Format

Send to

Choose Destination
Basic Clin Pharmacol Toxicol. 2016 Oct;119(4):349-52. doi: 10.1111/bcpt.12596. Epub 2016 May 27.

Measurement of Rhodamine 123 in Three-Dimensional Organoids: A Novel Model for P-Glycoprotein Inhibitor Screening.

Author information

1
Shanghai Key Laboratory of Regulatory Biology, Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, Shanghai, China.
2
Department of Molecular and Cellular Medicine, Center for Cancer and Stem Cell Biology, Institute of Biosciences and Technology, Texas A&M University Health Science Center, Houston, TX, USA.
3
Shanghai Key Laboratory of Regulatory Biology, Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, Shanghai, China. usxinwang@gmail.com, xwang@bio.ecnu.edu.cn.

Abstract

P-glycoprotein (P-gp), as the most important efflux transporter in intestines, plays the key role to determine the bioavailability of many drugs. The three-dimensional (3D) organoid model is suitable to imitate small intestinal epithelium. In this study, a rapid, sensitive and efficient method to measure rhodamine 123 (Rh123, P-gp substrate) in 3D organoids was developed to analyse P-gp-mediated drug transport. Ultrasonic cell disruptor was used to smash the organoid, and automatic microplate reader was used for detecting the concentration of Rh123 (λex /λem = 485/520 nm). Moreover, verapamil, quinidine and mitotane were used to make validation about this newly developed approach. All three P-gp inhibitors significantly inhibited the transport of Rh123 into 3D organoids. Therefore, the above-mentioned method could serve as a new model for P-gp inhibitor screening in a high-throughput way.

PMID:
27060462
DOI:
10.1111/bcpt.12596
[Indexed for MEDLINE]
Free full text

Supplemental Content

Full text links

Icon for Wiley
Loading ...
Support Center