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

doi:10.1063/1.5139373

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 proceeding › Conference contribution › peer-review

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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 language	English
Title of host publication	4th Biomedical Engineering''s Recent Progress in Biomaterials, Drugs Development, Health, and Medical Devices
Subtitle of host publication	Proceedings of the International Symposium of Biomedical Engineering, ISBE 2019
Editors	Kenny Lischer, Tomy Abuzairi, Siti Fauziyah Rahman, Misri Gozan
Publisher	American Institute of Physics Inc.
ISBN (Electronic)	9780735419445
DOIs	https://doi.org/10.1063/1.5139373
Publication status	Published - 10 Dec 2019
Event	4th 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 2019 → 24 Jul 2019

Publication series

Name	AIP Conference Proceedings
Volume	2193
ISSN (Print)	0094-243X
ISSN (Electronic)	1551-7616

Conference

Conference	4th International Symposium of Biomedical Engineering�s Recent Progress in Biomaterials, Drugs Development, Health, and Medical Devices, ISBE 2019
Country/Territory	Indonesia
City	Padang, West Sumatera
Period	22/07/19 → 24/07/19

Keywords

intrahepatic
OCT1
primaquine
transporter

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1063/1.5139373

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Louisa, M., Suyatna, F. D., Wanandi, S. I., Asih, P. B. S., & Syafruddin, D. (2019). Intrahepatic transport of primaquine with OCT1: An in vitro study in HepG2 cells. In K. Lischer, T. Abuzairi, S. F. Rahman, & M. Gozan (Eds.), 4th Biomedical Engineering''s Recent Progress in Biomaterials, Drugs Development, Health, and Medical Devices: Proceedings of the International Symposium of Biomedical Engineering, ISBE 2019 Article 040011 (AIP Conference Proceedings; Vol. 2193). American Institute of Physics Inc.. https://doi.org/10.1063/1.5139373

Louisa, Melva ; Suyatna, Frans D. ; Wanandi, Septelia Inawati et al. / Intrahepatic transport of primaquine with OCT1 : An in vitro study in HepG2 cells. 4th Biomedical Engineering''s Recent Progress in Biomaterials, Drugs Development, Health, and Medical Devices: Proceedings of the International Symposium of Biomedical Engineering, ISBE 2019. editor / Kenny Lischer ; Tomy Abuzairi ; Siti Fauziyah Rahman ; Misri Gozan. American Institute of Physics Inc., 2019. (AIP Conference Proceedings).

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title = "Intrahepatic transport of primaquine with OCT1: An in vitro study in HepG2 cells",

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.",

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author = "Melva Louisa and Suyatna, {Frans D.} and Wanandi, {Septelia Inawati} and Asih, {Puji B.S.} and Din Syafruddin",

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language = "English",

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publisher = "American Institute of Physics Inc.",

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Louisa, M , Suyatna, FD , Wanandi, SI, Asih, PBS & Syafruddin, D 2019, Intrahepatic transport of primaquine with OCT1: An in vitro study in HepG2 cells. in K Lischer, T Abuzairi, SF Rahman & M Gozan (eds), 4th Biomedical Engineering''s Recent Progress in Biomaterials, Drugs Development, Health, and Medical Devices: Proceedings of the International Symposium of Biomedical Engineering, ISBE 2019., 040011, AIP Conference Proceedings, vol. 2193, American Institute of Physics Inc., 4th International Symposium of Biomedical Engineering�s Recent Progress in Biomaterials, Drugs Development, Health, and Medical Devices, ISBE 2019, Padang, West Sumatera, Indonesia, 22/07/19. https://doi.org/10.1063/1.5139373

Intrahepatic transport of primaquine with OCT1: An in vitro study in HepG2 cells. / Louisa, Melva ; Suyatna, Frans D.; Wanandi, Septelia Inawati et al.
4th Biomedical Engineering''s Recent Progress in Biomaterials, Drugs Development, Health, and Medical Devices: Proceedings of the International Symposium of Biomedical Engineering, ISBE 2019. ed. / Kenny Lischer; Tomy Abuzairi; Siti Fauziyah Rahman; Misri Gozan. American Institute of Physics Inc., 2019. 040011 (AIP Conference Proceedings; Vol. 2193).

Research output: Chapter in Book/Report/Conference proceeding › Conference contribution › peer-review

TY - GEN

T1 - Intrahepatic transport of primaquine with OCT1

T2 - 4th International Symposium of Biomedical Engineering�s Recent Progress in Biomaterials, Drugs Development, Health, and Medical Devices, ISBE 2019

AU - Louisa, Melva

AU - Suyatna, Frans D.

AU - Wanandi, Septelia Inawati

AU - Asih, Puji B.S.

AU - Syafruddin, Din

PY - 2019/12/10

Y1 - 2019/12/10

N2 - 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.

AB - 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.

KW - intrahepatic

KW - OCT1

KW - primaquine

KW - transporter

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U2 - 10.1063/1.5139373

DO - 10.1063/1.5139373

M3 - Conference contribution

AN - SCOPUS:85076759973

T3 - AIP Conference Proceedings

BT - 4th Biomedical Engineering''s Recent Progress in Biomaterials, Drugs Development, Health, and Medical Devices

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PB - American Institute of Physics Inc.

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ER -

Louisa M , Suyatna FD , Wanandi SI, Asih PBS, Syafruddin D. Intrahepatic transport of primaquine with OCT1: An in vitro study in HepG2 cells. In Lischer K, Abuzairi T, Rahman SF, Gozan M, editors, 4th Biomedical Engineering''s Recent Progress in Biomaterials, Drugs Development, Health, and Medical Devices: Proceedings of the International Symposium of Biomedical Engineering, ISBE 2019. American Institute of Physics Inc. 2019. 040011. (AIP Conference Proceedings). doi: 10.1063/1.5139373

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

Abstract

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Keywords

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