Zentz Frédéric, Le Guillou Régis, Labia Roger, Sirot Danielle, Linard Boris, Valla Alain
C.N.R.S., Chimie et Biologie des Substances Naturelles, 6, rue de l'Université, 29000 Quimper, France.
Farmaco. 2004 Nov;59(11):879-86. doi: 10.1016/j.farmac.2004.07.007.
We have synthesized a series of 3-substituted succinimides and their in vitro antibacterial activities have been tested towards Gram-positive and Gram-negative bacteria from the ATCC collection. Some of them possess significant antibacterial activity against Gram-positive organisms (Staphylococcus aureus ATCC 25923 and Enterococcus faecalis ATCC 29212) but all are poorly active or inactive against Gram-negative organisms (Escherichia coli ATCC 25922 and Pseudomonas aeruginosa ATCC 27853). The compounds with the lowest minimal inhibitory concentrations (esters of 3-hydroxy succinimides) are also the most cytotoxic against green monkey Vero cell line (ATCC CCL-81) and could explain that perhaps apoptosis should be implicated in eukaryotic cell cytotoxicity of succinimides.
我们合成了一系列3-取代琥珀酰亚胺，并测试了它们对美国典型培养物保藏中心（ATCC）收集的革兰氏阳性菌和革兰氏阴性菌的体外抗菌活性。其中一些对革兰氏阳性菌（金黄色葡萄球菌ATCC 25923和粪肠球菌ATCC 29212）具有显著的抗菌活性，但对革兰氏阴性菌（大肠杆菌ATCC 25922和铜绿假单胞菌ATCC 27853）均活性较差或无活性。最低最小抑菌浓度的化合物（3-羟基琥珀酰亚胺酯）对绿猴Vero细胞系（ATCC CCL-81）的细胞毒性也最大，这可能解释了琥珀酰亚胺对真核细胞的细胞毒性可能与细胞凋亡有关。
