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Application of deoxyshikonin

A technology of deoxyshikonin and its use, applied in the field of medicine

Inactive Publication Date: 2014-03-12
CHONGQING MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005]Deoxyshikonin (5,8-dihydroxy-2-(4-methyl-3-phenyl)-1,4-naphthalenedione) Purchased from Bailingwei Technology Co., Ltd. (http: / / wwwjkchemical.com / ), it has been reported that deoxyshikonin has anticancer activity, (Rajasekar S, et al, J Ethnopharmacol.2012Nov21; 144(2): 335-45. ) and can induce the apoptosis of human promyelocytic leukemia cells (YoonY, et al, PlantaMed.1999Aug; 65(6):532-5.) (Wang R, Expert Opin Ther Pat.2012Sep; 22(9): 977 -97.) But so far there is no report of this drug as an antibacterial agent1

Method used

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  • Application of deoxyshikonin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1: In vitro kinase activity test of traditional Chinese medicine monomers.

[0022] Kinase-Glo provided by promega company was used in in vitro kinase activity assay Plus Luminescent Kinase Assay kit, the experimental steps are strictly in accordance with the instructions attached to the kit. Proceed as follows:

[0023] 1. Main reagents and instruments:

[0024] ATP was purchased from Sigma;

[0025] Plus Luminescent Kinase Assay was purchased from Promega Company Cat#V3772:

[0026] Enzyme reaction buffer: 40mM Tris-HCl[pH7.5], 20mM MgCl2, 0.1mg / ml BSA;

[0027] The microplate reader is Tecan GENios; the microplate plate is costar R solid white, fiat-bottom96-well plates; electric heating constant temperature water bath: Beijing Changan Scientific Instrument Factory HH-W21CY600 type.

[0028] 2. Experimental steps:

[0029] Detect the inhibitory effect of the traditional Chinese medicine monomer concentration of 200 μM on VicK kinase:

[0030] 100...

Embodiment 2

[0044] The mensuration of embodiment 2 minimum inhibitory concentration (MIC, minimal inhibitory concentration) and minimum bactericidal concentration (MBC, minimal bactericidal concentration)

[0045] 1. MIC adopts micro broth dilution method

[0046] 1) Aseptic operation, add antibacterial drug solutions of different concentrations after doubling dilution to a sterilized 96-well polystyrene plate, add drug solution to the 1st to 11th wells, 10 μl per well, and do not add to the 12th well drug as a growth

[0047] According to the same time as DMSO control.

[0048] 2) Dilute the bacterial suspension prepared by the growth method or the direct bacterial suspension method with a concentration equivalent to 0.5 McFarland turbidimetric standard to 1:1000 in the broth, add 200 μl to each well, seal it and place it in the normal room at 37°C. In the air incubator, incubate for 16-20h to judge the result.

[0049] 3) Judging the results, the minimum drug concentration that compl...

Embodiment

[0055] Embodiment: 3 Chinese medicine monomers are to the bacteriostasis of Staphylococcus aureus (step is with embodiment 2)

[0056] Table 4: Inhibitory effects of deoxyshikonin and PNC (penicillin) on Staphylococcus aureus

[0057]

[0058] ATCC29213, 8506305, 8569082, and 854899 were all from the Laboratory Department of Chongqing Children's Hospital, and were identified as Staphylococcus aureus by BD's PHOENIX-100 automatic microbial identification instrument.

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Abstract

The invention discloses application of deoxyshikonin (5,8-dihydroxy-2-(4-methyl-3-phenyl)-1,4-naphthalenedione) as a histidine kinases VicK inhibitor in vitro or to preparation of the histidine kinases VicK inhibitor. Deoxyshikonin exerts certain antibacterial action on in-vivo streptococcus pneumonia and clinical penicillin-resistant streptococcus pneumonia; moreover, combined deoxyshikonin and penicillin exert a good antibacterial effect on streptococcus pneumonia and has substantial bacteriostatic action on staphylococcus aureus.

Description

technical field [0001] This study involves the field of medical technology, specifically the traditional Chinese medicine monomer deoxyshikonin (5,8-dihydroxy-2-(4-methyl-3-phenyl)-1,4-naphthalenedione) as histidine Use of Acid Kinase VicK Inhibitors. Background technique [0002] The two-component system (TCS) is the main signal transduction system in bacteria. It not only participates in the basic life activities of bacteria, but more importantly, it is closely related to the pathogenicity and drug resistance of many pathogenic bacteria. Bacterial TCS systems have the following two characteristics: Histidine kinases and response regulators in different types of bacteria have obvious homology, especially the amino acid residues in the active center, so this system regulation method is common in bacteria sex. The TCS regulatory system is unique to bacteria (mainly Gram-positive bacteria and a few Gram-negative bacteria), and mammals do not have this signal transduction mec...

Claims

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Application Information

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IPC IPC(8): A61K31/122A61K31/43A61P31/04
Inventor 尹一兵张雪梅张帅胥文春刘宇思
Owner CHONGQING MEDICAL UNIVERSITY
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