CytocromeP4501A1 is implicated in cancer because it oxidizes polyaromatic hydrocarbonsinto more carcinogenic compounds.  Variousscientists have tested resveratrol and other stilbenes for their ability to inhibit Cytocrome P4501A1. Weassayed CYP4501A1 with 5�M ethoxyresorufin, 120�M NADPH, 1.5pM CYP4501A1, and a range of inhibitorconcentrations using 4 other stilbenes and 3 pyrroles, all synthesized fromcommon substituted anilines, for a 2 min reaction at 37 oC. Testsshowed that 3 pyrroles and 1 stilbene inhibited the enzyme. The stilbene, 1,1'-Ninylenedi-p-plenyleneldiethanolinhibited CYP4501A1 with an IC 50 value of 8.70 �M, which is similar to resveratrol whose IC50 was measured at7.81�M in our lab. Michaelis-Menten kineticexperiments showed that 1,1'-Ninylenedi-p-plenyleneldiethanol was a purenoncompetive inhibitor with a Ki of 5.14�M, which was lower than the literature value of resveratrol which is9.89�M. The pyrrols �OCH3, -OH,and -NO2 had a higher IC50 than resveratrol at 49.2�m, 75�m, >1000�m respectively.

Potentially preventing cancer with the inhibition of
Cytocrome P4501A1 by various stilbenes and pyrrols

241st National Meeting (2011)

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Potentially preventing cancer with the inhibition of Cytocrome P4501A1 by various stilbenes and pyrrols