Quercetin-3-rhamnoglucoside (rutin) stimulates transport of organic anion compounds mediated by organic anion transporting polypeptide 2B1
作者： Jiro Ogura , Takahiro Koizumi , Masahiro Segawa , Keisuke Yabe , Kaori Kuwayama
DOI: 10.1002/BDD.1882
关键词:
摘要: Quercetin-3-rhamnoglucoside (rutin) has a wide spectrum of biochemical and pharmacological activities. Rutin is absorbed mainly in its unmetabolized form. Organic anion transporting polypeptide (OATP) 2B1 major uptake transporter the intestine. Thus, it important for prevention adverse events to understand drug interactions mediated by OATP2B1 absorption process. This study assessed effect rutin on transport OATP2B1. stimulated estrone-3-sulfate (E-3-S), taurocholic acid (TCA), cholic (CA) rosuvastatin OATP2B1, but not p-coumaric or ferulic acid. The EC50 was 2.32 μm. Km value E-3-S presence (9.21 μm) almost same as that absence (8.53 μm). On other hand, Vmax (270 pmol/mg protein/min) 1.2-fold higher than (218 protein/min). Moreover, expression level cell membrane increased treatment with 5 min without alteration total level. increase localization at surface detected immunocytochemistry. stimulatory little weak may affect substrates, because taken daily foods intestinal concentration would reach range
elsevier.com
sci-hub.se 参考文章(23)
Ikumi Tamai, Takashi Nozawa, Minako Koshida, Jun‐ichi Nezu, Yoshimichi Sai, Akira Tsuji, Functional characterization of human organic anion transporting polypeptide B (OATP-B) in comparison with liver-specific OATP-C. Pharmaceutical Research. ,vol. 18, pp. 1262- 1269 ,(2001) , 10.1023/A:1013077609227
William F. Hodnick, Frances S. Kung, William J. Roettger, Craig W. Bohmont, Ronald S. Pardini, Inhibition of mitochondrial respiration and production of toxic oxygen radicals by flavonoids. A structure-activity study. Biochemical Pharmacology. ,vol. 35, pp. 2345- 2357 ,(1986) , 10.1016/0006-2952(86)90461-2
S ITAGAKI, T KUROKAWA, C NAKATA, Y SAITO, S OIKAWA, M KOBAYASHI, T HIRANO, K ISEKI, In vitro and in vivo antioxidant properties of ferulic acid: a comparative study with other natural oxidation inhibitors. Food Chemistry. ,vol. 114, pp. 466- 471 ,(2009) , 10.1016/J.FOODCHEM.2008.09.073
Shirou Itagaki, Setsu Oikawa, Jiro Ogura, Masaki Kobayashi, Takeshi Hirano, Ken Iseki, Protective effects of quercetin-3-rhamnoglucoside (rutin) on ischemia-reperfusion injury in rat small intestine Food Chemistry. ,vol. 118, pp. 426- 429 ,(2010) , 10.1016/J.FOODCHEM.2009.04.103
Jeremy P.E Spencer, George Chowrimootoo, Ruksana Choudhury, Edward S Debnam, S.Kaila Srai, Catherine Rice-Evans, The small intestine can both absorb and glucuronidate luminal flavonoids. FEBS Letters. ,vol. 458, pp. 224- 230 ,(1999) , 10.1016/S0014-5793(99)01160-6
Hidetoshi ARIMA, Hitoshi ASHIDA, Gen-ichi DANNO, Rutin-enhanced antibacterial activities of flavonoids against Bacillus cereus and Salmonella enteritidis Bioscience, Biotechnology, and Biochemistry. ,vol. 66, pp. 1009- 1014 ,(2002) , 10.1271/BBB.66.1009
Shrestha Sharma, Asgar Ali, Javed Ali, Jasjeet K. Sahni, Sanjula Baboota, Rutin : therapeutic potential and recent advances in drug delivery. Expert Opinion on Investigational Drugs. ,vol. 22, pp. 1063- 1079 ,(2013) , 10.1517/13543784.2013.805744
Yoshimichi Sai, Yosuke Kaneko, Satsuki Ito, Keisuke Mitsuoka, Yukio Kato, Ikumi Tamai, Per Artursson, Akira Tsuji, PREDOMINANT CONTRIBUTION OF ORGANIC ANION TRANSPORTING POLYPEPTIDE OATP-B (OATP2B1) TO APICAL UPTAKE OF ESTRONE-3-SULFATE BY HUMAN INTESTINAL CACO-2 CELLS Drug Metabolism and Disposition. ,vol. 34, pp. 1423- 1431 ,(2006) , 10.1124/DMD.106.009530
Masahiro Segawa, Jiro Ogura, Satoru Seki, Shirou Itagaki, Natsuko Takahashi, Masaki Kobayashi, Takeshi Hirano, Hiroaki Yamaguchi, Ken Iseki, Rapid Stimulating Effect of the Antiarrhythmic Agent Amiodarone on Absorption of Organic Anion Compounds Drug Metabolism and Pharmacokinetics. ,vol. 28, pp. 178- 186 ,(2013) , 10.2133/DMPK.DMPK-12-RG-010
Anna Koenen, Heyo K Kroemer, Markus Grube, Henriette E Meyer zu Schwabedissen, Current understanding of hepatic and intestinal OATP-mediated drug-drug interactions. Expert Review of Clinical Pharmacology. ,vol. 4, pp. 729- 742 ,(2011) , 10.1586/ECP.11.58