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Diazeniumdiolate Schiff base copper complex, preparation method and biological activity

A technology of diazenium diol and copper complex, which is applied in the field of biomedicine and can solve problems such as sequence-specific DNA fragmentation

Active Publication Date: 2020-10-23
CHANGSHA CHARISM BIOSCIENCES CO LTD +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The oxidative breakage of DNA by metal complexes can be divided into breakages targeting sugar rings and breakages targeting bases according to the breakage site. Although the oxidation of breakages targeting bases cannot directly cause DNA strand breaks, it does Under the action of alkali, heat, enzymes, etc., site-specific and even sequence-specific DNA fragmentation will eventually occur
There are no reports of natural copper ion complexes containing diazeniumdiolate

Method used

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  • Diazeniumdiolate Schiff base copper complex, preparation method and biological activity
  • Diazeniumdiolate Schiff base copper complex, preparation method and biological activity
  • Diazeniumdiolate Schiff base copper complex, preparation method and biological activity

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Preparation of copper complexes:

[0053] Strain Streptomyces sp. CB00271 was grown in a 250 mL flat-bottomed flask containing 50 mL of tryptic soy broth. The fermentation medium contains 15g of soluble starch per liter, 5g of cottonseed powder, CuSO 4 0.1g, NaI5mg, CaCO 3 2 g, adjust the pH to 7.0 before autoclaving. The seed culture (10vol%) was transferred to the fermentation medium and cultivated at 30°C and 230-250 rpm for 7 days, while adding macroporous adsorption resin HP20 or DA201-H to the fermentation medium (the amount of resin added 3g per 100mL fermentation broth).

[0054] The resin was separated by centrifugation with H 2 O washed and dried in air at room temperature. It was then eluted three times each with 3 L of MeOH and concentrated under vacuum. In 2L PE:H 2 O(1:1) and 3L EtOAc:H 2 O (1:1) was extracted three times to obtain ethyl acetate soluble fraction. The ethyl acetate soluble extract was then concentrated in vacuo to give a crude ex...

Embodiment 2

[0074] Cytotoxic activity test of GE1:

[0075] The GE1 of the present invention is now tested for its anti-tumor activity in vitro on four different types of tumor cell lines B16-F10, 4T1, A549, and KPL-4. Cytotoxicity of GE1 was assessed by the CCK8 assay. The Cell Counting Kit, referred to as CCK kit, is a WST-8 (chemical name: 2-(2-methoxy-4-nitrophenyl)-3-(4-nitrophenyl)-5-(2, 4-disulfophenyl)-2H-tetrazolium monosodium salt) is a rapid and highly sensitive detection kit widely used in cell proliferation and cytotoxicity. WST-8 is an upgraded product of MTT, and its working principle is: in the presence of electron coupling reagents, it can be reduced by dehydrogenase in mitochondria to generate highly water-soluble orange-yellow formazan; the color depth It is directly proportional to cell proliferation and inversely proportional to cytotoxicity; the absorbance value is measured at a wavelength of 450nm using a microplate reader, which indirectly reflects the number of ...

Embodiment 3

[0079] In vitro antibacterial activity test of GE1:

[0080] GE1 of the present invention can be used to treat bacterial infections.

[0081] Test GE1 against standard Staphylococcus aureus (Staphylococcus aureus ATCC 29213), Staphylococcus aureus (Staphylococcus aureus 115), Micrococcus luteus (Micrococcus luteus ATCC10240), Bacillus subtilis (Bacillus subtilis CMCC 63501) and Escherichia coli (Escherichia coli ) antibacterial activity. The minimum inhibitory concentration (MIC) was determined using the broth microdilution method. Strains were grown overnight and diluted to 10 in Mueller-Hinton broth 6 CFU / mL. Dissolve GE1 in DMSO and serially dilute to 8 concentrations (0.25, 0.5, 1, 2, 4, 8, 16, 32 μg / mL) on each 96-well plate. Vancomycin was dissolved in DMSO and serially diluted to 8 concentrations (0.125-16 μg / mL) on each 96-well plate. Mix 50 μL of GE1 or vancomycin and 50 μL of bacteria solution in each well. Vancomycin and untreated medium served as positive and...

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Abstract

The invention relates to the technical field of biological medicines, in particular to a diazeniumdiolate Schiff base copper complex with a novel structure and a preparation method of the diazeniumdiolate Schiff base copper complex. Meanwhile, preliminary in-vitro test is carried out on the biological activity of the diazeniumdiolate schiff base copper complex, and it is found that the diazeniumdiolate schiff base copper complex has obvious cytotoxic activity and gram-positive bacterium resisting activity. The diazeniumdiolate Schiff base copper complex disclosed by the invention is a naturalcopper complex containing diazeniumdiolate discovered for the first time, has a good application prospect in the field of biological activity, and can be used as a potential anti-cancer drug and a novel antibacterial agent.

Description

technical field [0001] The invention relates to a novel natural copper ion complex, a preparation method and its anti-tumor application, and belongs to the technical field of biomedicine. Background technique [0002] Copper is an essential trace element in fundamental biological processes in living cells, an essential catalytic cofactor for proteins, and a catalyst for redox cycles. The importance of copper homeostasis in humans is illustrated by the devastating consequences of two genetic disorders, the Menkes and Wilson (WD) diseases, which lead to systemic copper deficiency or overload, respectively. Copper ion complexes can act as proteasome inhibitors, superoxide dismutase mimics, DNA intercalators, and inducers of apoptosis by promoting the production of reactive oxygen species ROS. Copper(I) has an affinity for thioether and thiol groups, while copper(II) preferentially coordinates oxygen or imidazole nitrogen groups and interacts with protein structures, regulates ...

Claims

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Application Information

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IPC IPC(8): C07D413/14A61K31/555A61P35/00A61P31/04C12P17/16C12R1/465
CPCC07D413/14A61P35/00A61P31/04C12P17/16C07B2200/13
Inventor 段燕文黄勇龚邦
Owner CHANGSHA CHARISM BIOSCIENCES CO LTD