【摘要】 黄连临床上用于消渴症治疗已有2千余年历史,其治疗2型糖尿病(T2D)的疗效获得实验和RCT临床研究的支持。古人应用黄连治疗糖尿病多以粉末形式如丸剂入药,前期研究表明,黄连粉末中有效成分小檗碱(BER)及药根碱(JAT)在大鼠体内药代动力学特征及降低血糖血脂药理活性较其单体化合物具有明显优势。鉴于肝脏是调节血糖浓度的主要器官,以肝细胞为研究对象,从体外探讨肝细胞对黄连粉末中有效成分BER和JAT与各单体化合物的摄取差异,将药物与肝细胞于37℃、5%CO2培养箱中培养2 h,单体化合物组及黄连粉末组BER和JAT浓度分别为10、5、1μmol·L-1及2.5、1.25、0.25μmol·L-1,肝细胞经过洗涤、灭活及提取,提取液采用HPLC测定药物含量。结果表明肝细胞对BER和JAT均有一定程度摄取,且黄连粉末中BER和JAT摄取量明显高于单一化合物,提示黄连用于治疗T2D选用粉末形态具有一定科学依据,黄连活性成分与肝细胞的特异性结合提示在研究其降糖活性时应关注其对肝脏的影响。更多还原

【Abstract】 Rhizoma coptidis has been used to treat the symptoms of diabete in clinic for 2 thousand years in history and has been confirmed for the treatment of type 2 diabetes( T2D) by the experiments and RCT clinical research in present. Rhizoma coptidis was usually applied to the treatment of diabetes in powder form such as pill by the ancients. In the early researches,berberine( BER) and jateorhizine( JAT) in Rhizoma Coptidis powder showed superior pharmacokinetic characteristics and excellent activity activity of lowering blood glucose and lipid than their pure compounds. This article comparatively studied the uptake of cells of the mice liver as an organs regulating blood glucose to berberine and jateorhizine in Rhizoma coptidis powder and their pure compounds,combined liver cells and drugs to incubate at 37 ℃ for 2 hours in 5% CO2 incubator,the BER and concentrations were 10,5,1 μmol/L and 2. 5,1. 25,0. 25 μmol/L in pure compounds and Rhizoma Coptidis powder grourps. The contents of extracting solution of liver cells after washing and inactivating were measured by HPLC. The results showed that the liver cells could absorb BER and JAT in some way,and the absorptivity of BER and JAT in Rhizoma Coptidis powder was higher than their pure compounds. It provided the scientific basis for oral application of Rhizoma Coptidis powder in the treatment of T2 D. The specific combination of liver cells and active ingredients suggested that we should focus on the effects on liver when the hypoglycemic mechanism of Rhizoma Coptidis was studied.更多还原