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本文探讨了阿勒泰黄芪不同提取物对蛋白酪氨酸磷酸酯酶1B(PTP1B)的抑制作用。采用分光光度法测定了提取物中的黄酮和皂苷含量;通过体外酶促动力学方法检测了不同提取物对PTP1B的影响,并确定了抑制类型;并采用氧化酶法检测了阿勒泰黄芪提取物对细胞利用葡萄糖能力的作用。结果表明,阿勒泰黄芪8种提取物(E1～8)中黄酮含量分别为5.09、10.46、3.58、3.23、53.91、21.77、5.76和7.49 mg/mL,其中E1、E2、E6、E7、E8皂苷含量分别为16.53、27.45、21.90、10.21和8.96 mg/mL;各提取物对PTP1B活性均表现出抑制作用,其中E1、E2、E7、E8的IC50分别为34.8、4.7、7.35和7.15μg/mL,E1、E7和E8是竞争性抑制,E2是混合型竞争性抑制。E1、E2、E5、E7和E8较明显的提高了CHO-K1细胞对葡萄糖的利用。提示皂苷可能是阿勒泰黄芪抑制PTP1B活性的主要物质,通过PTP1B途径有效了提高细胞利用葡萄糖的能力。本研究为阿勒泰黄芪开发为防治糖尿病及改善胰岛素抵抗的药物或保健品提供实验依据。
This article explores the different inhibitory effects of Altay Astragalus extract on protein tyrosine phosphatase 1B (PTP1B). The contents of flavonoids and saponins in the extracts were determined by spectrophotometry. The effects of different extracts on PTP1B were tested by in vitro enzymatic kinetics and the type of inhibition was determined. Oxidase method was used to detect the effects of Altay astragalus extract Cells use the power of glucose. The results showed that the contents of flavonoids in the eight kinds of extracts of Altay Astragalus (E1 ~ 8) were 5.09,10.46,3.58,3.23,53.91,21.77,5.76 and 7.49 mg / mL, respectively, of which E1, E2, E6, E7 and E8 16.53, 27.45, 21.90, 10.21 and 8.96 mg / mL, respectively. All the extracts showed inhibitory activity on PTP1B activity. The IC50 of E1, E2, E7 and E8 were 34.8, 4.7, 7.35 and 7.15 μg / E1, E7 and E8 are competitive inhibitors and E2 is mixed competitive inhibitor. E1, E2, E5, E7 and E8 significantly increased glucose utilization in CHO-K1 cells. Suggesting that saponins Altay may Astragalus PTP1B inhibit the activity of the main substances through the PTP1B pathway effectively improve the ability of cells to use glucose. This study provides the experimental basis for the development of Altay astragalus for the prevention and treatment of diabetes and insulin resistance drugs or health products.