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Research Communication

Olive Oil Phenols Inhibit Human Hepatic Microsomal Activity

Center for Pharmaceutical Research, School of Pharmacy and Medical Sciences, University of South Australia, SA, 5000, Australia

¹To whom correspondence should be addressed.

We have examined the inhibition of human hepatic microsomal androstenedione 6ß-hydroxylation and both reductive and oxidative 17ß-hydroxysteroid dehydrogenase (17ß-HSD) activity by complex phenols found in olive oil. Structurally similar compounds were also examined for comparison. Androstenedione 6ß-hydroxylase activity was inhibited by oleuropein glycoside, hydroxytyrosol and gallic acid. Oleuropein glycoside, hydroxytyrosol, gallic acid and dihydroxybenzoic acid also inhibited reductive 17ß-HSD activity. Oxidative 17ß-HSD activity was not inhibited by any of the compounds tested; however gallic acid stimulated activity by 30%. Androstenedione 6ß-hydroxylase activity showed atypical kinetics. For oleuropein glycoside, hydroxytyrosol and gallic acid the apparent K_i values were determined to be 80, 77 and 70 µmol/L, respectively. Analysis of structural features of inhibitory compounds established that a 3,4-dihydroxyphenyl ethanol structure was required for inhibition of androstenedione 6ß-hydroxylase for this group of compounds.

KEY WORDS: • humans • cytochrome P450 • 17ß-hydroxysteroid dehydrogenase • CYP3A