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Medicinal application of chromone compound

The technology of a compound and chromone, applied in the field of medicine, can solve the problems of heavy financial burden on patients and the high price of targeted therapy drugs, and achieve high-efficiency anti-tumor activity

Inactive Publication Date: 2013-06-19
KUNMING UNIV OF SCI & TECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, most of the targeted drugs entering clinical application are developed by foreign pharmaceutical companies. These targeted drugs are expensive and cause a heavy economic burden to patients.

Method used

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  • Medicinal application of chromone compound
  • Medicinal application of chromone compound
  • Medicinal application of chromone compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Embodiment 1: the extraction separation of chromone compound

[0020] In September 2008, Yunnan cohosh was collected from Yangla Township, Daocheng County, Sichuan Province ( Cimicifuga yunnanensis 1.5Kg of aerial part sample, the plant species name was identified by researcher Qiu Minghua from Kunming Institute of Botany, and the crude drug specimens are deposited in State Key Laboratory of Phytochemistry and Western Plant Resources Sustainable Utilization, Kunming Institute of Botany, Chinese Academy of Sciences (KUN No. 200809007).

[0021] Crush 1.5Kg of the aerial part of Cimicifuga yunnanensis, soak and extract with 95% methanol (5L) at room temperature for 3 times, each time for 1 day; combine the extracts, concentrate under reduced pressure at 50°C until no methanol is evaporated, and obtain 137.8g of extract , extract (137.8g) mixed with 250g silica gel, normal pressure forward silica gel (2000g) column chromatography, chloroform-methanol (100:0, 50:1, 20:1,...

Embodiment 2

[0030] Example 2: Antitumor activity experiment of chromone compound KY12

[0031] 1. Construction of screening cells: wild-type mice were used as carriers, and p53 gene-deleted mouse embryonic fibroblasts (p53 - / - cells) to construct mouse tumor cells (p53 - / - +S+Ras, p53 - / - +V+Ras), the specific steps are as follows:

[0032] (1) Construction of vectors for Ras mutant genes and vectors expressing p53S mutant genes

[0033] For the construction method of the vector, see the method in patent ZL200910095184.3, that is, the p53S or Ras mutant gene cDNA is connected into the PQCXIP vector by conventional genetic engineering methods, and the p53S or Ras sequence constructed in the vector is verified by sequencing. The vector used in p53 - / - The p53S or Ras mutant gene is introduced into the cells.

[0034] (2) Transfection of p53S or Ras mutant gene vector

[0035] (a) Preparation of phoenix cells

[0036] The day before transfection, phoenix cells (human embryonic kid...

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Abstract

The invention discloses new application of a chromone compound KY12 in preparation of a targeted anti-tumor medicament. Experimental results show that the compound KY12 can selectively kill tumor cells with tumor specific mutant genes p53 and Ras under the concentration which is nontoxic for wild normal mouse embryo fibroblasts, namely the compound has application potential for preparing the personalized treatment medicament for the tumor specific mutant genes p53 and Ras.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to the application of a chromone compound in the preparation of targeted antitumor drugs. Background technique [0002] Tumor is a kind of fatal disease that seriously threatens human health. Its pathogenesis has not been fully elucidated, and the treatment effect is not satisfactory. Most of the drugs currently routinely used in tumor therapy are designed for the regulation of DNA replication or cytoskeleton in the process of cell proliferation. While these drugs kill rapidly proliferating tumor cells, they are also highly toxic to normal proliferating cells (such as bone marrow stem cells, etc.) On the contrary, the resistance of the tumor decreases, and it is difficult to obtain a good therapeutic effect. Therefore, using molecular targeted screening technology, targeting tumor cell-specific gene mutation products, screening small molecular compounds that can inhibit the act...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61P35/00
Inventor 吴晓明邱明华张继虹年寅唐文如王海燕罗瑛陆思千贾舒婷
Owner KUNMING UNIV OF SCI & TECH
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