Department of Pharmaceutical Sciences, University of Antwerp, Antwerp, Belgium.
Phytochemistry. 2010 May;71(7):785-91. doi: 10.1016/j.phytochem.2010.02.005. Epub 2010 Feb 26.
Preliminary screening of a series of medicinal plants, traditionally used in Tanzania, showed an IC(50) of 15.6-31.2 microg/ml for the crude extract of the root of Ormocarpum kirkii S. Moore (Papilionaceae) against Plasmodium falciparum. A bioguided isolation was performed in order to isolate the active constituents. Twelve constituents were obtained and identified using NMR and MS data, and optical rotation measurements. The compounds comprised seven (I-3,II-3)-biflavonoids, three (I-3,II-3)-bi-4-phenyldihydrocoumarins, an isoflavanone and a C-glucosylated flavone. Six compounds, liquiritigeninyl-(I-3,II-3)-naringenin, apigeninyl-(I-3,II-3)-naringenin, 7-O-beta-D-glucopyranosylchamaejasmin, (3R,4S,3''R,4''S)-5,5''-di-O-methyldiphysin, 7-O-beta-D-glucopyranosyldiphysin, and 4''-hydroxydiphysolone, were isolated in addition to six known components. The compounds were evaluated for antimicrobial activity in a broad screening panel, including P. falciparum. Seven of these showed antiplasmodial activity; isochamaejasmin being the most active with an IC(50) of 7.3+/-3.8 microM, but the selectivity was rather limited. Thus, these constituents may contribute, at least in part, to the antimalarial use of O. kirkii in traditional medicine.
对坦桑尼亚传统使用的一系列药用植物进行初步筛选，结果显示，奥罗卡普鲁姆·基尔基（Ormocarpum kirkii）根的粗提取物对恶性疟原虫（Plasmodium falciparum）的 IC50 为 15.6-31.2μg/ml。为了分离活性成分，进行了生物导向分离。使用 NMR 和 MS 数据以及旋光测量法获得并鉴定了 12 种成分。这些化合物包括 7 种（I-3,II-3）双黄酮、3 种（I-3,II-3）双-4-苯二氢香豆素、异黄酮和 C-葡萄糖基化黄酮。有 6 种化合物，甘草素基-（I-3,II-3）-柚皮素、芹菜素基-（I-3,II-3）-柚皮素、7-O-β-D-吡喃葡萄糖基查马酮、（3R,4S,3''R,4''S）-5,5''-二-O-甲基金丝桃苷、7-O-β-D-吡喃葡萄糖基二氢金丝桃苷和 4''-羟基二氢金丝桃苷，除了 6 种已知成分外，还分离出了这些化合物。对这些化合物进行了广谱筛选，包括恶性疟原虫，评估其抗菌活性。其中 7 种具有抗疟原虫活性；异查马酮的活性最高，IC50 为 7.3+/-3.8μM，但选择性相当有限。因此，这些成分可能至少部分地促成了奥罗卡普鲁姆·基尔基在传统医学中的抗疟用途。
