Application of germacrone in preparing HSV (Herpes Simplex Virus) resisting medicine

A technology of herpes simplex virus and gemmazone, which is applied in the field of medicine, can solve the problems of increasing the treatment of HSV infection, undetected, difficulties, etc., and achieve a good effect of anti-herpes simplex virus activity

Inactive Publication Date: 2013-10-02
SHENZHEN NEPTUNUS PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] 1. Some nucleoside drugs such as iodeoxyguanosine, vidarabine, ganciclovir, etc. are mutagens, resulting in lower safety in use;
[0009] 2. The emergence of drug-resistant strains increases the difficulty in the treatment of HSV infection
[0010] Gemacone i

Method used

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  • Application of germacrone in preparing HSV (Herpes Simplex Virus) resisting medicine
  • Application of germacrone in preparing HSV (Herpes Simplex Virus) resisting medicine
  • Application of germacrone in preparing HSV (Herpes Simplex Virus) resisting medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment 1: the preparation of gemmaquinone

[0026] The branches and leaves of Rhododendron xing'an were extracted twice with 80% ethanol under reflux, each time for 2 hours, the extracts were combined, concentrated under reduced pressure until there was no alcohol smell, centrifuged, and the supernatant was put on a macroporous resin chromatography column, and first washed with purified water Elute 3 column volumes, then elute 3 column volumes with 50% concentration ethanol, and then use 70% concentration ethanol to elute 5 column volumes, collect 70% concentration ethanol eluate, concentrate under reduced pressure, and crystallize to obtain Crude gemacerone, after dissolving the crude gemacerone in methanol, standing and recrystallizing, the pure gemacerone (purity>95.0%) can be obtained.

Embodiment 2

[0027] Embodiment 2: Anti-herpes simplex virus effect test of gemmaquinone in vitro

[0028] 1. Materials

[0029] 1.1 Strains: HSV-1, HSV-2.

[0030] 1.2 Cell model: monkey kidney cell line Vero.

[0031] Culture conditions: DMEM+10% fetal bovine serum, 37°C, 5% CO 2 .

[0032] 1.3 Testing samples: See Table 1 for sample numbers and concentrations.

[0033] 2. Principles and methods

[0034] 2.1 Drug cytotoxicity detection

[0035] The alamarBlue (Invitrogen Company) kit was used to detect the toxic effect of drugs on cells.

[0036] Experimental principle: alamarBlue is a redox indicator that produces absorbance changes and fluorescent signals based on metabolic activity. AlamarBlue is easily soluble in water, and its oxidized form enters the cells and is reduced by mitochondrial enzymes to produce measurable fluorescence and color changes, which are used for quantitative analysis of cell viability and cell proliferation and in vitro cytotoxicity studies. This assay ...

Embodiment 3

[0054] Embodiment 3: Gemasolone is to the protective effect test of HSV-1 infection mouse

[0055] 1. Materials

[0056] 1.1 Strains The standard herpes simplex virus type I (HSV-1) SM44 strain was passaged in Vero cells.

[0057] 1.2 Animals Clean grade Kunming mice, half male and half male, mass 20±2g.

[0058] 1.3 The concentrations of gemmacone and acyclovir in samples are shown in Table 2.1 and 2.2.

[0059] 2. Test method

[0060] 48 Kunming mice were randomly divided into 6 groups: blank control group (0.9% normal saline); The equestrian high-dose group (40mg / Kg) and the positive drug control group (acyclovir 100mg / Kg) were given continuous intraperitoneal injection for 11 days. The mice were inoculated with the virus on the 4th day after administration (except the blank control group).

[0061] 2.1 Determination of body weight, life extension rate and mortality of virus-infected mice

[0062] The mice were weighed every two days, and the body weight changes and s...

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PUM

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Abstract

The invention relates to an application of germacrone in preparing an HSV (Herpes Simplex Virus) resisting medicine. By taking HSV-1 (Herpes Simplex Virus type 1) and HSV-II (Herpes Simplex Virus type 2) strains and Vero (Rabies Purified Vaccine for Human Use) cells as experimental subjects, the HSV resisting activity of the germacrone is researched. The result shows that the germacrone has the good HSV resisting activity. As the germacrone is used for preparing the HSV treating/preventing medicine, an important development and application prospect for preventing and treating diseases caused by the HSV infection is achieved.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to the application of gemmaconone in anti-herpes simplex virus drugs. Background technique [0002] Herpes simplex virus, including herpes simplex virus type I (HSV-1) and type II virus (HSV-2), is a relatively large (100-150×10-3 μg) envelope with an icosahedral capsid. Membrane virus, which contains double-stranded DNA, has at least 70 polypeptides encoded in its genome. This large amount of regulatory information enables virus particles to control their gene expression and adapt to a variety of complex situations in infected cells. Once the virus is transmitted to a susceptible individual, HSV replicates in the epithelial cells of the mucosal surface, after which the virus infects the peripheral terminals of the neurons innervating the site of infection and then translocates to the nucleus via the axons of the neurons . Viral DNA enters the nuclear site of neurons, thereby est...

Claims

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Application Information

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IPC IPC(8): A61K31/122A61P31/22
Inventor 谭道鹏严启新曾伟珍陈艳萍王宇冯汉林
Owner SHENZHEN NEPTUNUS PHARM CO LTD
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