactive (IC(50) > 32 μg/mL; CC(50) > 64 μg/mL). The antimalarial activity of the pure constituents and of the methanol extract from the stem bark of Diospyros sanza-minika is reported for the first time. The results provide interesting baseline information for the potential use of the crude extract well as some of the isolated compounds in the search for novel antimalarial compounds.
从柿科植物桑扎敏卡茎皮中提取的甲醇提取物以及从该粗提物中分离得到的五种去甲橙皮苷衍生物，对其抗疟原虫 falciparum K1 的体外活性和对 MRC-5 细胞的细胞毒性进行了评价。发现 4-O-(3'-甲基没食子酰基)去甲橙皮苷（IC500.6 μg/mL；CC5024.7 μg/mL）是最有效的化合物，其次是 4-O-没食子酰基去甲橙皮苷（IC503.9 μg/mL；CC50>64 μg/mL）和 11-O-p-羟基苯甲酰基去甲橙皮苷（IC504.9 μg/mL；CC50>64 μg/mL）。去甲橙皮苷和 4-O-对羟基苯甲酰基去甲橙皮苷（IC50>32 μg/mL；CC50>64 μg/mL）无活性。这是首次报道柿科植物桑扎敏卡茎皮的纯成分和甲醇提取物的抗疟活性。这些结果为粗提物以及一些分离得到的化合物在寻找新型抗疟化合物方面的潜在应用提供了有趣的基础信息。
