EFFECT OF SEX HORMONES ON THE EXPRESSION OF GENES ENCODING ORGANIC ANION-TRANSPORTING POLYPEPTIDES OATP1B1/OATP1B3 IN VITRO

Introduction. OATP1B1 and OATP1B3 are influx proteins belonging to the SLC transporter family and providing substrate transport into hepatocytes. The mechanisms of their regulation are currently being actively studied. Aim. To study the effect of sex hormones on the expression of the SLCO1B1 and SLCO1B3 genes encoding OATP1B1 and OATP1B3, respectively. Material and methods. The study was performed on the HepG2 cell line. Estradiol, progesterone, and testosterone were added to the cells at concentrations of 1 nM, 10 nM, 100 nM, 1 μM, 10 μM, 100 μM and incubated for 24 h. After incubation, total RNA was isolated and gene expression was tested by real-time polymerase chain reaction. Results. Estradiol at concentrations of 10 and 100 μM increased the expression of the SLCO1B1 gene encoding OATP1B1 by 50.9% (p=0.027) and 60.2% (p=0.009), respectively. Testosterone at a concentration of 1 μM increased the expression of the SLCO1B1 gene by 53.2% (p=0.014), at a concentration of 10 μM – by 62.7% (p=0.004), at a concentration of 100 μM – by 66.7% (p=0.0026). Estradiol at concentrations of 1, 10 and 100 μM increased the expression of the SLCO1B3 gene by 80.3% (p=0.0021)

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Journal
Problems of Biological Medical and Pharmaceutical Chemistry
Published
2025-06-11
DOI
https://doi.org/10.29296/25877313-2025-06-03
Primary Topic
Drug Transport and Resistance Mechanisms
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article
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article

EFFECT OF SEX HORMONES ON THE EXPRESSION OF GENES ENCODING ORGANIC ANION-TRANSPORTING POLYPEPTIDES OATP1B1/OATP1B3 IN VITRO

Pelageya D. Erokhina, A. V. Shchulkin, Marina Konopleva, Yu. V. Abalenikhina et al.
Problems of Biological Medical and Pharmaceutical Chemistry
Drug Transport and Resistance Mechanisms
article

EFFECT OF SEX HORMONES ON THE EXPRESSION OF GENES ENCODING ORGANIC ANION-TRANSPORTING POLYPEPTIDES OATP1B1/OATP1B3 IN VITRO

Pelageya D. Erokhina, A. V. Shchulkin, Marina Konopleva, Yu. V. Abalenikhina, E. N. Yakusheva, А А Слепнев, M. Kurganova
article en

Abstract

Introduction. OATP1B1 and OATP1B3 are influx proteins belonging to the SLC transporter family and providing substrate transport into hepatocytes. The mechanisms of their regulation are currently being actively studied. Aim. To study the effect of sex hormones on the expression of the SLCO1B1 and SLCO1B3 genes encoding OATP1B1 and OATP1B3, respectively. Material and methods. The study was performed on the HepG2 cell line. Estradiol, progesterone, and testosterone were added to the cells at concentrations of 1 nM, 10 nM, 100 nM, 1 μM, 10 μM, 100 μM and incubated for 24 h. After incubation, total RNA was isolated and gene expression was tested by real-time polymerase chain reaction. Results. Estradiol at concentrations of 10 and 100 μM increased the expression of the SLCO1B1 gene encoding OATP1B1 by 50.9% (p=0.027) and 60.2% (p=0.009), respectively. Testosterone at a concentration of 1 μM increased the expression of the SLCO1B1 gene by 53.2% (p=0.014), at a concentration of 10 μM – by 62.7% (p=0.004), at a concentration of 100 μM – by 66.7% (p=0.0026). Estradiol at concentrations of 1, 10 and 100 μM increased the expression of the SLCO1B3 gene by 80.3% (p=0.0021)

Problems of Biological Medical and Pharmaceutical Chemistry
Ryazan State Medical University named after Academician I.P. Pavlov (RU)
Openalex Percentile: Top 77%
Drug Transport and Resistance Mechanisms
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EFFECT OF SEX HORMONES ON THE EXPRESSION OF GENES ENCODING ORGANIC ANION-TRANSPORTING POLYPEPTIDES OATP1B1/OATP1B3 IN VITRO — Pelageya D. Erokhina, A. V. Shchulkin, et al. · Problems of Biological Medical and Pharmaceutical Chemistry (2025) | TGRS Research Map | TGRS