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Effects of three Chinese patent medicines against cardiovascular diseases on the in vitro activities of rat liver microsomal CYP450 four subtypes

Rurun Huang, Jiao Yang, Shan Liu, Yucheng Mu, Yong Lai

Article ID: 1911
Vol 3, Issue 1, 2022

DOI: https://doi.org/10.54517/ccr.v3i1.1911
VIEWS - 46 (Abstract)

Abstract

Objective: To evaluate the effects of Shensong Yangxin capsule, Qiliqiangxin capsule and Tongmai Yangxin Pill on the in vitro activities of four subtypes of rat liver microsomal CYP450 enzyme CYP1A2, CYP2C11, CYP2D1 and CYP3A1. Method: 15.04 μmol·L^-1 caffeine, 4.98 μmol·L^-1 omeprazole, 7.81 μmol·L^-1 metoprolol and 6 μmol·L^-1 midazolam is the specific probe substrate of CYP1A2, CYP2C11, CYP2D1 and CYP3A1 respectively. Three Chinese patent medicines against cardiovascular diseases are co incubated with the mixed probe substrate of four CYP450 enzyme subtypes in rat liver microsomes respectively. The remaining probe substrate in rat liver microsomes incubation system is measured by HPLC to calculate the inhibition percentage of corresponding enzyme activity and calculate the IC₅₀ value. Results: compared with the blank group, the activities of sub enzymes decreased with the increase of the concentration of three drugs (P < 0.05); The IC₅₀ values of three drugs on rat liver microsomal CYP1A2, CYP2C11, CYP2D1 and CYP3A1 were 1.896, 31.97, 12.37 and 1.357 respectively μmol·L^-1; Qiliqiangxin capsule>100, 1.513, 35.2, 6.669 μmol·L^-1; Tongmai Yangxin pill>100, 33.970, 0.566, 14.380 μmol·L^-1 . Conclusion: Shensong Yangxin capsule has moderate inhibitory effect on CYP1A2 and CYP3A1, Qiliqiangxin capsule has moderate inhibitory effect on CYP2C11 and CYP3A1, Tongmai Yangxin pill has strong inhibitory effect on CYP2D1, and other effects are not obvious.

Keywords

rat liver microsomes; Shensong Yangxin Capsule; Qiliqiangxin capsule; Tongmai Yangxin pill; CYP450 enzyme

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