期刊
JOURNAL OF ANTIBIOTICS
卷 56, 期 3, 页码 253-258出版社
JAPAN ANTIBIOT RES ASSN
DOI: 10.7164/antibiotics.56.253
关键词
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A-500359 A, C, R G and capuramycin inhibited bacterial phospho-N-acetylmuramyl-pentapeptide-translocase (translocase 1: EC 2.7.8.13) with IC50 values of 0.017, 0.12, 0.53, 0.14 and 0.018 mum, respectively. Consistently, A-500359 A, C and capuramycin inhibited in vitro peptidoglycan biosynthesis. A-500359 A exhibited reversible inhibition, which was mixed type and noncompetitive with respect to UDP-MurNAc-(N-epsilon-Dns)pentapeptide (Ki=0.0079 muM) and undecaprenyl-phosphate. respectively. A-500359 A, C, D and G showed antimicrobial activity against Mycobacterium smegmatis. As a single intravenous injection of A-500359 A at a dose of 500 mg/kg showed no toxicity in mice, it was suggested that the capuramycin derivatives might become candidates as novel therapeutic agents for various diseases caused by Mycobacteria including tuberculosis.
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