Emendörfer Fernanda, Emendörfer Fabiane, Bellato Fernanda, Noldin Vânia Floriani, Cechinel-Filho Valdir, Yunes Rosendo Augusto, Delle Monache Franco, Cardozo Alcíbia Maia
Programa de Mestrado em Ciências Farmacêuticas e Núcleo de Investigações Químico-Farmacêuticas, University of Vale do Itajaí, Itajaí 88302-202, Santa Catarina, Brazil.
Biol Pharm Bull. 2005 May;28(5):902-4. doi: 10.1248/bpb.28.902.
This study describes the antispasmodic activity of some fractions and cynaropicrin, a sesquiterpene lactone from Cynara scolymus, cultivated in Brazil, against guinea-pig ileum contracted by acetylcholine. The dichloromethane fraction showed the most promising biological effects, with an IC(50) of 0.93 (0.49-1.77) mg/ml. Its main active component, the sesquiterpene lactone cynaropicrin, exhibited potent activity, with IC(50) of 0.065 (0.049-0.086) mg/ml, being about 14-fold more active than dichloromethane fraction and having similar potency to that of papaverine, a well-known antispasmodic agent. The results confirm the popular use of artichoke for the treatment of gastrointestinal disturbances, and encourage new studies on this compound, in order to obtain new antispasmodic agents.
本研究描述了巴西种植的洋蓟中一些馏分及洋蓟苦素(一种倍半萜内酯)对乙酰胆碱所致豚鼠回肠收缩的解痉活性。二氯甲烷馏分显示出最有前景的生物学效应,其半数抑制浓度(IC50)为0.93(0.49 - 1.77)mg/ml。其主要活性成分倍半萜内酯洋蓟苦素表现出强效活性,IC50为0.065(0.049 - 0.086)mg/ml,活性约为二氯甲烷馏分的14倍,且与知名解痉剂罂粟碱的效力相似。结果证实了洋蓟在治疗胃肠道紊乱方面的广泛应用,并鼓励对该化合物开展新的研究,以获得新的解痉剂。