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Application of carborane derivatives, nano compound preparation and application of nano compound preparation

A nano-composite and derivative technology, which is applied in the directions of boron compound active ingredients, medical preparations containing active ingredients, inorganic active ingredients, etc. and other problems, to achieve the effect of treating bacterial infection and good antibacterial activity

Active Publication Date: 2012-01-25
SOUTHEAST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since these three new carborane derivatives and their nanocomposite preparations were synthesized for the first time by our research group, there are no relevant reports on the antibacterial activity of the new carborane derivatives and their nanocomposite preparations in domestic and foreign patents and other documents.

Method used

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  • Application of carborane derivatives, nano compound preparation and application of nano compound preparation
  • Application of carborane derivatives, nano compound preparation and application of nano compound preparation
  • Application of carborane derivatives, nano compound preparation and application of nano compound preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1 The Minimum Inhibitory Concentration Test of Three Carborane Derivatives

[0025] 1.1 Preparation of test drugs: three carborane derivatives shown in structural formulas (1), (2) and (3) were respectively prepared into high-concentration mother solutions with dimethyl sulfoxide, and then diluted with double distilled water The concentration was 1600, 800, 400, 200, 100, 50, 25, 12.5, 6.25μg / mL. Test drugs were stored at -4°C. Before the experiment, the drug was taken out of the 37°C water bath and mixed, shaken well, and the pharmacodynamic experiment was carried out. In the experiment, the final concentration of DMSO should be strictly controlled below 0.5 % (v / v) to ensure that there is no cytotoxicity to the organism.

[0026] 1.2 Experimental strains and culture methods: Standard strains: Staphylococcus aureus (CGMCC1.89), Klebsiella pneumoniae (ATCC700600), Acinetobacter baumannii (ATCC19606), Proteus mirabilis (ATCC12453). Clinical resistant strains...

Embodiment 2

[0029] Example 2 Time-kill curves of three carborane derivative nanocomposite formulations against Staphylococcus aureus, such as figure 1 , 2 , 3.

[0030] Antibacterial characteristics of three carborane derivatives (1), (2), (3) nanocomposite formulations against clinically resistant Staphylococcus aureus strain SA321 were evaluated by time-killing curves. It was tested at different concentrations of 12.5, 25, 50, 100, 200 μg / mL. The bacterial suspension was added with the above-mentioned final concentration of drugs, and the bacterial suspension without drug was set as the control group, and then they were placed in a constant temperature incubator at 37°C for cultivation, and different time intervals were taken at 0, 4, 8, 12, The 16 and 24 h culture solution was counted on the plate colony, and the bactericidal activity was defined as greater than 3 times log compared with the control group 10 Decrease in CFU / mL. The test results showed that the relevant antibac...

Embodiment 3

[0031] Example 3 Comparative test of antibacterial percentage of three carborane derivatives and their nanocomposite preparations

[0032] The cell density is 2 x 10 5 CFU / mL standard strain GCMCC1.89 and bacterial suspension of clinical drug-resistant strain SA321 were added with different final concentrations (8, 16, 32 μg / mL) of compound (1), (2), (3) preparations, not The drug-dosed bacterial suspension was set as the control group, and then placed in a constant temperature incubator at 37°C for 24 hours, and the absorbance value at 600nm was measured with an ultraviolet spectrophotometer. Bacterial inhibition percentage=[1-(OD tested -OD blank ) / (OD control -OD blank )]×100.

[0033] The test results showed that there was no significant difference in the antibacterial percentage of the three carborane derivatives and their nanocomposite preparations against the sensitive and resistant strains of Staphylococcus aureus (P > 0.05). There was no significant differen...

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Abstract

The invention provides carborane derivatives and application thereof. The structural formulas of three relative novel carborane derivatives are shown as (1), (2) and (3), and antibacterial medicines used as active ingredients of a medicine have the effects of resisting clinically common pathogenic bacteria (staphylococcus aureus, acinetobacter baumannii, klebsiella pneumonia, and proteus mirabilis), and also have the same-degree effect of resisting multidrug-resistant staphylococcus aureus strains and can inhibit multidrug resistance of the multidrug-resistant staphylococcus aureus strains, wherein a compound (2) can react with medicine-resistant staphylococcus aureus extracellular proteins, so adhesion of bacteria on the surface of an organism is reduced, and the formation of a medicine-resistant strain biological film is inhibited. The toxicity and invasiveness of staphylococcus aureus are reduced, treatment efficiency is improved, an adverse effect caused by using a large amount ofantibiotics is avoided, and a novel compound is provided for finding a novel medicine for resisting medicine resistance bacteria.

Description

technical field [0001] The invention relates to the field of nano-medicine, in particular to carborane derivatives and nano-composite preparations thereof, which are pharmaceutical active ingredients or pharmaceutical compositions, their antibacterial effect, and their application in the development of antibacterial drugs. [0002] Background technique [0003] Antibacterial drugs generally refer to drugs that have bactericidal or bacteriostatic activity against pathogens at a certain concentration, including various antibiotics and chemically synthesized drugs. At present, the commonly used antibacterial drugs used in clinical practice in the world are mainly divided into eight categories according to their structure: β-lactams; aminoglycosides; tetracyclines; fluoroquinolones; folic acid pathway inhibitors; chloramphenicol; glycopeptides; Macrolides. Its main mechanisms of action are: interference with cell wall formation; inhibition of nucleic acid synthesis; inhibition...

Claims

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Application Information

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IPC IPC(8): A61K31/69A61P31/04A61K33/38
Inventor 王雪梅李水红燕红
Owner SOUTHEAST UNIV
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