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目的测定黄连中的3种生物碱小檗碱、药根碱、巴马汀对痢疾杆菌生长代谢的影响,从热力学角度研究小檗碱类生物碱抑菌作用的量效关系。方法以微量热法测定小檗碱类生物碱作用于痢疾杆菌生长代谢的热谱曲线,并得出相应的热动力学参数,如生长速率常数、产热功率、最大热功率出现时间、抑制率、传代时间等,根据热动力学模型,拟合了3种生物碱产热功率-质量浓度关系,并进行初步的量效关系分析。结果小檗碱、药根碱、巴马汀对痢疾杆菌的生长代谢均有不同程度的抑制作用,在0.08～1.20 mg/mL内随着质量浓度的增加,最大热功率出现时间和传代时间延长,生长速率常数降低和最大产热功率降低,抑制率增加,且与药物质量浓度呈现一定的量效关系。结论 3种生物碱对痢疾杆菌的抑菌活性的强度顺序为小檗碱>巴马汀>药根碱,从热力学角度研究抑菌类中药的量效关系具有定量、灵敏、快速等优势。
OBJECTIVE To determine the effects of berberine, jatrorrhizine and palmatine on the growth and metabolism of dysentery bacilli in berberine, and to study the relationship between the inhibitory effects of berberine alkaloids and the bacteriostasis in thermodynamics. Methods The thermogram of berberine alkaloids acting on the growth and metabolism of Shigella dysenteriae was determined by microcalorimetry and the corresponding thermokinetic parameters such as growth rate constant, calorific power, time of maximum heat power and inhibition rate , The passage time, etc. According to the thermokinetic model, the relationship between the thermogenic power and mass concentration of three alkaloids was fitted and the preliminary quantitative-effective relationship analysis was carried out. Results Berberine, jatrorrhizine and palmatine all inhibited the growth and metabolism of Shigella dysenteriae to varying degrees. With the increase of mass concentration, the maximum heating power appeared and the passage time prolonged in 0.08-1.20 mg / mL , The decrease of growth rate constant and the decrease of maximum heat-producing power, the increase of inhibition rate, and the dose-effect relationship with the drug concentration. Conclusion The order of intensity of antibacterial activity of three alkaloids to Shigella dysenteriae is berberine> palmatine> jatrorrhizine. To study the dose-effect relationship of antibacterial traditional Chinese medicine is quantitative, sensitive and rapid from thermodynamic point of view.