Effects of myricetin, an antioxidant, on the pharmacokinetics of losartan and its active metabolite, EXP-3174, in rats: possible role of cytochrome P450 3A4, cytochrome P450 2C9 and P-glycoprotein inhibition by myricetin

The Journal of Pharmacy and Pharmacology
Dong-Hyun ChoiJun-Shik Choi

Abstract

The effects of myricetin, a natural flavonoid, on the pharmacokinetics of losartan and its active metabolite, EXP-3174, were investigated in rats. Losartan and myricetin interact with cytochrome P450 (CYP) enzymes and P-glycoprotein, and the increase in the use of health supplements may result in myricetin being taken concomitantly with losartan as a combination therapy to treat or prevent cardiovascular diseases. The pharmacokinetic parameters of losartan and EXP-3174 were determined after oral administration of losartan (9 mg/kg) to rats in the presence or absence of myricetin (0.4, 2 and 8 mg/kg). The effects of myricetin on P-glycoprotein as well as CYP3A4 and CYP2C9 activity were also evaluated. Myricetin inhibited CYP3A4 and CYP2C9 enzyme activity with a 50% inhibition concentration of 7.8 and 13.5 microm, respectively. In addition, myricetin significantly enhanced the cellular accumulation of rhodamine 123 in MCF-7/ADR cells overexpressing P-glycoprotein in a concentration-dependent manner. The pharmacokinetic parameters of losartan were significantly altered by myricetin compared with the control. The presence of myricetin (2 or 8 mg/kg) increased the area under the plasma concentration-time curve of losartan by 31.4-61...Continue Reading

References

May 15, 1997·Analytical Biochemistry·C L CrespiB W Penman
Apr 29, 1998·European Journal of Clinical Pharmacology·K M KaukonenP J Neuvonen
Apr 10, 1999·Journal of Clinical Pharmacology·A M MeadowcroftJ A Pieper
Sep 28, 1999·Trends in Plant Science·R A Dixon, C L Steele
May 4, 2000·Journal of Agricultural and Food Chemistry·S H HäkkinenA R Törrönen
Jul 13, 2000·European Journal of Drug Metabolism and Pharmacokinetics·P A KellyH W Strobel
Aug 15, 2000·Annual Review of Nutrition·J B German, R L Walzem
Feb 28, 2002·The Journal of Pharmacology and Experimental Therapeutics·Carolyn L CumminsLeslie Z Benet
Aug 16, 2003·Naunyn-Schmiedeberg's Archives of Pharmacology·Radka VáclavíkováIvan Gut
Aug 3, 2004·The Journal of Pharmacy and Pharmacology·Lisa L von MoltkeDavid J Greenblatt
Jul 9, 2005·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Jun-Shik Choi, Hyo-Kyung Han
Apr 15, 2008·Phytomedicine : International Journal of Phytotherapy and Phytopharmacology·B XueLb Chen
Apr 18, 2008·The Journal of Pharmacy and Pharmacology·Yong-Ji Piao, Jun-Shik Choi
May 1, 2008·Drug Metabolism and Pharmacokinetics·Mariko KobayashiKazuyuki Ueno
May 2, 2008·Archives of Pharmacal Research·Yong-Ji Piao, Jun-Shik Choi
Feb 20, 2009·Biopharmaceutics & Drug Disposition·Joong-Hwa ChungJun-Shik Choi
Mar 24, 2009·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Catarine Massucato Nishijima NishijimaClélia Akiko Hiruma-Lima
Mar 24, 2009·Phytotherapy Research : PTR·Roshan TiwariMauro Ballero
Jun 10, 2009·The Journal of Pharmacy and Pharmacology·Young-Ah ChoJun-Shik Choi

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Citations

Apr 9, 2014·Evidence-based Complementary and Alternative Medicine : ECAM·Fahad I Al-JenoobiSaleh A Al-Suwayeh
Oct 31, 2015·Journal of Toxicology and Environmental Health. Part a·Sung Ha RyuKyu-Bong Kim
May 22, 2016·European Journal of Drug Metabolism and Pharmacokinetics·Tian LanGuo-Xin Hu
Feb 12, 2017·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Tianyun HaoShuai Qian
Jun 15, 2011·Acta Pharmacologica Sinica·Si-hyung YangJun-shik Choi
Nov 24, 2016·World Journal of Surgery·Ilana LevyElad Schiff
Mar 3, 2019·European Journal of Drug Metabolism and Pharmacokinetics·Dan LouJia-Yang He
Sep 13, 2019·Evidence-based Complementary and Alternative Medicine : ECAM·Weina MaLiang Zhao
Jun 24, 2018·Naunyn-Schmiedeberg's Archives of Pharmacology·Lucie NavrátilováFrantišek Trejtnar
Aug 22, 2020·Free Radical Biology & Medicine·Antonis D TsiailanisAndreas G Tzakos
Jul 10, 2014·Journal of Agricultural and Food Chemistry·Annie J KingFahkirah Roslan

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