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Application of lutein and derivative thereof in preparing anti-glioma drug

A glioma and lutein technology, applied in the direction of anti-tumor drugs, drug combinations, active ingredients of hydroxyl compounds, etc., can solve the problems of unreported lutein anti-glioma activity and difficulties in artificial chemical synthesis of lutein

Active Publication Date: 2019-01-11
CHINA PHARM UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, artificial chemical synthesis of lutein is difficult, so it can only be extracted from natural plants
There is no report on the anti-glioma activity of lutein

Method used

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  • Application of lutein and derivative thereof in preparing anti-glioma drug
  • Application of lutein and derivative thereof in preparing anti-glioma drug
  • Application of lutein and derivative thereof in preparing anti-glioma drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1 Extraction of Chemical Components in Porphyra laver and Screening of Active Parts

[0036] Grind Porphyra laver into powder, soak in 95% ethanol solution, the ratio of solid to liquid is 1:7, ultrasonic treatment for 30min, continuous leaching for 7 days, suction filtration of the leaching solution, concentration by rotary evaporation at 50°C under low pressure, Sequentially adopt an equal volume of petroleum ether, ethyl acetate and n-butanol to carry out static extraction, each organic phase is continuously extracted 3 times, each extraction is 4h, and each organic phase is combined respectively, and the concentrated solid extract by rotary evaporation under low pressure ( figure 1 ), the three extract phases were detected by thin layer chromatography ( figure 2 ). The proliferation curve of U87 cells was determined by RTCA method ( image 3 ), and finally determined that the optimal inoculation density of cells was 60,000 / mL, the drug addition time was 2...

Embodiment 2

[0039] Example 2 Separation, purification and structural identification of lutein

[0040] Preliminary separation and purification of the combined phase of petroleum ether and ethyl acetate extraction phases was carried out by silica gel column chromatography, and the steps were as follows: ① Sample mixing (sand making): Dissolve an appropriate amount of extract in a 500mL round-bottomed flask with appropriate amount of petroleum ether and ethyl acetate , add an appropriate amount of 200-300 mesh silica gel, and spin-steam to make sand. It is required to be completely adsorbed, loose and not agglomerated. ②Column packing: The dry method is used to load the sample, the height ratio of the sample sand to the silica gel is about 1:20, and the total height of the packed column is about 3 / 4 of the column height. Run the column with petroleum ether and compact it with a pressurizer. ③Elution: Gradient elution with petroleum ether-ethyl acetate eluent, the ratio is petroleum ether:e...

Embodiment 3

[0041] Embodiment 3 Lutein dehydration

[0042] The substrate lutein (1g, 1.76mmol) was added to a mixed solvent of 6ml concentrated hydrochloric acid and 60m water, and heated to reflux after the addition was complete. After the reaction was completed, it was extracted with diethyl ether (30ml×3), and the organic phases were combined, dried and then column chromatographed to obtain 0.8g of the target product with a yield of 83%.

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Abstract

The invention relates to the field of marine drugs and specifically discloses a method for extracting, separating and purifying lutein from porphyra haitanensis, a research on in vitro activity of lutein to malignant glioma cells and the research on the mechanism of lutein in restraining U87 cell migration. According to the invention, the lutein is acquired in the manner of using an ultrasonic-assisted organic solvent for extracting porphyra haitanensis and combining silica-gel column chromatography with SephadexLH-20 chromatography. The acquired lutein has higher purity and is capable of obviously restraining proliferation of U87 cells and U251 cells, obviously restraining migration capacity of U87 cells, obviously boosting apoptosis of U87 cells and effectively reducing the expression ofmigration-related signaling proteins, such as p-p38, MAPK, p-ERK1 / 2 and p-MEK in U87 cells.

Description

technical field [0001] The invention belongs to the field of marine drug development, and specifically relates to the extraction, separation, purification and structural identification of lutein in Porphyra laver, the research on the anti-glial cell activity of lutein in vitro and the exploration of the anti-glioma cell migration mechanism of lutein. technical background [0002] Glioma is the most common primary brain tumor, accounting for 32% of all primary central nervous system tumors. The World Health Organization (WHO) divides brain gliomas into four grades, more than half of which are the most malignant glioblastoma multiforme (GBM). GBM is locally heterogeneous and highly invasive, with fast growth. Make complete surgical resection difficult, easy to relapse, and easy to produce drug resistance. Moreover, due to the existence of the blood-brain barrier, most drugs cannot directly reach the tumor site. At present, the structure of the blood-brain barrier is not very ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/047A61P35/00A61P27/02A61P9/10
CPCA61K31/047A61P9/10A61P27/02A61P35/00
Inventor 刘煜闫忠辉李小平别雨薇纪雪梅
Owner CHINA PHARM UNIV
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