Kusch Peter, Deininger Susanne, Specht Sabine, Maniako Rudeka, Haubrich Stefanie, Pommerening Tanja, Lin Paul Kong Thoo, Hoerauf Achim, Kaiser Annette
Department of Applied Natural Sciences, Bonn-Rhein-Sieg University of Applied Sciences, Justus Von Liebig Street 20, 53359 Rheinbach, Germany.
J Parasitol Res. 2011;2011:368692. doi: 10.1155/2011/368692. Epub 2011 May 25.
Balanites aegyptiaca (Balanitaceae) is a widely grown desert plant with multiuse potential. In the present paper, a crude extract from B. aegyptiaca seeds equivalent to a ratio of 1 : 2000 seeds to the extract was screened for antiplasmodial activity. The determined IC(50) value for the chloroquine-susceptible Plasmodium falciparum NF54 strain was 68.26 μg/μL ± 3.5. Analysis of the extract by gas chromatography-mass spectrometry detected 6-phenyl-2(H)-1,2,4-triazin-5-one oxime, an inhibitor of the parasitic M18 Aspartyl Aminopeptidase as one of the compounds which is responsible for the in vitro antiplasmodial activity. The crude plant extract had a K(i) of 2.35 μg/μL and showed a dose-dependent response. After depletion of the compound, a significantly lower inhibition was determined with a K(i) of 4.8 μg/μL. Moreover, two phenolic compounds, that is, 2,6-di-tert-butyl-phenol and 2,4-di-tert-butyl-phenol, with determined IC(50) values of 50.29 μM ± 3 and 47.82 μM ± 2.5, respectively, were detected. These compounds may contribute to the in vitro antimalarial activity due to their antioxidative properties. In an in vivo experiment, treatment of BALB/c mice with the aqueous Balanite extract did not lead to eradication of the parasites, although a reduced parasitemia at day 12 p.i. was observed.
埃及蒺藜(蒺藜科)是一种广泛种植的具有多种用途潜力的沙漠植物。在本文中,对埃及蒺藜种子的粗提物进行了抗疟活性筛选,该粗提物与种子的比例为1∶2000。测定了氯喹敏感的恶性疟原虫NF54株的半数抑制浓度(IC50)值为68.26μg/μL±3.5。通过气相色谱 - 质谱联用仪对提取物进行分析,检测到6 - 苯基 - 2(H)-1,2,4 - 三嗪 - 5 - 酮肟,一种寄生性M18天冬氨酰氨肽酶抑制剂,是负责体外抗疟活性的化合物之一。该植物粗提物的抑制常数(Ki)为2.35μg/μL,并呈现剂量依赖性反应。该化合物耗尽后,测定的抑制作用显著降低,Ki为4.8μg/μL。此外,还检测到两种酚类化合物,即2,6 - 二叔丁基苯酚和2,4 - 二叔丁基苯酚,其IC50值分别为50.29μM±3和47.82μM±2.5。由于其抗氧化特性,这些化合物可能有助于体外抗疟活性。在体内实验中,用埃及蒺藜水提取物处理BALB/c小鼠,虽然在感染后第12天观察到寄生虫血症有所降低,但并未导致寄生虫被根除。