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Houttuynoid and preparation method and application thereof

A technology of hybrid flavonoids and houttuyniacin, which is applied in the preparation of sugar derivatives, chemical instruments and methods, pharmaceutical formulations, etc., can solve the problems of unclear antiviral mechanism, unclear mechanism, and in-depth research on interaction.

Active Publication Date: 2013-09-18
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example, extracts or components of traditional Chinese medicines such as Caulis Spatholobus, Rhubarb, Polygonum cuspidatum, Astragalus, and peony all have good anti-HSV activity, but most of them are extracts of traditional Chinese medicines, and their antiviral mechanism is unclear. No breakthroughs have been made, the determination of active ingredients, the relationship between structure and efficacy, and the interaction between active ingredients still need to be further studied

Method used

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  • Houttuynoid and preparation method and application thereof
  • Houttuynoid and preparation method and application thereof
  • Houttuynoid and preparation method and application thereof

Examples

Experimental program
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Embodiment 1

[0057] Example 1: Extraction and separation of Houttuyniatin hybrid flavonoids in Houttuynia cordata

[0058] Take 5 kg of Houttuynia cordata Thunb., a plant of the genus Houttuynia cordata Thunb., and extract it under reflux with 50% ethanol water (100°C) for 3 times, 2 hours each time, combine the extracts, and depressurize Concentrate to an extract to obtain the total extract. Suspend the total extract with an aqueous solution of 8 times the amount (mass / volume, g / ml), centrifuge at 3000rpm, get the supernatant and carry out macroporous adsorption resin (AB-8) column chromatography separation, with ethanol-water volume ratio From 0: 100, 20: 80, 40: 60, 60: 40, 80: 20 and 95: 5 as eluent gradient elution, obtain 6 fractions ZA to ZF respectively, for fraction ZD (ethanol-water volume ratio 60:40 eluted fractions) were subjected to ODS medium and low pressure column chromatography (5×30cm, Eyela), and methanol-water volume ratios were obtained from 10:90, 30:70, 50:50, 70:3...

Embodiment 2

[0096] Example 2: Anti-herpes simplex virus activity analysis of houttuydine heterozygous flavonoids

[0097] The houttuynoid houttuynoids disclosed in this patent are shown below A (compound 1), B (compound 3), C (compound 4), D (compound 9), E (compound 10), F (compound 2), G (compound 5), H (compound 6), I (compound 7), J (compound 8), K (compound 11) and L (compound 12) anti-herpes simplex virus in vitro activity, while showing flavonoid Compounds hyperin (Hyperin) and rutin (Rutin), and positive control drug acyclovir (Acyclovir) anti-herpes simplex virus in vitro activity.

[0098] The specific method is as follows: Add 50ul of 0.5MOI HSV / Blue (recombinant reporter virus with lacZ gene coding frame) virus solution and 50ul of the sample diluted to 50uM by DMSO into the Vero cells growing into a single layer in the cell culture plate liquid. At the same time, a solvent control with an equilibrium concentration of DMSO, a control without adding samples, and a cell blank ...

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Abstract

The invention discloses houttuynoids and a preparation method and application thereof. The houttuynoids have a structural formula as represented by formula (I) which is described in the invention; in the formula (I), R1 is represented by formula (I), formula (II), formula (IV), formula (V), formula (VI), formula (VII), formula (VIII), formula (IX) or formula (X) as described in the invention, and R2 is hydrogen or is represented by formula (XI), formula (XII), formula (XIII) or formula (XIV) as described in the invention. 12 houttuynoids are separated from Saururaceae Houttuynia cordata Thunb. and are all furan-flavones with novel structures. An in-vitro anti-herpes simplex virus activity screening system is used for evaluating activity of the houttuynoids, and it is found that the houttuynoids can effectively inhibit a herpes simplex virus; thus, the houttuynoids have effects on preventing and treating herpes simplex virus infection, can be applied to preparation of drugs used for resisting the herpes simplex virus and have good research and development prospects.

Description

Technical field: [0001] The invention belongs to the field of natural product chemistry, and in particular relates to a class of houttuyfonate hybrid flavonoids and its preparation method and application. Background technique: [0002] Herpes Simplex Virus (HSV) is the most common pathogen in humans. HSV is spherical, and the complete virus consists of core, capsid, envelope and envelope. The core contains double-stranded DNA that is wound into a filamentous reel. The capsid is icosahedral and consists of 162 shell particles with a diameter of 100 nm. The outer layer of the capsid is covered by a membrane with uneven thickness. The outermost layer is a typical lipid bilayer membrane with protrusions. The diameter of the enveloped virus is 150-200nm. The capsule surface contains gB, gC, gD, gE, gG, gH glycoproteins. The HSV genome is a linear DNA molecule consisting of covalently linked long (L) and short (S) segments. Each fragment contains a single sequence and invert...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H17/07C07H1/08A61K31/7048A61P31/22
Inventor 姚新生彭涛高昊朱钦昌陈少丹李婷肖高铿吴红玲
Owner JINAN UNIVERSITY
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