Szczegóły publikacji

Opis bibliograficzny

Novel method of measurement of in vitro drug uptake in OATP1B3 overexpressing cells in the presence of dextran / Anna KOWAL-CHWAST, Ewelina GABOR-WORWA, Nilesh Gaud, Dawid Gogola, Agnieszka Piątek, Adrian Zarębski, Peter Littlewood, Marek SMOLUCH, Krzysztof Brzózka, Kamil Kuś // Pharmacological Reports ; ISSN 1734-1140. — 2024 — vol. 76 iss. 2, s. 400–415. — Bibliogr. s. 414–415, Abstr. — Publikacja dostępna online od: 2024-03-26. — A. Kowal-Chwast - dod. afiliacja: Ryvu Therapeutics S. A., Kraków

Autorzy (10)

Słowa kluczowe

dextranin vitro uptakeOATP1B3

Dane bibliometryczne

ID BaDAP153073
Data dodania do BaDAP2024-05-10
Tekst źródłowyURL
Rok publikacji2024
Typ publikacjiartykuł w czasopiśmie
Otwarty dostęptak
Czasopismo/seriaPharmacological Reports


Background In predictions about hepatic clearance (CLH), a number of studies explored the role of albumin and transporters in drug uptake by liver cells, challenging the traditional free-drug theory. It was proposed that liver uptake can occur for transporter substrate compounds not only from the drug's unbound form but also directly from the drug-albumin complex, a phenomenon known as uptake facilitated by albumin. In contrast to albumin, dextran does not exhibit binding properties for compounds. However, as a result of its inherent capacity for stabilization, it is widely used to mimic conditions within cells. Methods The uptake of eight known substrates of the organic anion-transporting polypeptide 1B3 (OATP1B3) was assessed using a human embryonic kidney cell line (HEK293), which stably overexpresses this transporter. An inert polymer, dextran, was used to simulate cellular conditions, and the results were compared with experiments involving human plasma and human serum albumin (HSA). Results This study is the first to demonstrate that dextran increases compound uptake in cells with overexpression of the OATP1B3 transporter. Contrary to the common theory that highly protein-bound ligands interact with hepatocytes to increase drug uptake, the results indicate that dextran's interaction with test compounds does not significantly increase concentrations near the cell membrane surface. Conclusions We evaluated the effect of dextran on the uptake of known substrates using OATP1B3 overexpressed in the HEK293 cell line, and we suggest that its impact on drug concentrations in liver cells may differ from the traditional role of plasma proteins and albumin.

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