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Intestinal alpha-glucosidase inhibitors and a process for the isolation and use thereof

A technology for glucosidase and inhibitory activity, which is applied in the field of α-glucosidase inhibitors and can solve problems such as application limitations

Inactive Publication Date: 2009-03-25
COUNCIL OF SCI & IND RES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Although the above-mentioned α-glucosidase inhibitors are being used in clinical practice, their use has been found to be limited due to side effects such as abdominal pain, flatulence, diarrhea in the colon (Uchida, R, Nasu, A et. al Chem ..Pharm.Bull 47, 187-193, 1999)

Method used

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  • Intestinal alpha-glucosidase inhibitors and a process for the isolation and use thereof
  • Intestinal alpha-glucosidase inhibitors and a process for the isolation and use thereof
  • Intestinal alpha-glucosidase inhibitors and a process for the isolation and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0104] Experimental protocol: Method for isolating orogenin A, chrysin and baicalin.

[0105] Dry powdered stem bark (200 g) was first defatted with gasoline in a Soxhlet extractor. After filtering the hexane extract, a light yellow powdery solid was obtained. The solid (2 g) was chromatographed on a 3.5 cm diameter column packed with 60 cm high silica gel (60-120 mesh).

[0106] The column was continuously eluted with 1% methanol in chloroform to obtain orogenin A. The yield of orogenin A was about 1.2 grams.

[0107] The column was further eluted with 2% methanol in chloroform to give chrysin. The yield of chrysin was about 0.2 grams.

[0108] The column was further eluted with 3% methanol in chloroform to give baicalein. The yield of baicalein was about 0.5 grams.

[0109] In the hexane fractions such as oreolin A, chrysin, baicalin and unidentified compound, the ratio of the three active compounds to the unidentified compound was the following ratio 60:10:25:5.0.

[0...

Embodiment 2

[0120] Example 2: Determination of intestinal α-glucosidase inhibitory activity:

[0121] Rat intestinal acetone powder (sigma chemicals, USA) in normal saline at a ratio of 100:1 (weight / volume) was suitably sonicated. The supernatant obtained after centrifugation at 3000 rpm for 30 min at 25 °C was processed into a crude source of mammalian intestinal α-glucosidase. 10 microliter samples prepared from extracts or molecules (5 mg / ml in DMSO) were incubated with 50 microliters of crude enzyme in 100 microliters of 100 mM phosphate buffer (pH 6.8) for 5 minutes. Then 50 microliters of matrix (5 mM, p-nitrophenyl α-D-glucopyranoside prepared in buffer) was added. After 5 minutes of incubation, released p-nitrophenol was read spectrophotometrically at 405 nm. For control and blank readings, 10 microliters of DMSO was added at the sample and 50 microliters of buffer at the matrix. To compensate for interference from colored compounds, prepare a separate blank sample and evaluat...

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Abstract

This invention provides a-glucosidase inhibitors isolated from Oroxylum indicum an Indian medicinal plant. Particularly, this invention provides hexane and acetone fraction of Oroxylum indicum wherein the hexane fraction comprises a-glucosidase active compounds of oroxylin A, chrysin and baicalain and acetone fraction comprises the compounds of oroxylin A, chrysin, baicalain, methoxy chrysin and oroxyloside methyl ester. This invention also relates to a process for the isolation of a-glucosidase inhibitory active compounds from the above said hexane and acetone fraction of Oroxylum indicum. This invention also provides the use of potent intestinal a-glucosidase inhibitors as active ingredients that can be used in pharmaceuticals, food products, health foods and specialized health care foods as anti hyperglycemic agent for prevention and treatment of post prandial hyperglycemia, hyperglycemia and related conditions in diabetes mellitus, obesity and disease conditions requiring hyperglycemic control as well as inhibition of a-glucosidase activity.

Description

technical field [0001] The present invention relates to an α-glucosidase inhibitor isolated from the Indian medicinal plant Oroxylum indicum. In particular, the present invention relates to the hexane and acetone moieties of Oryzae, wherein the hexane portion comprises the α-glucosidase active compounds Orizin A, Chrysin and Baicalein, and the acetone portion comprises the compounds Oryne Chrysin A, chrysin, baicalein, methoxychrysin and oroxyloside methylester. The present invention also relates to a method for isolating alpha-glucosidase inhibitory active compounds from the hexane and acetone fractions of the above-mentioned wood butterfly. [0002] The present invention also relates to the use of these potent intestinal alpha-glucosidase inhibitors as active ingredients, which can be used as antihyperglycemic agents in medicines, foods, health foods and specialized health foods to prevent and treat postprandial hyperglycemia hyperglycemia in diabetes mellitus and related ...

Claims

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Application Information

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IPC IPC(8): A61K36/185A61K31/352A61P3/04A61P3/10A61K31/70
CPCA61K36/185A61K31/352A61K31/70A61P3/04A61P3/10A61P43/00
Inventor J·M·拉奥S·B·卡穿干达A·K·蒂瓦里H·B·塔皮帕卡V·S·普莱拉P·K·索亚德瓦B·S·萨思特里A·Z·阿里J·S·亚达夫
Owner COUNCIL OF SCI & IND RES
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