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Insulin releasing and alpha-glucosidase inhibitory activity of ethyl acetate fraction of Acorus calamus in vitro and in vivo
Authors:Mei-mei Si  Jian-shu Lou  Chang-Xin Zhou  Juan-Na Shen  Hong-Hai Wu  Bo Yang  Qiao-Jun He  Hao-Shu Wu
Institution:1. Institute of Pharmacology & Toxicology and Biochemical Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, 388 Yu-hang-tang Road, Hangzhou, China;2. Department of Traditional Chinese Medicine and Natural Drug Research, College of Pharmaceutical Science, Zhejiang University, Hangzhou, China
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 2 g/kg glucose loading in normal mice. In addition, ACE as a mixed-type inhibitor inhibited alpha-glucosidase activity in vitro with an IC50 of 0.41 μg/ml, and 100 mg/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.
Keywords:AC  Acorus calamus L    ACB  n-butanol fraction of AC  ACE  ethyl acetate fraction of AC  ACP  petroleum ether fraction of AC  ACW  water fraction of AC  CMC-Na  sodium carboxymethyl cellulose  DMSO  dimethyl sulfoxide  PNPG  p-nitrophenyl-β-d-galactopyranoside
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