Application of alisol A in preparation of anti-atherosclerosis medicaments

A technique for atherosclerosis and alisol, which is applied in the application field of alisol A in the preparation of anti-atherosclerotic drugs, can solve problems such as the absence of alisol A, achieve clear ingredients, low toxicity, Meet the effect of clinical application

Active Publication Date: 2014-06-11
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no published literature that alisol A has anti-atherosclerosis and anti-vascular intimal hyperplasia effects

Method used

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  • Application of alisol A in preparation of anti-atherosclerosis medicaments
  • Application of alisol A in preparation of anti-atherosclerosis medicaments

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Extraction of medicinal materials:

[0021] Method 1: Take 1 kg of dried tubers of Alisma orientalis (Sam.) Juzep., made into decoction pieces, and extract twice with 7500ml of ethyl acetate for 0.5 hours each time. The extracts were combined, and the solvent was recovered under reduced pressure to obtain 40 g of dark brown extract.

[0022] Method 2: Take 3 kg of dried tubers of Alisma orientalis (Sam.) Juzep., crushed into coarse particles, leak with 75% ethanol, combine the leaked liquid, and recover the solvent under reduced pressure to obtain a dark brown soak 110g of paste.

[0023] Method 3: Take 2 kg of dry tubers of Alisma orientalis (Sam.) Juzep., crush them into coarse particles, and place them in CO 2 In the supercritical extraction instrument, extraction conditions: CO 2 The pressure is 24-35MPa, the extraction temperature is 41-55°C, and the extraction time is 1.5h to obtain 65g of dark brown extract.

[0024] Method 4: Take 1 kg of dried tubers of Alisma orienta...

Embodiment 2

[0026] Preparation of Alismaol A:

[0027] Weigh 10g of the extract of Example 1 and apply D101 type macroporous adsorption resin. After eluting 10 column volumes with 20% ethanol, use 70% ethanol to elute 5 column volumes. Collect 70% ethanol eluate and reduce The solvent was recovered under pressure to obtain 2 g of yellow oil; 2 g of yellow oil was dissolved in 65% methanol, and the target compound was separated by preparative HPLC. The separation conditions are: C18 column, mobile phase is 65% methanol, flow rate is 50ml / min, and detection wavelength is 208nm. 100 mg of Alismaol A23-acetate with a purity of 95% by weight was obtained.

[0028] High resolution mass spectrum: m / z: 513.35505, C 30 H 50 O 5 Na + [M+Na], its molecular formula is C 30 H 50 O 5 .

[0029] C 13 NMR(δ): 223.79, 139.20, 136.95, 79.63, 74.77, 70.69, 70.46, 58.42, 50.73, 49.82, 48.81, 42.00, 41.98, 38.34, 35.54, 35.20, 34.80, 32.13, 31.82, 30.44, 30.03, 29.92, 29.10 , 27.37, 26.62, 26.20, 24.59, 23.79, 21...

Embodiment 3

[0031] Weigh 10 g of Alismadiol A in Example 2, add 8 g of starch, 2 g of microcrystalline cellulose, and 0.2 g of magnesium stearate, mix them uniformly, and prepare tablets, capsules or granules using methods known in the art.

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Abstract

The invention discloses an application of alisol A in preparation of anti-atherosclerosis medicaments. Animal tests prove that the alisol A has a significant treatment effect on an arteriosclerosis model of an ApoE-/- mouse which is fed with a high-fat diet and combined with carotid artery injury surgery. The medicament disclosed by the invention has relatively low toxicity and is suitable for long-term use. The invention provides the medicament for treating arteriosclerosis, which has the advantages of exact curative effect, definite ingredients and controllable quality, and can meet the needs of clinical applications, by applying the modern medicine theory. The effect of inhibiting vascular intimal hyperplasia of the ApoE-/- mice after carotid artery injuries, caused by high-fat diets, of the alisol A is firstly disclosed by the invention, thereby showing that the alisol A has an obvious effect on treating the arteriosclerosis.

Description

Technical field [0001] The invention relates to a new application of Alismaol A in medicine. Background technique [0002] Cardiovascular disease has become the number one killer threatening human health. According to a report by the World Health Organization in 2004, one in three deaths is caused by cardiovascular disease. Atherosclerosis is a cardiovascular event such as cerebral infarction and myocardial infarction. The main reason. [0003] Preventing the occurrence of atherosclerosis and promoting the regression of arterial plaque are fundamental measures to reduce the incidence and mortality of cardiovascular and cerebrovascular diseases. Currently, drugs for the treatment of atherosclerosis, such as atorvastatin, have published clinical research results showing that atorvastatin is the only anti-atherosclerotic drug that has been proven to reduce cardiovascular events better than vascular double eyelid surgery. Its inhibitory effect on vascular intimal hyperplasia is indep...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/56A61P9/10
Inventor 侯惠民程志红
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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