ArticleJournal of experimental & clinical cancer research : CR2016
Inhibitory effects of lapachol on rat C6 glioma in vitro and in vivo by targeting DNA topoisomerase I and topoisomerase II.
Article in Journal of experimental & clinical cancer research : CR, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 31 citations in OpenAlex.
- Silk Fibroin-Stabilized Lapachol Microemulsion Enhances Antiglioma Activity In Vitro.Chemistry & biodiversity · 2026Article
- Radiotherapy-associated changes in the miR-124/SP1 axis in a rat glioma model.Iranian journal of basic medical sciences · 2026Article
- Lapachol interferes with the cell cycle and inhibits proliferation and migration of bladder tumor cells with effects on ncRNA expression.Scientific reports · 2025Article
- The first endovascular rat glioma model for pre-clinical evaluation of intra-arterial therapeutics.Interventional neuroradiology : journal of peritherapeutic neuroradiology, surgical procedures and related neurosciences · 2025Article
- Chitosan Nanoparticles Enhance the Antiproliferative Effect of Lapachol in Urothelial Carcinoma Cell Lines.Pharmaceutics · 2025Article
- Indium(III) complexes with lapachol: cytotoxic effects against human breast tumor cells and interactions with DNA.Journal of biological inorganic chemistry : JBIC : a publication of the Society of Biological Inorganic Chemistry · 2024Article
- Preclinical evaluation of L-fucoside from lapachol-loaded nanoemulsion as a strategy to breast cancer treatment.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie · 2024Article
- Suppression of PI3K/Akt/mTOR pathway in chrysoeriol-induced apoptosis of rat C6 glioma cells.In vitro cellular & developmental biology. Animal · 2022Article
- β-Lapachone Induces Acute Oxidative Stress in Rat Primary Astrocyte Cultures that is Terminated by the NQO1-Inhibitor Dicoumarol.Neurochemical research · 2020Article
- Development of long-circulating lapachol nanoparticles: formation, characterization, pharmacokinetics, distribution and cytotoxicity.RSC advances · 2020Article
- Antileishmanial activity of terpenylquinones on Leishmania infantum and their effects on Leishmania topoisomerase IB.International journal for parasitology. Drugs and drug resistance · 2019Article
- Synthesis and Evaluations of Novel Apocynin Derivatives as Anti-Glioma Agents.Frontiers in pharmacology · 2019Article
- The anti-vascular endothelial growth factor receptor-1 monoclonal antibody D16F7 inhibits invasiveness of human glioblastoma and glioblastoma stem cells.Journal of experimental & clinical cancer research : CR · 2017Article
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundLapachol is a natural naphthoquinone compound that possesses extensive biological activities. The aim of this study is to investigate the inhibitory effects of lapachol on rat C6 glioma both in vitro and in vivo, as well as the potential mechanisms.
methodsThe antitumor effect of lapachol was firstly evaluated in the C6 glioma model in Wistar rats. The effects of lapachol on C6 cell proliferation, apoptosis and DNA damage were detected by 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium (MTS)/ phenazinemethosulfate (PMS) assay, hoechst 33358 staining, annexin V-FITC/PI staining, and comet assay. Effects of lapachol on topoisomerase I (TOP I) and topoisomerase II (TOP II) activities were detected by TOP I and TOP II mediated supercoiled pBR322 DNA relaxation assays and molecular docking. TOP I and TOP II expression levels in C6 cells were also determined.
resultsHigh dose lapachol showed significant inhibitory effect on the C6 glioma in Wistar rats (P < 0.05). It was showed that lapachol could inhibit proliferation, induce apoptosis and DNA damage of C6 cells in dose dependent manners. Lapachol could inhibit the activities of both TOP I and II. Lapachol-TOP I showed relatively stronger interaction than that of lapachol-TOP II in molecular docking study. Also, lapachol could inhibit TOP II expression levels, but not TOP I expression levels.
conclusionThese results showed that lapachol could significantly inhibit C6 glioma both in vivo and in vitro, which might be related with inhibiting TOP I and TOP II activities, as well as TOP II expression.
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