Valencia Lorena, Muñoz Diana Lorena, Robledo Sara María, Echeverri Fernando, Arango Gabriel Jaime, Vélez Iván Darío, Triana Omar
Biología y Control de Enfermedades Infecciosas, Instituto de Biología, Universidad de Antioquia, Medellín, Colombia.
Biomedica. 2011 Oct-Dec;31(4):552-9. doi: 10.1590/S0120-41572011000400010.
The treatment of Chagas disease is based on only two drugs with limited efficacy and significant side effects. The rich biodiversity of the Colombian flora makes bio-prospecting a potential alternative in the search for new antiparasitic drugs.
Potential trypanocidal activity and cytotoxicity was assessed in extracts from 23 Colombian plants.
Extracts of leaves, stems, or of the whole plants were obtained in solvents of a range of polarities. The activity against Trypanosoma cruzi epimastigotes and the cytotoxicity were evaluated by the MTT enzymatic micro-method. Extracts active against epimastigotes and with low cytotoxicity were also tested on trypomastigotes and intracellular amastigotes.
Among the extracts, biological activity was confirmed in 4 species. The extracts were active on epimastigotes and trypomastigotes; one was active also against amastigotes. The latter extract was isolated from the plant Hieronyma antioquensis and presented IC(50) of 3.1 mg/ml for epimastigotes, 11.5 mg/ml for trypomastigotes and 2.9 mg/ml for amastigotes. The selectivity indexes were 25, 7, and 27 respectively.
The extract from H. antioquensis proved a promising candidate for Chagas disease treatment. Futhermore, the MTT enzymatic micromethod was a useful tool for screening biological activity on epimastigotes and other stages of the parasite for further extract trials.
恰加斯病的治疗仅基于两种疗效有限且副作用显著的药物。哥伦比亚丰富的植物生物多样性使得生物勘探成为寻找新型抗寄生虫药物的潜在替代方法。
评估23种哥伦比亚植物提取物的潜在杀锥虫活性和细胞毒性。
采用一系列不同极性的溶剂提取叶片、茎或整株植物。通过MTT酶促微量法评估对克氏锥虫前鞭毛体的活性和细胞毒性。对前鞭毛体有活性且细胞毒性低的提取物也在锥鞭毛体和细胞内无鞭毛体上进行了测试。
在提取物中,4种植物的生物活性得到确认。这些提取物对前鞭毛体和锥鞭毛体有活性;有一种对无鞭毛体也有活性。后一种提取物从安蒂奥基亚希罗尼玛属植物中分离得到,对前鞭毛体的半数抑制浓度(IC50)为3.1毫克/毫升,对锥鞭毛体为11.5毫克/毫升,对无鞭毛体为2.9毫克/毫升。选择性指数分别为25、7和27。
安蒂奥基亚希罗尼玛属植物的提取物被证明是治疗恰加斯病的一个有前景的候选药物。此外,MTT酶促微量法是筛选对前鞭毛体和寄生虫其他阶段生物活性以进行进一步提取物试验的有用工具。