新型碳青霉烯类抗生素LJC 10,627的肾脱氢肽酶-I稳定性
Renal dehydropeptidase-I stability of LJC 10,627, a new carbapenem antibiotic.
作者信息
Hikida M, Kawashima K, Nishiki K, Furukawa Y, Nishizawa K, Saito I, Kuwao S
机构信息
Biological Research Laboratories, Lederle Ltd., Saitama, Japan.
出版信息
Antimicrob Agents Chemother. 1992 Feb;36(2):481-3. doi: 10.1128/AAC.36.2.481.
Abstract
LJC 10,627 is a new parenteral carbapenem antibiotic. LJC 10,627 stability against human renal dehydropeptidase-I was compared with that of imipenem. Hydrolysis of this compound was not detectable by spectrophotometrical assay. Even after a 2-h incubation of antibiotics with this enzyme at 30 degrees C, the concentration of LJC 10,627 remained at 92.3% of the initial concentration, whereas imipenem completely disappeared. Thus, it was found that this compound was highly stable against human renal dehydropeptidase-I. Furthermore, LJC 10,627 had a low affinity for this enzyme, as indicated by the high Ki value (0.38 mM).
摘要
LJC 10,627是一种新型的肠外碳青霉烯类抗生素。将LJC 10,627对人肾脱氢肽酶-I的稳定性与亚胺培南进行了比较。通过分光光度法检测不到该化合物的水解情况。即使在30℃下将抗生素与该酶孵育2小时后，LJC 10,627的浓度仍保持在初始浓度的92.3%，而亚胺培南则完全消失。因此，发现该化合物对人肾脱氢肽酶-I具有高度稳定性。此外，如高Ki值（0.38 mM）所示，LJC 10,627对该酶的亲和力较低。
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