Anticancer potential of synthetic costunolide and dehydrocostus lactone derivatives: A systematic review

Background

Costunolide (Cos) and dehydrocostus lactone (DhC) are naturally occurring sesquiterpene lactones with potent anticancer properties. Despite their promising bioactivity, limitations such as poor solubility, metabolic instability, and off-target toxicity restrict their clinical application. To overcome these challenges, synthetic derivatives have been developed to enhance cytotoxicity, selectivity, and pharmacokinetics.

Method

ology: Following Preferred Reporting Items for Systematic Review and Meta-Analyses (PRISMA) guidelines, a systematic literature was conducted across PubMed, SciFinder, ScienceDirect, Scopus, and Wiley Online Library. Thirteen studies published between 2006 and 2024 met the inclusion criteria, focusing on the anticancer properties of synthetic Cos and DhC derivatives.

Results

Synthetic modifications, particularly amino and triazole conjugations, improved tumor selectivity and water solubility, while maintaining or enhancing cytotoxic potency. The most effective derivatives induced apoptosid, cell cycle arrest, and oxidative stress in various cancer cell lines. However, pharmacokinetic data remain limited, and only one study included in vivo evaluation.

Conclusion

Synthetic derivatives of Cos and DhC exhibit enhanced anticancer potential and improved pharmacokinetic properties, making them promising candidates for drug potential. However, further in vivo studies and clinical trials are necessary to validate their therapeutic efficacy and safety.