A review on structural modifications of parthenin extracted from Parthenium hysterophorus L

Parthenin is a sesquiterpene lactone extracted from Parthenium hysterophorus that possesses a broad spectrum of biological activities, including anti-inflammatory, antimicrobial, anticancer, and allelopathic properties. However, its clinical applications are hindered by cytotoxicity, poor solubility, low bioavailability, and instability in physiological conditions. To address these challenges, numerous structural modifications have been explored to improve its pharmacokinetic properties while enhancing its therapeutic potential. This review provides a comprehensive overview of the chemical modifications of parthenin, including hydroxylation, halogenation, Michael addition, and lactone ring alterations. Modifications, particularly in the lactone and cyclopentenone rings, can significantly enhance its anticancer, antimicrobial, and anti-inflammatory activities while reducing toxicity. The review also highlights recent pharmacological advancements and outlines promising directions for future drug development based on the parthenin derivatives. Overall, the study underscores the value of parthenin and its derivatives as innovative therapeutic agents and contributes to the progress of natural product-based drug design.