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Brefeldin A and derivative and application thereof

A technology of brefeldia and feldspar, which is applied in the direction of medical preparations containing active ingredients, organic active ingredients, antiviral agents, etc., can solve the problems of large toxic and side effects

Active Publication Date: 2016-05-11
浙江美新控股有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Although this strategy has several treatment options in clinical practice, the results are still not satisfactory. Although the activator is effective, it has a lot of toxic side effects, so it is very important to find a suitable activator

Method used

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  • Brefeldin A and derivative and application thereof
  • Brefeldin A and derivative and application thereof
  • Brefeldin A and derivative and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1F29-61A

[0086] The obtained fractions were separated by reverse-phase high-performance liquid chromatography (SepaxAmethystC-18 (5μm, 21.2×250mm) chromatographic column, detection wavelength 210nm), and the mobile phase used was a methanol-water system with a volume ratio of 55:45 and wasocratic at 10mL / min. Elution, collect the chromatographic peak of 36-39min, recover solvent, obtain compound F29-61A, such as Figure 1-4 and 1-5 Shown, according to nuclear magnetic resonance data, its structure is as follows, is formula I structure, R 1 is OH; R 2 for H; R 3 for H; R 4 is OH; R 5 for H; R 6 for CH 3 , the molecular formula is C 16 h 24 o 4 , The compound was identified as brefeldin A.

[0087]

[0088] C11 cells were planted in a 96-well plate at 2×10E4 cells per well, and 100 μL of 1640 medium (Gibco) containing 10% FBS (Gibco) was added to each well. After the cells were treated with F29-61A for 24 / 48h, the green fluorescent expression of the cells was observed under...

Embodiment 2F29-63F

[0092] The obtained fractions were separated by reverse-phase high-performance liquid chromatography (SepaxAmethystC-18 (5μm, 21.2×250mm) chromatographic column, detection wavelength 210nm), the mobile phase used was a methanol-water system with a volume ratio of 65:35 and an isocratic flow rate of 12mL / min. After eluting, collecting the chromatographic peak at 36-40 min, and recovering the solvent, the compound F29-63F having anti-HIV latent activity of the present invention can be obtained. Such as diagram 2-1 , 2-2 , 2-3, 2-4, 2-5, 2-6, 2-7, according to the NMR data, the compound was identified as 7,7-dimethoxybrefeldinC.

[0093]

Embodiment 3F29-84

[0095] The obtained fractions were separated by reversed-phase high-performance liquid chromatography (SepaxAmethystC-18 (5μm, 21.2×250mm) chromatographic column, detection wavelength 210nm), the mobile phase used was a methanol-water system with a volume ratio of 50:50 and an isocratic flow rate of 10mL / min. After elution, the chromatographic peaks at 26-30 min were collected, and the solvent was recovered to obtain compound F29-84F. Such as Figure 3-1 , 3-2 , 3-3, 3-4, 3-5, 3-6, 3-7, according to the NMR data, the compound was identified as 6α-hydroxybrefeldinC.

[0096]

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Abstract

The invention discloses brefeldin A (BFA) and a derivative and application thereof. The brefeldin A has the extremely high anti-HIV latency activity, and the series compound is obtained through a static culture fermentation method and chemical modification. The brefeldin A and the derivative thereof are of a structure shown as a formula (I) (please see the formula in the description), wherein R1-R5 represent H, OH, CH3, OCH3 and (OCH3)2 or OCOCH3 respectively, and R6 represents CH3. The brefeldin A and the derivative thereof can serve as anti-HIV latency drugs and can be applied to preparation of a drug for treating an AIDS jointly with an antiretroviral drug, when the brefeldin A and the derivative thereof are jointly applied with the antiretroviral drug, the brefeldin A and the derivative thereof can enable latent HIVs in infected cells to be expressed, have the effect of intervening HIV latency and can clear the activated and infection-latent cells to accelerate clearance of a latent virus storage, and the wide application prospect is achieved.

Description

technical field [0001] The invention relates to the field of drugs for treating AIDS, in particular to a brefeldin A and its derivatives and applications. Background technique [0002] Acquired Immunodeficiency Syndrome (AIDS) is an infectious disease caused by HIV infection that seriously endangers people's life and health. At present, the clinical treatment of AIDS is mainly Highly active antiretroviral therapy (HAART), which not only effectively controls HIV replication, but also can rebuild the immune function of AIDS patients. People hope to completely eliminate HIV in the body by virtue of HAART, so as to achieve the goal of completely curing AIDS. Since the first HIV nucleoside reverse transcriptase inhibitor zidovudine (AZT) was approved in 1987, more than 30 anti-HIV chemotherapeutic drugs have entered clinical use. In the absence of an effective HIV / AIDS vaccine, the combined use of these drugs can significantly change the nature of HIV, greatly reduce the morbid...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D313/00A61K31/365A61K45/06A61P31/18
CPCC07D313/00
Inventor 马忠俊胡志飞朱焕章
Owner 浙江美新控股有限公司
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