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Structure-activity relationships of anthraquinones in the decrease of intestinal motility.

D H Kuo·S C Kuo·J T Cheng
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Abstract

The effects of substituted anthraquinones on intestinal motility were evaluated in-vitro using rabbit small intestinal strips. This structure-activity relationship study revealed the critical requirement of a hydroxy group at R2 position. The intestinal motility was inhibited 50% (IC50) by emodine (8 microM), 2-hydroxy anthraquinone (20 microM), 2,6-dihydroxy anthraquinone (25 microM), 2,7-dihydroxy anthraquinone (10 microM), 1,2,4-trihydroxy anthraquinone (80 microM) and 1,2,5,8-tetra-hydroxyanthraquinone (9 microM). The presence of other polar groups at R2 position such as an amino, aldehyde and carboxylic acid group significantly reduced the activity (IC50 360-400 microM). The presence of a methyl group and esterification of the carboxylic acid at R2 position was found to abolish the activity. These data are useful for the future development of anthraquinones as laxative agents.

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AnimalsAnthraquinonesCatharticsGastrointestinal MotilityIn Vitro TechniquesMaleRabbitsStructure-Activity RelationshipJournal Article

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D H Kuo, S C Kuo, J T Cheng. 2000. Structure-activity relationships of anthraquinones in the decrease of intestinal motility.. https://doi.org/10.1211/0022357001774516

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