A kind of baicalein activity probe and its synthesis method and application

A synthetic method and technology of baicalein, applied in the field of chemical biology, can solve the problems of unclear and indistinguishable anti-cancer mechanism of baicalein

Active Publication Date: 2020-12-25
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

This strategy may fail to distinguish whether the found "anti-cancer mechanism" is the "cause" of baicalein's anti-cancer effect or the "consequence" of its anti-cancer effect
Many speculations reflect that the anti-cancer mechanism of baicalein is actually not clear

Method used

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  • A kind of baicalein activity probe and its synthesis method and application
  • A kind of baicalein activity probe and its synthesis method and application
  • A kind of baicalein activity probe and its synthesis method and application

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Experimental program
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Effect test

Embodiment 1

[0034]1. Baicalein’s "precise anti-cancer" cell and animal model experiments:

[0035]The applicant has performed proliferation inhibition experiments of baicalein on the immortalized normal liver cell line L-02, liver cancer cell lines HuH7 and HepG2, and calculated the IC50 value. It turns out that asfigure 1 As shown, the cytotoxicity of baicalein to the normal liver cell line L-02 is significantly less than that of the liver cancer cell lines HuH7 and HepG2. In addition, the applicant established a diethylnitrosamine-induced mouse liver cancer model, and then intervened with baicalein, and found that baicalein has a significant therapeutic effect on liver cancer mice, and it has a significant therapeutic effect on normal mice given the same dose. It did not show liver toxicity and did not cause weight loss in mice. Therefore, it can be considered that baicalein is safe to the liver and the whole of mice while showing obvious anti-cancer activity.

[0036]2. Synthesis and bioequivalenc...

Embodiment 2

[0046]1. Cell culture:

[0047]Hela, HepG2, HuH7 cells (from the Chinese Type Culture Collection (Wuhan, China)) 37°C, 5% CO2Cultured in Dulbecco's modified Eagle medium (DMEM, Thermo Fisher Scientific) supplemented with 10% fetal bovine serum (Thermo Fisher Scientific) and 1% penicillin-streptomycin (Thermo Fisher Scientific).

[0048]2. RNA interference

[0049]The siRNA constructs listed below were designed and synthesized by GenePharma (Shanghai, China). In the modeling stage before baicalein treatment, based onRNAiMAX (Thermo Fisher Scientific) protocol for interference.

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Abstract

The invention discloses a baicalein active probe, and provides a synthetic method and application of the baicalein active probe. The active probe uses baicalein as a reaction group, uses diethyleneimine as a photocrosslinking group, and uses alkynyl as a biologically orthogonal group. A structural formula is as follows: (Please see the specification for the formula). The baicalein active probe hasthe beneficial effects that (1) an anticancer mechanism based on a cell oxidative phosphorylation pathway is a novel anticancer mechanism, and is possible to achieve the effect of selectively killingcancer cells; (2) baicalein is the first discovered activator of the cell oxidative phosphorylation pathway; and (3) key proteins ATP4A(P20648), ATP5A1(P25705), ATP5F1(P24539), ATP5L(O75964), ATP6V1A(P38606), ATP6V1H(Q9UI12), ATP12A(P54707) and NDUFA13(Q9P0J0) in the cell oxidative phosphorylation pathway are targets for the development of novel anticancer drugs.

Description

Technical field[0001]The invention relates to the technical field of chemical biology, in particular to a baicalein active probe and its synthesis method and application.Background technique[0002]Cancer has always been the enemy of mankind. According to the latest statistics of the World Health Organization (http: / / gco.iarc.fr / today), in 2018 alone, there were 18 million cancer patients worldwide and more than 9 million deaths due to cancer; 4.2 million cancer patients in my country , The death toll from cancer exceeds 2.8 million. In particular, the number of liver cancer patients and deaths in my country has exceeded 50% of the world's liver cancer incidence and deaths. It is estimated that by 2030, the number of deaths due to liver cancer in my country will exceed 600,000 each year. The most effective treatment for liver cancer is liver transplantation, but because of the high cost of surgery and the scarcity of suitable donors, its clinical application is greatly limited (Forner...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D405/12A61K31/396A61P35/00
Inventor 王初戴建业
Owner PEKING UNIV
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