Andrographolide is neither a human organic anion transporter 1 (hOAT1) substrate nor inhibitor

Abstract

Andrographolide, a major bioactive compound isolated from Andrographis paniculata (Burm. F.) Nees, was evaluated for its effects on the hOAT1 membrane transporter. Substrate determination and inhibition of hOAT1-mediated uptake transport assay was carried out using recombinant CHO-hOAT1 cells. The results showed that the uptake ratio of andrographolide was less than 2.0 at all concentrations tested, indicating that andrographolide is not a hOAT1 substrate. Andrographolide has no significant effects on the p-aminohippuric acid uptake and on the mRNA and protein expression of hOAT1. In conclusion, andrographolide may not pose a drug–herb interaction risk related to hOAT1.

Keywords:

• Andrographolide
• drug–herb interaction
• hOAT1
• membrane transporter
• toxicity

Acknowledgments

The authors would like to thank Prof Ryan M. Pelis for the OAT homology model.

Disclosure statement

The authors would like to declare that there is no conflict of interests.

Additional information

Funding

The authors would like to acknowledge the funding from Sciencefund Grant (02-05-23-SF0002), Ministry of Science, Technology and Innovation (MOSTI) and RUI grant (1001/CIPPT/811283) from Universiti Sains Malaysia. CYM was sponsored by the MyBrain15 scheme, Ministry of Education Malaysia.