Katayama N, Nozaki Y, Okonogi K, Ono H, Harada S, Okazaki H
J Antibiot (Tokyo). 1985 Sep;38(9):1117-27. doi: 10.7164/antibiotics.38.1117.
A Gram-negative bacterium produces new monocyclic beta-lactam antibiotics with a formylamino substituent, named formadicins A, B, C and D. The producing bacterium was taxonomically characterized and designated as Flexibacter alginoliquefaciens sp. nov. YK-49. Formadicins have narrow antibacterial spectra. They are highly active against some species of Pseudomonas, Proteus and Alcaligenes. Of the four, formadicin C shows the most potent antibacterial activity. Several amino acids such as glycine, D-alanine and D-leucine were antagonistic against formadicins. Formadicins, especially formadicins A and C having the formylamino substituent bound to the 3-position of a beta-lactam nucleus, were highly resistant to hydrolysis by various types of beta-lactamases. Formadicins A and C showed affinity for penicillin-binding proteins (PBPs) 1A and 1B in Pseudomonas aeruginosa IFO 3080, but formadicin B and nocardicin A showed affinity only for PBP 1B. Formadicins A and C did not lyse Escherichia coli LD-2 solely at their MICs, but when combined with mecillinam each induced a rapid lysis of this organism.
一种革兰氏阴性细菌产生了带有甲酰氨基取代基的新型单环β-内酰胺抗生素，命名为甲酰杀菌素A、B、C和D。对产生该抗生素的细菌进行了分类学鉴定，并将其指定为嗜藻溶杆菌新种YK-49。甲酰杀菌素具有较窄的抗菌谱。它们对某些假单胞菌属、变形杆菌属和产碱菌属的菌种具有高度活性。在这四种甲酰杀菌素中，甲酰杀菌素C表现出最强的抗菌活性。几种氨基酸，如甘氨酸、D-丙氨酸和D-亮氨酸，对甲酰杀菌素具有拮抗作用。甲酰杀菌素，特别是在β-内酰胺核的3位带有甲酰氨基取代基的甲酰杀菌素A和C，对各种类型的β-内酰胺酶具有高度抗性。甲酰杀菌素A和C对铜绿假单胞菌IFO 3080中的青霉素结合蛋白（PBPs）1A和1B具有亲和力，但甲酰杀菌素B和诺卡杀菌素A仅对PBP 1B具有亲和力。甲酰杀菌素A和C在其最低抑菌浓度（MIC）下单独作用时不会使大肠杆菌LD-2裂解，但与美西林联合使用时，每种都会诱导该菌快速裂解。
