ArticleScientific reports2021
The benzylisoquinoline alkaloids, berberine and coptisine, act against camptothecin-resistant topoisomerase I mutants.
Article in Scientific reports, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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13 citing papers in PubMed.
- Discovery of natural RORγt inhibitor using machine learning, virtual screening, and in vivo validation.Journal of advanced research · 2026Article
- Coptisine regulates PI3K/AKT pathway to block bladder cancer progression: a study based on network pharmacology, in vitro and in vivo assays.Hereditas · 2025Article
- A Mechanistic Approach to Replacing Antibiotics with Natural Products in the Treatment of Bacterial Diarrhea.Biomolecules · 2025Review
- Natural phytochemical-based strategies for antibiofilm applications.Chinese medicine · 2025Review
- DNA repair and the contribution to chemotherapy resistance.Genome medicine · 2025Review
- Pharmacological properties and therapeutic potential of berberine: a comprehensive review.Frontiers in pharmacology · 2025Review
- Synthesis and Evaluation of (Bis)benzyltetrahydroisoquinoline Alkaloids as Antiparasitic Agents.JACS Au · 2024Article
- Exploring active ingredients and mechanisms of Coptidis Rhizoma-ginger against colon cancer using network pharmacology and molecular docking.Technology and health care : official journal of the European Society for Engineering and Medicine · 2024Article
- Herbal Therapies for Cancer Treatment: A Review of Phytotherapeutic Efficacy.Biologics : targets & therapy · 2024Review
- Natural Products and Their Derivatives as Inhibitors of the DNA Repair Enzyme Tyrosyl-DNA Phosphodiesterase 1.International journal of molecular sciences · 2023Review
- Mechanism of action of non-camptothecin inhibitor Genz-644282 in topoisomerase I inhibition.Communications biology · 2022Article
- Isoquinoline Alkaloids fromInternational journal of molecular sciences · 2022Article
- Screening Papaveraceae as Novel Antibiofilm Natural-Based Agents.Molecules (Basel, Switzerland) · 2021Article
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13 authors.
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Abstract
DNA replication inhibitors are utilized extensively in studies of molecular biology and as chemotherapy agents in clinical settings. The inhibition of DNA replication often triggers double-stranded DNA breaks (DSBs) at stalled DNA replication sites, resulting in cytotoxicity. In East Asia, some traditional medicines are administered as anticancer drugs, although the mechanisms underlying their pharmacological effects are not entirely understood. In this study, we screened Japanese herbal medicines and identified two benzylisoquinoline alkaloids (BIAs), berberine and coptisine. These alkaloids mildly induced DSBs, and this effect was dependent on the function of topoisomerase I (Topo I) and MUS81-EME1 structure-specific endonuclease. Biochemical analysis revealed that the action of BIAs involves inhibiting the catalytic activity of Topo I rather than inducing the accumulation of the Topo I-DNA complex, which is different from the action of camptothecin (CPT). Furthermore, the results showed that BIAs can act as inhibitors of Topo I, even against CPT-resistant mutants, and that the action of these BIAs was independent of CPT. These results suggest that using a combination of BIAs and CPT might increase their efficiency in eliminating cancer cells.
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