Artichoke Extract Standardization for HDL Elevation

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Solution Overview

Problem

The reproducibility of Cynara scolymus extracts is low due to variations in plant biomass and drying conditions, making it difficult to evaluate therapeutic activity and compare with other drugs, with existing extracts providing only modest cholesterol reduction and inconsistent HDL cholesterol increases.

Innovation Solution

A novel extract with high flavonoids and sesquiterpenes is produced from the leaves of selected artichoke cultivars, specifically grown using organic techniques and dried at controlled temperatures, ensuring consistent active ingredient content and enhanced therapeutic effects, including increased HDL cholesterol levels.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of manufacture

If Cynara scolymus extracts are prepared from plant biomass with varying growing conditions, then the production cost and accessibility are improved, but the reproducibility and consistency of active ingredient content deteriorate

Engineering Contradiction:
Improveproduction accessibilityVSAvoidactive ingredient content consistency
Core Design Contradiction:
Ease of manufactureVSManufacturing precision

Solution Approach 1:

The patent applies parameter changes by precisely controlling drying temperature (60-100°C) and duration (18-72 hours) to maintain consistent active ingredient content across different batches. This standardization of processing parameters resolves the contradiction between ease of manufacture and manufacturing precision by establishing reproducible conditions that can be widely implemented while ensuring consistent extract quality.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs preliminary action by selecting and cultivating specific plant varieties with known active ingredient profiles before extraction. By pre-characterizing the plant biomass and establishing controlled growing conditions, the patent ensures that the starting material consistently yields extracts with reproducible therapeutic activity, thereby resolving the contradiction between accessibility and consistency.

Inventive Principle:
Principle #10Preliminary action

2Ease of operation

If existing Cynara scolymus extracts are used, then the treatment accessibility is improved, but the therapeutic efficacy for increasing HDL cholesterol deteriorates

Engineering Contradiction:
Improvetreatment accessibilityVSAvoidHDL cholesterol increase effectiveness
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent achieves reliable HDL cholesterol increase by changing the compositional parameters of the extract through controlled drying processes that preserve heat-sensitive flavonoids and sesquiterpenes. This results in an extract with optimized active ingredient profiles that consistently demonstrate therapeutic efficacy while remaining accessible for clinical use.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent utilizes composite materials by combining multiple active ingredients (flavonoids, sesquiterpenes, and other phytochemicals) in specific ratios achieved through controlled extraction. This composite approach enhances the reliability of HDL cholesterol elevation compared to single-compound preparations, while the natural origin maintains treatment accessibility.

Inventive Principle:
Principle #40Composite materials

3Manufacturing precision

If drying conditions are optimized to preserve active ingredients, then the therapeutic activity consistency is improved, but the processing time and energy consumption increase

Engineering Contradiction:
Improvetherapeutic activity consistencyVSAvoiddrying processing time
Core Design Contradiction:
Manufacturing precisionVSLoss of time

Solution Approach 1:

The patent optimizes the trade-off between therapeutic consistency and processing time by establishing specific drying parameters: temperatures between 60-100°C and durations of 18-72 hours. These parameter ranges are carefully selected to preserve heat-sensitive active ingredients while avoiding excessively long processing times, thereby resolving the contradiction between manufacturing precision and time loss.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs periodic action by using intermittent or cyclic drying processes that allow periods of heat application followed by rest periods. This approach preserves active ingredients through controlled thermal exposure while reducing total processing time compared to continuous high-temperature drying, thus balancing therapeutic consistency with time efficiency.

Inventive Principle:
Principle #19Periodic action

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 extract significantly reduces total and LDL cholesterol, increases HDL cholesterol by 19%, and normalizes lipid and carbohydrate balances, effectively treating dyslipidaemia, dyspepsia, and non-alcoholic liver steatosis, with consistent results across patient groups.

Implementation Method 1

the cynaropicrin present in the extract of the invention also acts at hepatic level on the enzymes that regulate HDL biosynthesis

Methodology Applied
Scientific EffectCholesterol metabolism modulation:

Implementation Method 2

flavonoids, which perform a hypolipaemic action associated with cholesterol synthesis

Methodology Applied
Scientific EffectHypolipaemic action:

Implementation Method 3

Globe artichoke (Cynara scolymus) extracts are known for their choleretic, cholagogic, anti-dyspepsia and mildly cholesterol-reducing action

Methodology Applied
Scientific EffectCholeretic effect:

Implementation Method 4

caffeoylquinic acids, which perform a choleretic, blood-sugar reducing and liver-protecting effect

Methodology Applied
Scientific EffectBlood-sugar reducing action:

Implementation Method 5

cynaropicrin, which performs an anti-inflammatory action due to interaction with nuclear factor NFkB and TNF-α

Methodology Applied
Scientific EffectAnti-inflammatory action:

Data Source

PatentUS9687468B2<i>Cynara scolymus </i>extracts for the treatment of dyslipidaemia
Publication Date: 2017.06.27 INDENA SPA

AI summary

The present invention relates to the preparation of Cynara scolymus leaf extracts, which are useful for the prevention and treatment of dyslipidaemia, in particular to increase HDL cholesterol in patients at cardiovascular risk. Said extracts are useful to normalize the lipid and carbohydrate balances and significantly increase the value of HDL cholesterol by favorably changing the LDL/HDL ratio, especially in post-infarction patients with drug-induced dyslipidaemia.