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Separation method and application of gallic acid ethyl ester

2019-04-30 来源:亚科官网

 

Ethyl gallate (EG) is a safer polyphenol antitumor active compound selected from the genus Stellera chamaejasme by pharmacological experiments. It is a versatile fine chemical product used primarily in the organic synthesis, food, light industry and electronics industries.
Method for separating gallic acid ethyl ester
Separation and purification of ethyl gallate from ethyl acetate layer of Stellera chamaejasme by silica gel column chromatography, Sephadex LH-20 gel column chromatography and semi-preparative high performance liquid chromatography were carried out by MTT method at different concentrations and times. Growth inhibition of three tumor cells under conditions. RESULTS: Ethyl gallate had a certain inhibitory effect on the growth of colon cancer LOVO cells, lung cancer A549 cells and oral squamous cell carcinoma CAL-27 cells. After 72 hours of drug treatment, the maximum inhibition rate reached 74. 67 ± 0. 47) %, (62.01 ± 1.27)% and (37.17 ± 2.12)%. Conclusion: The ethyl gallate extracted and extracted from the ethyl acetate layer of Stellera chamaejasme has antitumor activity in vitro.
Application of gallic acid ethyl ester
1. Anti-tumor: Ethyl gallate has an inhibitory effect on liver cancer, gastric cancer and breast cancer. The experiment uses silica gel column chromatography, Sephadex LH-20 gel column chromatography and semi-preparative high performance liquid chromatography from Stellera chamaejasme. The extraction of ethyl gallate from sorghum was carried out with high purity, and it was confirmed by screening of antitumor activity in vitro that ethyl gallate was one of the antitumor active ingredients of Stellera chamaejasme. The LOVO, A549, and CAL-27 cells all inhibited the proliferation of tumor cells, and the effects of the drug on different cells were different, and the effect on LOVO cells was the most significant.
There is also a laboratory extracting ethyl gallate (EG) from the dried roots of Stellera chamaejasme, which is expressed in human breast cancer estrogen receptor, ie, ER-MDA-MB-231 cells and estrogen receptor expression, ie ER+ MCF-7 cells were studied. The results showed that EG can down-regulate the expression of Bcl-2 and up-regulate the expression of Bax, suggesting that EG can down-regulate Bcl-2/Bax expression and induce MDA-MB-231 cells. Death, thereby inhibiting breast cancer cell proliferation. EG is also one of the most important bioactive ingredients in the treatment of breast cancer.
In addition, studies have shown that the use of ethyl gallate for colon cancer cell Lovo apoptosis drugs, mainly to solve the serious problem of toxic side effects of colon cancer chemotherapy; ethyl gallate can effectively inhibit colon cancer cell proliferation, induce colon Apoptosis of cancer cells Lovo, and its target was found to up-regulate the expression of caspase-3, caspase-8, and caspase-9. This compound induces the action mechanism of colon cancer cells and activates mitochondrial pathway and death receptor pathway closely related. Gallic acid ethyl ester is less toxic and safe. The present invention finds the mechanism and target of inhibiting the proliferation of colon cancer by ethyl gallate, and provides a theoretical basis for the clinical application of ethyl gallate as a drug.
2. Antidiarrheal effect: Studies have shown that ethyl gallate as the active ingredient or the only active ingredient is used to prepare antidiarrheal drugs. Ethyl gallate can significantly inhibit the contraction of isolated intestinal smooth muscle in mice, which can significantly reduce the rate of mouse loose stools, can significantly reduce the serum motilin and gastrin levels in diabetic rats, improve intestinal function, indicating ethyl gallate It has a significant antidiarrheal effect and is expected to be used as an active ingredient in the preparation of antidiarrheal drugs, especially for the preparation of drugs for treating diarrhea or diabetic gastrointestinal disorders, and has broad application prospects.
Related links: ethyl gallate
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