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Application of N-[(2,3-di-2-furoquinoline-6-yl)amino]-(dimethylamino)-methanol in preparing anti-AIDS medicaments

A kind of furaquinoline, dimethylamino technology, applied in the field of biomedicine, can solve problems such as poor curative effect

Inactive Publication Date: 2009-12-02
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But even if the most effective treatment plan is used, its treatment only accounts for 20% to 50% of the number of patients treated, and the curative effect is not good.

Method used

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  • Application of N-[(2,3-di-2-furoquinoline-6-yl)amino]-(dimethylamino)-methanol in preparing anti-AIDS medicaments

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1 Utilizes BIAcore Molecular Interaction Instrument to Verify Virtual Screening Results

[0041] The BIAcore molecular interaction instrument is based on surface plasmon resonance technology to track the interaction between biomolecules without any markers, thus ensuring the authenticity of the experimental results to the greatest extent. During the experiment, the target biomolecules (CypA ​​protein) were immobilized on the surface of the sensor chip, and then the small molecule compounds were dissolved in the solvent and flowed over the surface of the chip. The monitor can track the changes in the whole process of binding and dissociation between molecules in the detection solution and target biomolecules on the chip surface in real time. Through the binding data of BIAcore, we finally identified 12 small molecular compounds that can bind to CypA, and calculated the equilibrium-dissociation constant KD of these small molecular compounds binding to CypA. Its e...

Embodiment 2

[0042] Example 2 Proves the ability of small molecule compounds to inhibit CypA enzyme activity by using enzyme activity experiments

[0043] There are many methods for measuring CyP activity, but α-chymotrypsin-coupled enzymic assay is the most commonly used. The principle is that the oligopeptide substrate containing proline, such as N-succinyl-Ala-Ala-Pro-Phe p-nitroanilide (N-Succinyl-Ala-Ala-Pro-Phep-nitroanilide) in the solution The formula and trans structures are in balance, and CyP can catalyze the cis-trans isomerization of the substrate, that is, catalyze the change of proline from cis to trans; when it is in the trans structure, the C-terminal p-nitroanilide is α- The chymotrypsin is cleaved to release the pigment group p-nitroaniline, and the PPIase activity of CyP can be obtained by continuously measuring the change of the absorbance value at 390nm.

[0044] We took the reaction without small molecule inhibitors as the control reaction, measured the inhibition r...

Embodiment 3

[0045] Embodiment 3 compound anti-HIV-1 virus increment test

[0046] MT-2 cells were planted in a 96-well plate, 10 per well 4 indivual. The medium is RPMI 1640 medium containing 10% fetal bovine serum. HIV-1 virus was used to infect the cells with 100 50% tissue infection equivalents, and at the same time, the compound was added with different concentration gradients and cultured overnight (the well without compound was used as the blank control). The next day, replace with fresh medium without small molecule compounds. On the fourth day, get 100uL of the culture supernatant, add 5% volume of Triton-X100 to obtain the virus lysate, and then use the ELISA method to measure the p24 protein content (p24 is the coat protein of HIV-1, which can be used as a measure of the number of virions) index of). Simply put, the double-antibody sandwich method is used to measure the amount of p24 protein produced in each well. Coat the plate with anti-HIV immunoglobulin overnight (pH 9....

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Abstract

The invention belongs to the field of biological medicines, and in particular relates to application of a micromolecule compound with anti-HIV actively in preparing anti-AIDS medicaments. The invention provides application of N-[(2,3-di-2-furoquinoline-6-yl)amino]-(dimethylamino)-methanol in preparing the anti-HIV medicaments. The compound can inhibit CypA actively, the enzyme activity inhibition IC50 value (micron) reaches 3.47 + / - 0.92, and the compound has obvious inhibition to p24 protein of HIV-1 virus. The N-[(2,3-di-2-furoquinoline-6-yl)amino]-(dimethylamino)-methanol added to solution containing HIV can inhibit the replication of the HIV. The compound has the ability of inhibiting the replication of the HIV-1 virus, is a medicament designed aiming at a cell target, is not easy to form drug tolerance, and is suitable for the requirement on lifelong medication of AIDS patients.

Description

technical field [0001] The invention relates to the field of biomedicine, and relates to the application of a small molecular compound with anti-HIV activity in the preparation of anti-AIDS drugs. Background technique [0002] Human immunodeficiency virus (HIV) is a special class of retroviruses. It has a high degree of variability, can specifically infect and kill the main immune cell population, and can induce enhanced antibodies. In recent years, due to the better understanding of the pathogenesis of HIV infection, new and more effective drugs have been developed, such as protease inhibitors (pi) and non-nucleoside reverse transcriptase inhibitors (nnrti). The mechanism of action and application of commonly used anti-HIV drugs are briefly described as follows. [0003] 1. Protease Inhibitors [0004] Mechanism of action of protease inhibitor pi: Proteases are essential for gag, gagpol polyproteins and post-translational processing, structural proteins that form the cor...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4709A61P31/18A61K31/498
Inventor 余龙陈帅赵雪梅胡海荣唐丽莎
Owner FUDAN UNIV
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