ArticleACS omega2023
Copper-Plumbagin Complex Produces Potent Anticancer Effects by Depolymerizing Microtubules and Inducing Reactive Oxygen Species and DNA Damage.
Article in ACS omega, 2023. 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, 30 citations in OpenAlex.
- Synthesis and Characterization of Juglone-Derived cu (II), Mn (II) and Zn (II) Complexes and Investigation of Their Cytotoxic Activities Against Lung and Colon Cancer Cells in Vitro and in Silico.Journal of applied toxicology : JAT · 2026Article
- Spectroscopic evaluation of the interaction of myoglobin with biomedically relevant compounds.Journal of biological inorganic chemistry : JBIC : a publication of the Society of Biological Inorganic Chemistry · 2026Article
- Metal thiosemicarbazonates as dual mR2 RNR and colchicine-site tubulin inhibitors: from biochemical inhibition to mitotic arrest in MCF-7 breast cancer cells.Inorganic chemistry frontiers · 2026Article
- Article
- Ligand-Engineered Cu(II) Complexes Suppress Stemness and Drug Resistance in Triple-Negative Breast Cancer.ACS medicinal chemistry letters · 2026Article
- Article
- Synergistic Inhibition of Colon Cancer Cell Proliferation via p53, Bax, and Bcl-2 Modulation by Curcumin and Plumbagin Combination.ACS omega · 2025Article
- The Occurrence, Uses, Biosynthetic Pathway, and Biotechnological Production of Plumbagin, a Potent Antitumor Naphthoquinone.Molecules (Basel, Switzerland) · 2025Review
- The phytochemical plumbagin: mechanism behind its "pleiotropic" nature and potential as an anticancer treatment.Archives of toxicology · 2024Review
- Pharmacological Features and Therapeutic Implications of Plumbagin in Cancer and Metabolic Disorders: A Narrative Review.Nutrients · 2024Review
- Are the metal identity and stoichiometry of metal complexes important for colchicine site binding and inhibition of tubulin polymerization?Dalton transactions (Cambridge, England : 2003) · 2024Article
- Oxidative Stress in Breast Cancer: A Biochemical Map of Reactive Oxygen Species Production.Current issues in molecular biology · 2024Review
- Targeting the initiator to activate both ferroptosis and cuproptosis for breast cancer treatment: progress and possibility for clinical application.Frontiers in pharmacology · 2024Review
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Here, we have synthesized a copper complex of plumbagin (Cu-PLN) and investigated its antiproliferative activities in different cancer cells. The crystal structure of Cu-PLN showed that the complex was square planar with a binding stoichiometry of 1:2 (Cu/Plumbagin). Cu-PLN inhibited the proliferation of human cervical carcinoma (HeLa), human breast cancer (MCF-7), and murine melanoma (B16F10) cells with half-maximal inhibitory concentrations (IC50) of 0.85 ± 0.05, 2.3 ± 0.1, and 1.1 ± 0.1 μM, respectively. Plumbagin inhibited the proliferation of HeLa, MCF-7, and B16F10 cells with IC50 of 7 ± 0.1, 8.2 ± 0.2, and 6.2 ± 0.4 μM, respectively, showing that Cu-PLN is a stronger antiproliferative agent than plumbagin. Interestingly, Cu-PLN showed much stronger toxicity against breast carcinoma and skin melanoma cells than noncancerous breast epithelial and skin fibroblast cells, indicating its specific cytotoxicity toward cancer cells. A short exposure of Cu-PLN triggered microtubule disassembly in cultured cancer cells, and the complex also inhibited the polymerization of purified tubulin much more strongly than plumbagin. Furthermore, Cu-PLN inhibited the binding of colchicine to tubulin. In addition to microtubule depolymerization, the antiproliferative mechanism of Cu-PLN involved induction of reactive oxygen species, reduction of the mitochondrial membrane potential, and DNA damage. Moreover, the cytotoxic effects of Cu-PLN reduced significantly in cells pre-treated with
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