2010Chinese Journal of Hospital PharmacyRequires access

Inductive effect of quercetin,kaempferol and rutin on liver microsomal cytochrome P450 enzymes in rats

Min Huang

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Abstract

OBJECTIVE To study the inductive effect of quercetin,kaempferol and rutin on liver microsomal six cytochrome P450 enzymes in rats.METHODS Male SD rats were administered daily dose of quercetin (10,50,250 mg·kg-1),kaempferol (10,50,250 mg·kg-1) and rutin (90 mg·kg-1),ig,for 10 consecutive days.The levels of CYP450 activity,mRNA,protein in rat liver microsome were analyzed by LC/MS/MS,RT-PCR,Western blot,respectively.RESULTS CYP1A2 protein expression was increase by 31.1%,82.4%,119.3% in a dose-dependent manner with quercetin at 10,50,250 mg·kg-1,respectively.250 mg·kg-1 quercetin also increased CYP1A2 mRNA 86.3%,CYP1A2 activity 44.2%,CYP2E1 protein 54.3%,CYP2E1 activity 36.7%.50 and 250 mg·kg-1 kaempferol increased CYP1A2 mRNA and protein 36.2%,86.8% and 110.5%,204.1%,respectively.CYP1A2 activity was also increase by 18.3%,30.1%,53.9% with three dose of kaempferol.CYP1A2 activity,mRNA and protein expression were induced by 90 mg·kg-1 rutin,increased by 62.1%,90.7%,176.2%,respectively.Rutin also increased CYP2C11 activity 30.6%.CONCLUSION Quercetin,kaempferol and rutin can induce several CYP isoforms in rats,which means the possibility of drug-drug interactions.

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OBJECTIVE To study the inductive effect of quercetin,kaempferol and rutin on liver microsomal six cytochrome P450 enzymes in rats.METHODS Male SD rats were administered daily dose of quercetin (10,50,250 mg·kg-1),kaempferol (10,50,250 mg·kg-1) and rutin (90 mg·kg-1),ig,for 10 consecutive days.The levels of CYP450 activity,mRNA,protein in rat liver microsome were analyzed by LC/MS/MS,RT-PCR,Western blot,respectively.RESULTS CYP1A2 protein expression was increase by 31.1%,82.4%,119.3% in a dose-dependent manner with quercetin at 10,50,250 mg·kg-1,respectively.250 mg·kg-1 quercetin also increased CYP1A2 mRNA 86.3%,CYP1A2 activity 44.2%,CYP2E1 protein 54.3%,CYP2E1 activity 36.7%.50 and 250 mg·kg-1 kaempferol increased CYP1A2 mRNA and protein 36.2%,86.8% and 110.5%,204.1%,respectively.CYP1A2 activity was also increase by 18.3%,30.1%,53.9% with three dose of kaempferol.CYP1A2 activity,mRNA and protein expression were induced by 90 mg·kg-1 rutin,increased by 62.1%,90.7%,176.2%,respectively.Rutin also increased CYP2C11 activity 30.6%.CONCLUSION Quercetin,kaempferol and rutin can induce several CYP isoforms in rats,which means the possibility of drug-drug interactions.

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Available abstract

OBJECTIVE To study the inductive effect of quercetin,kaempferol and rutin on liver microsomal six cytochrome P450 enzymes in rats.METHODS Male SD rats were administered daily dose of quercetin (10,50,250 mg·kg-1),kaempferol (10,50,250 mg·kg-1) and rutin (90 mg·kg-1),ig,for 10 consecutive days.The levels of CYP450 activity,mRNA,protein in rat liver microsome were analyzed by LC/MS/MS,RT-PCR,Western blot,respectively.RESULTS CYP1A2 protein expression was increase by 31.1%,82.4%,119.3% in a dose-dependent manner with quercetin at 10,50,250 mg·kg-1,respectively.250 mg·kg-1 quercetin also increased CYP1A2 mRNA 86.3%,CYP1A2 activity 44.2%,CYP2E1 protein 54.3%,CYP2E1 activity 36.7%.50 and 250 mg·kg-1 kaempferol increased CYP1A2 mRNA and protein 36.2%,86.8% and 110.5%,204.1%,respectively.CYP1A2 activity was also increase by 18.3%,30.1%,53.9% with three dose of kaempferol.CYP1A2 activity,mRNA and protein expression were induced by 90 mg·kg-1 rutin,increased by 62.1%,90.7%,176.2%,respectively.Rutin also increased CYP2C11 activity 30.6%.CONCLUSION Quercetin,kaempferol and rutin can induce several CYP isoforms in rats,which means the possibility of drug-drug interactions.

Key concepts: Rutin, Quercetin, CYP1A2, Kaempferol, Microsome, CYP2E1, Chemistry, Cytochrome P450

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