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Application of Monascus Pigment Components and Its Derivatives in the Preparation of Anticancer Photosensitizers

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, complex active ingredients, and large skin phototoxicity and side effects. problems, to achieve the effect of expanding the application field, significant growth, and small toxic and side effects

Active Publication Date: 2017-03-08
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 ProfimerSodium, 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. After cooling, it is inoculated with Monascus and placed in solid state fermentation at 30℃ for 8 days. 505nm), containing red pigments (erythroscine and monascorubin) 10.1 g / kg, orange pigments (erythematine and monascorubin) 48.3 g / kg, yellow pigments (monascoxine and monascus) 41.9 g / kg.

[0039] The fermented product is extracted with a 70% mass fraction of ethanol solution at a solid-liquid ratio of 1:10 in a 60°C water bath, and then concentrated in a vacuum to 1 / 2 of the original volume, that is, a crude extract of the monascus 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] Take two 96-well plates as the non-light group and the light group respectively, and culture the Hela cells in the logarithmic growth phase in two 96-well plates. After the cells are fully attached an...

Embodiment 2

[0042] Purification of monascus pigment components:

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

[0044] Take 3 96-well plates and set them as the monascin-illuminated group, the monascorubin-illuminated group, and the lupusamine-illuminated group, and culture the Hela cells in the logarithmic growth phase in three 96-well plates, and wait until the cells are fully attached After growth, add equivalent amounts of monascin,...

Embodiment 3

[0046] Preparation of monascorubin derivative N-glutaryl monascorubamine: 1 g of monascorubin prepared in Example 2 was dissolved in 100 mL ethanol solution with a mass fraction of 70%, and placed in a water bath at 60 ℃ Add 10 mL of monosodium glutamate (1mol / L), and after reacting for 1 hour, use a silica gel column for purification, elution with anhydrous methanol, collect the eluted sample of N-glutaryl monascus red amine, and concentrate in vacuo to the original volume 1 / 2 means that the crystals are precipitated, and the N-glutaryl monascinolamine crystals are determined by HPLC-MS. The molecular weight is 511 and the purity is 99.1%.

[0047] Preparation of 4-hydroxyerythenamine derivative of Erythenamine: 1 g of Erythenamine prepared in Example 2 was dissolved in 100 mL of ethanol with a mass fraction of 70%, and 5 mL of sodium borohydride (1 mol) was added in a water bath at 30 ℃. / L), after reacting for 1 hour, use silica gel column purification, elution with anhydrous ...

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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 monascus pigment component and its derivatives in the preparation of an anticancer photosensitizer. Background technique [0002] Cancer, also known as malignant tumor, is a malignant growth formed by the body under the action of various carcinogenic factors. The local tissue cells have lost the normal regulation of their growth at the gene level, leading to its clonal abnormal proliferation. It is second only to Cardiovascular disease is the second most fatal human disease, which seriously threatens people's health and lives, and is a difficult and difficult disease that has plagued the medical profession for a long time. As the pace of modern life continues to accelerate, environmental pollution is becoming more and more serious, food safety, ionizing radiation and other issues have further increased the risk of human cancer...

Claims

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Application Information

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Patent Type & Authority Patents(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