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Baicalin is a substrate of OATP2B1 and OATP1B3
Author(s) -
KalaposKovács Bernadett,
Juhász Viktória,
TemesszentandrásiAmbrus Csilla,
Magda Balázs,
Szabó Pál T.,
Antal István,
Klebovich Imre,
Krajcsi Péter
Publication year - 2018
Publication title -
phytotherapy research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.019
H-Index - 129
eISSN - 1099-1573
pISSN - 0951-418X
DOI - 10.1002/ptr.6095
Subject(s) - baicalin , chemistry , organic anion transporter 1 , biochemistry , substrate (aquarium) , organic anion , transporter , biology , ion , chromatography , gene , ecology , high performance liquid chromatography , organic chemistry
The use and significance of baicalin, the main bioactive component found in Radix Scutellaria, have been on the rise due to its interesting pharmacological properties. Baicalin, a low passive permeability compound, is directly absorbed from the upper intestine and its hepatic elimination is dominant. However, interaction but no transport studies have implicated organic anion‐transporting polypeptides in its cellular uptake. By using mammalian cells stably expressing the uptake transporters of interest, we are showing that baicalin is a potent substrate of Organic anion‐transporting polypeptide 2B1 (OATP2B1) and less potent substrate of OATP1B3. OATP2B1 and OATP1B3 transport baicalin and may play a role in the hepatic uptake of baicalin formed in the intestine.