Application of naphthoquinone compounds

A compound and a technology of naphthoquinone are applied in the application field of naphthoquinone compounds in the preparation of anti-multidrug-resistant tumor drugs, and can solve the problems of necrosis-like morphological changes, inability to inhibit, cell membrane rupture and the like

Inactive Publication Date: 2008-08-06
ZHEJIANG UNIV
View PDF0 Cites 9 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] 2. Overexpression of multidrug resistance-associated protein (MRP)
[0016] 4. Overexpression of anti-apoptotic proteins Bcl-2 and Bcl-xL leads to apoptosis resistance of tumor cells
[0021] In 2005, Professor Yuan Junying of Harvard Medical School and her colleagues confirmed a new form of programmed necrosis - necroptosis, which has the following main characteristics: 1. Necrotic morphological changes, early Rupture of cell membrane; 2, mitochondrial membrane potential decline; 3, necrosis accompanied by autophagy; 4, the increase of intracellular reactive oxygen species is not the key factor of cell death; 5, this programmed necrosis can be specifically controlled by a Inhibited by a small molecule (necrostatin-1), and currently commonly used inhibitors cannot inhibit this death

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Application of naphthoquinone compounds
  • Application of naphthoquinone compounds
  • Application of naphthoquinone compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0087] Example 1: The ability of naphthoquinone compounds to kill tumor cells is not affected by P-gp

[0088] Experimental Materials:

[0089] K562, MCF-7 / wt cell lines are all from American Type Culture Collection (ATCC) company. The drug-resistant cell lines K562 / ADR and MCF-7 / ADR were obtained from the drug induction screening of this research group. Naphthoquinone compounds were purchased from Tokyo Chemical Industry Co., Ltd., Japan. 3-(4,5-Dimethyl-2-thiazole)-2,5-diphenyltetrazolium bromide (MTT) was purchased from Sigma.

[0090] experimental method:

[0091] The IC of naphthoquinone compounds against K562, MCF-7 / wt and their corresponding P-gp high-expressing resistant strains K562 / ADR, MCF-7 / ADR 50 Calculation. After different concentrations of naphthoquinone compounds act on cells for 72 hours, the IC is calculated by MTT method 50 .

[0092] Experimental results:

[0093] After 72 hours of drug action, the IC50 of naphthoquinone compounds against drug-resistant cell l...

Embodiment 2

[0096] Example 2: The ability of naphthoquinone compounds to kill tumor cells is not affected by MRP1

[0097] Experimental Materials:

[0098] The HL60 cell line was purchased from American Type Culture Collection (ATCC) company. The drug-resistant cell line HL60 / ADR is the result of drug induction and screening of this research group. Naphthoquinone compounds were purchased from Tokyo Chemical Industry Co., Ltd., Japan. 3-(4,5-Dimethyl-2-thiazole)-2,5-diphenyltetrazolium bromide (MTT) was purchased from Sigma.

[0099] experimental method:

[0100] The IC of naphthoquinone compounds against HL60 and its corresponding MRP1 resistant strain HL60 / ADR 50 Calculation. After different concentrations of naphthoquinone compounds act on cells for 72 hours, the IC is calculated by MTT method 50 .

[0101] Experimental results:

[0102] After 72 hours of drug action, the IC of naphthoquinone compounds on the parent cell line and drug-resistant cell line 50 It is very close, some even lower...

Embodiment 3

[0105] Example 3: The ability of naphthoquinone compounds to kill tumor cells is not affected by BCRP

[0106] Experimental Materials:

[0107] The MCF-7 / wt cell line and its drug-resistant cell line MCF-7 / mx were purchased from American Type Culture Collection (ATCC) company. Naphthoquinone compounds were purchased from Tokyo Chemical Industry Co., Ltd., Japan. 3-(4,5-Dimethyl-2-thiazole)-2,5-diphenyltetrazolium bromide (MTT) was purchased from Sigma.

[0108] experimental method:

[0109] IC of naphthoquinone compounds against MCF-7 / wt and its corresponding BCRP high-expressing resistant strain MCF-7 / mx 50 Calculation. After different concentrations of naphthoquinone compounds act on cells for 72 hours, the IC is calculated by MTT method 50 .

[0110] Experimental results:

[0111] After 72 hours of drug action, the IC of naphthoquinone compounds against drug-resistant cell lines 50 They are basically lower than the parent cell lines, indicating that these compounds can overcome...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

PropertyMeasurementUnit
molecular weightaaaaaaaaaa
Login to view more

Abstract

The invention provides application of naphthoquinones compound in preparing multidrug resistant tumor drug. The naphthoquinones compound is extracted or synthesized from gromwell plant by the prior art; the effective components of the naphthoquinones compound comprise iso-alkannin which is antimer of the gromwell and derivatives thereof. The naphthoquinones compound can take effect on the multidrug resistant tumor cells without being influenced by such tumor drug-resistant proteins as P-gp, MRP1 and BCRP, etc. and high expressions of anti-apoptotic proteins of Bc1-2 and Bc1-XL; the compound has lethal effects on the multidrug resistant tumor cells obviously superior to the presently common used and typical tumor resistant drugs; the lethal effects of the naphthoquinones compound on the multidrug resistant tumor cells is consistent with the parent drug-sensitive cells; the naphthoquinones compound is low toxic and has promising clinical application prospect therefore.

Description

Technical field [0001] The invention belongs to the use of the effective ingredients of traditional Chinese medicine, and mainly relates to the application of naphthoquinone compounds in the preparation of drugs with anti-multidrug resistance tumor effects. Background technique [0002] Comfrey is distributed in most provinces and regions in my country. It has anti-inflammatory, astringent and antipyretic effects. Its root is used in medicine and has been used clinically with definite curative effect. Comfrey was first recorded in "Shen Nong's Materia Medica" as a traditional Chinese medicine for measles prevention and treatment. Shikonin is the main ingredient of anti-inflammatory. Comfrey is rich in shikonin and its derivatives, its content accounts for 3 to 6.5%, the color is deep red, the chemical structure is naphthoquinones, and it can transmit mesons in the oxidation-reduction reaction in the organism. It has hemostatic, anti-inflammatory, antibacterial, antiviral and anti...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/22A61K31/122A61K31/341A61P35/00
Inventor 胡汛宣嫣艳
Owner ZHEJIANG UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap