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However, there is no induction data for macrophages, the primary site of rifampicin\u2019s anti-tuberculosis action. THP-1 cells were differentiated (200\u00a0nM phorbol 12-myristate-13-acetate; 72\u00a0h) and polarized to M1 macrophages (50\u00a0ng\/mL lipopolysaccharide (LPS), 20\u00a0ng\/mL interferon-gamma (IFN\u03b3); 48\u00a0h) or M2 macrophages (20\u00a0ng\/mL interleukin 4 (IL-4) and interleukin 13 (IL-13) each; 48\u00a0h). Peripheral blood mononuclear cells (PBMC) from a healthy volunteer were differentiated using a commercial kit and polarized to M1 (10\u00a0ng\/mL LPS and 50\u00a0ng\/mL IFN\u03b3; 72\u00a0h) or to M2 cells (20\u00a0ng\/mL IL-4 and IL-13 each; 72\u00a0h). Polarized macrophages were exposed to 10\u00a0\u00b5M rifampicin for 1\u00a0week and mRNA levels of ABCB1, ABCG2 (coding for breast cancer resistance protein), and SLCO2B1 (coding for organic anion-transporting polypeptide 2B1) were evaluated by quantitative real-time polymerase chain reaction. P-gp protein levels were evaluated by Western blot analysis.\u00a0Rifampicin enhanced ABCB1 in THP-1-derived M1 cells (fivefold) and M2 cells (sixfold; protein increased by 50%), but not in PBMC-derived macrophages (linear regression model). However, this effect was not significant in the three-way ANOVA, given the strong influence of macrophage polarization (M1 vs. M2) and macrophage source (THP-1 vs. PBMC). ABCG2 was enhanced twofold in THP-1-derived M2 cells (linear regression model), while SLCO2B1 remained unaffected by rifampicin. In conclusion, ABCB1 expression in macrophages differs by the cell model (THP-1 cell line vs. primary PBMC) and the polarization phenotype (M1 vs. M2). Strong rifampicin-mediated enhancements of ABCB1 were only observed in THP-1-derived M1 and M2 cells.<\/jats:p>","DOI":"10.1007\/s00210-026-05231-x","type":"journal-article","created":{"date-parts":[[2026,3,25]],"date-time":"2026-03-25T05:53:56Z","timestamp":1774418036000},"page":"14561-14569","update-policy":"https:\/\/doi.org\/10.1007\/springer_crossmark_policy","source":"Crossref","is-referenced-by-count":0,"title":["Impact of rifampicin on P-glycoprotein (ABCB1) expression in M1 and M2 macrophages derived from the THP-1 monocytic cell line or peripheral blood mononuclear cells"],"prefix":"10.1007","volume":"399","author":[{"given":"Katharina","family":"Hamburg","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Anna","family":"Staszelis","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Camilo","family":"Scherkl","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Johanna","family":"Weiss","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Julia Carolin","family":"Stingl","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Dirk","family":"Theile","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"297","published-online":{"date-parts":[[2026,3,25]]},"reference":[{"key":"5231_CR1","doi-asserted-by":"publisher","first-page":"949","DOI":"10.1016\/j.bcp.2005.06.018","volume":"70","author":"N Albermann","year":"2005","unstructured":"Albermann N, Schmitz-Winnenthal FH, Z\u2019graggen K, Volk C, Hoffmann MM, Haefeli WE, Weiss J (2005) Expression of the drug transporters MDR1\/ABCB1, MRP1\/ABCC1, MRP2\/ABCC2, BCRP\/ABCG2, and PXR in peripheral blood mononuclear cells and their relationship with the expression in intestine and liver. 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