Macrocyclic Amide WH-21091 Antibacterial Antitumor Fermentation
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Solution Overview
Problem
Current antibacterial drugs face challenges due to emerging diseases and antibiotic resistance in bacteria, while cancer remains a significant threat, necessitating the development of new effective drugs with broad-spectrum antibacterial and antitumor activities.
Innovation Solution
A macrocyclic amide WH-21091, derived from symbiotic bacteria such as Xenorhabdus and Photorhabdus, is developed, along with its analogs, pharmaceutically acceptable salts, solvates, polymorphs, esters, tautomers, or prodrugs, which are produced through fermentation and purification processes, and can be used to treat infections and cancers.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional antibiotics are used to treat bacterial infections, then initial treatment effectiveness is achieved, but bacterial resistance develops rendering normal dosage insufficient
Solution Approach 1:
The patent employs parameter changes by modifying the chemical structure of macrocyclic compounds to create novel derivatives with enhanced antibacterial activity. The systematic variation of structural parameters (R1-R15 substituents) enables optimization of biological activity while overcoming bacterial resistance to conventional antibiotics.
Solution Approach 2:
The invention utilizes composite materials by combining macrocyclic amide structures with diverse substituent groups (R1-R15) to create compounds with multifaceted biological activities. This structural composite approach enables simultaneous antibacterial and antitumor properties, addressing multiple pathological challenges.
2Reliability
If new antibacterial substances are discovered from soil microbes, then broad-spectrum antibacterial activity is achieved, but the complexity of isolation and purification increases
Solution Approach 1:
The patent applies extraction principles by isolating macrocyclic amide compounds from microbial fermentation broths through systematic purification steps including concentration, solvent extraction, column chromatography, and preparative HPLC. This progressive extraction approach separates the active compounds from complex microbial metabolites.
Solution Approach 2:
The invention employs segmentation by dividing the purification process into distinct stages: initial concentration and precipitation, followed by solvent extraction, then column chromatography separation, and finally preparative HPLC purification. Each stage segments the complex mixture into progressively purer fractions.
3Reliability
If macrocyclic amide compounds are produced through fermentation, then natural production is achieved, but the productivity and yield are limited
Solution Approach 1:
The patent applies preliminary action by optimizing fermentation conditions (pH, temperature, aeration, nutrient composition) before macrocyclic amide production to maximize microbial growth and metabolite synthesis. Pre-culture conditions are carefully controlled to enhance subsequent productivity.
Solution Approach 2:
The invention uses parameter changes by systematically varying fermentation parameters (pH 6.0-7.5, temperature 25-37°C, aeration rates, carbon-to-nitrogen ratios) to optimize both the natural production authenticity and the yield of macrocyclic amide compounds during different fermentation stages.
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
WH-21091 demonstrates significant antibacterial activity against drug-tolerant bacteria and antitumor activity, offering a new generation of broad-spectrum antibiotics and antitumor agents, effective against various bacterial infections and cancers, including those resistant to common antibiotics.
Implementation Method 1
A macrocyclic amide WH-21091, derived from symbiotic bacteria such as Xenorhabdus and Photorhabdus, is developed, along with its analogs, pharmaceutically acceptable salts, solvates, polymorphs, esters, tautomers, or prodrugs, which are produced through fermentation and purification processes
Data Source
AI summary
Macrocyclic amide WH-21091 with antibacterial and antitumor activities, its analogs, preparation methods and uses thereof. The said macrocyclic amides are prepared by microbes of Xenorhabdus and Photorhabdus, or they can be prepared by other living beings through transgenic techniques. The compositions of the said macrocyclic amide and its analogs can be used as drugs and/or agricultural chemicals for treatment of microbial infections, especially for treatment of infectious diseases of Staphylococcus aureus with drug resistance. The said compositions can also be used as drugs for treatment of cancers of human beings or animals.