Mode of action of thiocoraline, a natural marine compound with anti-tumour activity
Open accessAbstract
Thiocoraline, a new anticancer agent derived from the marine actinomycete Micromonospora marina, was found to induce profound perturbations of the cell cycle. On both LoVo and SW620 human colon cancer cell lines, thiocoraline caused an arrest in G1 phase of the cell cycle and a decrease in the rate of S phase progression towards G2/M phases, as assessed by using bromodeoxyuridine/DNA biparametric flow cytometric analysis. Thiocoraline does not inhibit DNA-topoisomerase II enzymes in vitro, nor does it induce DNA breakage in cells exposed to effective drug concentrations. The cell cycle effects observed after exposure to thiocoraline appear related to the inhibition of DNA replication. By using a primer extension assay it was found that thiocoraline inhibited DNA elongation by DNA polymerase alpha at concentrations that inhibited cell cycle progression and clonogenicity. These studies indicate that the new anticancer drug thiocoraline probably acts by inhibiting DNA polymerase alpha activity.
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Marine Natural Products: A Source of Novel Anticancer Drugs
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“Thiocoraline cytotoxic action was found mediated via an arrest in G1 phase of the cell cycle and a decrease in the rate of S phase progression towards G2/M phases, as assessed using bromodeoxyuridine/DNA biparametric flow cytometric analysis [117].”
MethodAntitumor compounds from marine actinomycetes
Olano, C., Méndez, C., & Salas, J. A. (2009) · Marine Drugs · doi:10.3390/md7020210 · Cited by 330 · see citing works
- Authors
- Erba, E., Bergamaschi, D., Ronzoni, S., Faretta, M., Taverna, S., Bonfanti, M., Catapano, C. V., Faircloth, G., Jimeno, J., & D’Incalci, M.
- Affiliations
- Mario Negri Institute for Pharmacological Research (IT)
- Medical University of South Carolina (US)
- PharmaMar (Spain) (ES)
- Venue
- British Journal of Cancer
- Published
- 1999-05-07
- Volume
- 80
- Issue
- 7
- Pages
- 971-980
- ISSN
- 0007-0920 (ISSN-L)
- 1532-1827
- PMC
- PMC2363046
- OpenAlex
- W2052430670
- Cited by
- 103
- References
- 13
- Citations by year
- 2026: 5 · 2025: 4 · 2024: 6 · 2022: 8 · 2021: 7 · 2020: 6 · 2019: 5 · 2017: 3 · 2016: 7 · 2015: 8 · 2014: 5 · 2013: 6 · 2012: 5
- FWCI
- 0.34
- Type
- journal article
- Language
- en
- Open access
- hybrid
- doi.org
- Licence
- cc-by-nc-sa
- www.springer.com/tdm (unspecified)
- Locations
- British Journal of Cancer (publishedVersion, cc-by-nc-sa)
- Europe PMC (PubMed Central) (publishedVersion, cc-by)
- PubMed Central (publishedVersion, cc-by)
- PubMed (publishedVersion)
- Queen Mary Research Online (Queen Mary University of London) (submittedVersion, cc-by-nc-sa)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Cancer therapeutics and mechanisms
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Toxicology › Bioactive Compounds and Antitumor Agents
- Health Sciences › Medicine › Oncology › Cancer-related Molecular Pathways
- Keywords
- marine actinomycetes, anticancer agents, cell cycle arrest, G1 cell cycle arrest, DNA replication inhibition, DNA polymerase alpha, colon cancer, mechanism of action, topoisomerase II
- MeSH terms
- Anti-Bacterial Agents, Antibiotics, Antineoplastic, Bromodeoxyuridine, Cell Cycle, Cell Division, DNA, DNA-Directed DNA Polymerase, Flow Cytometry, Humans, Peptides, Time Factors, Tumor Cells, Cultured, Tumor Stem Cell Assay, Inhibitory Concentration 50, Depsipeptides
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