Intrahepatic transport of primaquine with OCT1: An in vitro study in HepG2 cells

Melva Louisa, Frans D. Suyatna, Septelia Inawati Wanandi, Puji B.S. Asih, Din Syafruddin

Research output: Chapter in Book/Report/Conference proceedingConference contributionpeer-review

Abstract

Primaquine is presently the only drug available as anti-hypnozoites in the treatment of malaria caused by Plasmodium vivax. Due to its hydrophilic properties, it was estimated that the uptake of primaquine to its target (liver) to be very difficult. This study was aimed to understand the mechanism of primaquine uptake to the hepatocytes through the transport protein, OCT1 (organic cationic transporter 1). This was an in vitro experiment in HepG2 cells. The HepG2 cells were propagated in vitro following the procedure published previously. The intracellular concentrations of primaquine were quantified using HPLC coupled with photodiode array detection (HPLC-PDA). The mRNA expression of OCT1 was determined using quantitative RT-PCR. To determine whether the uptake of primaquine to the hepatocytes was transported by OCT1, we quantify intracellular primaquine concentrations and analyze the mRNA OCT1 expressions in the cells treated with primaquine +/- OCT1 inhibitor (quinidine). OCT1 inhibitor (quinidine) decreased the intracellular levels of primaquine significantly in almost all the concentrations investigated. The exposure of primaquine with quinidine consistently reduced the expression of OCT1 mRNA compared with primaquine alone. In conclusion, primaquine is efficiently transported by OCT1 in HepG2 cells. OCT1 is thought to be one of the target protein to increase the uptake of primaquine to the hepatocytes.

Original languageEnglish
Title of host publication4th Biomedical Engineering''s Recent Progress in Biomaterials, Drugs Development, Health, and Medical Devices
Subtitle of host publicationProceedings of the International Symposium of Biomedical Engineering, ISBE 2019
EditorsKenny Lischer, Tomy Abuzairi, Siti Fauziyah Rahman, Misri Gozan
PublisherAmerican Institute of Physics Inc.
ISBN (Electronic)9780735419445
DOIs
Publication statusPublished - 10 Dec 2019
Event4th International Symposium of Biomedical Engineering�s Recent Progress in Biomaterials, Drugs Development, Health, and Medical Devices, ISBE 2019 - Padang, West Sumatera, Indonesia
Duration: 22 Jul 201924 Jul 2019

Publication series

NameAIP Conference Proceedings
Volume2193
ISSN (Print)0094-243X
ISSN (Electronic)1551-7616

Conference

Conference4th International Symposium of Biomedical Engineering�s Recent Progress in Biomaterials, Drugs Development, Health, and Medical Devices, ISBE 2019
CountryIndonesia
CityPadang, West Sumatera
Period22/07/1924/07/19

Keywords

  • intrahepatic
  • OCT1
  • primaquine
  • transporter

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