Spasmolytic and antidiarrhoeal properties of the Yucatec Mayan medicinal plant Casimiroa tetrameria

• Published in: Journal of pharmacy and pharmacology 2005-09, Vol.57 (9), p.1081-1085
• Main Authors: Heinrich, Michael, Heneka, Bilkis, Rimpler, Horst, Ankli, Anita, Sticher, Otto, Kostiza, Thomas
• Format: Article
• Language: English
• Subjects: Animals; Antidiarrheals - chemistry; Antidiarrheals - isolation & purification; Antidiarrheals - pharmacology; Casimiroa; Digestive System Diseases - drug therapy; Disease Models, Animal; Drug Evaluation, Preclinical - methods; Ethanol - chemistry; Ethanol - pharmacology; Gastric Acid - secretion; Guinea Pigs; Helicobacter pylori - drug effects; Helicobacter pylori - growth & development; Ileum - drug effects; Ileum - pathology; Medicine, Traditional; Mexico - ethnology; Muscle Relaxation - drug effects; Muscle Relaxation - physiology; Muscle, Smooth - drug effects; Parasympatholytics - chemistry; Parasympatholytics - isolation & purification; Parasympatholytics - pharmacology; Phytotherapy; Plant Extracts - chemistry; Plant Extracts - isolation & purification; Plant Extracts - therapeutic use; Plant Leaves - chemistry; Plants, Medicinal - chemistry
• ISSN: 0022-3573; 2042-7158
• DOI: 10.1211/jpp.57.9.0002

The Maya of the Yucatán peninsula commonly use the leaves of Casimiroa tetrameria for treating gastrointestinal disorders, notably diarrhoea and dysentery, as well as gastrointestinal cramps. The phytochemical investigation resulted in the isolation of 13 compounds: eight polymethoxylated flavonoids (two as minor components with a main constituent), four flavonoid glycosides and one furanocoumarin. In this study we used two well‐established models in order to assess the gastrointestinal effects of C. tetrameria extracts and isolated compounds: the USSING‐chamber, a pharmacological model for diarrhoea, and the isolated guinea pig ileum, a model for modulatory effects on ileum contraction. Extracts and the class of polymethoxylated flavonoids showed strong inhibitory effects in both models, which provides ex‐vivo evidence for the use of this botanical drug in the treatment of several gastrointestinal problems, most notably diarrhoea. The crude extract, polymethoxylated flavonoid‐rich fractions and the polymethoxylated flavonoids tested showed prominent antisecretory activity. Polymethoxylated flavonoid‐rich fractions also inhibited the histamine‐induced contractions in the guinea pig model. The effects are not due to a single compound, but to a large number of structurally related compounds that all contribute to the effect.