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菖蒲乙酸乙酯部位的体外和体内胰岛素释放及α-葡萄糖苷酶抑制活性。

Insulin releasing and alpha-glucosidase inhibitory activity of ethyl acetate fraction of Acorus calamus in vitro and in vivo.

机构信息

Institute of Pharmacology & Toxicology and Biochemical Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, 388 Yu-hang-tang Road, Hangzhou, China.

出版信息

J Ethnopharmacol. 2010 Mar 2;128(1):154-9. doi: 10.1016/j.jep.2009.12.044. Epub 2010 Jan 4.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

The radix of Acorus calamus L. (AC) is widely used in the therapy of diabetes in traditional folk medicine of America and Indonesia, and we previously reported the insulin sensitizing activity of the ethyl acetate fraction of AC (ACE).

AIM OF THE STUDY

To investigate the insulin releasing and alpha-glucosidase inhibitory activity of ACE in vitro and in vivo.

MATERIALS AND METHODS

Insulin releasing and alpha-glucosidase inhibitory effects of different fractions from AC were detected in vitro using HIT-T15 cell line and alpha-glucosidase enzyme. Furthermore, effects of ACE orally on serum glucose were detected in fasted and glucose/amylum challenged normal mice.

RESULTS

AC and ACE increased insulin secretion in HIT-T15 cells as gliclazide did. As in vivo results, ACE (400 and 800 mg/kg) significantly decreased fasting serum glucose, and suppressed the increase of blood glucose levels after 2g/kg glucose loading in normal mice. In addition, ACE as a mixed-type inhibitor inhibited alpha-glucosidase activity in vitro with an IC(50) of 0.41 microg/ml, and 100mg/kg of it clearly reduced the increase of blood glucose levels after 5 g/kg amylum loading in normal mice.

CONCLUSIONS

Apart from its insulin sensitizing effect, ACE may have hypoglycemic effects via mechanisms of insulin releasing and alpha-glucosidase inhibition, and thus improves postprandial hyperglycemia and cardiovascular complications.

摘要

民族药理学相关性

菖蒲根茎(AC)被广泛用于美国和印度尼西亚传统民间医学中的糖尿病治疗,我们之前曾报道过 AC 的乙酸乙酯部分(ACE)具有胰岛素增敏活性。

研究目的

研究 ACE 在体外和体内的胰岛素释放和α-葡萄糖苷酶抑制活性。

材料和方法

使用 HIT-T15 细胞系和α-葡萄糖苷酶酶在体外检测 AC 的不同部分的胰岛素释放和α-葡萄糖苷酶抑制作用。此外,在禁食和葡萄糖/淀粉挑战的正常小鼠中,口服 ACE 对血清葡萄糖的影响。

结果

AC 和 ACE 像格列齐特一样增加了 HIT-T15 细胞中的胰岛素分泌。作为体内结果,ACE(400 和 800mg/kg)显著降低了空腹血清葡萄糖水平,并抑制了正常小鼠 2g/kg 葡萄糖负荷后血糖水平的升高。此外,ACE 作为一种混合类型抑制剂,在体外以 0.41μg/ml 的 IC50 抑制α-葡萄糖苷酶活性,100mg/kg 的 ACE 明显降低了正常小鼠 5g/kg 淀粉负荷后血糖水平的升高。

结论

除了其胰岛素增敏作用外,ACE 还可能通过胰岛素释放和α-葡萄糖苷酶抑制机制发挥降血糖作用,从而改善餐后高血糖和心血管并发症。

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