4-Aminosalicylic Acid

4-Aminosalicylic acid is an antimetabolite of p-aminobenzoic acid (PABA; Item No. 18659) that has antibacterial activity.^1,2 It is active against streptomycin-sensitive and -resistant strains of M. tuberculosis (MICs = 0.78 and 0.39 µg/ml, respectively), an effect that can be reversed by PABA.¹ 4-Aminosalicylic acid is an alternative substrate for mycobacterial dihydropteroate synthase (FolP1) and misincorporation into the folate pathway leads to accumulation of several folate-dependent metabolites including serine, homocysteine, dUMP, and AICAR, markers of folate pathway inhibition, in a concentration-dependent manner.² It reverses manganese-induced increases in rat hippocampal levels of NOD-like receptor protein 3 (NLRP3), cleaved caspase-1, and phosphorylated p65, markers of NLRP3 inflammasome-dependent pyroptosis, when administered at a dose of 300 mg/kg.³ 4-Aminosalycilic acid is also a building block that has been used in the synthesis of luminescent lanthanide complexes.⁴ Formulations containing 4-aminosalicylic acid have been used in the treatment of tuberculosis.

WARNING This product is not for human or veterinary use.

1. Youmans, G.P., Raleigh, G.W., and Youmans, A.S. The tuberculostatic action of para-aminosalicylic acid. J. Bacteriol. 54(4), 409-416 (1947).

2. Chakraborty, S., Gruber, T., Barry, C.E., III, et al. Para-aminosalicylic acid acts as an alternative substrate of folate metabolism in Mycobacterium tuberculosis. Science 339(6115), 88-91 (2013).

3. Peng, D., Li, J., Deng, Y., et al. Sodium para-aminosalicylic acid inhibits manganese-induced NLRP3 inflammasome-dependent pyroptosis by inhibiting NF-κB pathway activation and oxidative stress. J. Neuroinflammation 17(1), 343 (2020).

4. Terai, T., Ito, H., Kikuchi, K., et al. Salicylic-acid derivatives as antennae for ratiometric luminescent probes based on lanthanide complexes. Chemistry 18(24), 7377-7381 (2012).