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Anticancer and Anti-Inflammatory Potential of Coptisine As a Planar Quaternary Benzo[C]Phenanthridine Alkaloid With G-Quadruplex Dna Telomeric Induction Activity Publisher Pubmed



Valipour M1 ; Sheibani M2, 3 ; Dibaei M4 ; Khatir ZZ5 ; Ayati A6 ; Motafeghi F7 ; Irannejad H5
Authors
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Authors Affiliations
  1. 1. Microbial Biotechnology Research Center, Iran University of Medical Sciences, Tehran, Iran
  2. 2. Razi Drug Research Center, Iran University of Medical Sciences, Tehran, Iran
  3. 3. Department of Pharmacology, School of Medicine, Iran University of Medical Sciences, Tehran, Iran
  4. 4. Department of Pharmaceutics, Faculty of Pharmacy, Biopharmaceutics and Pharmacokinetic Division, Tehran University of Medical Sciences, Tehran, Iran
  5. 5. Department of Medicinal Chemistry, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran
  6. 6. Medicinal and Natural Products Chemistry Research Center, Shiraz University of Medical Sciences, Shiraz, Iran
  7. 7. Reproductive Endocrine Research Center, Endocrine Research Institute, Shahid Beheshti University of Medical Sciences, Tehran, Iran

Source: Drug Development Research Published:2025


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. © 2025 Wiley Periodicals LLC.
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