EFFECTS OF THE NONSTEROIDAL ECDYSONE AGONIST, TEBUFENOZIDE, ON LIVER CYP ACTIVITIES

Document Type : Original Articles

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Abstract

The non-steroidal ecdysone agonist tebufenozide was orally administered to Wistar rats for 5 days to examine their effects on the liver cytochrome P450 (CYP) activities. Also Michaelis-Menten kinetics of the metabolic reactions catalyzed by liver CYPs were studied after adding tebufenozide to the assay system to investigate its possible inhibitory effects on liver CYPs activities. These reactions included ethoxyresorufin O-deethylation, tolbutamide hydroxylation, bufuralol 1-hydroxylation, and midazolam 1,4-hydroxylation, for CYP1A, 2C, 2D, and 3A activities, respectively. Results revealed no any significant alteration in the activities of the tested microsomal enzymes after oral administration of tebufenozide. none of the examined CYPs was inhibited by tebufenozide as the Ki values were very high (more than 9000 M). We can conclude that tebufenozide is considered safe and can be a good alternate for the traditional insecticides.

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