Use of betulinic acid in preparing glycosidase inhibitor medicine

The technology of a glycosidase inhibitor, betulinic acid, is applied in the field of natural medicinal chemistry to achieve the effects of simple preparation process, improved economic efficiency 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 betulinic acid in preparing glycosidase inhibitor medicine
  • Use of betulinic acid in preparing glycosidase inhibitor medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Example 1 : Preparation of betulinic acid from dry leaves of Lagerstroemia tomentosa

[0019] 1.1 Instruments and reagents

[0020] H NMR spectrum ( 1 H-NMR), carbon nuclear magnetic resonance spectrum ( 13 C-NMR) and two-dimensional nuclear magnetic resonance spectrum (2D NMR) were measured by INOVA type superconducting nuclear magnetic resonance spectrometer (VARIANINOVA-400MHz) (tetramethylsilyl ether as 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 analytically pure, The boiling range of petroleum ether is 60-90° C.; the thin plate (TLC) detection uses 254nm and 365nm ultraviolet lamps; the color developer uses 10% sulfuric acid-ethanol and bromocresol green solution.

[0021] 1.2 Plant source and id...

Embodiment 2

[0029] Example 2 : Preparation of betulinic acid from fresh leaves of Lagerstroemia tomentosa

[0030] 2.1 Instruments and reagents: Same as Example 1.

[0031] 2.2 Plant source and identification: Same as Example 1.

[0032] 2.3 Extraction and separation

[0033] The sample (fresh leaves of Lagerstroemia tomentosa, weighing 0.5 kg) 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. Dissolve the crude extract in 2 liters of hot water, extract with petroleum ether (2 liters / time, 3 times in total), evaporate the solvent under reduced pressure, and use 10 grams of 100-200 mesh silica gel to obtain the petroleum ether extract (10.1 grams) Mix the sample, and use a silica gel column (200-300 mesh, 150 g) for column chromatography, and use petroleum ether-ethyl acetate (100:0-0:...

Embodiment 3

[0035] Example 3 : Preparation of betulinic acid (betulinic acid) in crape myrtle tomentosa stems and root bark

[0036] 3.1 Instruments and reagents: Same as Example 1.

[0037] 3.2 Plant source and identification: Same as Example 1.

[0038] 3.3 Extraction and separation

[0039] The sample (crape myrtle tomentosa stems and root bark, dry weight 0.5 kg) was pulverized 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 43 grams of brown viscous crude extract. Dissolve the crude extract in 2 liters of hot water, extract with petroleum ether (2 liters / time, 3 times in total), evaporate the solvent under reduced pressure, and use 10 grams of 100-200 mesh silica gel to obtain the petroleum ether extract (12.2 grams) Mix the sample, and use a silica gel column (200-300 mesh, 150 g) for column chromatography, and use petroleum ether-ethyl acetate (100:0-0:100)...

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PUM

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Abstract

The invention provides the application of betulinic acid and salts thereof suitable for medical purpose in the preparation of a drug of a glycosidase inhibitor. The compound of the invention is the compound of lupeol type pentacyclic triterpene acid obtained by separating lagerstroemia plants. Pharmacological tests prove that the compound has obvious effect in inhibiting Alpha-glucosidase, the inhibitory activity of which exceeds acarbose 100% for initial therapy. Therefore, drug compositions made from the compound or the salts thereof suitable for medical purpose and drug excipients or carriers allowable for preparation can be applied to the preparation of drugs for preventing or treating Type II Diabetes, namely, noninsulin-dependent diabetes mellitus. The constitutional formula shown in formula (1) of the invention is shown as above.

Description

technical field [0001] The present invention relates to the field of natural medicinal chemistry, in particular, the present invention relates to the use of betulinic acid, a pentacyclic triterpene acid compound isolated from Lagerstroemia genus, for the preparation of glycosidase inhibitor drugs. The compound has the biological activity of potently inhibiting α-glucosidase, so the compound or its pharmaceutically acceptable salt, and the pharmaceutical composition prepared with the pharmaceutical excipient or carrier allowed by the formulation can be expected to be used as a glucosidase inhibitor The medicine is especially used for preventing and treating type II diabetes, that is, non-insulin-dependent diabetes mellitus. Background technique [0002] With the advancement of science and technology and the improvement of living standards, the incidence of diabetes is increasing worldwide. According to statistics, diabetes occurs in about 3% of people, and the total number o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/56A61K36/185A61P3/10
Inventor 郑汉其窦辉张荣平娄旭董晓武赵昱约阿施·史托克希特郝小江曾苏
Owner ZHEJIANG UNIV
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