Application of polyphenolic compound

A technology of polyphenolic compounds and compounds, applied in the application field of polyphenolic compounds, can solve the problems of weak cell activity, drug resistance, cytotoxicity, etc.

Inactive Publication Date: 2016-01-06
SHANGHAI INST OF ORGANIC CHEM CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] The technical problem to be solved by the present invention is to overcome the narrow anti-tumor spectrum and drug resistance of existing mTOR inhibitors that have been used for tumor treatment; the specificity is low, and it is easy to produce cytotoxicity to normal cells; in clinical trials , weak cell activity, low blood concentration and other defects, and provides a polyphenolic compound application

Method used

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  • Application of polyphenolic compound
  • Application of polyphenolic compound
  • Application of polyphenolic compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] Substrate peptide STTPGGTLFSTTPG (the sequence of the substrate peptide is shown in SEQIDNO: 1 in the sequence listing, referring to the mTOR kinase test method of PerkinElmer Company), the substrate peptide was synthesized by Jill Biochemical (Shanghai) Co., Ltd., and its N 5-carboxyfluorescein (5-FAM) labeling is carried out at the end to facilitate fluorescence detection and improve the sensitivity of detection. The peptide structure of the obtained substrate peptide is shown in formula II:

[0061]

[0062] mTORC1 used in the examples was purchased from Sigma Reagent Co., Ltd., product number: SRP0364; salvianolic acid A was purchased from Shanghai Yuanye Reagent Company, product number: YY90055; salvianolic acid C was purchased from Shanghai Yuanye Reagent Company, product number: YY90623.

[0063] Prepare 25 mL of enzyme reaction buffer: 50 mM 4-hydroxyethylpiperazineethanesulfonic acid (Hepes), pH adjusted to 7.5 by 4M NaOH, 2 mM 1,4-dithiothreitol, 10 mM magn...

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Abstract

The invention discloses application of a polyphenolic compound. The polyphenolic compound shown in formula I can be used for preparing an mTOR inhibitor, especially an mTORC1 inhibitor. The invention further discloses application of the polyphenolic compound in the preparation of medicine for preventing and / or treating cancer, metabolic disorder syndrome, neurodegenerative diseases or inflammation. The diseases include diseases which are prevented and / or treated by inhibiting the catalytic activity of the enzyme of mTORC1. Preferably, the diseases include cancer, metabolic disorder syndrome, neurodegenerative diseases or inflammation. The polyphenolic compound can effectively inhibit the catalytic activity of the enzyme of mTOR and is good in curative effect on the cancer, metabolic disorder syndrome, neurodegenerative diseases or inflammation.

Description

technical field [0001] The present invention relates to the application of a polyphenolic compound. Background technique [0002] Mammalian target of rapamycin (mTOR) is an atypical highly conserved serine / threonine protein kinase, also known as FK506-binding protein 12 (FKBP12)-binding protein of rapamycin complex (FRAP ), or the target protein of rapamycin and FKBP12 (RAFT), which belongs to the phosphoinositide kinase-related protein kinase family (Phosphatidylinositol3-kinase (PI3K)-likekinase (PIKK) superfamily of kinases). In cells, it exerts its physiological activity mainly by forming two protein complexes with different functions, mammalian target of rapamycin complex 1 (mTORC1) and mammalian target of rapamycin complex 2 (mTORC2). mTORC1 contains mTOR, Raptor, Deptor, PRAS40 and mLST8, while mTORC2 contains mTOR, Riptor, Deptor, Protor, mSin1 and mLST8. The main function of mTORC1 is to regulate protein synthesis and cell cycle progression, while mTORC2 plays an ...

Claims

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Application Information

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IPC IPC(8): A61K31/343A61K31/216A61P35/00A61P3/00A61P25/00A61P29/00A61P35/02A61P9/12A61P3/10A61P3/04A61P25/14A61P25/16A61P25/28A61P19/02A61P17/06A61P1/16A61P11/00A61P13/12
Inventor 康经武张艳梅
Owner SHANGHAI INST OF ORGANIC CHEM CHINESE ACAD OF SCI
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