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Method for determining binding constants of echinocandins medicine and protein

A technology of echinocandins and binding constants, which is applied in the field of determination of echinocandin drugs and protein binding constants, can solve the problems of inaccuracy, long measurement and analysis time, shorten analysis time and reduce electrolyte dissociation Effect

Inactive Publication Date: 2014-08-20
TIANJIN UNIV
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Problems solved by technology

[0007] In order to solve the problems existing in the prior art, the present invention provides a method for determining the binding constant between echinocandin drugs and proteins, which overcomes the long and inconvenient time for the determination and analysis of the binding constant between receptor ligands in the prior art. Accurate problem, successfully determined the binding constant of echinocandin B (ECB) and protein, which has a certain reference value in the process of drug research, and this method can also be used for the interaction between other echinocandin drugs and proteins, It can be extended to other ligand-receptor interactions

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  • Method for determining binding constants of echinocandins medicine and protein
  • Method for determining binding constants of echinocandins medicine and protein

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Embodiment

[0035] Determination of the Binding Constant of Echinocandin B and BSA

[0036] (1) Using capillary electrophoresis equipment, wash the capillary successively with 0.1M sodium hydroxide aqueous solution, water, and 20mM Tris-phosphate buffer solution with pH=7.4, and then fill the capillary with buffer or fill with 1, 2, 3 , 4 and 5 μM bovine serum albumin (BSA) buffer solution, use the following steps (2)-(7) to measure the effective electrophoretic mobility μ of echinocandin B in the buffer solution respectively 0 , and the effective electrophoretic mobility μ of echinocandin B in the above-mentioned series of buffers with BSA concentrations 1 ;

[0037] (2) The first sample injection: the method of air pressure injection (0.5psi) is used to inject the sample into the capillary for 3 seconds, and the injected sample contains echinocandin B and the neutral marker N, N- Mixtures of dimethylformamide (DMF);

[0038] (3) Propelling of the sample: insert the capillary sampling...

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Abstract

The invention discloses a method for determining binding constants of an echinocandins medicine and protein. Aiming at a hotspot echinocandins medicine developed from an existing antifungal medicine, the pressure-driven affinity capillary electrophoresis method is used for rapidly and accurately determining the binding constants of a receptor and a ligand; the binding of ECB (Echinocandins B) and BSA (Bull Serum Albumin) is determined, effective electrophoresis mobility of ECB in protein buffering solutions with different concentration can be accurately determined, and then the binding constants are calculated. The method is used for determining the binding of ECB and BSA so as to determine that ECB belongs to a strong binding type medicine; the method provides data support on knowing medicine effect expression of the echinocandins medicine and provides optimization evidences to subsequent data screening.

Description

technical field [0001] The invention relates to the field of drug screening, in particular to a method for determining the binding constant of echinocandin drugs and proteins. Background technique [0002] The pharmacokinetic characteristics of new drugs obtained through drug screening in the human body are decisive for their success in the market, and the binding strength of drugs to proteins can directly affect their transportation, distribution, and metabolism in vivo , and its efficacy and the generation of toxic and side effects. After the organism ingests the drug, it will enter the blood circulation of the organism and combine with blood components such as albumin, α-globulin, β-globulin, γ-globulin or red blood cells. In the serum, the drug effect is stable It is related to the concentration of free drugs in serum. In pharmacology, it is generally believed that only free drugs can pass through the cell membrane through diffusion or carrier transport, and reach the a...

Claims

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Application Information

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IPC IPC(8): G01N27/447
Inventor 李优鑫包建民高赫男孟晓璐
Owner TIANJIN UNIV
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