Application of flavonoids

A technology of flavonoids and compounds, applied in the application field of flavonoids, can solve the problems of cytotoxicity, low blood drug concentration, narrow anti-tumor spectrum, etc.

Inactive Publication Date: 2016-01-27
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 kind of application of flavonoids

Method used

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  • Application of flavonoids
  • Application of flavonoids
  • Application of flavonoids

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] 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:

[0060]

[0061]

[0062] The mTORC1 used in the examples was purchased from Sigma Reagent Co., Ltd., product number: SRP0364.

[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 magnesium chloride, 1 mM ethylene glycol bis(2 -aminoethyl ether) tetraacetic acid, 0.01% (v / v, the same below) Tween 20 and 3mM manganese chloride.

[0064] Use 2 μL of enzyme re...

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Abstract

The invention discloses application of flavonoids. As shown in formula I, the flavonoids can be used for preparing an mTOR inhibitor, and in particular an mTORC1 inhibitor. The invention discloses application of the flavonoids in preparing medicines for preventing and / or treating cancers, metabolic disorder syndrome, neurodegenerative disease or inflammation. The diseases are prevented and / or treated by inhibiting the catalytic activity of enzyme of the mTORC1 in the field, and preferably the diseases are cancers, metabolic disorder syndrome, neurodegenerative disease or inflammation. The flavonoids disclosed by the invention can be used for effectively inhibiting the catalytic activity of the enzyme of the mTOR, and can show a good curative effect on cancers, metabolic disorder syndrome, neurodegenerative disease or inflammation.

Description

technical field [0001] The invention relates to the application of a flavonoid 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 important r...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61K31/7048A61P35/00A61P35/02A61P3/00A61P25/00A61P29/00A61P9/12A61P3/10A61P9/10A61P3/04A61P25/28A61P19/02A61P17/06A61P1/16A61P11/00A61P13/12A61P25/14A61P25/16
Inventor 康经武张艳梅
Owner SHANGHAI INST OF ORGANIC CHEM CHINESE ACAD OF SCI
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