ArticlePloS one2012
The natural anticancer agent plumbagin induces potent cytotoxicity in MCF-7 human breast cancer cells by inhibiting a PI-5 kinase for ROS generation.
Article in PloS one, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
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Who cites it
28 citing papers in PubMed, 77 citations in OpenAlex.
- Plumbagin Disrupts Biofilm Integrity and Resistance Gene Expression in Carbapenem-ResistantJournal of microbiology and biotechnology · 2026Article
- Different Derivatives of Plumbagin Analogue: Bioavailability and Their Toxicity Studies.Food science & nutrition · 2025Review
- Anticancer therapeutic potential of genusFood science & nutrition · 2024Review
- Edeine BmBio · 2024Article
- Plumbagin Exhibits Genotoxicity and Induces G2/M Cell Cycle Arrest via ROS-Mediated Oxidative Stress and Activation of ATM-p53 Signaling Pathway in Hepatocellular Cells.International journal of molecular sciences · 2023Article
- Synthesis and Characterization of Plumbagin S-Allyl Cysteine Ester: Determination of Anticancer Activity In Silico and In Vitro.Applied biochemistry and biotechnology · 2022Article
- Plumbagin promotes mitochondrial mediated apoptosis in gefitinib sensitive and resistant A549 lung cancer cell line through enhancing reactive oxygen species generation.Molecular biology reports · 2020Article
- The Hsp90 Inhibitor, Monorden, Is a Promising Lead Compound for the Development of Novel Fungicides.Frontiers in plant science · 2020Article
- Molecular pathways related to the control of proliferation and cell death in 786-O cells treated with plumbagin.Molecular biology reports · 2019Article
- Bioactive Compounds: Natural Defense Against Cancer?Biomolecules · 2019Review
- Plumbagin-induced oxidative stress leads to inhibition of NaScientific reports · 2019Article
- Traditional Chinese medicine-combination therapies utilizing nanotechnology-based targeted delivery systems: a new strategy for antitumor treatment.International journal of nanomedicine · 2019Review
- 3-Chloroplumbagin Induces Cell Death in Breast Cancer Cells Through MAPK-Mediated Mcl-1 Inhibition.Frontiers in pharmacology · 2019Article
- Plumbagin induces ROS-mediated apoptosis and cell cycle arrest and inhibits EMT in human cervical carcinoma cells.RSC advances · 2018Article
- Review
- Plumbagin sensitizes breast cancer cells to tamoxifen-induced cell death through GRP78 inhibition and Bik upregulation.Scientific reports · 2017Article
- Selective mode of action of plumbagin through BRCA1 deficient breast cancer stem cells.BMC cancer · 2016Article
- Phytoconstituents with Radical Scavenging and Cytotoxic Activities fromDiseases (Basel, Switzerland) · 2016Article
- Acetylamine derivative of diospyrin, a plant-derived binaphthylquinonoid, inhibits human colon cancer growth in Nod-Scid mice.Investigational new drugs · 2015Article
- Mannich bases in medicinal chemistry and drug design.European journal of medicinal chemistry · 2015Review
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7 authors.
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No grant is acknowledged in the PubMed record.
Abstract
Drug-induced haploinsufficiency (DIH) in yeast has been considered a valuable tool for drug target identification. A plant metabolite, plumbagin, has potent anticancer activity via reactive oxygen species (ROS) generation. However, the detailed molecular targets of plumbagin for ROS generation are not understood. Here, using DIH and heterozygous deletion mutants of the fission yeast Schizosaccharomyces pombe, we identified 1, 4-phopshatidylinositol 5-kinase (PI5K) its3 as a new molecular target of plumbagin for ROS generation. Plumbagin showed potent anti-proliferative activity (GI(50); 10 µM) and induced cell elongation and septum formation in wild-type S. pombe. Furthermore, plumbagin dramatically increased the intracellular ROS level, and pretreatment with the ROS scavenger, N-acetyl cysteine (NAC), protected against growth inhibition by plumbagin, suggesting that ROS play a crucial role in the anti-proliferative activity in S. pombe. Interestingly, significant DIH was observed in an its3-deleted heterozygous mutant, in which ROS generation by plumbagin was higher than that in wild-type cells, implying that its3 contributes to ROS generation by plumbagin in this yeast. In MCF7 human breast cancer cells, plumbagin significantly decreased the level of a human ortholog, 1, 4-phopshatidylinositol 5-kinase (PI5K)-1B, of yeast its3, and knockdown of PI5K-1B using siPI5K-1B increased the ROS level and decreased cell viability. Taken together, these results clearly show that PI5K-1B plays a crucial role in ROS generation as a new molecular target of plumbagin. Moreover, drug target screening using DIH in S. pombe deletion mutants is a valuable tool for identifying molecular targets of anticancer agents.
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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.