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

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Problems solved by technology

However, there are few reports on the active lead substances and drugs that have bee

Method used

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  • Use of arjunolic acid in preparing glycosidase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0017] Example 1 :Preparation of arjunolic acid in dried leaves of Lagerstroemia indica

[0018] 1.1 Instruments and reagents

[0019] Proton Nuclear Magnetic Resonance Spectroscopy ( 1 H-NMR), carbon nuclear magnetic resonance spectroscopy ( 13 C-NMR) and two-dimensional nuclear magnetic resonance spectroscopy (2D NMR) are measured by INOVA superconducting nuclear magnetic resonance spectrometer (VARIAN INOVA-400MHz) (tetramethylsilyl ether is the internal standard); electrospray mass spectrometry (ESI-MS) is determined by Measured by Bruker Esquire 3000+ mass spectrometer, silica gel for column chromatography (100-200, 200-300) and silica gel GF254 (10-40 mesh) for thin layer chromatography were purchased from Qingdao Ocean Chemical Factory; all reagents used were analytical pure , The boiling range of petroleum ether is 60-90°C; the ultraviolet lamp of 254nm and 365nm is used for thin plate (TLC) detection; the developer uses 10% sulfuric acid-ethanol and bromocresol green so...

Example Embodiment

[0028] Example 2 :Preparation of arjunolic acid in fresh leaves of Lagerstroemia indica

[0029] 2.1 Apparatus and reagents: same as in Example 1.

[0030] 2.2 Plant source and identification: the same as in Example 1.

[0031] 2.3 Extraction and separation

[0032] The samples (fresh leaves weighing 0.5 kg) were chopped immediately with a knife and extracted twice with 95% ethanol at room temperature for 24 hours each time. After cooling, the extracts were combined and concentrated under reduced pressure to obtain 35 grams of brownish black viscous Like crude extract. The crude extract was dissolved in 2 liters of hot water, petroleum ether was defatted (2 liters / each, 3 times in total), then extracted with ethyl acetate (2 liters / each, 5 times in total), and the solvent was evaporated under reduced pressure. The obtained ethyl acetate extract (8.3 g) was mixed with 10 g of 100-200 mesh silica gel, and was chromatographed on a silica gel column (200-300 mesh, 150 g), and then p...

Example Embodiment

[0034] Example 3 :Preparation of arjunolic acid in the stems, branches and root bark of Lagerstroemia indica

[0035] 3.1 Instruments and reagents: the same as in Example 1.

[0036] 3.2 Plant origin and identification: the same as in Example 1.

[0037] 3.3 Extraction and separation

[0038] The sample (dry weight of stems, branches and root bark 0.5 kg) was crushed and extracted twice with 95% ethanol at room temperature for 24 hours each time. After cooling, the extracts were combined and concentrated under reduced pressure to obtain 43 grams of brown viscous crude extract. Things. The crude extract was dissolved in 2 liters of hot water, petroleum ether was defatted (2 liters / each, 3 times in total), then extracted with ethyl acetate (2 liters / each, 5 times in total), and the solvent was evaporated under reduced pressure. The obtained ethyl acetate extract (9.6 g) was mixed with 10 g of 100-200 mesh silica gel, and was chromatographed on a silica gel column (200-300 mesh, 15...

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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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