Tripterygium wilfordii Composition for Drug-Resistant Cancer

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Solution Overview

Problem

Current Tripterygium wilfordii compositions for treating cancer are limited by low efficacy and high toxicity, particularly due to the low content of active components like triptolide, which can cause adverse side effects such as nausea, vomiting, and liver damage.

Innovation Solution

A composition combining specific compounds like triptolide with other active molecules (e.g., 1-desacetylwilforgine, Triptergulide, Demethylzeylasteral, and Triptobenzene) at optimized ratios, separated using high-performance liquid chromatography (HPLC), to enhance cancer inhibition while reducing toxicity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If Tripterygium wilfordii composition is used to treat cancer, then anti-tumor effect is improved, but toxicity increases

Engineering Contradiction:
Improveanti-tumor effectVSAvoidtoxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent segments the complex Tripterygium wilfordii extract into individual pure compounds (triptolide, tripterine, etc.) with defined structures and activities. This segmentation allows for precise control of each component's dosage and effect, separating the anti-tumor active ingredients from the toxic elements in the crude extract.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent changes the concentration parameters of active compounds by establishing specific content ranges (e.g., triptolide 0.01-5 mg/g, tripterine 0.01-5 mg/g) in the composition. This parameter optimization allows maximizing anti-tumor efficacy while minimizing toxicity by controlling the dosage of each active ingredient.

Inventive Principle:
Principle #35Parameter changes

2Ease of operation

If single Tripterygium wilfordii composition is used, then simplicity of treatment is improved, but efficacy is limited due to low active component content

Engineering Contradiction:
Improvesimplicity of treatmentVSAvoidefficacy
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent creates a composite pharmaceutical composition containing multiple purified Tripterygium wilfordii compounds (triptolide, tripterine, and other active ingredients) in specific ratios. This composite approach combines the anti-tumor effects of different compounds while maintaining simplicity of administration as a single formulation.

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The patent merges multiple active compounds from Tripterygium wilfordii (triptolide, tripterine, and other isolated components) into a single integrated composition. This combining of multiple effective ingredients enhances overall efficacy while preserving the ease of single-agent administration.

Inventive Principle:
Principle #5Merging (Combining)

3Reliability

If high concentration of triptolide is used to enhance anti-tumor effect, then cancer inhibition is improved, but adverse side effects increase

Engineering Contradiction:
Improvecancer inhibitionVSAvoidadverse side effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent uses other Tripterygium compounds (such as tripterine and additional isolated components) as intermediary substances that work synergistically with triptolide. These intermediary compounds enhance the anti-tumor effect at lower triptolide concentrations, thereby reducing the direct toxic effects of high-dose triptolide.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent formulates a composite composition where triptolide is combined with other active compounds in optimized ratios. This composite material approach distributes the anti-tumor activity across multiple ingredients, allowing effective cancer inhibition at reduced triptolide concentrations and thus minimizing adverse side effects.

Inventive Principle:
Principle #40Composite materials

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 drug-resistant cancer cell proliferation with reduced toxicity, demonstrating improved efficacy and synergistic effects compared to single triptolide treatments, with enhanced safety profiles.

Implementation Method 1

subjecting compounds in a mixture of a Tripterygium wilfordii suspension cell extracting solution-derived analytical sample and a Tripterygium wilfordii suspension cell culture solution-derived analytical sample to high-performance liquid chromatography (HPLC) separation

Methodology Applied
Scientific EffectChromatography: Chromatography

Data Source

PatentUS20230310531A1Tripterygium wilfordii composition for inhibiting drug-resistant cancer, and preparation method and use thereof
Publication Date: 2023.10.05 HUAQIAO UNIVERSITY
  • US20230310531A1 patent drawing
  • US20230310531A1 patent drawing
  • US20230310531A1 patent drawing

AI summary

The present disclosure provides a Tripterygium wilfordii composition for inhibiting a drug-resistant cancer. The composition is prepared by triptolide (TP) with any one or two compounds selected from the group consisting of 1β-(E-cinnamoyloxy)-4a-hydroxy-5a,7β,11-triacetoxy-8β-nicotinoyloxy-dihydroagarofuran, Demethylzeylasteral, Triptobenzene R, (3S,4S,5R,10S)-3,19-dihydroxy-7-ox-oabieta-8,11,13-triene, and Triptobenzene B. In the present disclosure, the composition has a lower toxicity and an enhanced drug effect for inhibiting proliferation of drug-resistant tumor cells than those of the TP. Compared with the single TP, the composition has an effect of attenuation and synergia.