Glechoma longituba Extract for DPP4 Inhibition

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Solution Overview

Problem

Current treatments for diabetes mellitus, kidney diseases, and weight management lack effective solutions for regulating blood glucose, blood lipids, and weight loss, particularly in diabetic patients, with existing extracts from Glechoma longituba (Nakai) Kupr. not fully utilizing its potential antidiabetic and lipid-regulating compounds.

Innovation Solution

An extract of Glechoma longituba (Nakai) Kupr. comprising luteolin-7-O-[β-glucuronosyl(1→2)β-glucuronic acid] and apigenin-7-O-[β-glucuronosyl(1→2)β-glucuronic acid] is developed, with specific concentrations of these compounds, obtained through an aqueous extraction and alcoholic precipitation process, to create a medicament for decreasing blood glucose, blood lipids, and treating kidney diseases.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If traditional extraction methods (65% ethanol extract) are used to obtain Glechoma longituba extract, then the extract contains total flavones with some blood glucose decreasing activity, but the extract does not contain the specific active compounds luteolin-7-O-[β-glucuronosyl(1→2)β-glucuronic acid] and apigenin-7-O-[β-glucuronosyl(1→2)β-glucuronic acid] with potent DPP4 inhibitory activity

Engineering Contradiction:
Improveantidiabetic activityVSAvoidcontent of active compounds
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The patent changes the extraction parameters by using aqueous extraction followed by alcoholic precipitation instead of traditional 65% ethanol extraction. This parameter change enables the isolation of specific glucuronide compounds (luteolin-7-O-[β-glucuronosyl(1→2)β-glucuronic acid] and apigenin-7-O-[β-glucuronosyl(1→2)β-glucuronic acid]) that have potent DPP4 inhibitory activity, thereby improving both the reliability and quantity of active compounds in the extract

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent applies extraction by selectively isolating specific active compounds from the Glechoma longituba plant material. Through aqueous extraction and alcoholic precipitation, the patent extracts and concentrates the specific glucuronide compounds with DPP4 inhibitory activity, separating them from other plant constituents to achieve a extract with high content of the desired active substances

Inventive Principle:
Principle #2Taking out (Extraction)

2Reliability

If existing Glechoma longituba extracts are used, then the extract provides some metabolic regulation effects, but the extract lacks sufficient potency for effective treatment of diabetes mellitus and kidney diseases

Engineering Contradiction:
Improvetreatment efficacyVSAvoidextraction process complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent modifies the extraction parameters by employing aqueous extraction followed by alcoholic precipitation, which selectively isolates compounds with DPP4 inhibitory activity. This parameter change transforms the extract into a potent therapeutic agent for diabetes and kidney diseases while maintaining a relatively simple two-step extraction process

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent uses alcohol as an intermediary substance in the extraction process. By adding alcohol to the aqueous extract, the patent precipitates specific compounds while leaving others in solution, thereby selectively isolating the active ingredients with DPP4 inhibitory activity without requiring complex chromatographic separation methods

Inventive Principle:
Principle #24Intermediary (Mediator)

3Quantity of substance

If conventional extraction methods are used, then the extraction process is simple, but the extract does not achieve optimal concentration of active compounds for effective blood glucose and blood lipid regulation

Engineering Contradiction:
Improveconcentration of active compoundsVSAvoidextraction process simplicity
Core Design Contradiction:
Quantity of substanceVSEase of manufacture

Solution Approach 1:

The patent optimizes the extraction parameters by using aqueous extraction followed by alcoholic precipitation. This parameter optimization achieves high concentration of active compounds (luteolin-7-O-[β-glucuronosyl(1→2)β-glucuronic acid] and apigenin-7-O-[β-glucuronosyl(1→2)β-glucuronic acid]) in the final extract while maintaining a simple two-step process that is easy to manufacture

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The extraction process utilizes the inherent solubility characteristics of the active compounds. The aqueous extraction step dissolves the polar glucuronide compounds, and the subsequent alcoholic precipitation step automatically concentrates them through selective precipitation, allowing the system to self-separate and concentrate the active ingredients without requiring additional purification equipment or complex operations

Inventive Principle:
Principle #25Self-service

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 effectively inhibits DPP4 activity, reduces blood glucose levels, decreases blood lipids, and aids in weight loss, demonstrating significant antidiabetic and lipid-regulating effects, as shown by enhanced acute oral glucose tolerance and insulin secretion in animal models.

Implementation Method 1

The aqueous extract liquid is treated with alcohol to precipitate, thereby obtaining the extract of Glechoma longituba

Methodology Applied
Scientific EffectPrecipitation: Precipitation

Data Source

PatentEP3120847B1Glechoma longituba extract for the treatment of kidney diseases or diabetes mellitus
Publication Date: 2023.11.08 SHANGHAI AINHERB BIOTECH CO LTD
  • EP3120847B1 patent drawingFigure 1
  • EP3120847B1 patent drawingFigure 2
  • EP3120847B1 patent drawingFigure 3

AI summary

Disclosed is a Glechoma longituba (Nakai) Kupr. extract, specifically compounds I and II, a preparation method for same, and a use thereof in preparing a medicament for blood glucose decease, blood lipids decrease, weight loss, and kidney disease treatment or a method for treatment of said diseases, and a composition containing the extract.