三黄方及其单味药药效物质基础的血清药物化学研究

Study on Effective Substances of San Huang preparation and Its Single Herbs by Serum Pharmacochemistry

目的:研究三黄方抗内毒素及黄连炮制品改善胰岛素抵抗的药效物质基础。方法:分别采用体外抗内毒素活性实验和3T3-L1前脂肪细胞胰岛素抵抗模型试验,以及HPLC血清指纹图谱等血清药物化学研究方法。结果:(1)三黄方中大黄素、大黄酚、大黄酸、4-(4′-羟基苯基)-2-丁酮-4′-O-β-D-(6″-O-没食子酰基)-吡喃葡萄糖苷、10,10′-双6-羟基芦荟大黄素、小檗碱和黄芩苷为体内入血成分,并与体外抗内毒素活性相关。(2)黄连炮制品中非洲防己碱、表小檗碱和小檗碱为体内入血成分,并与体外改善胰岛素抵抗活性相关。结论:大黄中的大黄素、大黄酚等5种成分,黄芩中的黄芩苷,黄连中的小檗碱等可能是三黄方抗内毒素的药效物质基础;非洲防己碱、表小檗碱和小檗碱可能是黄连炮制品改善胰岛素抵抗活性的药效物质基础。

This work aimed to study the effective substances of San Huang preparation＇s antiendotoxin and the processed products of eoptidis chinensis in improving insulin resistance. The antiendotoxin activity experiments in vitro were carried out, the 3T3-L1 preadipocytes cell model of insulin resistance was established, and serum pharmaco- chemistry methods were adopted. Emodin, chrysophanol, rhein, 4-（4＇-hydroxyphenyl）-2-butanone-4＇-O-β-D-（6″- O-galloyl）-glucopyranoside, 10,10＇-double 6-hydroxy aloe-emodin, berberine and baicalin migrating to the blood were detected and determined to be associated with the activity of anti-endotoxin in vitro. Palmatine, epiberberine, berberine of processed products of coptidis migrating to the blood were detected and determined to be associated with the activity of improving insulin resistance in vitro. The results show that rhubarb, emodin, chrysophanol, baicalin of scutellaria, berberine of coptis, etc. may be the effective substances of San Huang preparation; palmatine, epiberberine and berberine may be the effective substances of the processed products of coptidis chinensis in improving insulin resistance.