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首页> 外文期刊>Biophysical Chemistry: An International Journal Devoted to the Physical Chemistry of Biological Phenomena >Calculation of concentrations of equilibrium components in an in vitro activity test of vancomycin antibiotics and the possible mode of action.
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Calculation of concentrations of equilibrium components in an in vitro activity test of vancomycin antibiotics and the possible mode of action.

机译：万古霉素体外活性试验中平衡成分浓度的计算以及可能的作用方式。

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摘要

The vancomycin group of antibiotics is considered to act by binding the bacterial cell wall mucopeptide precursor terminating in -L-Lys-D-Ala-D-Ala. The dimerization of these antibiotics is also believed to play a role in the action. In this paper, we analyzed the equilibria in the in vitro antibacterial activity test of the vancomycin antibiotics both with and without the cell wall precursor analogue di-acetyl-L-Lys-D-Ala-D-Ala (DALAA). Based on the equilibria and concentration balance, we obtained 10 equations (seven quadratic equations and three linear equations) containing 10 equilibrium concentrations which relate to the antibiotic, cell wall precursor and DALAA. A computer program was written to solve these equations from known dimerization constant and the binding constants (both monomer and dimer) with DALAA of the antibiotic. The concentrations in the test for vancomycin and eremomycin were obtained. The antibiotic activity of these antibiotics may be quantitatively correlated with their dimerization constants and the binding constants through the calculation. By analyzing the calculated results, we concluded that the cell wall-bound dimer may be the major contributor to the antibiotic activity in the case of eremomycin, while the cell wall-bound monomer is possibly the determinant for the activity of vancomycin.
机译：万古霉素类抗生素被认为通过结合终止于-L-Lys-D-Ala-D-Ala的细菌细胞壁粘肽前体起作用。这些抗生素的二聚作用也被认为在该作用中起作用。在本文中，我们分析了万古霉素抗生素在有或没有细胞壁前体类似物二乙酰基-L-Lys-D-Ala-D-Ala（DALAA）的体外抗菌活性测试中的平衡性。基于平衡和浓度平衡，我们获得了10个方程（七个二次方程和三个线性方程），其中包含10个与抗生素，细胞壁前体和DALAA有关的平衡浓度。编写了一个计算机程序，从已知的二聚化常数和与抗生素的DALAA的结合常数（单体和二聚体）求解这些方程。获得测试中万古霉素和埃雷霉素的浓度。这些抗生素的抗生素活性可以通过计算与它们的二聚化常数和结合常数定量相关。通过分析计算结果，我们得出结论，在埃雷霉素的情况下，细胞壁结合的二聚体可能是抗生素活性的主要贡献者，而细胞壁结合的单体可能是万古霉素活性的决定因素。

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