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Compound with anti-herpes-virus function

An anti-herpes virus and herpes virus technology, applied in the field of compounds, can solve the problems of large side effects and application restrictions, and achieve the effects of low toxicity, low adverse reactions and wide application prospects

Inactive Publication Date: 2014-09-10
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The compounds provided by the present invention against herpes virus include: Nucleosides Compounds provided by the present invention: the first generation is acyclovir (ACV, treats HSV and VZV infection), the second generation is ganciclovir, valacyclovir, and the third generation It is famciclovir etc., has certain curative effect, but these compounds provided by the present invention have bigger side effect, and application is subject to certain restriction, therefore be very necessary on the basis of prior art, seek and develop a kind of anti-herpes virus effect Compounds provided by the present invention with strong and small adverse reactions

Method used

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] The preparation of embodiment 1 new compound

[0021] Carry out solid fermentation of the croton to obtain the fermented croton, then reflux the fermented croton with 50-80% methanol to extract 3 times, each time for 2 hours, and concentrate the extract to obtain an extract, suspend the extract in water, and successively use 6 Double the volume of ethyl acetate and 6 times the volume of n-butanol for extraction to obtain the ethyl acetate site and n-butanol site, then use silica gel column chromatography with dichloromethane-methanol system as eluent, the resulting n-butanol Gradient elution at the butanol site (100:1, 100:5, 100:10, 100:20, 100:30, 100:40, 100:50), TLC tracking, combined dichloromethane-methanol (100:30, 100:40), elution liquid, concentrated, recrystallized and purified to obtain a new compound—crotontriazolidine (1-β-D-ribofuranose-6-amino-1,2,3-triazolo[5,4-d]pyridine ).

[0022] The compound is white needle crystal, slightly soluble in water, solu...

Embodiment 2

[0030] Embodiment 2 anti-herpes virus experiment

[0031] 1 Experimental method

[0032] 1.1 Compound Toxicity Test

[0033] Culture Vero cells in 10% calf serum RPMI-1640 medium, press 1×10 5 Inoculated into 96-well cell culture plates, 0.2 mL per well, grown into monolayer cells for 18-24 hours, discarded the supernatant, and set aside. The compound provided by the present invention (crotontriazolidine) was cultured for 72 hours in double-folded concentrations of the medium, 200 μL per well, and 4 duplicate wells for each concentration. Add 20 μL of 5 mg / ml MTT solution to each well, continue to incubate for 4 hours, pour off the supernatant, add 0.2 mL DMSO, measure O.D value with 570-630 nm dual-wavelength method, and calculate TC50 of the compound provided by the invention.

[0034] 1.2 CPE test and MTT test of compounds against HSV-I

[0035] vero cells by 1 x 10 5 Inoculated into 96-well cell culture plates, 0.2 mL per well, grown into monolayer cells for 18-24 hou...

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Abstract

The invention discloses a compound with an anti-herpes-virus function; the compound has the following advantages such as easily obtained raw materials, relatively low cost, sustainable development and wide application prospect. According to the invention, experimental results show that the activity of the novel compound obtained by separation in resisting herpes simplex virus is high; in addition, toxic experimental results show that the compound provided by the invention is relatively low in effective dose, low in toxicity, low in adverse reaction, and safe to use; and meanwhile, the compound can be prepared into various medicine dosage forms with various excipients, so that the compound is convenient for clinical application.

Description

technical field [0001] The present invention relates to a compound, in particular to a compound with anti-herpes virus effect. Background technique [0002] People have a fast-paced life and high pressure in life. When their immunity is low, they are prone to herpes virus infection. Among them, HSV-1 infection can cause cold sores, herpetic paronychia and other skin rashes such as traumatic herpes, herpetic eczema, and herpetic cornea. HSV-2 can cause genital herpes, herpetic proctitis, etc., with various clinical manifestations, often atypical or asymptomatic, and can cause latent infection, which is easily overlooked by people, and is also an important factor for the horizontal and vertical transmission of HSV . The current anti-herpes virus compounds provided by the present invention include: nucleosides Compounds provided by the present invention: the first generation is acyclovir (ACV, treating HSV and VZV infection), the second generation is ganciclovir, valacyclovir,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07H19/23C12P19/38A61K31/706A61P31/22
Inventor 董伟潘扬孙钰詹瑧彭薇
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE