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Use of arjunolic acid in preparing glycosidase inhibitor

A technology of glycosidase inhibitor, terminalisoleic acid, which is applied in the field of natural medicinal chemistry to achieve the effects of low pollution, convenient extraction and environmental friendliness

Inactive Publication Date: 2009-04-29
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are few reports on the active lead substances and drugs that have been isolated and determined to use α-glucosidase inhibitors as the mechanism of action.

Method used

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  • Use of arjunolic acid in preparing glycosidase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Example 1 : Preparation of arjunolic acid from dried leaves of Lagerstroemia tomentosa

[0018] 1.1 Instruments and reagents

[0019] H NMR spectrum ( 1 H-NMR), carbon nuclear magnetic resonance spectrum ( 13 C-NMR) and two-dimensional nuclear magnetic resonance spectrum (2D NMR) were determined by INOVA type superconducting nuclear magnetic resonance spectrometer (VARIAN INOVA-400MHz) (tetramethylsilyl ether was internal standard); electrospray mass spectrometry (ESI-MS) was determined by Bruker Esquire 3000+ mass spectrometer, silica gel (100-200, 200-300) for column chromatography and silica gel GF254 (10-40 mesh) for thin layer chromatography were purchased from Qingdao Ocean Chemical Factory; all reagents used were of analytical grade , wherein the boiling range of petroleum ether is 60-90°C; thin plate (TLC) detection with 254nm and 365nm ultraviolet lamps; chromogen with 10% sulfuric acid-ethanol and bromocresol green solution.

[0020] 1.2 Plant source and i...

Embodiment 2

[0028] Example 2 : Preparation of arjunolic acid from fresh leaves of Lagerstroemia tomentosa

[0029] 2.1 Instruments and reagents: Same as Example 1.

[0030] 2.2 Plant source and identification: Same as Example 1.

[0031] 2.3 Extraction and separation

[0032] The sample (0.5 kg of fresh leaf weight) was immediately minced with a knife and extracted twice at room temperature with 95% ethanol for 24 hours each time. The extracts were cooled and combined, and concentrated under reduced pressure to obtain 35 grams of brown-black viscous crude extract. The crude extract was dissolved in 2 liters of hot water, degreased with petroleum ether (2 liters / time, 3 times in total), then extracted with ethyl acetate (2 liters / time, 5 times in total), and the solvent was evaporated under reduced pressure, The obtained ethyl acetate extract (8.3 grams) was mixed with 10 grams of 100-200 mesh silica gel, and was subjected to column chromatography on a silica gel column (200-300 mesh,...

Embodiment 3

[0034] Example 3 : Preparation of arjunolic acid from stems and root bark of Lagerstroemia tomentosa

[0035] 3.1 Instruments and reagents: Same as Example 1.

[0036] 3.2 Plant source and identification: Same as Example 1.

[0037] 3.3 Extraction and separation

[0038] The sample (0.5 kg dry weight of stems, branches and root bark) was pulverized and extracted twice at room temperature with 95% ethanol for 24 hours each time. things. The crude extract was dissolved in 2 liters of hot water, degreased with petroleum ether (2 liters / time, 3 times in total), then extracted with ethyl acetate (2 liters / time, 5 times in total), and the solvent was evaporated under reduced pressure, The obtained ethyl acetate extract (9.6 grams) was mixed with 10 grams of 100-200 mesh silica gel, and was subjected to column chromatography on a silica gel column (200-300 mesh, 150 grams), and was mixed with petroleum ether-acetone (100:0-0: 100) is the gradient elution of the eluent, and ever...

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Abstract

The invention provides the application of arjunolic acid or salts thereof suitable for medical purpose in the preparation of a drug of an Alpha-glucosidase inhibitor. The invention is characterized in that strong effective Alpha-glucosidase inhibitor is extracted and separated from lagerstroemia plants which has rich source, are easy to be extracted and can be recycled for a plurality of times, thus not only promoting economic benefit, but also being environment-friendly. Furthermore, the monomeric compound product of the Alpha-glucosidase inhibitor is stable and is convenient to be stored. Pharmacological tests prove that the arjunolic acid has powerful effect in inhibiting Alpha-glucosidase, wherein, physiological change or diseases caused by or related to the Alpha-glucosidase includes but is not limited to Type II Diabetes. The monomeric compound product of the Alpha-glucosidase inhibitor can be further developed into the drugs for clinically treating NIDDM, thereby having better prospect for marketization. The constitutional formula of compound of the arjunolic acid is shown as above.

Description

technical field [0001] The present invention relates to the field of natural medicine chemistry, in particular, the present invention relates to the pharmaceutical use of arjunolic acid, a pentacyclic triterpene acid compound isolated from Lagerstroemia genus, for the preparation of glycosidase inhibitor drugs. This compound, namely 2α, 3β, 23-trihydroxy-olean-12-ene-28-acid has the biological activity of potently inhibiting α-glucosidase, so this compound or its pharmaceutically acceptable salt, and The pharmaceutical composition prepared from the pharmaceutical excipients or carriers allowed by the formulation can be expected to be used as a glycosidase inhibitor drug, especially a drug for preventing and treating type II diabetes, that is, non-insulin-dependent diabetes. Background technique [0002] Diabetes is a common clinical endocrine and metabolic disease. With the advancement of science and technology and the improvement of living standards, the incidence of diabe...

Claims

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Application Information

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IPC IPC(8): A61K31/56A61K36/185A61P3/10
Inventor 张荣平窦辉郑汉其贾婕周长新赵昱约阿施·史托克希特巫秀美曾苏郝小江
Owner ZHEJIANG UNIV
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