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Application of monascus color components and derivatives thereof in fighting cancers

A technology of monascus pigments and derivatives, which is applied in the field of pharmaceutical biotechnology and drug development, can solve problems that have not been further revealed, and achieve the effect of small toxic and side effects and efficient induction of apoptosis

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 color components and derivatives thereof in fighting cancers
  • Application of monascus color components and derivatives thereof in fighting cancers
  • Application of monascus color components and derivatives thereof in fighting cancers

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Preparation of Monascus Pigment Crude Extract:

[0035] 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.

[0036] 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.

[0037] Human liver cancer cells Hep-G2, human neuroma cells SH-5Y, colon cancer cells HT-29, human gastric cancer cells BGC-823, AGS and MKN4...

Embodiment 2

[0039] Preparation of Monascus Pigment Purified Components:

[0040] 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 Monascus, Monascus Red and Erythematamine were collected respectively Component elution samples were vacuum concentrated to 1 / 2 of the original volume and then crystals were precipitated. Monascus, monascus rubin and erythematamine component crystals were determined by HPLC-MS, and their molecular weights were 358, 382 and 353, respectively, and the purity 99.3%, 98.6% and 98.9%.

[0041] Human liver cancer cells Hep-G2, human neuroma cells SH-5Y, colon cancer cells HT-29, human gastric cancer cells BGC-823, AGS and MKN45 were routinely cultured at 37°C and 5% CO2. Cancer cells were inoculated in a 96-well plate with a cell concentration of 2500 cells / well. The components of monascus, monascus and erythem...

Embodiment 3

[0043] Preparation of monascus rubin derivative N-glutaryl monascus red amine: take 1 g of monascus rubin prepared in Example 2 and dissolve it in 100 mL of 70% ethanol solution, add 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 crystals were determined by HPLC-MS, with a molecular weight of 511 and a purity of 99.1%.

[0044] Preparation of erythematamine derivative 4-hydroxyerythematamine: Dissolve 1 g of erythematamine prepared in Example 2 in 100 mL of 70% ethanol solution, add 5 mL of sodium borohydride (1 mol / L) at 30 ° C, react for 1 hour and use Silica gel column purification, eluting with anhydrous methanol, collecting the eluted sample of 4-hydroxyerythematamine component, vacuum concentrating to 1 / 2 of the...

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Abstract

The invention provides application of monascus color components and derivatives thereof in preparing the drugs for fighting cancers, belonging to the technical field of monascus compound application. The invention solves the problem of narrower application range of the monascus color components and derivatives thereof in the prior art. The series compound comprises rubropunctamine, monascorubramine, monascin, ankaflavin, rubropunctatin, monascorubrine, monasfluore A, monasfluore B and derivatives thereof. The compound can be used as the drug and health care product additive for preventing and treating cancers and has little toxic or side effects on normal cells of human bodies.

Description

technical field [0001] The invention relates to the fields of pharmaceutical biotechnology and pharmaceutical development, and more specifically relates to the application of the red yeast pigment components and derivatives thereof as anticancer drugs. 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 polyketide synthases (Polyketide Synthases, PKS). ...

Claims

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Application Information

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IPC IPC(8): A61K31/365A61K31/4355A61K31/352A61P35/00A23L1/30A23L33/10
Inventor 郑允权郭养浩石贤爱
Owner FUZHOU UNIV
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