Bortoluzzi Aline Antunes Maciel, Staffen Izabela Virginia, Banhuk Fernanda Weyand, Griebler Aline, Matos Patricia Karoline, Ayala Thaís Soprani, da Silva Edson Antonio Alves, Sarragiotto Maria Helena, Schuquel Ivânia Teresinha Albrecht, Jorge Tereza Cristina Marinho, Menolli Rafael Andrade
Center of Medical and Pharmaceutical Sciences, Western Parana State University (UNIOESTE), 2069 Universitaria St., Cascavel, PR, Brazil.
Center of Exact Sciences and Technology, Western Parana State University (UNIOESTE), 2069 Universitaria St., Cascavel, PR, Brazil.
Saudi J Biol Sci. 2021 Jan;28(1):99-108. doi: 10.1016/j.sjbs.2020.08.036. Epub 2020 Sep 1.
is the agent of Chagas disease, an infection that affects around 8 million people worldwide. The search for new anti- drugs are relevant, mainly because the treatment of this disease is limited to two drugs. The objective of this study was to investigate the trypanocidal and cytotoxic activity and elucidate the chemical profile of extracts from the roots of the . Roots from were submitted to successive extractions with hexane, dichloromethane, and methanol, resulting in LCH, LCD, and LCM extracts, respectively. Characterization of extracts was done using H-RMN, C-RMN, CC and TLC. Treatment of forms (epimastigotes, trypomastigotes, and amastigotes) with crescent concentrations of LCH, LCD, and LCM was done for 72, 48, and 48 h, respectively. After this, the percentage of inhibition and IC/LC were calculated. Benznidazole was used as a positive control. Murine macrophages were treated with different concentrations of both extracts for 48 h, and after, the cellular viability was determined by the MTT method and CC was calculated. The chalcones derricin and lonchocarpine were identified in the hexane extract, and for the first time in the genus , the presence of a dihydrolonchocarpine derivative was observed. Other chalcones such as isocordoin and erioschalcone B were detected in the dichloromethane extract. The dichloromethane extract showed higher activity against all tested forms of than the other two extracts, with IC values of 10.98, 2.42, and 0.83 µg/mL, respectively; these values are very close to those of benznidazole. Although the dichloromethane extract presented a cytotoxic effect against mammalian cells, it showed selectivity against amastigotes. The methanolic extract showed the lowest anti- activity but was non-toxic to peritoneal murine macrophages. Thus, the genus had demonstrated in the past action against epimastigotes forms of but is the first time that the activity against infective forms is showed, which leading to further studies with tests.
是恰加斯病的病原体,这种感染影响着全球约800万人。寻找新的抗寄生虫药物很有意义,主要是因为这种疾病的治疗仅限于两种药物。本研究的目的是研究锥虫杀灭活性和细胞毒性,并阐明[植物名称]根提取物的化学特征。[植物名称]的根依次用己烷、二氯甲烷和甲醇进行提取,分别得到LCH、LCD和LCM提取物。提取物的表征采用高分辨核磁共振氢谱(H-RMN)、碳谱(C-RMN)、柱色谱(CC)和薄层色谱(TLC)。分别用浓度递增的LCH、LCD和LCM处理[寄生虫名称]的三种形态(前鞭毛体、锥鞭毛体和无鞭毛体)72小时、48小时和48小时。之后,计算抑制率和半数抑制浓度/最低杀菌浓度(IC/LC)。苯硝唑用作阳性对照。用不同浓度的两种提取物处理小鼠巨噬细胞48小时,然后用MTT法测定细胞活力并计算细胞毒性浓度(CC)。在己烷提取物中鉴定出查耳酮德里辛和羽扇豆碱,并且在[植物属名]中首次观察到二氢羽扇豆碱衍生物的存在。在二氯甲烷提取物中检测到其他查耳酮,如异柯多因和毛鱼藤酮B。二氯甲烷提取物对所有测试的[寄生虫名称]形态均显示出比其他两种提取物更高的活性,其半数抑制浓度分别为10.98、2.42和0.83μg/mL;这些值与苯硝唑的值非常接近。虽然二氯甲烷提取物对哺乳动物细胞有细胞毒性作用,但对无鞭毛体显示出选择性。甲醇提取物显示出最低的抗寄生虫活性,但对小鼠腹膜巨噬细胞无毒。因此,[植物属名]过去已证明对[寄生虫名称]的前鞭毛体形态有作用,但首次显示出对感染性形态的活性,这导致需要通过[具体测试名称]测试进行进一步研究。