Inactivation of new carbapenem antibiotics by dehydropeptidase-I from porcine and human renal cortex.

Inactivation of new carbapenem antibiotics by dehydropeptidase-I from porcine and human renal cortex.
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来自猪和人肾皮质的脱氢肽酶-I 使新型碳青霉烯类抗生素失活。

DOI:
10.1093/jac/30.2.129
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发表时间:
1992
期刊:
The Journal of antimicrobial chemotherapy
影响因子:
--
通讯作者:
S. Mitsuhashi
S. Mitsuhashi
中科院分区:
--
文献类型:
--
作者:
M. Hikida;K. Kawashima;M. Yoshida;S. Mitsuhashi

文献摘要

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比较了新型碳青霉烯类抗生素帕尼培南、美罗培南和LJC 10,627对猪和人肾脱氢肽酶-I(DHP-I)的稳定性。对肾脏DHP-I水解的稳定性顺序为:LJC 10,627大于美罗培南大于帕尼培南大于亚胺培南。在30 ℃下将药物与猪或人酶孵育4小时后,残留活性百分比如下:LJC分别为10,627,73.7%和95.6%;美罗培南分别为0.2%和28.7%;帕尼培南分别为0%和4.3%;亚胺培南分别为0%和0.1%。这些结果表明,LJC 10,627对肾DHP-I具有极高的稳定性。
The stability of the new carbapenem antibiotics, panipenem, meropenem and LJC 10,627, against porcine and human renal dehydropeptidase-I (DHP-I) was compared with that of imipenem. The order of stability to hydrolysis by renal DHP-I was: LJC 10,627 greater than meropenem greater than panipenem greater than imipenem. After incubation of the drugs with porcine or human enzyme at 30 degrees C for 4 h, the percentages of residual activity were as follows: LJC 10,627, 73.7% and 95.6%, respectively; meropenem, 0.2% and 28.7%, respectively; panipenem, 0% and 4.3%, respectively; and imipenem, 0% and 0.1%, respectively. These results demonstrate that LJC 10,627 has extremely high stability against renal DHP-I.