ArticleMolecules (Basel, Switzerland)2022
Dual Topoisomerase I/II Inhibition-Induced Apoptosis and Necro-Apoptosis in Cancer Cells by a Novel Ciprofloxacin Derivative via RIPK1/RIPK3/MLKL Activation.
Article in Molecules (Basel, Switzerland), 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 29 citations in OpenAlex.
- Ciprofloxacin beyond antibacterial therapy: pharmacological mechanisms, anticancer activity, and translational limitations.Naunyn-Schmiedeberg's archives of pharmacology · 2026Review
- Enhanced Antitumor Response in Breast Cancer via Parthanatos Activation Mediated by the Synergistic Effect of Etoposide and Resveratrol.Current issues in molecular biology · 2026Article
- Dexpanthenol mitigates trauma-induced lung injury by modulating RIPK1/RIPK3/MLKL-mediated necroptosis in rats.Scientific reports · 2026Article
- Rosmarinic Acid as a Potential Therapeutic Agent against Neuroblastoma: Anticancer Activity and Molecular Docking Insights.Anti-cancer agents in medicinal chemistry · 2026Article
- Design, Synthesis, and Mechanistic Study of Novel Ciprofloxacin/Thiazole Chalcone Hybrids as Potential Anticancer Agents.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Etoposide-induced cancer cell death: roles of mitochondrial VDAC1 and calpain, and resistance mechanisms.Molecular oncology · 2025Article
- (R)-WAC-224, a new anticancer quinolone, combined with venetoclax and azacitidine overcomes venetoclax-resistant AML through MCL-1 downregulation.Scientific reports · 2025Article
- Article
- Ciprofloxacin-encapsulated solid lipid nanoparticles: a comprehensive biochemical analysis of cytotoxic effects, proliferation inhibition, and apoptotic induction in KG1-a leukemia cells.Medical oncology (Northwood, London, England) · 2025Article
- From Infection to Tumor: Exploring the Therapeutic Potential of Ciprofloxacin Derivatives as Anticancer Agents.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Unveiling the potential of marine peptides in leukemia: mechanistic insights and future horizon in peptide research.Turkish journal of medical sciences · 2025Review
- The Imidazacridine Derivative LPSF/AC-05 Induces Apoptosis, Cell Cycle Arrest, and Topoisomerase II Inhibition in Breast Cancer, Leukemia, and Lymphoma.Current cancer drug targets · 2025Article
- PANoptosis: Novel insight into regulated cell death and its potential role in cardiovascular diseases (Review).International journal of molecular medicine · 2024Review
- Selagibenzophenone B and Its Derivatives:ACS bio & med chem Au · 2024Article
- Recent Development of Fluoroquinolone Derivatives as Anticancer Agents.Molecules (Basel, Switzerland) · 2024Review
- Advancements in Synthetic Strategies and Biological Effects of Ciprofloxacin Derivatives: A Review.International journal of molecular sciences · 2024Review
- Vincamine Ameliorates Epithelial-Mesenchymal Transition in Bleomycin-Induced Pulmonary Fibrosis in Rats; Targeting TGF-β/MAPK/Snai1 Pathway.Molecules (Basel, Switzerland) · 2023Article
- Synthesis of NovelAntibiotics (Basel, Switzerland) · 2023Article
- Article
- Curative Effect of AD-MSCs against Cisplatin-Induced Hepatotoxicity in Rats is Potentiated by Azilsartan: Targeting Oxidative Stress, MAPK, and Apoptosis Signaling Pathways.Stem cells international · 2023Article
Corrections and comments
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Authors and funding
8 authors at 5 institutions in 2 countries.
Funding
Abstract
Fluoroquinolones (FQs) are synthetic broad-spectrum antimicrobial agents that have been recently repurposed to anticancer candidates. Designing new derivatives of FQs with different moieties to target DNA topoisomerases could improve their anticancer efficacy. The present study aimed to synthesize a novel ciprofloxacin derivative, examine its anticancer activity against HepG2 and A549 cancer cells, and investigate the possible molecular mechanism underlying this activity by examining its ability to inhibit the topo I/II activity and to induce the apoptotic and necro-apoptotic pathways. Molecular docking, cell viability, cell migration, colony formation, cell cycle, Annexin V, lactate dehydrogenase (LDH) release, ELISA, and western blotting assays were utilized. Molecular docking results showed that this novel ciprofloxacin derivative exerted dual topo I and topo II binding and inhibition. It significantly inhibited the proliferation of A549 and HepG2 cancer cells and decreased their cell migration and colony formation abilities. In addition, it significantly increased the % of apoptotic cells, caused cell cycle arrest at G2/M phase, and elevated the LDH release levels in both cancer cells. Furthermore, it increased the expression of cleaved caspase 3, RIPK1, RIPK3, and MLKL proteins. This novel ciprofloxacin derivative exerted substantial dual inhibition of topo I/II enzyme activities, showed antiproliferative activity, suppressed the cell migration and colony formation abilities for A549 and HepG2 cancer cells and activated the apoptotic pathway. In addition, it initiated another backup deadly pathway, necro-apoptosis, through the activation of the RIPK1/RIPK3/MLKL pathway.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.