Gilpin M L, Fulston M, Payne D, Cramp R, Hood I
Smithkline Beecham Pharmaceuticals, Betchworth, Surrey, U.K.
J Antibiot (Tokyo). 1995 Oct;48(10):1081-5. doi: 10.7164/antibiotics.48.1081.
Two novel metabolites, SB 212021 and SB 212305, have been isolated from a Streptomyces and shown to have molecular formulae of C15H10N2O5 and C20H17N3O8S, respectively. The structures were deduced by a combination of NMR techniques and mass spectral fragmentation patterns and shown to be novel members of the phenazine group of antibiotics. In the absence of added zinc, both compounds had IC50's of 1-75 microM for the Bacteroides fragilis 262 CfiA and Xanthomonas maltophilia L-1 metallo-beta-lactamases. The compounds also inhibited ACE with IC50's of 55 and 68 microM, respectively. Mode of action studies illustrate that the compounds inhibit some metalloenzymes by chelation of the active site metal ion. They exhibit poor antibacterial activity.
从一种链霉菌中分离出了两种新型代谢产物，即SB 212021和SB 212305，其分子式分别为C15H10N2O5和C20H17N3O8S。通过核磁共振技术和质谱裂解模式相结合推导其结构，结果表明它们是吩嗪类抗生素的新成员。在不添加锌的情况下，这两种化合物对脆弱拟杆菌262 CfiA和嗜麦芽窄食单胞菌L-1金属β-内酰胺酶的半数抑制浓度（IC50）均为1-75微摩尔。这两种化合物还分别以55和68微摩尔的IC50抑制血管紧张素转换酶（ACE）。作用机制研究表明，这些化合物通过螯合活性位点金属离子来抑制某些金属酶。它们的抗菌活性较差。
