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Composition containing 24-acetyl alisol A and 23-acetyl alisol B and application thereof in regulation of blood fat and preparation of HMG-CoA inhibitor

A technology of acetyl alisol and a composition is applied in the field of active ingredient compositions of traditional Chinese medicines, and achieves the effects of significantly regulating blood lipids, good blood lipid effect and strong inhibitory effect.

Active Publication Date: 2015-03-25
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Currently commonly used lipid-lowering Western medicines include statins, which are HMG-CoA reductase inhibitors, and their lipid-lowering effects are good, but they can cause liver toxicity such as cholestasis and elevated transaminases during liver metabolism.

Method used

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  • Composition containing 24-acetyl alisol A and 23-acetyl alisol B and application thereof in regulation of blood fat and preparation of HMG-CoA inhibitor
  • Composition containing 24-acetyl alisol A and 23-acetyl alisol B and application thereof in regulation of blood fat and preparation of HMG-CoA inhibitor
  • Composition containing 24-acetyl alisol A and 23-acetyl alisol B and application thereof in regulation of blood fat and preparation of HMG-CoA inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1 Preparation of 24-acetyl alisol A

[0021] Take 20kg of dry tubers of Alisma orientalis (Sam.) Juzep., cold soak and extract 10 times the amount of methanol for 4 times, and concentrate under low pressure to obtain 1600g of extract. After dispersing with water, extract with ethyl acetate and n-butanol in sequence to obtain 785 g of ethyl acetate and 531 g of n-butanol. Take 450g of the ethyl acetate part, use 100-200 mesh silica gel (2500g), and petroleum ether-ethyl acetate system for rough separation to obtain 25 components (Fr1-Fr25). Fr20 (2.9 g) was recrystallized from methanol / dichloromethane to obtain 800 mg of 24-acetyl alisol A with a purity of 95% by weight.

Embodiment 2

[0022] The preparation of embodiment 2 23-acetyl alisol B

[0023] Take 20 kg of dried tubers of Alisma orientalis (Sam.) Juzep., extract by cold immersion in 10 times the amount of methanol for 4 times, and concentrate under low pressure to obtain 1600 g of medicinal material extract. After dispersing with water, extract with ethyl acetate and n-butanol in sequence to obtain 785 g of ethyl acetate and 531 g of n-butanol. Take 450g of the ethyl acetate part, use 100-200 mesh silica gel (2500g), and petroleum ether-ethyl acetate system for rough separation to obtain 25 components (Fr1-Fr25). After Fr12 (3g) was separated by C18 column chromatography, after selecting suitable conditions by analytical HPLC, 770 mg of 23-acetyl alisitol B was prepared by semi-preparative liquid phase (95% methanol solution, isocratic elution), with a purity of 95 %(weight).

Embodiment 3

[0024] Example 3 Preparation of a composition composed of 24-acetyl alisol A and 23-acetyl alisol B

[0025] Method 1: Mix the products obtained in Example 1 and Example 2 according to 1:3 to obtain a composition composed of 24-acetyl alisol A and 23-acetyl alisol B;

[0026] Method 2: Mix the products obtained in Example 1 and Example 2 at a ratio of 1:10 to obtain a composition composed of 24-acetyl alisitol A and 23-acetyl alisitol B;

[0027] Method 3: Mix the products obtained in Example 1 and Example 2 according to 1:1 to obtain a composition composed of 24-acetyl alisol A and 23-acetyl alisol B;

[0028] Method 4: Mix the products obtained in Example 1 and Example 2 according to 1:0.5 to obtain a composition composed of 24-acetyl alisol A and 23-acetyl alisol B;

[0029] Method 5: Mix the products obtained in Example 1 and Example 2 at a ratio of 1:5 to obtain a composition composed of 24-acetyl alisol A and 23-acetyl alisol B;

[0030] Method 6: Mix the products obta...

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Abstract

The invention provides a composition containing 24-acetyl alisol A and 23-acetyl alisol B, and application thereof in regulation of blood fat and preparation of an HMG-CoA reductase inhibitor. In the composition, the weight ratio of 24-acetyl alisol A to 23-acetyl alisol B is 1:(0.5-15), preferably 1:3. Compared with use of 24-acetyl alisol A or 23-acetyl alisol B or the composition of 24-acetyl alisol A and 23-acetyl alisol B disclosed in the prior art under same dosage, the composition disclosed by the invention has the better effect of regulating blood fat; both 24-acetyl alisol A and 23-acetyl alisol B have the inhibiting effect to lipid metabolism key enzyme HMG-CoA reductase; the fact that the inhibiting effect of the composition of 24-acetyl alisol A and 23-acetyl alisol B is better than that of 24-acetyl alisol A or 23-acetyl alisol B is disclosed in the invention for the first time; and furthermore, the invention simultaneously provides the HMG-CoA reductase inhibitor comprising the composition.

Description

technical field [0001] The present invention relates to a traditional Chinese medicine active ingredient composition, in particular to the use of 23-acetyl alisol B and 24-acetyl alisol A in blood lipid regulation and preparation of trihydroxytrimethylglutaryl coenzyme A reductase inhibitors Applications. Background technique [0002] Lipid metabolism disorders include cholesterol (TC) abnormalities, triglyceride-rich (TG) lipoprotein metabolism abnormalities, and high-density lipoprotein metabolism (HDL-C) abnormalities. Studies have shown that changes in the biological activity of lipoprotein metabolic enzymes can cause changes in lipid metabolism, leading to lipid metabolism disorders and hyperlipidemia (HLP). There is a clear correlation between HLP and the morbidity and mortality of cardiovascular and cerebrovascular diseases and kidney diseases. Without effective intervention, hyperlipidemia and related diseases will become an important risk factor affecting people's...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/58A61P3/06A61K31/575
Inventor 徐飞吴启南谷巍陈军顾薇房方吕翔
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE