DIAZAQUINOMYCIN-A, A NEW ANTIFOLATE ANTIBIOTIC, INHIBITS THYMIDYLATE SYNTHASE
DIAZAQUINOMYCIN-A, A NEW ANTIFOLATE ANTIBIOTIC, INHIBITS THYMIDYLATE SYNTHASE
复制标题
DOI：
10.7164/antibiotics.38.1025
复制
发表时间：
1985-01-01
影响因子：
3.3
通讯作者：
OMURA, S
中科院分区：
文献类型：
--
作者：
MURATA, M;MIYASAKA, T;OMURA, S
二氮喹霉素A(DQM)对粪肠球菌生长的抑制作用可被胸腺嘧啶核苷完全逆转。相对大量的叶酸、二氢叶酸或亚叶酸也逆转了DQM的活性。DQM对Vero和Raji细胞有细胞毒作用，亚叶酸钙或胸腺嘧啶核苷可部分逆转DQM的细胞毒作用。酶实验发现，DQM与酶反应底物5，10-亚甲基四氢叶酸具有竞争性抑制粪肠球菌和艾氏腹水癌TMP合成酶的作用。
The inhibitory effect of diazaquinomycin A (DQM) on the growth of Enterococcus faecium was completely reversed by thymidine. Relatively large amounts of folate, dihydrofolate or leucovorin also reversed the activity of DQM. DQM showed cytotoxicity against Vero and Raji cells and the cytotoxicity was partially reversed by leucovorin or thymidine. With enzyme experiments, it was found that DQM inhibits TMP synthases from E. faecium and Ehrlich ascites carcinoma competitively with 5,10-methylenetetrahydrofolate, one of the substrates for the enzyme reaction.