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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
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  • 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

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  • Application of naphthoquinone compounds
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  • 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...

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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

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/22A61K31/122A61K31/341A61P35/00
Inventor 胡汛宣嫣艳
Owner ZHEJIANG UNIV
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