Tasdemir D, Brun R, Perozzo R, Dönmez A A
Institute of Organic Chemistry, University of Zurich, Switzerland.
Phytother Res. 2005 Feb;19(2):162-6. doi: 10.1002/ptr.1648.
A total of 58 extracts of different polarity were prepared from various organs of 16 species of Turkish plants and screened for their antitrypanosomal, antileishmanial and antiplasmodial activities. No significant activity was observed against Trypanosoma cruzi, whereas many extracts showed appreciable trypanocidal potential against T. brucei rhodesiense, with the CHCl(3)-soluble portion of Phlomis kurdica being the most active (IC(50) 2.7 microg[sol ]mL). Almost all extracts, particularly the CHCl(3) phases, exhibited growth inhibition activity against Leishmania donovani amastigotes. The CHCl(3)-solubles of Putoria calabrica roots (IC(50) 1.9 microg[sol ]mL), Wendlandia ligustroides leaves (IC(50) 2.1 microg[sol ]mL) and Rhododendron luteum leaves (IC(50) 2.3 microg[sol ]mL) displayed the highest leishmanicidal potential. The majority of the extracts also possessed antiplasmodial activity against the multi-drug resistant K1 Plasmodium falciparum strain. The most potent antiplasmodial activity was observed with the CHCl(3) extracts of Phlomis kurdica (IC(50) 1.5 microg[sol ]mL), P. leucophracta (IC(50) 1.6 microg[sol ]mL), Scrophularia cryptophila (IC(50) 1.8 microg[sol ]mL), Morina persica (IC(50) 1.9 microg[sol ]mL) and the aqueous root extract of Asperula nitida subsp. subcapitellata (IC(50) 1.6 microg[sol ]mL). Twenty-one extracts with significant antimalarial activity (IC(50) < 5 microg[sol ]mL) were also tested for their ability to inhibit the purified enoyl-ACP reductase (FabI), a crucial enzyme in the fatty acid biosynthesis of P. falciparum. The CHCl(3) extract of Rhododendron ungernii leaves (IC(50) 10 microg[sol ]mL) and the H(2)O-soluble portion of Rhododendron smirnovii leaves (IC(50) 0.4 microg[sol ]mL) strongly inhibited the FabI enzyme. The preliminary data indicate that some (poly)phenolic compounds are responsible for the FabI inhibition potential of these extracts. The presented work reports for the first time the antiprotozoal activity of nine different genera as well as a target specific antimalarial screening for the identification of P. falciparum FabI inhibitors from medicinal plant extracts.
从16种土耳其植物的各个器官中制备了总共58种不同极性的提取物,并对其抗锥虫、抗利什曼原虫和抗疟活性进行了筛选。未观察到对克氏锥虫有显著活性,而许多提取物对罗德西亚布氏锥虫显示出可观的杀锥虫潜力,其中库尔德糙苏的氯仿可溶部分活性最强(IC50为2.7微克/毫升)。几乎所有提取物,特别是氯仿相,对杜氏利什曼原虫无鞭毛体均表现出生长抑制活性。卡拉布里卡普托里亚根的氯仿可溶物(IC50为1.9微克/毫升)、女贞叶水锦树叶片(IC50为2.1微克/毫升)和黄杜鹃叶片(IC50为2.3微克/毫升)显示出最高的杀利什曼原虫潜力。大多数提取物对多药耐药的恶性疟原虫K1株也具有抗疟活性。在库尔德糙苏、白苞糙苏、隐花玄参、波斯刺参的氯仿提取物以及亚头状天蓝绣球水根部提取物中观察到最强的抗疟活性(IC50分别为1.5微克/毫升、1.6微克/毫升、1.8微克/毫升、1.9微克/毫升和1.6微克/毫升)。还对21种具有显著抗疟活性(IC50<5微克/毫升)的提取物抑制纯化的烯酰-ACP还原酶(FabI)的能力进行了测试,FabI是恶性疟原虫脂肪酸生物合成中的一种关键酶。温氏杜鹃叶片的氯仿提取物(IC50为10微克/毫升)和斯氏杜鹃叶片的水可溶部分(IC50为0.4微克/毫升)强烈抑制FabI酶。初步数据表明,一些(多)酚类化合物是这些提取物抑制FabI潜力的原因。本研究首次报道了9个不同属的抗原生动物活性以及针对从药用植物提取物中鉴定恶性疟原虫FabI抑制剂的靶向特异性抗疟筛选。