Antiprotozoal, Antibacterial and Antidiarrheal Properties from the Flowers of Chiranthodendron pentadactylon and Isolated Flavonoids

BACKGROUND: Chiranthodendron pentadactylon Larreat. (Sterculiaceae) is a Mexican plant used in traditional medicine for the treatment of heart disease symptoms and infectious diarrhea. OBJECTIVE: To evaluate in vitro antiprotozoal and antibacterial activities and in vivo antidiarrheal activity from the flowers of C. pentadactylon using the extract, fractions, and major isolated flavonoids. MATERIALS AND METHODS: Bioassay-guided fractionation of the methanol extract of C. pentadactylon (MECP) led to the isolation of five flavonoids, tiliroside, astragalin, isoquercitrin, (+)-catechin, and (-)-epicatechin. Antimicrobial activities were tested on two protozoa (Entamoeba histolytica and Giardia lamblia) and nine bacterial enteropathogens (two Escherichia coli strains, two Shigella sonnei strains, two Shigella flexneri strains, two Salmonella sp. strains, and Vibrio cholerae) isolated from feces of children with acute diarrhea or dysentery and resistant to chloramphenicol. Also, antidiarrheal activity was tested on cholera toxin-induced diarrhea in male Balb-c mice. RESULTS: Epicatechin was the most potent antiamoebic and antigiardial compound with IC(50) values of 1.9 μg/mL for E. histolytica and 1.6 μg/mL for G. lamblia; tiliroside showed moderate antiprotozoal activity against both protozoan. In contrast, in the antibacterial activity, tiliroside was the most potent compound on all microorganisms with minimum inhibitory concentration values less than 0.7 mg/mL. In the case of cholera toxin-induced diarrhea, epicatechin was the most potent flavonoid with IC(50) of 14.7 mg/kg. CONCLUSION: Epicatechin and tiliroside were the flavonoids responsible for antimicrobial andantidiarrheal activities of C. pentadactylon. Its antiprotozoal, antibacterial, and antidiarrheal properties are in good agreement with the traditional medicinal use of C. pentadactylon for the treatment of infectious diarrhea. SUMMARY: Epicatechin was the most potent antiamoebic and antigiardial compound with IC(50) values of 1.9 μg/mL for E. histolytica and 1.6 μg/mL for G. lamblia. Tiliroside showed antibacterial activity against all microorganisms tested with MIC values less than 0.7 mg/mL. Epicatechin was the most potent flavonoid on cholera toxin-induced diarrhea with IC(50) of 14.7 mg/kg. Abbreviations used: MECP: Methanol extract of C. pentadactylon