PMID: 16646298May 2, 2006Paper

Benzylpenicillin as an allosteric effector

Wiadomości lekarskie : organ Polskiego Towarzystwa Lekarskiego
Przemysław Zdziarski

Abstract

Benzylpenicillin (penicillin G) is a model drug for studies of drug-protein biochemical interactions. Furthermore the literature indicates that benzylpenicillin and protein conjugation is a universal phenomenon: benzylpenicillin is known to readily conjugate to proteins-serum albumin, globulin and others peptides to modify space structure and electrophoretical properties. The aim of the study was to test if the benzylpenicillin is an allosteric effector. Serum benzylpenicillin concentration in geometric progression was used. Then acid phosphatase (AcP), alanine aminotransferase (AIAT) activity and international normalized ratio (INR) was tested. Although benzylpenicillin influences AcP and INR, only AcP activity is directly proportional to the benzylpenicillin concentration (Pc): change of AcP activity was the derivative of Pc in 76% (R2 = 0.7635). Furthermore, the benzylpenicillin appears to be uncompetitive inhibitor of acid phosphatase (inhibitory constant Ki = 95.67M; Vmax = 34.843 nKat). On the contrary no effect of AIAT activity was observed. Unexpectedly INR was modified in irregular manner: in some concentrations of benzylpenicillin INR was over 25% lower than in control probe (INR approximately 0.6 vs. 0.82). Unfortuna...Continue Reading

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