ArticleBritish journal of pharmacology2010
5-Lipoxygenase inhibitors induce potent anti-proliferative and cytotoxic effects in human tumour cells independently of suppression of 5-lipoxygenase activity.
Article in British journal of pharmacology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 48 citations in OpenAlex.
- Radioiodination of Two Carborane-Based Dual Cyclooxygenase-2/5-Lipoxygenase Inhibitors and Their In Vitro and In Vivo Evaluation.Chembiochem : a European journal of chemical biology · 2026Article
- Exploratory Data Analysis of the In Vitro Effects of Novel Hydrazide-Hydrazone Antioxidants in the Context of In Silico Predictors.Antioxidants (Basel, Switzerland) · 2025Article
- The role of human 5-Lipoxygenase (5-LO) in carcinogenesis - a question of canonical and non-canonical functions.Oncogene · 2024Review
- Discovery of Novel Thiophene/Hydrazones: In Vitro and In Silico Studies against Pancreatic Cancer.Pharmaceutics · 2023Article
- Knock-out of 5-lipoxygenase in overexpressing tumor cells-consequences on gene expression and cellular function.Cancer gene therapy · 2023Article
- Carborane-Based Analog of Rev-5901 Attenuates Growth of Colon Carcinoma In Vivo.Molecules (Basel, Switzerland) · 2022Article
- Zileuton inhibits arachidonate-5-lipoxygenase to exert antitumor effects in preclinical cervical cancer models.Cancer chemotherapy and pharmacology · 2021Article
- Inhibitors of Human 5-Lipoxygenase Potently Interfere With Prostaglandin Transport.Frontiers in pharmacology · 2021Article
- PPAR-α Modulators as Current and Potential Cancer Treatments.Frontiers in oncology · 2021Review
- The Investigation of Lipoxygenases as Therapeutic Targets in Malignant Pleural Mesothelioma.Pathology oncology research : POR · 2020Article
- Cross-Talk between Cancer Cells and the Tumour Microenvironment: The Role of the 5-Lipoxygenase Pathway.International journal of molecular sciences · 2017Review
- Synthesis and Biological Evaluation ofIranian journal of pharmaceutical research : IJPR · 2017Article
- Haemanthus coccineus extract and its main bioactive component narciclasine display profound anti-inflammatory activities in vitro and in vivo.Journal of cellular and molecular medicine · 2015Article
- Revealing the macromolecular targets of complex natural products.Nature chemistry · 2014Article
- Methyl jasmonate: putative mechanisms of action on cancer cells cycle, metabolism, and apoptosis.International journal of cell biology · 2014Review
- Effects of flavocoxid, a dual inhibitor of COX and 5-lipoxygenase enzymes, on benign prostatic hyperplasia.British journal of pharmacology · 2012Article
- Molecular pharmacological profile of a novel thiazolinone-based direct and selective 5-lipoxygenase inhibitor.British journal of pharmacology · 2012Article
- On the inhibition of 5-lipoxygenase product formation by tryptanthrin: mechanistic studies and efficacy in vivo.British journal of pharmacology · 2012Article
- Cyclooxygenases and lipoxygenases in cancer.Cancer metastasis reviews · 2011Review
- 5-lipoxygenase: underappreciated role of a pro-inflammatory enzyme in tumorigenesis.Frontiers in pharmacology · 2010Article
Corrections and comments
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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
background and purposeCertain 5-lipoxygenase (5-LO) inhibitors exhibit anti-carcinogenic activities against 5-LO overexpressing tumour types and cultured tumour cells. It has been proposed therefore that 5-LO products significantly contribute to tumour cell proliferation. To date, the relationship between the inhibitory mechanisms of 5-LO inhibitors, which vary widely, and tumour cell viability has not been evaluated. This study addresses the anti-proliferative and cytotoxic potency of a number of 5-LO inhibitors with different inhibitory mechanisms in 5-LO-positive and 5-LO-negative tumour cells. EXPERIMENTAL APPROACH: Cell viability was measured by the WST-1 assay; cell proliferation was assessed using the bromodeoxyuridine (BrdU) incorporation assay. Cell death was analysed by annexin V staining, Western blot analysis of PARP (poly ADP-ribose polymerase) cleavage and a cytotoxicity assay. 5-LO product formation was quantified by a 5-LO activity assay. KEY
resultsThe common 5-LO inhibitors AA-861, Rev-5901 and MK-886 induced cytotoxic and anti-proliferative effects in 5-LO-positive Capan-2 pancreatic cancer cells; BWA4C and CJ-13,610 only caused anti-proliferative effects, while zileuton failed to impair cell viability. Moreover, the concentrations of the 5-LO inhibitors required to induce anti-proliferation and cytotoxicity highly exceeded those for suppression of 5-LO. Supplementation with mitogenic 5-LO products failed to protect Capan-2 cells from the effects of 5-LO inhibitors. Finally, the cytotoxic and anti-proliferative 5-LO inhibitors also potently reduced the viability of 5-LO-deficient tumour cell lines (HeLa, Panc-1 and U937). CONCLUSIONS AND IMPLICATIONS: Certain 5-LO inhibitors cause cytotoxic and anti-proliferative effects independently of suppression of 5-LO activity. Thus, the role of 5-LO overexpression in tumour cell viability remains unclear and requires further elucidation.
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