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  • 1 China Military Institute of Chinese Materia Medica, 302 Military Hospital of China, 100 West 4th Ring Middle Road, Beijing 100039, People's Republic of China
  • | 2 Pharmacy College, Hunan University of TCM, Changsha 410208, People's Republic of China
  • | 3 Pharmacy College, Jiangxi University of TCM, Nanchang 330 004, People's Republic of China
  • | 4 Pharmacy College, Chengdu University of TCM, Chengdu 610075, People's Republic of China
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Abstract

Using microcalorimetry, the characteristic metabolic heat flow power-time curves of S. aureus growth affected by Ursodesoxycholic acid and Hyodeoxycholic acid were measured at 37 °C. The thermal-kinetic parameters such as, growth rate constant k, the maximum power output (Pm), the time corresponding to the maximum power output (tp), total heat-production Qt, half inhibitory concentration of the drugs (IC50) were calculated from the growth curves. For both HDCA and UDCA, with the increasing of concentration, k, Pm, and Qt decreased, meanwhile, kc fit a linear equation, tp was prolonged correspondingly. Principle component analysis, the results indicated tp might be the main parameter in evaluating the antibacterial activity of HDCA and UDCA in microcalorimetric method. Combining with tp and IC50, the results revealed that the differences and trends of antibacterial activity of these bile acid derivatives were: HDCA > UDCA. Structure-activity relationship (SAR) analysis showed that the α-OH at C-3 and C-6 position at equal pace on the steroid nucleus enhanced the hydrophilicity of HDCA, which led to a stronger antibacterial effect than UDCA. In this study, a useful tool was provided to accurately evaluate the antibacterial effects of bile acid derivatives. The thermolysis curve recorded by microcalorimetry could provide a lot of kinetic and thermodynamic information for the study of growth process of living microbial, which could be helpful in the screening of high efficacy antibacterial agents.

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