Natural Product Chemistry, Biosciences, Council for Scientific and Industrial Research (CSIR), Pretoria, South Africa.
Planta Med. 2013 Sep;79(14):1380-4. doi: 10.1055/s-0033-1350691. Epub 2013 Aug 8.
Two hundred and seven extracts were prepared from sixty plants from South Africa and screened for in vitro activity against Trypanosoma brucei rhodesiense, Trypanosoma cruzi, Leishmania donovani, and Plasmodium falciparum. For the 21 extracts which inhibited the growth of one or more parasites with more than 95 % at 10 µg/mL, the IC50 values against all four protozoal parasites and cytotoxic IC50 values against L6 myoblasts were determined. Amongst the most notable results are the activities of Psoralea pinnata (IC50 of 0.15 µg/mL), Schkuhria pinnata (2.04 µg/mL), and Vernonia mespilifolia (1.01 µg/mL) against Trypansoma brucei rhodesiense. HPLC-based activity profiling was used to identify the active constituents in the extracts, and the germacranolide sesquiterpene lactones schkuhrin I and II from S. pinnata, and cynaropicrin from V. mespilifolia were identified, with IC50 values of 0.9, 1.5, and 0.23 µM, respectively.
从南非的 60 种植物中提取了 207 种提取物，并对其进行了体外抗非洲锥虫（Trypanosoma brucei rhodesiense）、克氏锥虫（Trypanosoma cruzi）、杜氏利什曼原虫（Leishmania donovani）和疟原虫（Plasmodium falciparum）的活性筛选。对于 21 种提取物，其在 10 µg/mL 时对一种或多种寄生虫的生长抑制率超过 95 %，测定了其对所有四种原生动物寄生虫的 IC50 值和对 L6 成肌细胞的细胞毒性 IC50 值。最显著的结果之一是 Psoralea pinnata（IC50 为 0.15 µg/mL）、Schkuhria pinnata（2.04 µg/mL）和 Vernonia mespilifolia（1.01 µg/mL）对非洲锥虫的活性。采用基于 HPLC 的活性分析来鉴定提取物中的活性成分，从 S. pinnata 中鉴定出了倍半萜内酯 Schkuhrin I 和 II，从 V. mespilifolia 中鉴定出了 Cynaropicrin，其 IC50 值分别为 0.9、1.5 和 0.23 µM。
