Fu-Lu Pan, Yan-Hua J I, Guo-Hua Y U, Qian Wang, Yan-Li Pan, Yang Liu
School of Chinese Materia Medica, Beijing University of Chinese Medicine Beijing 102488, China.
School of Life Sciences, Beijing University of Chinese Medicine Beijing 102488, China.
Zhongguo Zhong Yao Za Zhi. 2020 Sep;45(18):4472-4481. doi: 10.19540/j.cnki.cjcmm.20200729.201.
The combination index(CI) method was used to evaluate the combination inhibition mechanism of epicatechin gallate(ECG) and other tea polyphenols [epigallocatechin gallate(EGCG) and gallocatechin gallate(GCG)] on α-glucosidase. Herein, using ECG as research object, the surface plasmon resonance(SPR) analysis were employed to study the binding affinities and kinetic parameters of three tea polyphenols components on α-glucosidase, respectively. The concentration-time curve mathematical model of the drug in the unstirred water layer(the adjacent region of α-glucosidase) established previously by our group was used to evaluate the concentration-time curves of the tea polyphenols in the α-glucosidase vicinity. The prediction model of drug-α-glucosidase binding kinetics established by our group was used to evaluate the dynamic process of drug-α-glucosidase binding kinetics of different oral administration processes of ECG. Using acarbose as a reference, the accuracy of the model prediction was judged based on the difference between the prediction results and the actual clinical performance. Using the mathematical model of drug-α-glucosidase interaction, the drug-α-glucosidase binding kinetic characteristic curves of ECG in different administration processes were obtained, which indirectly proved that the synergistic effect of multi-component combination of traditional Chinese medicine and the clinical characteristics of repeat administration were scientific and reasonable.
采用组合指数（CI）法评估表没食子儿茶素没食子酸酯（ECG）与其他茶多酚[表没食子儿茶素没食子酸酯（EGCG）和没食子儿茶素没食子酸酯（GCG）]对α-葡萄糖苷酶的联合抑制机制。在此，以ECG为研究对象，采用表面等离子体共振（SPR）分析分别研究三种茶多酚成分与α-葡萄糖苷酶的结合亲和力和动力学参数。利用本课题组前期建立的药物在未搅拌水层（α-葡萄糖苷酶相邻区域）的浓度-时间曲线数学模型，评估茶多酚在α-葡萄糖苷酶附近的浓度-时间曲线。利用本课题组建立的药物-α-葡萄糖苷酶结合动力学预测模型，评估ECG不同给药过程中药物-α-葡萄糖苷酶结合动力学的动态过程。以阿卡波糖为对照，根据预测结果与实际临床疗效的差异判断模型预测的准确性。利用药物-α-葡萄糖苷酶相互作用数学模型，得到ECG在不同给药过程中的药物-α-葡萄糖苷酶结合动力学特征曲线，间接证明了中药多成分组合的协同效应及重复给药的临床特点具有科学性和合理性。
