Platycodin D and Statin Synergy for LDLR Expression

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Solution Overview

Problem

Current chemotherapeutic agents for hypercholesterolemia, such as statin-class drugs, have adverse side effects due to non-specific cytotoxicity and do not effectively lower cholesterol levels when administered in large doses, while the molecular mechanism of Platycodin D in treating hypercholesterolemia remains unclear, and its synergistic effect with existing agents is unconfirmed.

Innovation Solution

A pharmaceutical composition combining Platycodon grandiflorum extract or Platycodin D with a statin-class drug to induce expression of low-density lipoprotein receptor (LDLR) in hepatocytes, enhancing the therapeutic effect of statins and reducing cholesterol levels.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If statin-class drugs are administered in large doses to lower cholesterol levels, then cholesterol reduction effect is improved, but adverse side effects increase due to non-specific cytotoxicity

Engineering Contradiction:

Improvecholesterol reduction effectVSAvoidadverse side effects

Core Design Contradiction:

Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

Platycodin D acts as an intermediary substance that enhances the cholesterol-lowering effect of statin-class drugs through synergistic interaction. The compound works by inducing LDLR expression and stabilizing LDLR protein, thereby amplifying the therapeutic effect of statins at lower doses and reducing the need for high-dose administration that causes cytotoxicity.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention employs a composite therapeutic approach by combining Platycodin D with statin-class drugs to create a synergistic formulation. This composite strategy leverages the cholesterol-lowering mechanism of statins (HMG-CoA reductase inhibition) alongside Platycodin D's mechanism (LDLR expression induction and protein stabilization), achieving enhanced therapeutic effect with reduced individual drug dosages and minimized side effects.

Inventive Principle:

Principle #40Composite materials

2Quantity of substance

If statin-class drugs are administered to treat hypercholesterolemia, then cholesterol levels are lowered, but the molecular mechanism is not fully understood and synergistic effect with natural extracts is unconfirmed

Engineering Contradiction:

Improvecholesterol levelsVSAvoidmolecular mechanism understanding

Core Design Contradiction:

Quantity of substanceVSLoss of information

Solution Approach 1:

The invention incorporates feedback mechanisms by investigating and elucidating the molecular mechanisms through which Platycodin D enhances statin efficacy. Research has revealed that Platycodin D induces LDLR expression and stabilizes LDLR protein through specific molecular pathways, providing feedback on the synergistic mechanism and enabling optimized therapeutic strategies based on understood biological processes.

Inventive Principle:

Principle #23Feedback

Data Source

PatentUS20220175862A1Co-administration composition for preventing or treating hypercholesterolemia, containing balloon-flower extract or platycodin d derived therefrom as active ingredient

Publication Date: 2022.06.09 UNIVERSITY INDUSTRY COOPERATION GROUP OF KYUNG HEE UNIVERSITY

AI summary

Provided are a pharmaceutical composition and a method for preventing or treating hypercholesterolemia, the pharmaceutical composition including a Platycodon grandiflorum extract or Platycodin D derived therefrom, and a statin-class drug as active ingredients. Also disclosed is a method of increasing expression of low-density lipoprotein receptor, the method including the step of treating hepatocytes in vitro with a Platycodon grandiflorum extract or Platycodin D derived therefrom.