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Pan, Xiaolei, Wang, Li, Gruendemann, Dirk and Sweet, Douglas H. (2014). Inhibition of human organic cation transporters by the alkaloids matrine and oxymatrine. Fitoterapia, 92. S. 206 - 211. AMSTERDAM: ELSEVIER SCIENCE BV. ISSN 1873-6971

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Abstract

Human organic cation transporters (hOCTs; SLC22) are expressed in many organs, including intestine, liver, kidney, heart and brain, where they contribute to the absorption, distribution, and elimination of endogenous and exogenous substances. The alkaloids matrine and oxymatrine are widely used in herbal medicine for the treatment of cancer, as well as viral, and cardiac diseases. Their physicochemical properties indicated that they are potential inhibitors for hOCTs, leading to drug-drug interactions in vivo. Therefore, we assessed the inhibitory effects of matrine and oxymatrine on the function of hOCT1 (SLC22A1), hOCT2 (SLC22A2) and hOCT3 (SLC22A3) using stably transfected transporter-expressing cells. At 100-fold excess, oxymatrine exhibited marked inhibition of hOCT1-mediated substrate uptake (p < 0.05), while matrine failed to produce significant inhibition on hOCT1. The IC50 value for oxymatrine on hOCT1 was estimated as 513 +/- 132 mu M. While there was no significant inhibition of hOCT2 or hOCT3 at 100-fold excess, oxymatrine and matrine showed 42% and 88% inhibition of hOCT3-mediated substrate uptake at 3 and 6 mM, respectively. Considering the potential intestinal lumen and reported plasma concentrations of matrine and oxymatrine, these data suggest that drug-drug interactions may occur during hOCT1-mediated hepatic and renal uptake and during hOCT3-mediated intestinal absorption. (C) 2013 Elsevier B.V. All rights reserved.

Item Type:	Journal Article
Creators:	Creators Email ORCID ORCID Put Code Pan, Xiaolei UNSPECIFIED UNSPECIFIED UNSPECIFIED Wang, Li UNSPECIFIED UNSPECIFIED UNSPECIFIED Gruendemann, Dirk UNSPECIFIED UNSPECIFIED UNSPECIFIED Sweet, Douglas H. UNSPECIFIED UNSPECIFIED UNSPECIFIED
URN:	urn:nbn:de:hbz:38-450818
DOI:	10.1016/j.fitote.2013.11.009
Journal or Publication Title:	Fitoterapia
Volume:	92
Page Range:	S. 206 - 211
Date:	2014
Publisher:	ELSEVIER SCIENCE BV
Place of Publication:	AMSTERDAM
ISSN:	1873-6971
Language:	English
Faculty:	Unspecified
Divisions:	Unspecified
Subjects:	no entry
Uncontrolled Keywords:	Keywords Language ANION TRANSPORTERS; METABOLITE MATRINE; HERBAL MEDICINE; DOG PLASMA; 3 SLC22A8; PHARMACOKINETICS; INVOLVEMENT; COMPONENTS; THERAPY; FOOD Multiple languages Chemistry, Medicinal; Pharmacology & Pharmacy Multiple languages
URI:	http://kups.ub.uni-koeln.de/id/eprint/45081