Abstract
Bryonolic acid (BrA) is a pentacyclic triterpene present in several plants used in African traditional medicine such as Anisophyllea dichostyla R. Br. Here we investigated the in vitro anticancer properties of BrA. We report that BrA inhibits acyl-coA: cholesterol acyl transferase (ACAT) activity in rat liver microsomes in a concentration-dependent manner, blocking the biosynthesis of the cholesterol fatty acid ester tumour promoter. We next demonstrated that BrA inhibits ACAT in intact cancer cells with an IC50 of 12.6 ± 2.4 µM. BrA inhibited both clonogenicity and invasiveness of several cancer cell lines, establishing that BrA displays specific anticancer properties. BrA appears to be more potent than the other pentacyclic triterpenes, betulinic acid and ursolic acid studied under similar conditions. The inhibitory effect of BrA was reversed by exogenous addition of cholesteryl oleate, showing that ACAT inhibition is responsible for the anticancer effect of BrA. This report reveals new anticancer properties for BrA.
Highlights
Natural compounds are an important source of pharmacologically active molecules that have been continuously characterized for years in terms of structure and pharmacological potencies and use for drug development [1]
We report that Bryonolic acid (BrA) displayed esters were recently shown to act as tumour promoters making A cholesterol acyl transferase (ACAT) a new target in cancer research anticancer properties through the inhibition of cholesterol esterification
Cholesteryl esters have been recently identified as tumour promoters by showing they stimulated cancer cells clonogenicity and invasiveness and the inhibition of the cholesteryl esterification of fatty acids (ACAT) has been shown to represent a promising target for cancer management [18,29,30,35,36,37]
Summary
Natural compounds are an important source of pharmacologically active molecules that have been continuously characterized for years in terms of structure and pharmacological potencies and use for drug development [1]. We recently reported the chemopreventive properties of such as the mammalian steroidal alkaloid dendrogenin A [17,21,22,23,24], auraptene, a prenyloxycoumarin several natural substances such as the mammalian steroidal alkaloid dendrogenin A [17,21,22,23,24], from Citrus species [25] and vitamin E including tocopherol and tocotrienol compounds [26]. A prenyloxycoumarin from Citrus species [25] and vitamin E including tocopherol and that these compounds had capacities to inhibit different mitogenic pathways in cancer cells. We report that BrA displayed esters were recently shown to act as tumour promoters making ACAT a new target in cancer research anticancer properties through the inhibition of cholesterol esterification.
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