Journal of Clinical Toxicology
Open Access
ISSN: 2161-0495
+44 1478 350008
ISSN: 2161-0495
+44 1478 350008
Chae Bin Lee, Soo Kyung Bae, Soon Uk Chae and Jee Sun Min
The Catholic University of Korea, Republic of South Korea
Posters & Accepted Abstracts: J Clinic Toxicol
Organic anion transporting polypeptide (OATP) 1B3 plays an essential role in the hepatic uptake of many drugs and the assessment of OATP1B3-mediated drug-drug interactions is recently emphasized. The main active components of ginseng are ginsenosides, a diverse group of triterpenoid saponins that exert a variety of pharmacological activities including anti-inflammatory, anti-cancer, anti-diabetic, and cardioprotective effects. Of these, ginsenoside Rh2 is mainly recognized as an anti-cancer compound, and contains the two epimeric forms, 20(R)-Rh2 and 20(S)-Rh2. It was reported that the stereochemistry of the C-20 hydroxyl group [i.e. 20(R)-Rh2 and 20(S)-Rh2] not only plays a role in the pharmacodynamics of ginsenosides but also in their pharmacokinetic properties. The aim of this study was to evaluate the human organic anion transporting polypeptide 1B3 (OATP1B3)-mediated drug-drug interaction potential of ginsenoside Rh2 (Rh2) epimers, 20(R)Rh2 and 20(S)-Rh2, using human embryonic kidney 293 (HEK293) cells overexpressing OATP1B3 (HEK293-OATP1B3). The inhibition of estradiol 17�?²-D-glucuronide transport by ginsenoside Rh2 epimers were assessed in HEK293-OATP1B1. Our results showed that both 20(R)-Rh2 and 20(S)-Rh2 exhibited different potencies of stereoselective inhibition on the OATP1B3 uptake. 20(S)-Rh2 exerted marked inhibition with and IC50 value of 17.1�?±7.10 �?¼M, whereas their (R)-isomer did not inhibit OATP1B3 uptake activity.
Chae Bin Lee is a graduate student with major in Pharmacology/Pharmacokinetics from The Catholic University of Korea. Her research interest include: in vitro herb-drug interaction, nonclinical pharmacokinetics and bio analysis development.
E-mail: aribri727@catholic.ac.kr