Decarine

Decarine (Rutaceline) is a benzophenanthridine alkaloid found in Zanthoxylum species. Decarinewith shows anti-inflammatory, antimycobacterial, and anti-HIV activity. Decarine inhibits NO, TNF-α, IL-1β, IL-6, and IL-8 production in inflammatory cell models. Decarine inhibits growth of Mycobacterium tuberculosis strains, reduces intracellular Mycobacterium tuberculosis survival, and shows low cytotoxicity toward human macrophages. Decarine inhibits HIV replication in acutely infected lymphocytes. Decarine can be used for the researches of inflammation, tuberculosis, and HIV infection^[1][2][3]. In Vitro:Decarine (24 h) potently inhibits NO production in LPS (HY-D1056)-induced RAW 264.7 macrophages with an IC₅₀ of 48.43 μM, displaying anti-inflammatory activity without cytotoxicity^[1].
Decarine (10-20 μM; 24 h) significantly inhibits TNF-α and IL-1β production in LPS-induced THP-1 macrophages^[1].
Decarine (20 μM; 24 h) significantly inhibits IL-6 and IL-8 production in TNF-α + IL-1β-induced Caco-2 cells^[1].
Decarine (10-80 μM; 24 h) is non-toxic to THP-1 macrophages at concentrations up to 20 μM, but exhibits cytotoxicity at 40 μM and 80 μM^[1].
Decarine (5-40 μM; 24 h) is non-toxic to Caco-2 cells at concentrations up to 40 μM^[1].
Decarine (7-8 day) potently inhibits the in vitro growth of virulent Mycobacterium tuberculosis H37Rv (MIC = 1.6 μg/mL) and avirulent Mycobacterium tuberculosis H37Ra (MIC = 3.1 μg/mL)^[2].
Decarine (0.8-50 μg/mL; 7 day) exhibits low cytotoxicity against human THP-1 macrophages (IC₅₀ = 66.0 μg/mL) and has high selectivity indices (21.3 for Mycobacterium tuberculosis H37Ra, 41.2 for Mycobacterium tuberculosis H37Rv) for antimycobacterial activity^[2].
Decarine (1.6-25 μg/mL; 5 days) reduces intracellular Mycobacterium tuberculosis H37Rv survival in human THP-1 macrophages by almost two log units at 6.2 μg/mL after 5 days of exposure, with dose-dependent bactericidal activity^[2].
Decarine (4 days) potently inhibits HIV replication in acutely infected H9 lymphocyte cells with an EC₅₀ of <0.1 μg/mL and has a therapeutic index of >226, as it inhibits uninfected H9 cell growth with an IC₅₀ of 22.6 μg/mL^[3].