Abstract
Benzmalecene, a known hypocholesterolemic agent, inhibits the active absorption of taurocholate by the small intestine in vivo and in vitro. It is suggested that this action contributes to the hypocholesterolemic properties of benzmalecene. This action on the intestine is not specific since sugar and tyrosine transport are also affected. The extent to which the compound's hypocholesterolemic action depends on inhibition of active absorption of these as well as other nutrients has yet to be evaluated.
Structure activity studies indicate that the maleyl moiety of benzmalecene is not essential for activity. The α diastereoisomer compounds are more active than the comparable β compounds. Dehalogenation of the molecule has significant effects on potency.
Biochemical studies in a variety of systems suggest that a major action of benzmalecene is inhibition of the enzymes of the Krebs cycle.
Footnotes
- Received September 20, 1962.
- Accepted November 19, 1962.
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