[过渡金属配位化合物的生物学效应。顺铂、2-氨基吡啶氯化钯、克拉维酸和青霉烷酸砜CP 45,899在硝噻吩试验及Titertek/微量滴定自动系统中的β-内酰胺酶抑制作用]

[Biological effects of coordination compounds of transitional metals. The beta-lactamase inhibitory effect of cis-platin, 2-aminopyridine palladium chloride, clavulanic acid and penicillanic acid sulfonate CP 45,899 in the nitrocefin test and Titertek/microtiter automatic system].

作者信息

Fleck W F, Heyn B, Schröer H P

出版信息

Z Allg Mikrobiol. 1983;23(5):313-7. doi: 10.1002/jobm.3630230506.

Abstract

The beta-lactamase-inhibiting activity of 6m-ethyl-pyrid-2-yl-ammine palladium-dichloride (Pd 25681) and cis-dichloro-diammine-platinum(II) was studied and compared with the enzyme inhibitory action of potassium clavulanate and the penicillanic acid sulfone CP 45899. Using the nitrocefin test method and the Titertek/Microtiter equipment CP 45899 and potassium clavulanate were the strongest inhibitors of the Bacillus cereus beta-lactamase. Cis-dichloro-diammine-platinum(II) was fourfold less active than the palladium complex PD 25681 in äquimolar concentration. The following ID50 values were found: CP 45899: 0.0281 microgram; K-clavulanate: 0.1274 microgram; Pd 25681: 3.8603 microgram; cis-dichlorodiammine-platinum(II): 12.5120 microgram/100 microliter.

摘要

研究了6-甲基-吡啶-2-基-胺二氯化钯（Pd 25681）和顺式二氯二氨合铂（II）的β-内酰胺酶抑制活性，并与克拉维酸钾和青霉烷砜CP 45899的酶抑制作用进行了比较。使用硝噻吩试验方法和Titertek/微量滴定设备，CP 45899和克拉维酸钾是蜡状芽孢杆菌β-内酰胺酶的最强抑制剂。在等摩尔浓度下，顺式二氯二氨合铂（II）的活性比钯配合物PD 25681低四倍。发现以下半数抑制浓度（ID50）值：CP 45899：0.0281微克；克拉维酸钾：0.1274微克；Pd 25681：3.8603微克；顺式二氯二氨合铂（II）：12.5120微克/100微升。