CONICET-Universidad de Buenos Aires, Instituto de Química y Metabolismo del Fármaco (IQUIMEFA), Junín 956 2° floor, Buenos Aires 1113, Argentina.
Cátedra de Farmacognosia, Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires, Junín 956 2° floor, Buenos Aires 1113, Argentina.
Molecules. 2019 Mar 28;24(7):1209. doi: 10.3390/molecules24071209.
Sesquiterpene lactones are naturally occurring compounds mainly found in the Asteraceae family. These types of plant metabolites display a wide range of biological activities, including antiprotozoal activity and are considered interesting structures for drug discovery. Four derivatives were synthesized from estafietin (), isolated from (Asteraceae): 11βH,13-dihydroestafietin (), epoxyestafietin ( and ), 11βH,13-methoxyestafietin, () and 11βH,13-cianoestafietin. The antiprotozoal activity against and of these compounds was evaluated. Epoxyestafietin was the most active compound against trypomastigotes and amastigotes (IC values of 18.7 and 2.0 µg/mL, respectively). Estafietin () and 11βH,13-dihydroestafietin () were the most active and selective compounds on promastigotes (IC values of 1.0 and 1.3 μg/mL, respectively). The antiparasitic activity demonstrated by estafietin and some of its derivatives make them promising candidates for the development of effective compounds for the treatment of Chagas disease and leihsmaniasis.
倍半萜内酯是一类天然化合物，主要存在于菊科植物中。这些植物代谢产物具有广泛的生物活性，包括抗寄生虫活性，被认为是药物发现的有趣结构。从 Asteraceae 中分离得到的 estafietin () 合成了 4 种衍生物：11βH,13-dihydroestafietin ()、epoxyestafietin () 和 11βH,13-methoxyestafietin ()、11βH,13-cianoestafietin ()。评估了这些化合物对 和 的抗寄生虫活性。环氧 estafietin 对 运动型和无鞭毛体的活性最强（IC 值分别为 18.7 和 2.0 µg/mL）。estafietin () 和 11βH,13-dihydroestafietin () 对 前鞭毛体的活性最强且选择性最高（IC 值分别为 1.0 和 1.3 μg/mL）。estafietin 及其一些衍生物具有抗寄生虫活性，这使其成为开发有效治疗恰加斯病和利什曼病药物的有前途的候选物。
