Cynara scolymus (Compositae), popularly known as "alcachofra" or "artichoke", is widely cultivated In Mediterranean and American countries, and its sprout is commonly eaten as a vegetable. Its leaves are frequently used in folk medicine in many countries, to treat several ailments, including hepatitis, hyperlipidemia, and obesity, dyspeptic disorder, among others. Clinical and pre-clinical trials have confirmed the therapeutic potential of this plant, particularly in the treatment of hepato-biliary dysfunction and digestive complaints, and also its effectiveness in patients with irritable bowel syndrome and hyperlipoproteinemia, as well as its choleretic and antioxidant effects. 1-5)The literature reports several phenolic compounds as the main chemical constituents of artichoke leaves, such as cynarin, caffeic and chlorogenic acids, luteolin, cynaroside and scolymoside, and sesquiterpenes, such as cynaropicrin, which are indicated as the active principles of this plant. [6][7][8][9] In previous studies conducted in our laboratories, we have described the chemical and biological activities (cytotoxic and diuretic) of artichoke cultivated in Brazil. Our results showed that the main constituents are glycosyl flavonoids (cynaroside and scolymoside), along with cynaropicrin and lupeol.10) More recently, we have also demonstrated that methanolic extract of C. scolymus exhibits an antispasmodic profile against the action of acetylcholine on preparations with isolated guinea-pig ileum and rat duoden, by using experimental models in vitro. 11)In order to elucidate the antispasmodic component(s) of this plant, we carried out a bio-guided assay against acetylcholine in guinea pig-ileum. MATERIAL AND METHODS Plant Material, Preparation of Fractions and Isolation of CynaropicrinLeaves of Cynara scolymus were picked, in February 2000, from the "Central de Plantas" at Curitiba, in the State of Parana, southern Brazil. Air-dried leaves (1900 g) were macerated with methanol at room temperature for approximately 7 d, followed by the removal of solvent under reduced pressure to obtain the crude methanolic extract (CME). Afterwards, the CME was suspended in water and successively partitioned with solvents of increasing polarity (hexane, dichloromethane, ethyl acetate and butanol), yielding the respective fractions, according to the method previously described.12) The most active fraction, dichloromethane, was studied in more detail, and the most potent subfraction furnished the compound cynaropicrin, which was directly compared with an authentic sample previously isolated by us.10) All the fractions and compounds were dissolved in ethanol solution (10%) at the desired concentration, immediately prior to biological use.Animals Guinea-pigs (300-400 g) of both sexes were kept in automatically controlled temperature conditions (23Ϯ2°C), in 12 h light-dark cycles and with food and water "ad libitum". The animals were kept in the laboratory for 48 h prior to the experiments and their food was restrained 24 h before the experiments.Evalua...
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