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Uses of nordihydroguaiaretic acid (NDGA) and derivatives thereof in preventing transmission of sexually transmitted diseases

a technology of nordihydroguaiaretic acid and derivatives, which is applied in the field of virology, bacteriology and public health, can solve problems such as deficiency in prophylactic and therapeutic methods in the early stages of the diseas

Inactive Publication Date: 2009-06-18
KHANNA NIHARIKA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0010]The present invention is directed to a method for inhibiting proliferation of a microbe associated with a sexually transmitted disease or infection. The method comprises contacting the mi

Problems solved by technology

More specifically, the prior art is deficient in prophylactic and therapeutic methods against sexually-transmitted diseases or infections using nordihydroguaiaretic acid or derivatives or analogs thereof as a topical microbicide.

Method used

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  • Uses of nordihydroguaiaretic acid (NDGA) and derivatives thereof in preventing transmission of sexually transmitted diseases
  • Uses of nordihydroguaiaretic acid (NDGA) and derivatives thereof in preventing transmission of sexually transmitted diseases
  • Uses of nordihydroguaiaretic acid (NDGA) and derivatives thereof in preventing transmission of sexually transmitted diseases

Examples

Experimental program
Comparison scheme
Effect test

example 1

Microbicidal Compounds

[0049]Nordihydroguaiaretic Acid (NDGA)

[0050]NDGA is a purified extract of Larrea tridentata (Erimos Technologies).

[0051]NDGA Derivatives and Analogs

[0052]Tetra-O-methyl-nordihydroguaiaretic acid (M4N; FIG. 1A), tetra-O—(N,N-dimethyl)glycyl-nordihydroguaiaretic acid (G4N; FIG. 1B), 3′-O-methyl nordihydroguaiaretic acid (Mal.4; FIG. 1C), or tetra-O—(N-ethyl)piperidinyl-nordihydroguaiaretic acid (P4N) are derivatives of NDGA and are the active pharmaceutical ingredients of the microbicide. The microbicides may be hydrophobic, such as M4N, or water soluble such as G4N, Mal.4 or P4N.

[0053]Tetra-O-methyl-nordihydroguaiaretic acid (M4N) is a semi-synthetic derivative of NDGA synthesized by a two stage chemical methodology (Sigma Aldrich Fine Chemicals). tetra-O—(N,N-dimethyl)glycyl-nordihydroguaiaretic acid (G4N) is synthesized as described (3). 3′-O-methyl-nordihydroguaiaretic acid (Mal.4) also can be isolated from Larrea tridentata as disclosed in U.S. Pat. No. 6,29...

example 2

Screening Algorithm

[0054]The screening algorithm depicted in FIG. 2 is used to develop the microbicide. In summary, an HIV R5 cell attachment assay is conducted with a potential microbicidal compound and followed with an R5 cell to cell transmission assay. If the compound is found to be active, the next stage of secondary screening occurs, in which an HIV X4 attachment and fusion assay is performed, as well as an HIV X4 cell to cell transmission assay. In addition, cervical explant studies and Lactobacillus toxicity testing are performed. HIV R5 cell to cell transmission assays in seminal plasma and assessment of effects on semen and sperm are also performed.

Antiviral Assays in Fresh Human Peripheral Blood Mononuclear Cells (PBMCs)

[0055]PBMCs are isolated following Ficoll-Hypaque density centrifugation, and re-suspended at a cell density of 1×106 in medium supplemented with 2 μg / mL PHA. Following incubation for 24 hrs, the cells are collected by centrifugation, washed and suspended ...

example 3

In Vitro Anti-Viral Activity

Sp1 Transcription Factor Binding

[0061]Tetra-O-dimethylaminoglycyl-nordihydroguaiaretic acid (G4N) binds the major grove of the free DNA when it is uncomplexed with other proteins. The binding constant for the G4N / Sp1 enhancer sequence was calculated by the ethidium displacement technique at various phosphate buffer concentrations and pH values using a spectrofluorometer with excitation at 517 nm and emission at 596 nm. An apparent equilibrium binding constant (Kapp) of 3×106 M−1 was obtained by the equation Kapp=KEtBr[EtBr] / [G4N] which represents the concentration of the G4N causing a 50% reduction of the fluorescent intensity of DNA-ethidium solution. Tetra-O—(N-ethylpiperidinyl)-nordihydroguaiaretic acid (P4N) has been found to disrupt Sp1 transcription factor binding to the major groove of Sp1 site either by competition for binding or by altering the overall DNA conformation such that the major groove becomes incompatible for Sp1 binding G4N has been t...

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PUM

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Abstract

Provided herein are methods for inhibiting proliferation of a microbe associated with a sexually transmitted disease (STD) or infection and for preventing transmission of one or more sexually transmitted diseases in a subject at-risk for acquiring the same, including an HIV positive subject at risk for acquiring another sexually transmitted disease. The methods comprise contacting a microbe or cell thereof associated with the STD or administering to the subject nordihydroguaiaretic acid or a derivative or analog thereof. In HIV positive at-risk subjects one or more anti-retroviral drugs are co-administered.

Description

CROSS-REFERENCE TO RELATED APPLICATION[0001]This nonprovisional application claims benefit of priority under 35 U.S.C. §119(e) to provisional U.S. Ser. No. 60 / 917,344, filed May 11, 2007, now abandoned.BACKGROUND OF THE INVENTION[0002]1. Field of the Invention[0003]The present invention relates to the fields of virology, bacteriology and public health.[0004]Specifically, the present invention provides methods for treating or prophlactically treating sexually transmitted diseases or infections using a topical microbicide.[0005]2. Description of the Related Art[0006]HIV is a world wide epidemic with 14,000 new, preventable, sexually acquired infections per day. HIV remains a devastating illness with poor access to adequate therapy in most parts of the world, making it the most compelling area of focus. Despite the knowledge of successful HIV prevention strategies, i.e. condom use, reduction in the number of sexual partners, diagnosis and treatment of sexually transmitted infections, H...

Claims

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Application Information

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IPC IPC(8): A61K31/05A61P31/00A61K31/225A61K31/4545
CPCA61F5/445A61F2005/4486A61F5/4407A61F5/441A61P31/00
Inventor KHANNA, NIHARIKA
Owner KHANNA NIHARIKA
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