Ligustroflavone Rhoifolin Hyperin Composition for Influenza Neuraminidase Inhibition
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Solution Overview
Problem
Current treatments for influenza, including vaccines and traditional Chinese medicines, have limitations such as group selectivity, low protective rates, short duration, and side effects, while existing antiviral drugs like oseltamivir phosphate (Tamiflu) are expensive and cause adverse reactions, and there is a lack of evidence on the antiviral mechanisms of many traditional medicines.
Innovation Solution
A composition comprising ligustroflavone, rhoifolin, and hyperin, which inhibits influenza virus neuraminidase from hydrolyzing sialic acid on cell surfaces, preventing viral entry and replication, and is prepared in specific weight ratios and extracted using ethanol reflux and macroporous resin column methods.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If oseltamivir phosphate (Tamiflu) is used to treat influenza, then the antiviral effect is improved, but the cost increases and side effects occur
Solution Approach 1:
The patent replaces the expensive oseltamavir phosphate with a combination of traditional Chinese medicine compounds (ligustroflavone, rhoifolin, and hyperin) that are more cost-effective while maintaining antiviral efficacy. The composition uses readily available natural compounds instead of expensive synthetic drugs.
Solution Approach 2:
The patent converts traditional Chinese medicine formulations, which previously lacked proven antiviral mechanisms, into an effective neuraminidase inhibitor by identifying and standardizing the active compounds (ligustroflavone, rhoifolin, and hyperin) that specifically inhibit influenza virus replication.
2Reliability
If influenza vaccination is administered, then protective effect is achieved, but the protective period is short (3-6 months) and protective rate is low
Solution Approach 1:
The patent provides a medicinal composition that can be taken proactively to prevent influenza infection and replication, offering sustained protection beyond the temporary immune response of vaccines. The composition works continuously to inhibit viral activity rather than providing temporary post-exposure protection.
3Ease of operation
If nonspecific antiviral Chinese medicines are used, then treatment is provided, but the antiviral mechanism is unknown and effectiveness against influenza is unproven
Solution Approach 1:
The patent extracts and identifies the specific active compounds (ligustroflavone, rhoifolin, andhyperin) from traditional Chinese medicine sources, separating them from the complex mixture of compounds in whole herbs. This extraction process reveals the specific antiviral mechanisms of these individual compounds.
Solution Approach 2:
The patent changes the chemical parameter identification by using modern analytical methods to characterize the specific compounds in traditional medicines, transforming them from undefined mixtures into well-characterized molecules with known structures and mechanisms of action.
4Adaptability or versatility
If turpinia montana leaf and its components are used, then traditional therapeutic effects are achieved, but antiviral activity against influenza is unproven
Solution Approach 1:
The patent changes the functional parameter of turpinia montana leaf extracts by identifying and standardizing the specific compounds (ligustroflavone, rhoifolin, andhyperin) that provide antiviral activity, transforming traditional empirical use into scientifically validated therapy with measurable antiviral effects.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The composition effectively inhibits neuraminidase activity and reduces influenza virus replication, offering a potential treatment for influenza and its complications without the side effects of existing drugs, as demonstrated by experimental data showing significant inhibition of neuraminidase and virus replication.
Implementation Method 1
inhibits influenza virus neuraminidase from hydrolyzing sialic acid on cell surfaces
Implementation Method 2
extracted using ethanol reflux and macroporous resin column methods
Implementation Method 3
extracted using ethanol reflux and macroporous resin column methods
Data Source
AI summary
Disclosed is a composition comprising ligustroflavone, rhoifolin and hyperin, which is prepared according to rational weight ratio: 40% to 80% ligustroflavone, 5% to 45% rhoifolin and 1% to 40% hyperin. The composition can be used as a neuraminidase inhibitor for preventing and treating influenza, and can be formulated into pharmaceutically acceptable dosage forms.