Rifampicin is an ansamycin antibiotic that exhibits antibacterial, neuroprotective, and anti-inflammatory activities. Rifampicin inhibits bacterial DNA-dependent RNA polymerase, preventing formation of the initiation complex in transcription and suppressing RNA synthesis; it is active against Mycobacterium and is clinically used to treat tuberculosis. In microglia, rifampicin decreases expression of the 26S protease regulatory subunit (MSS1), suppressing inflammatory cytokine release. Additionally, rifampicin upregulates expression of LRP1 and P-gp at the blood brain barrier, increasing clearance of amyloid-β (Aβ) and displaying potential efficacy in the treatment of Alzheimer’s disease.
References
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Bi W, Jing X, Zhu L, et al. Inhibition of 26S protease regulatory subunit 7 (MSS1) suppresses neuroinflammation. PLoS One. 2012;7(5):e36142. PMID: 22629310.
Qosa H, Abuznait AH, Hill RA, et al. Enhanced brain amyloid-β clearance by rifampicin and caffeine as a possible protective mechanism against Alzheimer's disease. J Alzheimers Dis. 2012;31(1):151-65. PMID: 22504320.
Campbell EA, Korzheva N, Mustaev A, et al. Structural mechanism for rifampicin inhibition of bacterial rna polymerase. Cell. 2001 Mar 23;104(6):901-12. PMID: 11290327
