目的:探讨黄连有效成分及其组合物对荷糖小鼠胰岛素和胰高血糖素样肽1(GLP-1)分泌的影响。方法:制备黄连粉末模拟胃液溶出物并检测其中盐酸小檗碱(BER)、黄连碱(COP)、盐酸药根碱(JAT)、阿魏酸(FA)、盐酸巴马丁(BM)含量,结合BER治疗2型糖尿病(T2D)有效剂量确立其他成分剂量,组合物剂量为5种化合物剂量的1/10倍量。对照组灌服葡萄糖(2 g·kg-1),药物组灌服等剂量葡萄糖及不同药物。各组分别在灌服的前1 h及灌服1 h时眼眶静脉采血、灌服1.5 h时摘眼球采血,分离血清,采用酶联免疫吸附法(ELISA)检测血清中的GLP-1和胰岛素含量。结果:BER、COP、JAT、组合物及黄连粉末均能在1,1.5 h升高荷糖小鼠血清胰岛素浓度,与对照组比较,P〈0.05;BER、组合物及黄连粉均能在1,1.5 h升高荷糖小鼠血清GLP-1浓度,即促进GLP-1分泌;药物组其他成分呈现一定升高GLP-1水平作用趋势,但统计学差异不显著。结论:黄连及其部分活性成分能有效刺激小鼠GLP-1及胰岛素分泌,且低剂量组合物作用活性高于高剂量单个活性成分活性,黄连刺激肠道GLP-1分泌作用是其治疗T2D机制之一。
OBJECTIVE To investigate the secreting effects of Rhizoma Coptidis active ingredients and their combinations on insulin and glucagon-like peptide1(GLP-1)in glucose feeding mice.METHODS Rhizoma Coptidis powder was extracted with simulated gastric juice,and the ingredients in the extract such as berberine hydrochloride(BBR),coptisine(COP),jatrorrhizine hydrochloride(JAT),ferulic acid(FA),palmatine hydrochloride(PM),were detected.The doses of other ingredients were established based on BBR effective dose against type 2 diabetes(T2D),and the combination dose was 1/10 times the dose of 5 ingredients.The control group was orally administered glucose(2 g·kg-1),and the drug groups were administered equivalent glucose and different drugs.Blood was collected from orbital vein one hour before and after intragastric gavage,respectively,and 1.5 hours after gavage by picking eye balls.Serum was isolated from the plasma samples.The level of serum GLP-1 and insulin were measured respectively by using enzyme-linked immunosorbent assay(ELISA).RESULTS BER,COP,JAT,combination and Rhizoma Coptidis increased the serum insulin concentrations in glucose-bearing mice.BER,combination and Rhizoma Coptidis increased serum GLP-1 level 1 and 1.5 hours after gavage,compared with control group(P0.05).The other ingredients in drug group showed a trend of increasing GLP-1level,but without significant difference.CONCLUSION Rhizoma Coptidis and and parts of the active ingredients can effectively stimulate secretions of GLP-1 and insulin in mice.The activity of combination at low dose is higher than that of a single ingredient at high dose.The activity of stimulating intestinal secretion of GLP-1 is one of the mechanism of Rhizoma coptidisin to treat T2 D.