Marine Macrolides for Selective Anticancer Therapy

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Solution Overview

Problem

Current treatments for cancer lack effective, non-toxic bioactive compounds with significant anticancer activity.

Innovation Solution

Isolation and hemisynthesis of novel macrolide-type molecules from Verongidae sponges, specifically Suberea sp. sponges, which are converted into pharmaceutically acceptable salts, hydrates, or solvates for use in cancer treatment, involving maceration, extraction, and purification processes.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current cancer treatments are used, then cancer cells can be targeted, but high toxicity and lack of effectiveness are encountered

Engineering Contradiction:
Improveanticancer activityVSAvoidtoxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent extracts bioactive macrolide compounds specifically from marine sponges (Verongidae family, Suberea sp.) through maceration and extraction processes. This isolation of specific natural products with proven anticancer activity allows for targeted therapy while avoiding the toxicity associated with conventional cancer treatments.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent uses macrolide compounds as intermediary substances that mediate between the natural source (sponge) and the therapeutic effect (anticancer activity). These macrolides serve as bioactive intermediaries that can selectively target cancer cells while sparing normal cells, thus reducing toxicity.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Reliability

If novel macrolide compounds are isolated from sponges, then potent anticancer activity is achieved, but complex extraction and purification processes are required

Engineering Contradiction:
Improveanticancer activityVSAvoidextraction process complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The extraction process is segmented into distinct stages: maceration of sponge material, extraction with organic solvents, and purification steps. This segmentation allows for systematic isolation of macrolide compounds while managing the complexity of the overall process through structured, stepwise procedures.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent performs preliminary maceration and extraction steps to concentrate the macrolide compounds from the sponge matrix before final purification. This preliminary action simplifies subsequent isolation steps by pre-concentrating the bioactive compounds and removing bulk impurities.

Inventive Principle:
Principle #10Preliminary action

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 compounds demonstrate potent anticancer activity, inhibiting cell growth in various tumor cell lines, including melanoma, lung, and ovarian cancer, with potential for safe and effective pharmaceutical application.

Implementation Method 1

The compounds demonstrate potent anticancer activity, inhibiting cell growth in various tumor cell lines

Methodology Applied
Scientific EffectAnticancer activity:

Data Source

PatentUS9873715B2Macrolides useful as anticancer agents
Publication Date: 2018.01.23 PIERRE FABRE MEDICAMENT SAS
  • US9873715B2 patent drawing
  • US9873715B2 patent drawing
  • US9873715B2 patent drawing

AI summary

The present invention relates to a compound of the following formula (I) or to a salt, hydrate, or pharmaceutically acceptable solvate thereof, in which R is a monosaccharide or disaccharide residue. The hydroxyl functions of the monosaccharide or disaccharide residue are, independently, optionally substituted for a (C1-C6) alkyl or —C(O)NH—(C1-C6) alkyl group. The invention also relates to the method for preparing said compound, to a pharmaceutical composition containing same, and to the use thereof as a drug, particularly for cancer treatment.