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Antiviral azide-containing compounds

An azide and carbohydrate technology, applied in the field of pharmaceutical compositions of salts, can solve problems such as toxic side effects, bone marrow suppression, abnormal liver function and the like

Active Publication Date: 2016-06-08
LIFE TECH CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] While beneficial, these antiretroviral drugs often exhibit toxic side effects such as bone marrow suppression, vomiting, and abnormal liver function

Method used

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  • Antiviral azide-containing compounds
  • Antiviral azide-containing compounds
  • Antiviral azide-containing compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0187] Example 1: Labeling of HIV with azide-modified biomolecules

[0188] HIV in a T-150 flask NL4-3 Transfect CEMx174 cells and monitor virus production by reverse transcriptase activity until peak virus production is reached (typically 7-9 days after transfection). Prior to transfection, CEMx174 cells were spiked with the following azide-modified biomolecules: 15-azidopentadecanoic acid (50-100 μM), 12-azidododecanoic acid (50-100 μM ), tetraacetylated N-azidoacetylgalactosamine (20-40 μM) and tetraacetylated N-azidoacetyl-D-mannosamine (20-40 μM).

[0189] Infected cells were harvested at 12, 24, 72 hours and 14 days. Harvested cells are detached and lysed. Cell lysates were then mixed with Detection reagent, tetramethylrhodamine (TAMRA) alkyne and Protein Reaction Buffer Kit (Invitrogen, Carlsbad, CA) was mixed together. Cell lysate samples were run on one-dimensional gels to monitor changes in azide-labeled proteins over time ( figure 1 ).

[0190] Labeled vir...

Embodiment 2

[0192] Example 2: Inhibition of HIV infectivity

[0193] To examine the effect of the azide-modified biomolecules on the innate biology of the virus, azide-tagged viruses were isolated from transfected cells and tested in cell infection studies. Unlabeled HIV (concentration 1 / 100 of the test sample) was used as a control. Viral load was normalized to p24 abundance and viruses were incubated for 12 hours on a reporter cell line (TZM / BI). TZM / BI is a genetically engineered HeLa cell line expressing CD4, CXCR4 and CCR5 and containing Tat-inducible luciferase and β-Gal reporter genes. Virus infectivity was determined by measuring cellular luciferase activity with 2 different luciferase reagents. Results using a single-cycle replication system showed that biomolecules modified with the azides (specifically, 12-azidododecanoic acid, and to a lesser extent, 15-azidopentadecanoic acid and tetraacetylated N-azidoacetylgalactosamine)-tagged viruses had profound effects on viral infec...

Embodiment 3

[0194] Example 3: Toxicity Profile

[0195] Little or no toxicity was observed in different eukaryotic cell lines with these azide-modified biomolecules, suggesting that these compounds have a minimal toxicity profile,

[0196] and support their use in therapeutic settings.

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Abstract

Methods of using azide-modified biomolecules such as fatty acids, carbohydrates and lipids to treat virus-infected plants, insects or animals or to suppress the infectivity of viruses such as human immunodeficiency virus are provided. Also provided are methods of labeling viruses such as human immunodeficiency virus with azide-modified biomolecules such as fatty acids, carbohydrates or isoprenoid lipids. Also, methods for tracking viruses in vivo using azide-modified biomolecules such as fatty acids, carbohydrates or isoprenoid lipids are provided. The azide-modified biomolecules can be combined with pharmaceutically acceptable excipients to produce pharmaceutical compositions optionally containing other antiviral agents and / or delivery agents, such as lipids body.

Description

Background technique [0001] Viral infections cause high morbidity and mortality in humans and animals. In addition, viral infections also result in substantial agricultural losses, with plant viruses causing an estimated $60 billion in crop yield losses worldwide each year. Although considerable resources have been devoted to identifying compounds with antiviral properties, viral infections still pose significant risks to human health and agriculture. [0002] Additionally, the development of multidrug resistance, poor efficacy and / or toxicity limits the usefulness of most existing antiviral treatments. In fact, many antiviral treatments are highly toxic and can cause serious side effects, including heart damage, kidney failure and osteoporosis. Other challenges include creating drugs that are broadly applicable to combat many different types of viral infections, which is especially important in the treatment of immunocompromised individuals. [0003] One virus, specificall...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/00A61K31/19A61K31/20A61P31/00A61P31/18
CPCA61K31/7024A61K45/06A61K31/655A61K31/7088A61K38/212A61K38/215A61P31/00A61P31/12A61P31/14A61P31/18A61P31/20A61K2300/00
Inventor B.阿格纽D.格雷厄姆U.辛赫S.格里相
Owner LIFE TECH CORP