Antispasmodic activity of fractions and cynaropicrin from Cynara scolymus on guinea-pig ileum.
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.
Emendörfer
Fernanda
F
Programa de Mestrado em Ciências Farmacêuticas e Núcleo de Investigações Químico-Farmacêuticas, University of Vale do Itajaí, Itajaí 88302-202, Santa Catarina, Brazil.
Emendörfer
Fabiane
F
Bellato
Fernanda
F
Noldin
Vânia Floriani
VF
Cechinel-Filho
Valdir
V
Yunes
Rosendo Augusto
RA
Delle Monache
Franco
F
Cardozo
Alcíbia Maia
AM
D000818:Animals; D031943:Cynara scolymus; D004305:Dose-Response Relationship, Drug; D005260:Female; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects* / Q000502:physiology; D066298:In Vitro Techniques; D007783:Lactones / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D008297:Male; D010276:Parasympatholytics / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D018515:Plant Leaves; D012717:Sesquiterpenes / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*
D007783:Lactones; D010276:Parasympatholytics; D010936:Plant Extracts; D012717:Sesquiterpenes; C075687:cynaropicrin