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Dapsone

CAS No. : 80-08-0

MCE 国际站：Dapsone

产品活性：Dapsone (4,4′-Diaminodiphenyl sulfone) 是一种具有口服活性和血脑渗透通透性的磺酰类抗生素 (antibiotic)，具有抑菌、抗细菌和抗原虫活性。Dapsone 具有有效的抗麻风活性，抑制了麻风杆菌细胞提取物中叶酸的合成 (folate synthesis)。Dapsone 可用于皮肤病的研究，如麻风病、疱疹样皮炎、寻常痤疮等。

研究领域：Anti-infection  |  Metabolic Enzyme/Protease  |  Immunology/Inflammation  |  NF-κB

作用靶点：Antibiotic  |  Parasite  |  Bacterial  |  Reactive Oxygen Species

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.

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.

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