Laboratory of Phytochemistry, Center of Medical and Pharmaceutical Sciences, Western Parana State University, Cascavel, PR, Brazil.
Laboratory of Applied Immunology, Center of Medical and Pharmaceutical Sciences, Western Parana State University, Cascavel, PR, Brazil.
J Infect Dev Ctries. 2021 Mar 7;15(2):270-279. doi: 10.3855/jidc.12669.
Trypanosoma cruzi is the agent of Chagas' disease and affects approximately 6-8 million people worldwide. The search for new anti-T. cruzi drugs are relevant because only two drugs exist actually. The objective of this study was to investigate the effect of the extracts from the seeds of Lonchocarpus cultratus on T. cruzi, its cytotoxicity as well as to elucidate its chemical profile.
The characterization of the extracts was done using 1H-RMN. T. cruzi forms were treated with increasing concentrations of the extracts and after, the percentage of inhibition and IC50 or LC50 were calculated. Murine peritoneal macrophages were treated with different concentrations of the extracts to evaluate the cellular viability. The hemotoxicity was accessed by verifying the levels of hemolysis caused by the extracts on human red blood cells.
Chalcones isocordoin and lonchocarpin were detected in the dichloromethane extract, and chalcone lonchocarpin was detected in the hexane extract. The dichloromethane extract showed higher activity against all the forms of T. cruzi compared to the other two extracts, but the hexane showed the best selectivity index. The cytotoxicity observed in murine macrophages was confirmed in human erythrocytes, with dichloromethane extract having the highest toxicity. The methanolic extract showed the lowest anti-T. cruzi activity but was nontoxic to peritoneal murine macrophages and red blood cells.
L. cultratus extracts have the potential to be explored for the development of new anti-trypanosomal drugs. This study was the first to demonstrate the action of extracts from the genus Lonchocarpus on infecting forms of T. cruzi.
克氏锥虫是恰加斯病的病原体，影响全球约 600 万至 800 万人。寻找新的抗克氏锥虫药物是相关的，因为实际上只有两种药物存在。本研究的目的是研究 Lonchocarpus cultratus 种子提取物对克氏锥虫的作用、细胞毒性，并阐明其化学特征。
使用 1H-RMN 对提取物进行表征。用递增浓度的提取物处理克氏锥虫各期虫体，然后计算抑制率和 IC50 或 LC50。用不同浓度的提取物处理鼠腹腔巨噬细胞，以评估细胞活力。通过检测提取物对人红细胞引起的溶血程度来评估血液毒性。
在二氯甲烷提取物中检测到查耳酮异甘草素和 lonchocarpin，在正己烷提取物中检测到查尔酮 lonchocarpin。与其他两种提取物相比，二氯甲烷提取物对所有克氏锥虫各期虫体均表现出更高的活性，但正己烷提取物的选择性指数最佳。在鼠巨噬细胞中观察到的细胞毒性在人红细胞中得到证实，二氯甲烷提取物毒性最高。甲醇提取物对克氏锥虫的活性最低，但对腹腔鼠巨噬细胞和红细胞均无毒性。
L. cultratus 提取物具有开发新型抗锥虫药物的潜力。本研究首次证明了 Lonchocarpus 属提取物对感染型克氏锥虫的作用。
