Application of epigallocatechin gallate (EGCG) in preparation of targeted drug

A technology of epigallocatechin and gallate, which is applied in the field of preparation of drugs targeting estrogen receptor ER-α36 inhibition, and can solve problems such as incompletely clear mechanism of action

Inactive Publication Date: 2017-12-22
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

EGCG is a water-soluble component extracted from green tea. It is the component with the highest content of catechins. Studies have shown that it has antibacterial, antiviral, antioxidative, antiangioproliferative, anti-inflammatory and other effects, but the exact The mechanism of action is still unclear

Method used

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  • Application of epigallocatechin gallate (EGCG) in preparation of targeted drug
  • Application of epigallocatechin gallate (EGCG) in preparation of targeted drug
  • Application of epigallocatechin gallate (EGCG) in preparation of targeted drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1: Screening of ER-α36-targeted drugs in the MPD3 medicinal plant database

[0027] The MPD3 medicinal plant database contains 2295 phytochemicals, predicted by the protein-ligand docking software MOEv2014.0901, in Under the condition of 2.4GHz operating system and 8GB RAM (x86) operating platform, the phytochemicals that may target ER-α36 were screened according to molecular docking S score. According to the screening results, we selected the top 6 drugs for subsequent analysis, all of which were flavonoids, as shown in Table 1.

[0028] Table 1: Six possible ER-α36-targeting phytochemicals were screened by MOE protein-ligand docking software

[0029]

[0030] We further used Molinspiration software to evaluate the lipid-water partition coefficient, molecular weight, number of hydrogen bond donors, hydrogen bond acceptors, and number of rotatable bonds of the six substances screened out for pharmacokinetic prediction and evaluation. According to the "Lipi...

Embodiment 2

[0036] Example 2: Epigallocatechin gallate EGCG targetedly inhibits the proliferation of gastric signet ring cell carcinoma cells with high expression of ER-α36

[0037] Gastric signet ring cell carcinoma cells with differential expression of ER-α36 (ER-α36 highly expressed GCSR-1-6, ER-α36 lowly expressed GCSR-1-11) were selected to evaluate the effect of epigallocatechin gallate EGCG on Effect of differential expression of ER-α36 on growth inhibition of gastric signet ring cell carcinoma cells. Cells in the logarithmic growth phase were selected, and the seeding density of 96-well plate cells was 3000 / well, 37°C, 5% CO 2 After 10% FBS-RPMI1640 seed plate was cultured for 16h, the corresponding concentrations of EGCG (0, 6.25, 12.5, 25, 50, 100 μg / ml) prepared by 10% FBS-RPMI1640 were added to treat the cells. After 72h, after 1h incubation with 10% CCK-8, Bio-Rad iMark TM Microplate reader detects OD490nm absorbance, calculates IC 50 . The results showed that epigallocat...

Embodiment 3

[0038] Example 3: Epigallocatechin gallate EGCG targetedly inhibits the proliferation of breast cancer cells with high expression of ER-α36

[0039] Breast cancer cells with differential expression of ER-α36 (high expression of MDA-MB-231 in ER-α36 and low expression of MCF-7 in ER-α36) were selected to evaluate the expression difference of epigallocatechin gallate EGCG on ER-α36 The effect of breast cancer cell growth inhibition, the specific operation steps are as described in Example 2. The results showed that epigallocatechin gallate EGCG could inhibit cell proliferation in a dose-dependent manner, but in the breast cancer cell line MDA-MB-231 with high expression of ER-α36, its half inhibitory concentration was lower and the inhibitory effect was better. It shows a clear inhibitory effect on tumor cell proliferation due to the targeted binding and inhibition of ER-α36, see image 3 shown.

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Abstract

The invention provides application of epigallocatechin gallate (EGCG) in preparation of a targeted drug for inhibiting estrogen receptor (ER)-alpha 36. Biological experiments prove that the EGCG can remarkably inhibit the proliferation of tumor cells with high expression of ER-alpha 36, thus arresting a cell cycle at the G1 period, inhibiting cell migration and invasion abilities and inducing the occurrence of apoptosis. The EGCG is clear in target function, and is especially obvious in an inhibiting effect for tumor cells with abnormal expression of the ER-alpha 36. The EGCG can be used as an ER-alpha 36 specific targeting inhibitor for playing a role of inhibiting the cells with the abnormal expression of the ER-alpha 36. The application of the EGCG provides a new effective drug for the development of personalized treatment of clinical targeting ER-alpha 36 abnormality.

Description

technical field [0001] The invention belongs to the field of biomedicine, and relates to the application of epigallocatechin gallate (EGCG) in the preparation of drugs targeted at inhibiting estrogen receptor ER-α36. Background technique [0002] Estrogen receptor is an important receptor protein, which is expressed and plays corresponding roles in many different types of cells. In the classic mode of estrogen regulation, estrogen binds to estrogen receptor (ER), changes the conformation of the receptor, and transfers to the nucleus as a transcription factor to directly regulate the expression of target genes. Initiated estrogen signaling (ie genome regulation). Estrogen can also bind to the estrogen receptor located on the plasma membrane, and activate the cascade reaction of downstream signaling pathways through protein phosphorylation to indirectly regulate the expression of certain genes. This mechanism is called membrane-initiated estrogen signaling ( i.e. non-genomic...

Claims

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Application Information

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IPC IPC(8): A61K31/353A61P35/00
CPCA61K31/353
Inventor 曹江穆罕默德·赛义夫·拉赫曼穆罕默德·萧艾布谢雨琼
Owner ZHEJIANG UNIV
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