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Application of monascorubrin pigment component and derivatives thereof in preparation of anticancer photosensitizer

A technology of monascus pigments and derivatives, which is applied in the application field of monascus pigment components and their derivatives in the preparation of anticancer photosensitizers, which can solve the problem of unsatisfactory action spectrum, large skin phototoxicity and side effects, complex active ingredients, etc. problems, to achieve the effect of expanding the application field, significant growth, and small toxic and side effects

Active Publication Date: 2015-05-06
FUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The photosensitizers that have been approved for clinical use are mainly hematoporphyrin derivatives represented by Profimer Sodium, but they have serious defects such as complex active ingredients, large skin phototoxicity and side effects, and unsatisfactory action spectrum.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Preparation of Monascus Pigment Crude Extract:

[0038] 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. 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.

[0039] The fermented product is extracted in a 60°C water bath with a mass fraction of 70% ethanol solution at a solid-to-liquid ratio of 1:10, then concentrated in vacuum to 1 / 2 of the original volume, and the crude extract of the red yeast pigment component is precipitated, with a yield of 10.1% , the pigment component accounts for 78.9% of the total weight of the crude extract.

[0040] Two 96-well plates were taken as the no-light group and the light-light group respectively, and the Hela cells in the logarithmic growth ...

Embodiment 2

[0042] Purification of Monascus pigment components:

[0043] Purification of Monascus pigment components: The crude extract of Monascus pigment components prepared in Example 1 was separated and purified by HPLC (C18 column), and 80% methanol solution was used as eluent to collect Monascus and Monascus respectively. The red pigment and erythema amine components were eluted samples, concentrated in vacuum to 1 / 2 of the original volume and crystals were precipitated, and the obtained monascus, monascus red pigment and erythematamine component crystals were determined by HPLC-MS, and the molecular weights were respectively 358, 382 and 353 with a purity of 99.3%, 98.6% and 98.9% respectively.

[0044]Take three 96-well plates and set them as the monascus red pigment light group, the monascus red light light group, and the erythema amine light group respectively, and culture the Hela cells in the logarithmic growth phase in three 96-well plates, and wait until the cells are comple...

Embodiment 3

[0046] 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 ethanol solution with a mass fraction of 70%, and place it in a water bath at 60 °C Add 10 mL of monosodium glutamate (1mol / L), react for 1 hour, purify with silica gel column, elute with anhydrous methanol, collect the eluted sample of N-glutaryl monascus red amine component, and concentrate in vacuo to the original volume 1 / 2 crystals were precipitated, and the N-glutaryl monascus red amine crystals were determined by HPLC-MS. The molecular weight was 511 and the purity was 99.1%.

[0047] Preparation of erythematamine derivative 4-hydroxyerythematamine: 1 g of erythematamine prepared in Example 2 was dissolved in 100 mL of ethanol solution with a mass fraction of 70%, and 5 mL of sodium borohydride (1mol / L), after reacting for 1 hour, it was purified by silica gel column, eluted with anhydrous methanol, and the eluted ...

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PUM

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Abstract

The invention discloses application of a monascorubrin pigment component and derivatives thereof in preparation of an anticancer photosensitizer. The monascorubrin pigment component is a fermented product of monascus purpureus or an extracted and purified product of the fermented product, and comprises monascine, ankafaflavin, rubropunctatin, monascorubin, rubropunctamine, monascorubramine, monasfluore A and monasfluore B; the derivatives of the monascorubrin pigment component are synthesized by biotransformation or chemical modification of the monascorubrin pigment component. The compound can be used for preparing the photosensitizer in tumor phototherapy, is small in toxic and side effects on normal cells of a human body, and has a relatively good development prospect.

Description

technical field [0001] The invention belongs to the technical field of biotechnology and drug development, and specifically relates to the application of a red yeast pigment component and its derivatives in the preparation of an anticancer photosensitizer. Background technique [0002] Cancer, also known as malignant tumor, is a malignant hyperplasia formed by local tissue cells losing normal regulation of their growth at the gene level under the action of various carcinogenic factors, resulting in abnormal clonal proliferation. Cardiovascular disease is the second most lethal disease in human beings, which seriously threatens people's health and life, and is a difficult disease that has plagued the medical field for a long time. With the continuous acceleration of the pace of modern life, the increasingly serious environmental pollution, food safety, ionizing radiation and other issues have further increased the risk of human cancer. It can be seen that the prevention and ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K41/00A61P35/00
Inventor 郑允权潘启胜郭养浩石贤爱张云
Owner FUZHOU UNIV
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