Biotransformation and Biological Activity of Lactones
Summary
Lactones, characterised by their cyclic ester functionality, are ubiquitous natural and synthetic compounds that underpin a wide array of biological processes. In nature, sesquiterpene and terpenoid lactones serve as defence compounds, pheromones and signalling molecules, while synthetic analogues have been developed for pharmaceutical, agrochemical and flavour applications. Biotransformation—employing enzymes or whole cells—enables selective modifications such as hydroxylation, dehalogenation and ring expansion, yielding structural diversity and enantiomeric purity often inaccessible by conventional synthesis. These transformations can dramatically alter pharmacokinetic and bioactivity profiles, leading to new antimicrobial agents, anticancer leads and antimalarial drugs such as artemisinin derivatives. Advances in chemoenzymatic routes and engineered microbial catalysts have enhanced yield, selectivity and sustainability, offering green alternatives to harsh chemical methods. Structure–activity relationship studies have revealed that minor alterations in ring size, substituent position or stereochemistry can shift a compound from quorum-sensing modulator to potent cytotoxin. The convergence of biotransformation strategies with high-throughput screening and in silico design is reshaping the discovery pipeline, addressing global challenges such as antibiotic resistance and tumour heterogeneity while promoting renewable-feedstock utilisation.
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Biotransformation and Biological Activity of Lactones publication trend
The graph below shows the total number of articles in biotransformation and biological activity of lactones across all publications each year (not limited to Nature Index journals).
Technical terms
Lactone: A cyclic ester formed by intramolecular condensation of a hydroxy acid.
Biotransformation: Enzymatic or microbial conversion of a compound to structurally modified products.
Quorum sensing: Bacterial communication mechanism that regulates gene expression in response to cell density.
Hydrolytic dehalogenation: Enzymatic removal of a halogen atom from an organic molecule via hydrolysis.
References
- The use of the lactone motif in chemical communication. Natural Product Reports (2015).
- Biological Activity of Selected Natural and Synthetic Terpenoid Lactones. International Journal of Molecular Sciences (2021).
- Antimicrobial Activity of Lactones. Antibiotics (2022).
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