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Antibiotic effective ingredient and use thereof

A technology of active ingredients and antibacterial drugs, applied in the determination of antibacterial active ingredients and its application field, can solve the problems of reducing bacterial pathogenicity and drug resistance of pathogenic bacteria, so as to reduce pathogenicity and drug resistance Effect

Inactive Publication Date: 2009-03-18
NORTHWEST UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0008] Aiming at the problem of existing antibiotic resistance, the purpose of the present invention is to use the constructed QSI antibacterial drug screening system to screen Epimedium drug components, determine a kind of antibacterial active ingredient, and simultaneously propose Dihuoside A and its derivatives As the lead compound of antibacterial drugs in clinical application, the antibacterial ingredients can reduce the pathogenicity of bacteria without killing bacteria, and reduce the drug resistance of pathogenic bacteria

Method used

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  • Antibiotic effective ingredient and use thereof
  • Antibiotic effective ingredient and use thereof
  • Antibiotic effective ingredient and use thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0017] (1) The validity test of the constructed screening system and the working mode of the screening system with a multi-well plate.

[0018] Two reporter systems, PAOD100 (pKD-lasI) and PAOD100 (pKD-rhl), were used in a multi-well plate to screen traditional Chinese medicine ingredients. The screening of quorum sensing inhibitors (QSI) was carried out in a multi-well plate with transparent bottom using the M9 liquid medium containing Tmp antibiotics; the reporter strains PAOD100 (pKD-rhlA) and PAOD100 (pKD-lasI) culture liquid were inoculated into In a multi-well plate, add test sample, methanol or water control to each well, and cover with sterile mineral oil or transparent plastic film; the multi-well plate is shaken intermittently on a Wallac Victor 1420 multi-label analyzer, and its growth is measured every half an hour (OD 600 ) and luminescence value (CPS); if the sample contains QSI, the luminescence value will drop significantly. Analysis of the rough screening re...

Embodiment 2

[0027] Dihuoside A can be extracted by combining existing methods (Chinese Journal of Pharmaceutical Sciences 1996, 31(6): 332-334). Studies have shown that the distribution of bihuoside A in different parts of Epimedium is root>stem>leaves. Extracting bihuoside A from Epimedium includes leaching, impurity removal, extraction, multi-step elution through the column, Drying in five steps; icariin extract or total flavonoids extract of Epimedium can also be purchased, followed by silica gel and Sephadex column chromatography for separation. The extraction is based on ethanol solution as the extraction solvent, dichloromethane or dichloroethane as the impurity-removing solvent, dichloromethane, ethyl acetate and n-butanol for extraction and concentration respectively, and the ethyl acetate and n-butanol parts are combined. Silica gel column (100-200 mesh) for separation, chloroform, methanol gradient elution, the same fractions were combined, and the eighth part was separated by s...

Embodiment 3

[0029] The dihuoside A screened by the present invention is used as an antibacterial active ingredient, and its effective concentration is in the range of 40 μg / ml to 200 μg / ml; the effective dosage is 50 mg / l, and the reference dosage of a drug can be calculated according to the adult standard body weight of 50 kg. Contains 60% body fluid, 40% is intracellular fluid, 20% is extracellular fluid, and 5% of body weight in extracellular fluid is plasma, 15% is tissue fluid; that is, the time required to achieve this effective concentration in blood The reference dosage of the drug is 50kg×5%×50mg / l=125mg, but taking into account individual differences, administration methods and dosage forms, the dosage for a single oral or injection should be in the range of 1mg / kg-8mg / kg. Dihuoside A is soluble in water or organic solvents and can be made into tablets, pills, powders, granules for direct oral or sublingual or rectal administration. It can also be used for inhalation therapy. Inj...

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Abstract

The invention relates to an anti-bacterial active ingredient and an application thereof, the invention is a diphylloside A and the derivatives thereof which are determined through a QSI anti-bacterial drug screening system, the diphylloside A and the derivatives thereof can reduce the pathogenicity of bacteria on the premise of not killing the bacteria, belong to components of flavonoids and are derived from epimedium Chinese herbal medicines. As a bacterial quorum sensing system QS is participated in the regulation of the pathogenicity of pathogenic bacteria, the diphylloside A has the role of inhibiting the QS system and reducing the pathogenicity of the pathogenic bacteria of the QS system and is a broad-spectrum antibiotic drug; the diphylloside A can also be used for treating and preventing crop diseases and insect pests as a pesticide; the diphylloside A and the derivatives thereof are taken as lead compounds of anti-bacterial drugs, thereby developing novel anti-bacterial drugs to be applied in clinical and agricultural production; the diphylloside A and the derivatives thereof have the advantages of no drug resistance, easy obtainment of raw materials, easy preparation method and no toxicity or side effect, thereby having great significances for human health and agricultural production.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to the determination and application of an antibacterial active ingredient of a Chinese medicinal material. Background technique [0002] Traditional antibiotics refer to a class of substances and their derivatives produced by bacteria, molds or other microorganisms in the process of reproduction and metabolism, which can kill or inhibit other microorganisms, and are used to treat sensitive microorganisms (usually bacteria or fungi) infection. Penicillin, as the earliest antibacterial drug, successfully solved the clinical problem of Staphylococcus aureus infection; the macrolide and aminoglycoside antibiotics that came out later reduced the mortality rate of pneumonia and tuberculosis by 80%. So far, various antibiotics discovered play a huge role in the treatment of infectious diseases, most of which are synthesized by microorganisms, and two-thirds are produced b...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61P31/04A01N43/16A01P7/00
Inventor 段康民王媛王玥
Owner NORTHWEST UNIV
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