Dapsone

Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities^[1]. Dapsone?exerts effective antileprosy activity?and inhibits folate synthesis in cell extracts of?M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al^[2][3]. IC50 & Target: IC50: bacteriostatic; folate synthesis^[3] In Vitro: Dapsone are added to cell lysates (100 μg of protein) and DHPS activity assay is tested. Dapsone exhibits an IC₅₀ of 3.0 μg/ml for E. coli?C600 in DHPS activity assay, but the growth of E. coli C600 is not inhibited at 256 μg/ml Dapsone. For the recombinant strain carrying?M. leprae folP1?(pML101), Dapsone shows an IC₅₀?of 0.06 μg/ml and a MIC of 1 μg/ml^[3]. In Vivo: In L. major-infected BALB/c MiceDapsone (topical treatment; 50 mg/kg; twice daily; 30 days) leads to sizes lesions around 186 mm²?compared to 125 mm²?for control mice. Furthermore, the amount of DAP quantified in the lesions treated with DAP cream is 9.6±8.5 μg of DAP/mg of skin. However, the number of parasites found in the spleen is significantly lower in mice treated with the cream than in non-treated mice^[4].