Anticancer and Anti‐Inflammatory Potential of Coptisine as a Planar Quaternary Benzo[C]Phenanthridine Alkaloid With G‐Quadruplex DNA Telomeric Induction Activity

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Abstract
Coptisine, an isoquinoline‐based phytochemical, exhibits a broad spectrum of biological activities, including anticancer and anti‐inflammatory properties. Its planar chemical structure allows for the induction of anticancer effects by forming telomeric G‐quadruplex structures. Despite its promising medicinal benefits, the clinical utilization of this compound is limited by critical shortcomings such as low efficacy and poor pharmacokinetics. While in vitro studies demonstrate high cytotoxicity, in vivo research highlights its favorable toxicity profile, attributed to the conversion of its iminium form to a less toxic alkanolamine form within the physiological setting. Past endeavors have focused on rectifying these limitations through structural modifications to yield more efficacious molecules. In the current review, we provide an overview of the anti‐inflammatory and anticancer properties of coptisine and its semisynthetic derivatives, in conjunction with its pharmacokinetic profile, synthesis, and safety/toxicity considerations. This review draws upon information sourced from publications indexed in esteemed scientific databases like Web of Science, PubMed, and Scopus, among others. To prepare each section, we utilized Coptisine and section‐specific keywords, emphasizing recent literature findings (2014–2024) while maintaining a broad scope due to the study's nature. In conclusion, this review underscores coptisine's remarkable anticancer and anti‐inflammatory properties, suggesting that further exploration of structural modifications may yield semisynthetic derivatives with enhanced safety/toxicity profiles, pharmacokinetics, and therapeutic potential.

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