Plant Extract Endothelin-Converting Enzyme Inhibitors

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Solution Overview

Problem

Current materials fail to effectively inhibit endothelin-converting enzyme (ECE) activity, which contributes to conditions like hypertension and skin pigmentation issues, limiting their use in antihypertensive and skin whitening applications.

Innovation Solution

The use of plant extracts from Hiptage candicans, Piper sarmentosum, Solanum stramonifolium, Anaxagorea luzonensis, Smilax corbularia, Ardisia elliptica, Erythrina suberosa, and Hopea ferrea, which exhibit ECE inhibitory activity, are employed as active ingredients in endothelin-converting enzyme inhibitors, melanogenesis inhibitors, and skin whitening agents.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional ECE inhibitors like burnet extract are used, then some ECE inhibitory activity is achieved, but the inhibitory activity is insufficient for effective antihypertensive and skin whitening applications

Engineering Contradiction:
ImproveECE inhibitory activityVSAvoideffectiveness in antihypertensive and skin whitening applications
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The patent changes the parameter of ECE inhibitory activity by identifying and utilizing plant extracts with superior inhibitory potency compared to conventional inhibitors. The selected plant extracts (Hiptage candicans, Piper sarmentosum, Solanum stramonifolium, Anaxagorea luzonensis, Smilax corbularia, Ardisia elliptica, Erythrina suberosa, Dactyloctenium aegyptium, and Hopea ferrea) demonstrate enhanced ECE inhibition capability, transforming the insufficiency problem into an improved performance solution.

Inventive Principle:
Principle #35Parameter changes

2Productivity

If plant extracts with strong ECE inhibitory activity are used, then antihypertensive and skin whitening effects are enhanced, but the complexity of identifying and validating new plant materials increases

Engineering Contradiction:
Improveantihypertensive and skin whitening effectsVSAvoidcomplexity of identifying and validating new plant materials
Core Design Contradiction:
ProductivityVSDevice complexity

Solution Approach 1:

The patent applies preliminary action by pre-identifying and pre-validating plant materials with ECE inhibitory activity before their clinical application. The inventors have already screened and confirmed the ECE inhibitory properties of the selected plant extracts, establishing their efficacy in advance. This preliminary validation reduces the complexity and time required for subsequent clinical development and application.

Inventive Principle:
Principle #10Preliminary action

3Ease of manufacture

If existing plant materials with moderate ECE inhibitory activity are used, then the development process is simpler, but the therapeutic and cosmetic effects are insufficient

Engineering Contradiction:
Improvesimplicity of development processVSAvoidtherapeutic and cosmetic effects
Core Design Contradiction:
Ease of manufactureVSReliability

Solution Approach 1:

The patent employs copying by utilizing well-known plant materials that have been traditionally used in medicine and cosmetics. The selected plants (such as Piper sarmentosum, Solanum stramonifolium, and others) are established species with known safety profiles and traditional uses, allowing the development process to proceed with reduced complexity while achieving superior ECE inhibition and therapeutic effects compared to unvalidated new materials.

Inventive Principle:
Principle #26Copying

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

These plant extracts demonstrate significant ECE inhibitory activity, effectively reducing endothelin levels, thereby providing antihypertensive effects and skin whitening benefits, outperforming known ECE inhibitors like burnet extract.

Implementation Method 1

The enzyme, which converts the intermediate to the mature endothelin, is endothelin-converting enzyme (ECE). Conventionally, it has been reported that examples of a plant material having ECE inhibitory activity include extracts obtained from burnet (Sanguisorba officinalis), hawthorn (Crataegus laevigata), clove (Syzygium aromaticum), rose fruit (fruit of Rosa multiflora), gambir (Uncaria gambir), linden (Tilia miqueliana), licorice (Glycyrrhiza glabra), mulberry bark (Morus alba), rosemary (Rosmarinus officinalis), Assam tea plant (Camellia sinensis var. assamica), Japanese white birch (Betula platyphylla var. japonica), tormentilla (Potentilla tormentilla), thyme (Thymus), gentian (Gentiana lutea), geranium (Geranium nepalense), ginseng (Panax ginseng C. A. Mayer), cinchona (Cinchona succirubra), Japanese green gentian (Swertia japonica), centella (Centella asiatica), capillary artemisia (Artemisia capillaris), rehmannia root (Rehmannia glutinosa), honeysuckle (Lonicera japonica), and peppermint (Mentha piperita)

Methodology Applied
Scientific EffectEnzyme inhibition: Enzyme

Implementation Method 2

suppression of the expression of endothelin is considered to be useful, not only for prevention and/or treatment of the aforementioned various diseases, but also for prevention or amelioration of skin pigmentation

Methodology Applied
Scientific EffectMelanogenesis inhibition:

Data Source

PatentUS11278748B2Endothelin-converting enzyme inhibitor
Publication Date: 2022.03.22 KAO CORP

AI summary

Provision of a material, which has activity of inhibiting endothelin-converting enzyme and is effective for skin whitening or antihypertension. An endothelin-converting enzyme inhibitor comprising, as an active ingredient, at least one selected from the group consisting of Hiptage candicans, Piper sarmentosum, Solanum stramonifolium, Anaxagorea luzonensis, Smilax corbularia, Ardisia elliptica, Erythrina suberosa, Dactyloctenium aegyptium, Hopea ferrea and extracts thereof.