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Aldosterone derivative and preparation method thereof

An aldosterone and derivative technology, applied in the field of aldosterone derivatives and their preparation, can solve the problems of complete antigen stability and homogeneity, complete antigen specificity and poor immunogenicity, difficult to form site-specific cross-linking, etc., and achieve linear improvement. , Overcome differences in affinity, and promote the effect of popularization

Active Publication Date: 2019-04-05
GUANGDONG FAPON BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The purpose of the present invention is to solve the problem that the aldehyde group of aldosterone is unstable and easily produces side reactions, resulting in poor specificity and immunogenicity of the corresponding complete antigen; there are too many active groups of aldosterone, two hydroxyl groups, one ketone, and one aldehyde group, It is difficult to form site-specific cross-links when cross-linking with carrier proteins, resulting in the stability and homogeneity of the final complete antigen being affected

Method used

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  • Aldosterone derivative and preparation method thereof
  • Aldosterone derivative and preparation method thereof
  • Aldosterone derivative and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0099] Synthesis of MBHA resin with specific functional groups

[0100] 1. Weigh 100mg of MBHA resin (1) (sigma, 200-400 mesh, 0.5-1.0mmol / g), add 10ml of DMF (Chinese medicine) to dissolve, blow nitrogen or argon into the solution, and control the flow rate of the resin by adjusting the airflow Mixing degree, add 0.3mmol Fmoc-Thr-OH (Shanghai Jill), 0.6mmol EDC.HCl (sigma), 0.6mmol HOBT (Shanghai Jill), 1.8mmol DIPEA (Sinopharm), mix well, and react at room temperature for 1h.

[0101] 2. Stop the reaction, remove the reaction solution by filtration, wash twice with DMF, add 5ml DMF, 0.1mmol acetic anhydride and 0.3mmol DIPEA, and react at room temperature for 10min.

[0102] 3. Stop the reaction, remove the reaction solution by filtration, wash twice with DMF, add 10ml of 20% piperidine / DMF, and react at room temperature for 30min.

[0103] 4. Stop the reaction, remove the reaction solution by filtration, and wash twice with DMF to obtain MBHA resin (2) with specific functi...

Embodiment 2

[0107] Aldosterone Conjugated MBHA Resin

[0108] 1. Configure 10ml of a mixed solution of MeOH:DCM:DMF:AcOH=30:3:2:0.35, add to the MBHA resin (2) with specific functional groups obtained in the above steps, blow nitrogen or argon into the reaction solution, and pass Adjust the air flow to control the mixing degree of the resin, add 0.3mmol aldosterone, and react at room temperature.

[0109] 2. Stop the reaction, remove the reaction solution by filtration, wash twice with DCM, add 10ml DCM, 0.6mmol Boc2O and 0.9mmol DIPEA, and react at room temperature for 3h.

[0110] 3. Stop the reaction, remove the reaction solution by filtration, wash it twice with DCM, then filter it with suction for 1-2 hours until the resin is completely dry, weigh the mass to get 240 mg, and calculate according to the theoretical amount, 80 mg of MBHA resin (4) is about conjugated with 0.1 mmol aldosterone.

[0111] The synthetic route is as follows:

[0112]

Embodiment 3

[0114] Introducing the cross-link arm

[0115] 1. Introduction of succinic anhydride cross-linking arms

[0116] Weigh 80 mg of MBHA resin (4) that has been conjugated with aldosterone, dissolve it in 5 ml of DMF, blow nitrogen or argon into the reaction solution, and control the mixing degree of the resin by adjusting the air flow, add 0.3 mmol of succinic anhydride (Aladdin), 0.1mmol DMAP (Sinopharm), react at room temperature for 3h. Stop the reaction, remove the reaction solution by filtration, wash twice with DMF, and filter with suction for 1-2 hours until the resin is completely dry, then store it for use.

[0117] The reaction scheme is as follows:

[0118]

[0119] 2. Introduce γ-aminobutyric acid cross-linking arm

[0120] 1) Weigh 80 mg of MBHA resin (4) that has been conjugated with aldosterone, dissolve it in 5 ml of DMF, blow nitrogen or argon into the reaction solution, and control the mixing degree of the resin by adjusting the air flow, add 0.15 mmol met...

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Abstract

The invention relates to the field of aldosterone detection, in particular to an aldosterone derivative and a preparation method of the aldosterone derivative. According to the preparation method of the aldosterone derivative provided by the invention, by introducing a macromolecular solid phase such as resin in the preparation process, uniform distribution of aldosterone molecules in the final complete antigen and carrier protein and the uniform degree of complete antigen protein in a whole reaction system are controlled through the microscopic size difference of the resin, the aldosterone molecules and the carrier protein, and stability, homogeneity and linearity of the complete antigen protein in the enzyme-linked immunoreaction are well improved. The poor detection accuracy caused by the affinity difference between the complete antigen and the aldosterone molecules in blood in enzyme-linked immunologic diagnosis is overcome, the problems of false positive, false negative, missed detection and the like arising during detection are solved, the defects of chemiluminescence immunoassay relative to radioimmunoassay are overcome, and popularization of chemiluminescence immunoassay inthe clinical side is promoted.

Description

technical field [0001] The invention relates to the field of aldosterone detection, in particular to an aldosterone derivative and a preparation method thereof. Background technique [0002] Aldosterone is a steroid hormone (mineralocorticoid family), which is produced by the adrenal cortex and mainly acts on the kidneys to reabsorb sodium ions and water to maintain blood pressure stability. In general, aldosterone is a hormone that enhances the renal reabsorption of ions and water as part of the renin-angiotensin system. The amount of aldosterone in the blood is not only one of the important indicators of high blood pressure, it is also related to some diseases, such as insufficient secretion can lead to Addison's disease, and excess can lead to Conn syndrome (Conn syn-drome). [0003] As far as hypertension is concerned, the prevalence of hypertension in my country has been on the rise in recent years. The prevalence of hypertension in adults is as high as 33.5%. There ar...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/765C07K14/77C07K14/795C07K1/34
CPCC07K14/765C07K14/77C07K14/795C07K19/00Y02P20/55
Inventor 黄记有李瑞净张翼阳馨滢任凯瑜周峻
Owner GUANGDONG FAPON BIOTECH CO LTD
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