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Red sage root water soluble ingredient derivative ERJT-12 and its application in cancer resistance

A ERJT-12, water-soluble technology, applied in the fields of anti-tumor drugs, drug combinations, organic chemistry, etc., to achieve the effect of novel structure, feasible synthesis method, and significant anti-tumor activity in vitro

Inactive Publication Date: 2006-07-19
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the content of the above compounds in Salvia miltiorrhiza is only 0.1×10 -6 Therefore, it is of great significance if new derivatives with outstanding anti-tumor activity can be designed, synthesized and screened based on this natural compound

Method used

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  • Red sage root water soluble ingredient derivative ERJT-12 and its application in cancer resistance
  • Red sage root water soluble ingredient derivative ERJT-12 and its application in cancer resistance
  • Red sage root water soluble ingredient derivative ERJT-12 and its application in cancer resistance

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0013] The synthesis of embodiment 1 compound ERJT-12

[0014] Dissolve 3.0mmol compound ERJT-11 in 10mL DMF, add 20mmol POCl dropwise at 0°C 3 , r.t. stirred for 20 minutes, heated and stirred at 95°C for 2 hours, poured the reaction solution into 30ml ice-water solution of 3.8g sodium acetate and 4.6g ammonium chloride, extracted with dichloromethane (15mL×3), washed with saturated aqueous sodium chloride solution (5mL×3), anhydrous NaSO 4 Dry, and use 100-200 mesh silica gel column chromatography, eluting with ethyl acetate:petroleum ether=1:2 to obtain the product ERJT-12.

[0015] The synthetic route of ERJT-12 is:

[0016]

[0017] ERJT-12 was a light yellow solid with a yield of 54%. The product was analyzed by elemental analysis, IR spectrum, 1 H NMR spectrum, MS spectrum determination. The analysis results are as follows:

[0018] Elemental analysis (calculated value / measured value) (%): C 65.63 / 65.89, H 5.21 / 5.25;

[0019] IR spectrum υ: 3442, 1729, 1642, 1...

Embodiment 2

[0022] The in vitro experiment of the compound described in embodiment 2 invention

[0023] (1) Compound anti-tumor cell proliferation experiment in vitro

[0024] The selected cell lines include: human breast cancer MCF-7, human lung adenocarcinoma GLC82, human ovarian cancer HeLa, gastric adenocarcinoma MGC803, bladder cancer ECV304, oral epithelial cancer KB-3-1 and leukemia CCRF / CEM cells. The tumor cells in the logarithmic growth phase were taken to make a certain concentration of cell suspension and inoculated in a 96-well plate. A certain concentration of ERJT-12 was added to each well, and no compound was added to the control well. After culturing for 72 hours, add a certain amount of MTT, continue culturing for 4 hours, discard the culture medium, add 200ul dimethyl sulfoxide to each well, measure the absorbance value at 570 / 630nm dual-wavelength with a microplate reader, and calculate the inhibition rate of 50% of the cell growth. Compound concentration (IC 50 ). ...

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Abstract

The disclosed ERJT-12 as the derivative of water-soluble constituent of radix salvia miltiorrhiza is composed by natural 5-(3-hydroxypropyl)-7-methoxy-2-(3-methoxy-4- hydroxy)-3-benzo[b] furaldehyde. Wherein, this compound takes microtubule as target, has obvious growth inhibition to multiple human tumor cells, can block the MCF-7 cell on mitosis time, and restrains the polymerization of tubulin.

Description

technical field [0001] The invention relates to a derivative of the water-soluble component of salvia miltiorrhiza and its application in the preparation of antitumor drugs. Background technique [0002] The traditional Chinese medicine Salvia miltiorrhiza is the dry root and rhizome of Salvia miltiorrhizae Bge., SM, which is bitter in nature and slightly cold in taste. Salvia miltiorrhiza is one of the most widely used traditional Chinese medicines in our country, and has a long history of clinical application. Salvia miltiorrhiza was first recorded in "Shen Nong's Materia Medica", and many herbal medicines have been recorded in successive dynasties. "The Pharmacopoeia of the People's Republic of China" (the first part of the 2000 edition) summarizes the functions and indications of Salvia miltiorrhiza as promoting blood circulation and dredging collaterals, dispelling blood stasis and relieving pain, cooling blood and eliminating carbuncle, clearing away heart trouble and...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D307/86A61K31/343A61P35/00
Inventor 冼励坚杨华庞冀燕许遵乐
Owner SUN YAT SEN UNIV
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