Facultad de Bioquímica, Química y Farmacia, Universidad Nacional de Tucumán, Tucumán, Argentina.
CCT - CONICET - TUCUMAN, Tucumán, Argentina.
Nat Prod Res. 2021 Dec;35(23):5224-5228. doi: 10.1080/14786419.2020.1739682. Epub 2020 Mar 17.
Chagas disease is caused by and affects the poorest population in the Americas. Fourteen plant extracts and seventeen sesquiterpene lactones from the tribe Vernonieae (Asteraceae), were evaluated for the first time against . Cytotoxicity employing HeLa cells was also assessed. The best results were obtained with leaves and flowers rinse extracts from (E-1 and E-3) and (E-11 and E-13), with IC values <2 µg/mL, being E-1 the most active (IC = 0.8 µg/mL). Additionally, these extracts displayed a good selectivity (SI > 10). The most active sesquiterpene lactones, isolated from the extracts, were 2 (2methoxy-2,5-epoxy-8-methacryloxygermacra-3Z,11(13)-dien-6,12-olide) and 6 (2ethoxy-2,5-epoxy-8-angeloxygermacra-3Z,11(13)-dien-6,12-olide) from and 12 (8α-methacryloxyhirsutinolide 13-O-acetate) from , with IC of 1.5, 2.1 and 2.0 µM, respectively. These compounds showed SI values >14, better than those of the reference drug nifurtimox. Plants living in South American ecosystems could become a potential source of trypanocidal agents.
恰加斯病由 引起，影响美洲最贫困人群。首次对 Vernonieae 族（菊科）的 14 种植物提取物和 17 种倍半萜内酯进行了评估，以对抗 。还评估了用 HeLa 细胞进行细胞毒性。叶和花冲洗提取物来自 （E-1 和 E-3）和 （E-11 和 E-13）的效果最好，IC 值<2μg/mL，E-1 最活跃（IC = 0.8μg/mL）。此外，这些提取物表现出良好的选择性（SI > 10）。从提取物中分离出的最活跃的倍半萜内酯是 2（2-甲氧基-2,5-环氧-8-丙烯酰氧基- germacra-3Z,11(13)-二烯-6,12-内酯）和 6（2-乙氧基-2,5-环氧-8-当归酰氧基 germacra-3Z,11(13)-二烯-6,12-内酯）来自 ，以及 12（8α-丙烯酰氧基 hirsutinolide 13-O-醋酸酯）来自 ，IC 分别为 1.5、2.1 和 2.0μM。这些化合物的 SI 值>14，优于参考药物硝呋替莫。生活在南美生态系统中的植物可能成为杀锥虫剂的潜在来源。
