Effects of berberine on glucose metabolism in vitro

Effects of berberine on glucose metabolism in vitro
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DOI:
10.1053/meta.2002.34715
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发表时间:
2002-11-01
影响因子:
9.8
通讯作者:
Chen, JL
Chen, JL
中科院分区:
医学1区
文献类型:
--
作者:
Yin, J;Hu, RM;Chen, JL

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比较了小檗碱与二甲双胍、曲格列酮(TZD)的体外降糖作用。HepG2细胞系表型与人肝细胞相似,用于葡萄糖消耗(GC)研究。用甲基硫代四唑(MTT)法检测细胞增殖。在中高葡萄糖浓度(11.1 mmol/L)下,5 × 10(-6) mol/L ~ 1 × 10(-4) mol/L的小檗碱可使HepG2细胞的GC增加32% ~ 60% (P < 0.001 ~ P < 0.0001),与1 × 10(-3) mol/L的二甲双胍效果相当。小檗碱的降糖作用随着葡萄糖浓度的升高而减弱。当葡萄糖浓度为5.5 mmol/L时,其效力达到最大值,当葡萄糖浓度增加到22.2 mmol/L时,其效力消失。其降糖作用不依赖于胰岛素浓度,与二甲双胍相似,与TZD不同,其降糖作用依赖于胰岛素。添加胰岛素时,TZD的降糖作用优于二甲双胍(P < 0.001)。同时,还观察到药物对HepG2细胞有明显的毒性作用。用betaTC3细胞系进行胰岛素释放试验,未见小檗碱的促分泌作用。这些观察结果表明,小檗碱能够在肝细胞中发挥与胰岛素无关的降糖作用,类似于二甲双胍,但对胰岛素分泌没有影响。版权所有,爱思唯尔科学(美国)。版权所有。
The action of berberine was compared with metformin and troglitazone (TZD) with regard to the glucose-lowering action in vitro. HepG2 cell line, phenotypically similar to human hepatocytes, was used for glucose consumption (GC) studies. Cell proliferation was measured by methylthiotetrazole (MTT) assay. In moderate high glucose concentration (11.1 mmol/L), GC of HepG2 cells was increased by 32% to 60% (P < .001 to P < .0001) with 5 x 10(-6) mol/L to 1 X 10(-4) mol/L berberine, which was comparable to that with 1 X 10(-3) mol/L metformin. The glucose-lowering effect of berberine decreased as the glucose concentration increased. The maximal potency was reached in the presence of 5.5 mmol/L glucose, and it was abolished when the glucose concentration increased to 22.2 mmol/L. The effect was not dependent on insulin concentration, which was similar to that of metformin and was different from that of TZD, whose glucose-lowering effect is insulin dependent. TZD had a better antihyperglycemic potency than metformin when insulin was added (P < .001). In the meantime, a significant toxicity of the drug to HepG2 cells was also observed. The betaTC3 cell line was used for insulin release testing, and no secretogogue effect of berberine was observed. These observations suggest that berberine is able to exert a glucose-lowering effect in hepatocytes, which is insulin independent and similar to that of metformin, but has no effect on insulin secretion. Copyright 2002, Elsevier Science (USA). All rights reserved.