论文部分内容阅读
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。
Coptis clinical clinically used for the treatment of diabetes more than 2,000 years of history, its treatment of type 2 diabetes (T2D) efficacy trials and RCT clinical research support. The ancient application of berberine treatment of diabetes and more in the form of powder pills such as pills, preliminary studies have shown that berberine (Berberine Berberine) and jatrorrhizine (JAT) in rats pharmacokinetic characteristics and reduce blood glucose and lipid pharmacological activity Compared with its monomeric compounds has obvious advantages. In view of the fact that the liver is the main organ that regulates blood glucose concentration, the liver cells were used as the research object to investigate the uptake of BER and JAT from the liver cells by the hepatocytes in vitro. The drug and hepatocytes were incubated at 37 ℃, 5 % CO2 incubator for 2 h, the monomer compound and berberine powder BER and JAT concentrations were 10,5,1 μmol·L-1 and 2.5,1.25,0.25 μmol·L-1, after washing the liver cells off Live and extraction, extraction liquid HPLC determination of drug content. The results showed that the liver cells had a certain degree of uptake of BER and JAT, and the uptake of berberine and JAT in the berberine powder was significantly higher than that of a single compound, suggesting that rhizoma coptidis could be used as a scientific basis for the treatment of T2D powder. Specific binding tips in the study of its hypoglycemic activity should pay attention to its impact on the liver.