ArticleArchives of toxicology2026
Rifabutin boosts rifampicin accumulation in THP-1-derived M2 macrophages by inhibiting P-glycoprotein efflux activity.
Article in Archives of toxicology, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
M2 macrophages show higher efflux activity of the P-glycoprotein (P-gp) drug transporter and lower rifampicin uptake than M1 macrophages. Accordingly, in M2 macrophages rifampicin accumulation should be restored by potent P-gp inhibitors such as rifabutin. THP-1 cells were differentiated (200 nM phorbol-12-myristate 13-acetate for 72 h) and polarized (20 ng/mL interleukin 4 and interleukin 13 for 48 h) to M2 macrophages. P-gp inhibition by rifabutin was assessed through flow cytometry using rhodamine 123 (substrate) and compared to zosuquidar (positive P-gp inhibitor control). Ultra-performance liquid chromatography coupled to mass spectrometry (UPLC-MS/MS) was used to evaluate the cellular rifampicin accumulation after 2 h of exposure to 0.05, 0.1, or 0.5 µM rifampicin, with or without co-treatment of cells with rifabutin (0.01 µM, 0.1 µM, 1 µM, 10 µM). Rifabutin (IC
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