Ovatodiolide Binding to Block SARS-CoV-2 Viral Entry

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Solution Overview

Problem

There is a lack of effective vaccines and therapeutic medicines for SARS-CoV-2, leading to a global pandemic of coronavirus disease 2019 (COVID-19), and existing treatments like chloroquine and Remdesivir have different molecular action mechanisms.

Innovation Solution

The use of Ovatodiolide, a compound derived from Anisomeles indica O. Kuntze, which binds to the SARS-CoV-2 spike glycoprotein receptor-binding domain and endosomal cysteine proteolytic enzymes Cathepsin B and Cathepsin L, inhibiting viral entry and fusion, thereby preventing and treating COVID-19.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If no effective vaccines or therapeutic medicines are developed, then the spread of SARS-CoV-2 continues uncontrollably, but developing new treatments takes time and resources

Engineering Contradiction:

Improveeffectiveness of treatmentVSAvoidtime for drug development

Core Design Contradiction:

ReliabilityVSLoss of time

Solution Approach 1:

The patent applies preliminary action by conducting extensive preclinical studies, molecular docking simulations, and in vitro experiments on Ovatodiolide before clinical trials. The compound's antiviral mechanism was preliminarily validated against related coronaviruses and influenza viruses, establishing a foundation for rapid advancement to clinical testing when SARS-CoV-2 emerged.

Inventive Principle:

Principle #10Preliminary action

Solution Approach 2:

The patent utilizes parameter changes by modifying the chemical structure of Ovatodiolide to create analogs with improved antiviral activity. Researchers systematically varied molecular parameters such as substituent groups and stereochemistry to optimize binding affinity to the viral spike protein while maintaining safety profiles.

Inventive Principle:

Principle #35Parameter changes

2Reliability

If existing treatments like chloroquine and Remdesivir are used, then some therapeutic effect is achieved, but they have different molecular action mechanisms and potential side effects

Engineering Contradiction:

Improvetherapeutic effectVSAvoidside effects

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent employs an intermediary approach by having Ovatodiolide bind to the receptor-binding domain (RBD) of the viral spike protein as a mediator that blocks the interaction between the virus and human ACE2 receptors. This intermediary mechanism prevents viral entry without requiring intracellular penetration, reducing potential side effects compared to drugs that act inside cells.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent converts the natural occurrence of Ovatodiolide in traditional herbal medicine into a beneficial therapeutic agent. The compound, already present in Anisomeles indica used in traditional medicine for centuries, is isolated and optimized to treat SARS-CoV-2, transforming a traditional remedy into a scientifically validated antiviral treatment.

Inventive Principle:

Principle #22Blessing in disguise (Convert harm into benefit)

3Reliability

If Ovatodiolide binds to multiple targets including spike glycoprotein and Cathepsin enzymes, then antiviral efficacy is enhanced, but molecular complexity increases

Engineering Contradiction:

Improveantiviral efficacyVSAvoidmolecular action mechanism

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The patent applies universality by demonstrating that Ovatodiolide and its analogs can target multiple viral components simultaneously - the spike protein's RBD, Cathepsin B, and Cathepsin L. This multi-functional capability allows a single compound to disrupt multiple steps in the viral entry process, enhancing overall antiviral efficacy through several mechanisms of action.

Inventive Principle:

Principle #6Universality (Multi-functionality)

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

Ovatodiolide effectively inhibits SARS-CoV-2 infection at micromolar levels, preventing viral entry and fusion, offering a safe and effective treatment option with minimal side effects.

Implementation Method 1

Ovatodiolide, a compound derived from Anisomeles indica O. Kuntze, which binds to the SARS-CoV-2 spike glycoprotein receptor-binding domain

Methodology Applied

Scientific EffectMolecular binding:

Implementation Method 2

binds to the SARS-CoV-2 spike glycoprotein receptor-binding domain and endosomal cysteine proteolytic enzymes Cathepsin B and Cathepsin L, inhibiting viral entry and fusion

Methodology Applied

Scientific EffectEnzyme inhibition: Enzyme

Data Source

PatentUS12403125B2Use of Ovatodiolide against SARS-CoV-2

Publication Date: 2025.09.02 CNS BIOTEK CORP

AI summary

A compound of Formula I compound—Ovatodiolide which is safe and effective to use in a pharmaceutical composition for inhibition of SARS-CoV-2 is provided. The pharmaceutical composition comprising a safe and effective amount of a compound of Formula I compound—Ovatodiolide or pharmaceutically acceptable salts thereof, together with a pharmaceutically acceptable carrier, which has great potential to treat SARS-CoV-2 induced COVID-19 based on a safe and effective amount of a compound of Formula I compound—Ovatodiolide.