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New usage of eucommia ulmoides chemical composition as vessel protective agent

A vascular protective agent and application technology, applied in the new application field of Eucommia ulmoides chemical constituents as vascular protective agent

Inactive Publication Date: 2011-02-16
TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] There is nothing in the prior art about Eucommia ulmoides especially its extracts, more particularly its monomeric chemical constituents having effects such as vasoprotective and / or hypotensive etc.

Method used

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  • New usage of eucommia ulmoides chemical composition as vessel protective agent
  • New usage of eucommia ulmoides chemical composition as vessel protective agent
  • New usage of eucommia ulmoides chemical composition as vessel protective agent

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075] Embodiment 1: Preparation of 5 compounds in Eucommia ulmoides

[0076] Get 31.5Kg of eucommia medicinal material (purchased from Henan Xinyang Pharmaceutical Co., Ltd.), extract twice with 95% ethanol, once with 60% ethanol, combine the extracts, concentrate to no alcohol smell, disperse in water, and use petroleum ether, chloroform, Ethyl acetate and n-butanol extraction, the four solvent extracts were recovered solvent to obtain solids. The results are as follows: Eucommia ulmoides petroleum ether extract 153g, Eucommia chloroform extract 384g, Eucommia ethyl acetate extract 126g, Eucommia n-butanol extract 520g. Among them, the n-butanol extraction part of Eucommia adopts D101 macroporous adsorption resin column chromatography, and obtains 140g and 50g after gradient elution with 30% and 50% ethanol water systems respectively.

[0077] The separation and purification process of Eucommia ethanol extract and chloroform extraction part: 350 g of Eucommia chloroform e...

Embodiment 2

[0080] Example 2: Confirmation of the structures of 5 compounds in Eucommia ulmoides

[0081] The structures of the 5 compounds obtained in Example 1 were confirmed (entrusted to Tianjin University Analysis and Testing Center for detection, 500MHz NMR). The analysis results showed that the structures of these compounds were consistent with those reported in the literature, as follows.

[0082] Geniposide (EUB30-1), white powder: 1 HNMR (DMSO-d 6 , 400MHz): δ7.47(1H, s, H-3), 5.68(1H, s, H-7), 5.12(1H, d, J=6.8Hz, H-1), 4.53(1H, d, J=7.6Hz, H-1'), 4.14(1H, br d, J=14.4Hz, H-10a), 3.97(1H, br d, J=14.4Hz, H-10b), 3.66(3H, s ,-OCH 3), 3.15 (1H, m, H-5), 2.70 (1H, m, H-6a), 2.64 (1H, m, H-9), 2.05 (1H, br d, J=14.4Hz, H-6b ).

[0083] Wogonin (EUC-4), yellow needle crystals; 1 HNMR (DMSO-d 6 , 500MHz): δ12.50(s), 8.05(2H, m, H-2′, 6′), 7.60(3H, m, H-3′, 4′, 5′), 6.99(1H, s, H-6), 6.30 (1H, s, H-3), 3.84 (3H, s). 13 CNMR (DMSO-d 6 , 125MHz): δ182.7(C-4), 163.7(C-2), 15...

Embodiment 3

[0089] Example 3: 5 compounds in Eucommia have effects on Ca in A7r5 cells stimulated by high K+ 2+ concentration Impact

[0090] experiment method:

[0091] A7r5 cells (rat thoracic artery smooth muscle cells) were routinely cultured in DMEM medium without phenol red and containing 10% CS-FBS, at 5×10 4 Cells / well were seeded in a 96-well plate, cultured for 24 hours, and 100 μL was added to each well After Calcium 4 fluorescence reagent (Molecular Devices, USA), incubate in a 37°C incubator for 1h. After taking it out, add 50 μL with / without KCl (60 mmol·L -1 ) and different concentrations of drugs, under the conditions of excitation wavelength 485nm and emission wavelength 525nm, the fluorescence value of cells in each well was detected in real time, the detection time was 5min, and the corresponding fluorescence value was read. The data are represented by the percentage of the fluorescence value of cells in each well after drug addition to the fluorescence v...

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PUM

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Abstract

The invention relates to a new usage of eucommia ulmoides chemical composition as vessel protective agent, in particular to the new application of the eucommia ulmoides or eucommia ulmoides extractive for preparing the medicines as vessel protective agent and / or antihypertensions, or the medicines for curing and / or preventing angiogenesis disease. The eucommia ulmoides extractive contains at least one component selected from the group consisting of geniposide, wogonin, chiba A, alpha-oxygen-belta-D-glucopyranosyl-4,2',4'-trihydroxy dihydrochalcone and betulinic acid. According to the invention, the five chemical components or the eucommia ulmoides extractive containing the chemical components can be used as effective vessel protective agent and / or antihypertensions for curing and / or preventing angiogenesis disease.

Description

technical field [0001] The present invention relates to the new application of several chemical components in Eucommia ulmoides, in particular, chibain A, wogonin, α-oxygen-β-D-glucopyranosyl-4,2′,4 in eucommia ulmoides Pharmaceutical use of '-trihydroxydihydrochalcone, betulinic acid, and geniposide as vascular protective agents. Background technique [0002] The human vascular system has its own normal metabolic balance function, but abnormal vascular function can cause damage to the vascular system. For example, the proliferation of vascular smooth muscle cells is the pathological basis of atherosclerotic plaque formation and restenosis after coronary angioplasty; the increase of calcium ion concentration in smooth muscle cells can cause vasoconstriction, and abnormal vasomotor function can lead to hypertension happened. Some vascular protective agents can reduce blood pressure by antagonizing the increase of calcium ion concentration in vascular smooth muscle cells cau...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61P9/00A61P3/10A61K31/7048A61P25/06A61P9/12A61P25/00A61P13/12A61P9/14A61K129/00A61K36/46A61K31/56A61K31/352A61P9/10A61K31/7032
Inventor 高秀梅王虹苏艳芳樊官伟刘二伟王跃飞张伯礼
Owner TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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