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Application of monascus colors and derivatives in preparing drugs for treating cardiovascular and cerebrovascular diseases

A technology for cardiovascular and cerebrovascular diseases and monascus pigment, which is applied in cardiovascular system diseases, drug combinations, anti-tumor drugs, etc., can solve problems that have not been further revealed, and achieve remarkable human health, expand the application field, and have small toxic and side effects Effect

Inactive Publication Date: 2010-10-20
FUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Some new metabolites of Monascus Azaphilone were found, such as xanthomonasinA and B can inhibit the activity of NorI (a NO donor); MonascopyridineA and B can inhibit the growth of immortalized human kidney epithelial cells, EC50 is between 11-31 mol / L; the role of some structures has not been further revealed, such as MonasfluoreA and B

Method used

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  • Application of monascus colors and derivatives in preparing drugs for treating cardiovascular and cerebrovascular diseases
  • Application of monascus colors and derivatives in preparing drugs for treating cardiovascular and cerebrovascular diseases
  • Application of monascus colors and derivatives in preparing drugs for treating cardiovascular and cerebrovascular diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Preparation of the crude extract of Monascus pigment: Steam the rice until it is fully cooked, inoculate Monascus after cooling, and place it for solid-state fermentation at 30°C for 8 days, and the color value of the fermented product is 5100U / g (E 505nm), containing red pigment (erythromycin and monascus amine) 10.1g / Kg, orange pigment (erythematin and monascus red pigment) 48.3g / Kg, yellow pigment (monascus and monascus xanthin) 41.9g / Kg. The fermented product is extracted with 70% (weight ratio, the same below) ethanol solution (water bath at 60°C, solid-to-liquid ratio 1:10), then concentrated in vacuum to 1 / 2 of the original volume, and then the crude extract of the red yeast pigment component is precipitated. The yield 10.1%, the pigment component accounts for 78.9% of the total weight of the crude extract.

[0029] Experiments were performed using a mouse model of hyperlipidemia. The experiment adopts intragastric administration method, the high and low do...

Embodiment 2

[0035] Preparation of Monascus Pigment Purification Components: The crude pigment extract prepared in Example 1 was separated and purified by HPLC (C18 column), the elution condition was 80% methanol solution, and the Monascus, Monascus Red and Erythematamine groups were collected respectively Parts of the eluted samples were vacuum concentrated to 1 / 2 of the original volume and then crystals were precipitated. Monascus, monascus and erythematamine crystals were determined by HPLC-MS, and their molecular weights were 358, 382 and 353, respectively, and their purity was 99.3%. , 98.6% and 98.9%.

[0036] Experiments were performed using a mouse model of hyperlipidemia. The experiment adopts intragastric administration method, the high and low doses are 100mg / Kg and 20mg / Kg respectively, and the blank group, high fat model group and positive control group (lovastatin dosage 20mg / Kg) are used for comparison (as shown in Table 2 ). After 35 days, the total cholesterol and blood ...

Embodiment 3

[0042]Preparation of monascus rubin derivative N-glutaryl monascus red amine: 1 g of monascus rubin prepared in Example 2 was dissolved in 100 mL of 70% ethanol solution, and 10 mL of monosodium glutamate ( 1mol / L), after reacting for 1 hour, use silica gel column purification, elute with anhydrous methanol, collect N-glutaryl monascus red amine component elution sample, concentrate in vacuum to 1 / 2 of the original volume and then precipitate crystals, N- Glutaryl monascus red amine was determined by HPLC-MS, its molecular weight was 511, and its purity was 99.1%.

[0043] Preparation of erythematamine derivative 4-hydroxyerythematamine: Dissolve 1 g of monascus red pigment prepared in Example 2 in 100 mL of 70% ethanol solution, add 5 mL of sodium borohydride (1 mol / L) at 30° C., and react for 1 hour Afterwards, use silica gel column to purify, elute with anhydrous methanol, collect the eluted sample of 4-hydroxyerythematamine component, vacuum concentrate to 1 / 2 of the origi...

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Abstract

The invention provides application of monascus color components and derivatives thereof in preparing drugs for preventing and treating cardiovascular and cerebrovascular diseases, belonging to the technical field of monascus compound application. The series compound comprises rubropunctamine, monascorubramine, monascin, ankaflavin, rubropunctatin, monascorubrine, monasfluore A, monasfluore B and derivatives thereof. The compound has the functions of reducing triglyceride, total cholesterol and low density lipoprotein cholesterol and elevating high density lipoprotein cholesterol and can be used as the drug and health care product additive for preventing and treating cardiovascular and cerebrovascular diseases.

Description

technical field [0001] The invention relates to the technical field of application of red yeast rice compounds, in particular to the application of a red yeast rice pigment component and its derivatives in the preparation of drugs for preventing and treating cardiovascular and cerebrovascular diseases. Background technique [0002] The production and application of red yeast rice has a history of more than 1,000 years in my country. Red yeast rice is a traditional fermented product, which is often used for food coloring, wine making and medicinal purposes. Monascus pigment is a secondary metabolite produced during the growth of Monascus fungus. It is widely used as a natural food pigment and has certain antiseptic, anti-inflammatory and anti-oxidative biological activities. At present, the demand for red yeast pigment products at home and abroad is growing rapidly. [0003] Monascus pigment is an Azaphilone compound, which is synthesized by the metabolic pathway of fungal ...

Claims

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Application Information

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IPC IPC(8): A61K31/4355A61K31/365A61K31/352A61P9/00A61P35/00
Inventor 郑允权郭养浩石贤爱
Owner FUZHOU UNIV
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