Cepharanthine Pharmacology in Cancer Therapeutics

Cepharanthine (CEP) is a natural bisbenzylisoquinoline alkaloid extracted from Stephania species, known for over seven decades of clinical use. In oncology, CEP exerts a spectrum of antitumour actions: it induces apoptosis through mitochondrial and death‐receptor pathways, provokes cell‐cycle arrest at G₂/M or G₀/G₁ checkpoints, and elevates reactive oxygen species to disrupt redox balance. It also modulates key signalling cascades—such as Nrf2/Keap1, p53, JNK and PI3K/Akt—to impair proliferation, enhance chemosensitivity and reverse multidrug resistance mediated by P-glycoprotein. Network pharmacology and bioinformatics studies further implicate CEP in targeting cell‐cycle kinases and stemness‐related factors in lung and oesophageal malignancies. Despite its potent bioactivities, CEP’s poor water solubility and limited oral bioavailability have driven the development of inhalable, injectable or nanoparticulate formulations for improved tissue delivery. Taken together, CEP represents a versatile candidate for monotherapy and adjuvant therapy across a range of solid tumours, with ongoing efforts to optimise its pharmacokinetic and pharmacodynamic profiles.

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Cepharanthine Pharmacology in Cancer Therapeutics publication trend

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Technical terms

Apoptosis: Programmed cell death involving characteristic morphological and biochemical changes.

Cell‐cycle arrest: Halting of cell division at specific checkpoints (G₀/G₁ or G₂/M) to prevent proliferation.

Reactive oxygen species (ROS): Chemically reactive molecules containing oxygen that can induce oxidative stress and cell damage.

Nrf2/Keap1 pathway: A redox‐sensing mechanism regulating antioxidant gene expression and cellular defence against oxidative stress.

Multidrug resistance (MDR): The ability of cancer cells to evade chemotherapy, often via efflux transporters such as P-glycoprotein.

P-glycoprotein (P-gp): A membrane transporter that expels cytotoxic drugs from cells, contributing to chemotherapy resistance.

Cancer stemness: The property of tumour cells to self‐renew and differentiate, associated with treatment resistance and recurrence.

References

1. Cepharanthine, a regulator of keap1-Nrf2, inhibits gastric cancer growth through oxidative stress and energy metabolism pathway. Cell Death Discovery (2023).
2. Pharmacological Effects and Clinical Prospects of Cepharanthine. Molecules (2022).
3. Cepharanthine hydrochloride reverses the mdr1 (P-glycoprotein)-mediated esophageal squamous cell carcinoma cell cisplatin resistance through JNK and p53 signals. Oncotarget (2017).
4. Effect of Cepharanthine on the Stemness of Lung Squamous Cell Carcinoma Based on Network Pharmacology and Bioinformatics. BioMed Research International (2022).