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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 fields of drug biotechnology and drug development, can solve the problems that have not been further disclosed, and achieve the effects of less toxic side effects and high-efficiency inducing apoptosis activity.

Inactive Publication Date: 2012-05-30
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 xanthomonasin A and B can inhibit Nor I activity (a NO donor); Monascopyridine A and B can inhibit the growth of immortalized human kidney epithelial cells, EC50 between 11-31 mol / L; the role of some structures has not been further revealed, such as Monasfluore A 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 5100 U / g (E 505nm), containing red pigment (erythromycin and monascus amine) 10.1 g / Kg, orange pigment (erythematin and monascus red pigment) 48.3 g / Kg, yellow pigment (monascus and monascus xanthin) 41.9 g / 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 ...

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 glutamine at 60 °C Sodium monosodium acid (1mol / L), purified by silica gel column after reaction for 1 hour, eluted with anhydrous methanol, collected the eluted sample of N-glutaryl monascus red amine component, concentrated in vacuum to 1 / 2 of the original volume and then precipitated Crystal, N-glutaryl monascus red amine crystal was determined by HPLC-MS, its molecular weight was 511, and its purity was 99.1%.

[0044] Preparation of erythematamine derivative 4-hydroxyerythematamine: 1 g of erythematamine prepared in Example 2 was dissolved in 100 mL of 70% ethanol solution, and 5 mL of sodium borohydride (1mol / L) was added at 30°C to react After 1 hour, it was purified by silica gel column, eluted with anhydrous methanol, and the eluted sample of 4-hydroxyerythematamine component was ...

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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 andtreating 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 fungal polyketide synthase (Polyketide Synthases, PKS) metabolic pathway. eryt...

Claims

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Application Information

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