L-PGDS Production Promotion in Pericytes Using Vaccinia Tissue Extract

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Solution Overview

Problem

There is a lack of substances that effectively promote lipocalin-type prostaglandin D2 synthase (L-PGDS) production, which is crucial for brain-protective and sleep-promoting actions, and no effective screening methods for drugs targeting L-PGDS associated diseases such as cerebral infarction and Alzheimer's disease.

Innovation Solution

An extract from inflamed tissues of animals inoculated with vaccinia virus is used to promote L-PGDS production in ischemia-induced multipotent stem cells (iSCs), serving as an index for screening drugs with brain-protective and sleep-promoting actions, and is developed into a highly safe pharmaceutical preparation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If conventional methods are used to promote L-PGDS production, then L-PGDS levels increase, but no effective substances or screening methods exist currently

Engineering Contradiction:
ImproveL-PGDS productionVSAvoidavailability of promoting substances
Core Design Contradiction:
Quantity of substanceVSEase of manufacture

Solution Approach 1:

The patent uses vaccinia virus as an intermediary substance to stimulate L-PGDS production. The virus infects animal tissues, triggering an immune response that upregulates L-PGDS expression. This mediator approach solves the problem of finding effective promoting substances by using a biological agent that naturally induces L-PGDS synthesis through immune activation.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the biological state parameters of animal tissues by introducing vaccinia virus infection, which alters the expression levels of L-PGDS. By modifying the physiological condition (from healthy to virus-infected state), the system naturally increases L-PGDS production without requiring direct chemical intervention.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If L-PGDS production is increased, then brain-protective and sleep-promoting actions are enhanced, but screening methods for such drugs are lacking

Engineering Contradiction:
Improvebrain-protective actionVSAvoidscreening capability
Core Design Contradiction:
ReliabilityVSDifficulty of detecting and measuring

Solution Approach 1:

The patent establishes a feedback-based screening system where L-PGDS production levels serve as a measurable indicator of drug efficacy. By using L-PGDS expression as a feedback signal, researchers can screen and evaluate compounds that promote L-PGDS production, thereby identifying drugs with brain-protective and sleep-promoting actions through a quantifiable metric.

Inventive Principle:
Principle #23Feedback

Solution Approach 2:

The patent replaces complex functional assays for measuring brain protection and sleep promotion with a more straightforward molecular biology approach - measuring L-PGDS protein or mRNA levels. This substitution simplifies the screening process by using accessible molecular markers instead of requiring complex behavioral or physiological measurements.

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

3Productivity

If L-PGDS is used as a carrier for lipophilic molecules, then transport function is enhanced, but specificity of target delivery is reduced

Engineering Contradiction:
Improvetransport capacityVSAvoidtarget delivery specificity
Core Design Contradiction:
ProductivityVSMeasurement precision

Solution Approach 1:

The patent exploits the natural local quality of L-PGDS by targeting its overexpression to specific brain regions affected by disease. Rather than attempting to control where the carrier delivers molecules systemically, the approach uses localized upregulation of L-PGDS in diseased areas to create region-specific transport capacity, thereby maintaining target delivery specificity through spatial concentration of the carrier protein.

Inventive Principle:
Principle #3Local quality

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 increases L-PGDS production, reducing Aβ levels and improving cognitive function in Alzheimer's disease models, providing a therapeutic and preventive agent for cerebrovascular disorders and dementia, with minimal side effects.

Implementation Method 1

L-PGDS has a catalytic activity for isomerization of prostaglandin H2 (PGH2), which is a common intermediate reaction in prostaglandin biosynthesis, to prostaglandin D2 (PGD2)

Methodology Applied
Scientific EffectIsomerization:

Implementation Method 2

L-PGDS has a huge lipophilic pocket as compared to other lipocalins. Thus, it is thought that L-PGDS acts as a transporter protein and a scavenger for various lipophilic molecules in the brain

Methodology Applied
Scientific EffectLipophilic binding: Absorption (physical)

Implementation Method 3

when subarachnoid hemorrhage occurs, an intracerebral L-PGDS level is increased, and protects brain from neuronal damages by conjugating with bilirubin, a neurotoxic substance

Methodology Applied
Scientific EffectConjugation: Chemical Bonding

Implementation Method 4

L-PGDS strictly binds to a site essential for oligomerization of amyloid β-protein (Aβ, a senile plaque) to inhibit formation of Aβ deposition in cerebrospinal fluid and cytotoxicity

Methodology Applied
Scientific EffectProtein binding: Absorption (physical)

Data Source

PatentEP3733205B1Lipocalin-type prostaglandin d2 synthase production accelerating agent
Publication Date: 2025.11.19 NIPPON ZOKI PHARMACEUTICAL CO LTD
  • EP3733205B1 patent drawingFigure 1~2
  • EP3733205B1 patent drawingFigure 3~5
  • EP3733205B1 patent drawingFigure 6

AI summary

An object of the present invention is to provide a lipocalin-type prostaglandin D2 synthase (L-PGDS) production promoting agent, more specifically an L-PGDS production promoting agent in pericytes or ischemia-induced multipotent stem cells (iSCs) dedifferentiated from pericytes. In the present invention, it has been found that a substance having an L-PGDS production promoting action is contained in an extract from inflamed tissues inoculated with vaccinia virus. An L-PGDS production promoting agent is highly useful as a preventive, therapeutic or relapse preventive agent for a disease in which the effect by promotion of L-PGDS expression is expected to be effective, including a cerebrovascular disorder such as cerebral infarction, dementia such as Alzheimer's disease, or a sleep disorder.