Monascuspurpurone Compounds for Insulin Resistance Treatment
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Solution Overview
Problem
Current red yeast rice fermented with Monascus spp. products show anti-diabetic effects but the specific compounds responsible and their pharmacological mechanisms are not disclosed in prior arts.
Innovation Solution
A compound of formula (I), rel-(1S,7aR,3aR)-1-Hexanoyl-5,13-dimethyl-6-(2-oxopentyl)-7a,7-dihydrobenzofuran-2,4-dione, and its pharmaceutically acceptable derivatives, are used to promote adipocyte differentiation, increase PPARγ and C/EBPα activity, lower blood glucose, and treat insulin resistance, along with a process involving fermentation of rice with Monascus spp. and extraction using solvents like methanol or ethyl acetate.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If red yeast rice fermented with Monascus spp. is used to treat hyperlipidemia and lower blood glucose, then cholesterol-lowering and anti-diabetic effects are achieved, but the specific compounds responsible and their pharmacological mechanisms remain unidentified
Solution Approach 1:
The patent extracts and isolates specific monascuspurpurone compounds from the complex red yeast rice fermentation mixture. Through systematic extraction using solvents like methanol and ethyl acetate, followed by chromatographic separation, the invention identifies monascuspurpurone A, B, C, and D as the specific active compounds responsible for the therapeutic effects, thereby resolving the information loss about active constituents.
Solution Approach 2:
The patent segments the complex fermentation product into individual pure compounds for identification. By separating monascuspurpurone A, B, C, and D as distinct entities with defined chemical structures and properties, the invention enables individual characterization of each compound's pharmacological activity, mechanism of action, and metabolic profile, thus identifying the specific agents responsible for therapeutic effects.
2Quantity of substance
If conventional lipid-lowering drugs are used, then cholesterol levels decrease, but liver function is adversely affected and side effects occur
Solution Approach 1:
The patent identifies monascuspurpurone compounds as natural alternatives to conventional synthetic lipid-lowering drugs. These naturally occurring compounds from Monascus fermentation provide cholesterol-lowering effects through physiological mechanisms (inhibition of HMG-CoA reductase, modulation of lipid metabolism) without the hepatotoxicity and severe side effects associated with conventional drugs like statins, offering a safer therapeutic option.
Solution Approach 2:
The patent changes the therapeutic parameter from synthetic drug administration to natural compound extraction and identification. By characterizing monascuspurpurone compounds with their specific chemical structures, physical properties, and metabolic profiles, the invention provides a natural alternative that achieves lipid-lowering effects through physiological pathways without the harmful side effects of conventional pharmacological interventions.
3Quantity of substance
If red yeast rice fermented with Monascus spp. is used, then blood glucose levels are lowered and anti-diabetic effects are observed, but the mechanism of action on adipocyte differentiation and insulin resistance remains undisclosed
Solution Approach 1:
The patent extracts monascuspurpurone compounds and specifically investigates their effect on adipocyte differentiation and insulin sensitivity. Through in vitro and in vivo studies, the invention reveals that these compounds activate PPARγ and C/EBPα, promote adipocyte differentiation, and improve insulin sensitivity, thereby uncovering the pharmacological mechanisms responsible for the anti-diabetic effects of red yeast rice.
Solution Approach 2:
The patent segments the pharmacological mechanism into specific molecular pathways by identifying monascuspurpurone compounds as PPARγ agonists. The invention characterizes the compounds' ability to activate PPARγ and C/EBPα, regulate adipogenic gene expression, and improve insulin sensitivity, thereby elucidating the specific molecular mechanisms underlying the blood glucose-lowering and anti-diabetic effects.
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 compound effectively promotes adipocyte differentiation, increases PPARγ and C/EBPα activity, and lowers blood glucose, providing a method for preventing and treating insulin resistance and metabolic syndrome.
Implementation Method 1
red yeast rice fermented with Monascus spp.
Implementation Method 2
produce bioactive metabolites such as γ-aminobutyric acid (GABA), polyketides monacolin K, and demerumic acid
Implementation Method 3
extraction using solvents like methanol or ethyl acetate
Data Source
AI summary
The present invention relates to a monascuspurpurone compound of formula (I):or a pharmaceutically acceptable derivative thereof as described in the specification, the process for preparation of the same, and the composition comprising the same. The uses of a monascuspurpurone compound for promoting adipocyte differentiation, for increasing the activity of PPARγ and/or C/EBPα, for lowering blood glucose, for preventing and/or treating a disease or disorder related to insulin resistance, and for preventing and/or treating metabolic syndrome or its complications are also provided.