Rupestonic Acid-Alkaloid Complex Salt for Anti-Tumor Therapy

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Solution Overview

Problem

Current cancer treatments face challenges due to late-stage diagnosis and the development of multi-drug resistance, necessitating the development of novel anti-cancer drugs with high activity and low side effects.

Innovation Solution

A complex salt formed from rupestonic acid and alkaloids such as matrine, oxymatrine, sophocarpine, and sophoridine, prepared through dissolution in an organic solvent, which exhibits anti-tumor activity and is used in treating various cancers.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If traditional small-molecule anti-cancer drugs are used, then cancer treatment is provided, but multi-drug resistance occurs and treatment effectiveness decreases

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidmulti-drug resistance
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent creates a composite structure by forming a complex salt between rupestonic acid (a sesquiterpene compound with antiviral activity) and alkaloids (such as matrine, oxymatrine, sophocarpine, or sophoridine with known anti-tumor properties). This composite approach combines two different pharmacological agents into a single molecular complex, aiming to achieve synergistic anti-cancer effects while overcoming resistance mechanisms that developed against single-agent therapy

Inventive Principle:
Principle #40Composite materials

2Reliability

If novel anti-cancer drugs are developed, then high activity and low side effects are achieved, but drug development complexity increases

Engineering Contradiction:
Improveanti-cancer activityVSAvoiddrug development complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The complex salt formulation serves multiple functions simultaneously: it combines the anti-tumor activity of alkaloids with the antiviral and anti-inflammatory properties of rupestonic acid, provides synergistic cancer cell killing effects, and aims to overcome multi-drug resistance. This multi-functionality is achieved through a single preparative method involving dissolution in organic solvent and evaporation, simplifying the development process while enhancing therapeutic potential

Inventive Principle:
Principle #6Universality (Multi-functionality)

3Object-affected harmful factors

If traditional Chinese medicines are used, then mild toxic and side effects are achieved, but anti-tumor activity needs enhancement

Engineering Contradiction:
Improveside effectsVSAvoidanti-tumor activity
Core Design Contradiction:
Object-affected harmful factorsVSReliability

Solution Approach 1:

The patent modifies the pharmacological parameters of traditional Chinese medicine components by forming a complex salt structure. This chemical modification changes the bioavailability, pharmacokinetic properties, and biological activity of the individual components, enhancing anti-tumor effectiveness while preserving the favorable safety profile of traditional Chinese medicines

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS12024489B2Complex salt of rupestonic acid and alkaloid, preparation method therefor and use thereof
Publication Date: 2024.07.02 XIAMEN INST OF RARE EARTH MATERIALS
  • US12024489B2 patent drawing
  • US12024489B2 patent drawing
  • US12024489B2 patent drawing

AI summary

A complex salt formed from a compound of formula (I) and an alkaloid, a preparation method therefor and use thereof are provided. In particular, a complex salt formed from rupestonic acid and matrine, oxymatrine, sophocarpine and sophoridine, or a composition thereof, has potential efficacy in treating a tumor/cancer or preparing related medicaments.