Zheoat Ahmed M, Alenezi Samya, Elmahallawy Ehab Kotb, Ungogo Marzuq A, Alghamdi Ali H, Watson David G, Igoli John O, Gray Alexander I, de Koning Harry P, Ferro Valerie A
Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, Glasgow G4 0RE, UK.
Al-Manara College for Medical Sciences, Misan 10028, Iraq.
Pathogens. 2021 Feb 5;10(2):175. doi: 10.3390/pathogens10020175.
Trypanosomiasis and leishmaniasis are a group of neglected parasitic diseases caused by several species of parasites belonging to the family Trypansomatida. The present study investigated the antitrypanosomal and antileishmanial activity of chalcones and flavanones from , which grows in the wetlands of Iraq. The phytochemical evaluation of the plant yielded two chalcones, 2',4'-dimethoxy-6'-hydroxychalcone and 2',5'-dimethoxy-4',6'-dihydroxychalcone, and two flavanones, 5,7-dimethoxyflavanone and 5,8-dimethoxy-7-hydroxyflavanone. The chalcones showed a good antitrypanosomal and antileishmanial activity while the flavanones were inactive. The EC values for 2',4'-dimethoxy-6'-hydroxychalcone against (0.5 μg/mL), (2.5 μg/mL), and (5.2 μg/mL) indicated it was the most active of the compounds. None of the compounds displayed any toxicity against a human cell line, even at 100 µg/mL, or cross-resistance with first line clinical trypanocides, such as diamidines and melaminophenyl arsenicals. Taken together, our study provides significant data in relation to the activity of chalcones and flavanones from against both parasites in vitro. Further future research is suggested in order to investigate the mode of action of the extracted chalcones against the parasites.
锥虫病和利什曼病是一组被忽视的寄生虫病,由属于锥虫科的几种寄生虫引起。本研究调查了从生长在伊拉克湿地的植物中提取的查耳酮和黄烷酮的抗锥虫和抗利什曼原虫活性。对该植物的植物化学评估产生了两种查耳酮,即2',4'-二甲氧基-6'-羟基查耳酮和2',5'-二甲氧基-4',6'-二羟基查耳酮,以及两种黄烷酮,即5,7-二甲氧基黄烷酮和5,8-二甲氧基-7-羟基黄烷酮。查耳酮显示出良好的抗锥虫和抗利什曼原虫活性,而黄烷酮则无活性。2',4'-二甲氧基-6'-羟基查耳酮对布氏锥虫(0.5 μg/mL)、杜氏利什曼原虫(2.5 μg/mL)和热带利什曼原虫(5.2 μg/mL)的半数有效浓度表明它是这些化合物中活性最强的。即使在100 µg/mL的浓度下,这些化合物对人类细胞系均未显示出任何毒性,也未显示出与一线临床锥虫杀灭剂(如双脒和氨基苯胂)的交叉耐药性。综上所述,我们的研究提供了有关从该植物中提取的查耳酮和黄烷酮对两种寄生虫的体外活性的重要数据。建议进一步开展研究以探究提取的查耳酮对寄生虫的作用方式。