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Inhibitory Effect of Rhein on Cytochrome P_(450) Activity of Rat Liver Microsomes

Meng Xiang-le

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Abstract

Objective To evaluate the effects of rhein on the activity of cytochrome P450 3A(CYP3A) enzyme of rat liver microsomes. Methods Rat liver microsomes were incubated with various concentrations of rhein and testosterone in vitro. The inhibition of CYP3A activity by rhein was evaluated by the amount of 6β-hydroxytestosterone which was determined by HPLC. Results Rhein suppressed the CYP3A activity in rat liver microsomes,with IC50 =36.74 μmol·L-1 and Ki=20.73 μmol·L-1,respectively. Conclusion Rhein could decrease the enzyme activity of rat liver CYP3A in vitro.

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Objective To evaluate the effects of rhein on the activity of cytochrome P450 3A(CYP3A) enzyme of rat liver microsomes. Methods Rat liver microsomes were incubated with various concentrations of rhein and testosterone in vitro. The inhibition of CYP3A activity by rhein was evaluated by the amount of 6β-hydroxytestosterone which was determined by HPLC. Results Rhein suppressed the CYP3A activity in rat liver microsomes,with IC50 =36.74 μmol·L-1 and Ki=20.73 μmol·L-1,respectively. Conclusion Rhein could decrease the enzyme activity of rat liver CYP3A in vitro.

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Available abstract

Objective To evaluate the effects of rhein on the activity of cytochrome P450 3A(CYP3A) enzyme of rat liver microsomes. Methods Rat liver microsomes were incubated with various concentrations of rhein and testosterone in vitro. The inhibition of CYP3A activity by rhein was evaluated by the amount of 6β-hydroxytestosterone which was determined by HPLC. Results Rhein suppressed the CYP3A activity in rat liver microsomes,with IC50 =36.74 μmol·L-1 and Ki=20.73 μmol·L-1,respectively. Conclusion Rhein could decrease the enzyme activity of rat liver CYP3A in vitro.

Key concepts: CYP3A, Microsome, Microsoma, Cytochrome P450, In vitro, Enzyme, Chemistry, Cytochrome

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