ArticleBritish journal of pharmacology2012
On the inhibition of 5-lipoxygenase product formation by tryptanthrin: mechanistic studies and efficacy in vivo.
Article in British journal of pharmacology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 49 citations in OpenAlex.
- Pharmacokinetics and Acute Safety Evaluation of Tryptanthrin, A Bioactive Constituent of Indigo naturalis, Following Intravenous Administration in Mice.Journal of applied toxicology : JAT · 2026Article
- Chemistry and Biological Activity of 11Molecules (Basel, Switzerland) · 2026Review
- Alkaloids as Emerging Neuroprotective Agents for Neurodegenerative Disorders: Insights into Tryptanthrin and Its Derivatives.International journal of molecular sciences · 2026Review
- Tryptanthrin Down-Regulates Oncostatin M by Targeting GM-CSF-Mediated PI3K-AKT-NF-κB Axis.Nutrients · 2024Article
- Article
- Recent advances of tryptanthrin and its derivatives as potential anticancer agents.RSC medicinal chemistry · 2024Review
- Axl, Immune Checkpoint Molecules and HIF Inhibitors from the Culture Broth ofMolecules (Basel, Switzerland) · 2022Article
- Article
- Design, synthesis and biomedical evaluation of mostotrin, a new water soluble tryptanthrin derivative.International journal of molecular medicine · 2020Article
- Review
- Therapeutic Effects of Tryptanthrin and Tryptanthrin-6-Oxime in Models of Rheumatoid Arthritis.Frontiers in pharmacology · 2020Article
- A Biomimetic, One-Step Transformation of Simple Indolic Compounds toChemical research in toxicology · 2019Article
- Biologically active quinoline and quinazoline alkaloids part II.Medicinal research reviews · 2018Review
- Low-dose action of tryptanthrin and its derivatives against developing embryos of the sea urchin Strongylocentrotus intermedius.Environmental monitoring and assessment · 2018Article
- Study on pharmacokinetics and tissue distribution of single dose oral tryptanthrin in Kunming mice by validated reversed-phase high-performance liquid chromatography with ultraviolet detection.Integrative medicine research · 2017Article
- Sex differences in prostaglandin biosynthesis in neutrophils during acute inflammation.Scientific reports · 2017Article
- The novel benzimidazole derivative BRP-7 inhibits leukotriene biosynthesis in vitro and in vivo by targeting 5-lipoxygenase-activating protein (FLAP).British journal of pharmacology · 2014Article
- Elucidation of the molecular mechanism and the efficacy in vivo of a novel 1,4-benzoquinone that inhibits 5-lipoxygenase.British journal of pharmacology · 2014Article
- The staphylococcal enterotoxin (SE) family: SEB and siblings.Virulence · 2013Review
Corrections and comments
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Authors and funding
7 authors at 4 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeLeukotrienes (LTs) are pro-inflammatory mediators produced by 5-lipoxygenase (5-LO). Currently available 5-LO inhibitors either lack efficacy or are toxic and novel approaches are required to establish a successful anti-LT therapy. Here we provide a detailed evaluation of the effectiveness of the plant-derived alkaloid tryptanthrin as an inhibitor of LT biosynthesis. EXPERIMENTAL APPROACH: We analysed LT formation and performed mechanistic studies in human neutrophils stimulated with pathophysiologically relevant stimuli (LPS and formyl peptide), as well as in cell-free assays (neutrophil homogenates or recombinant human 5-LO) and in human whole blood. The in vivo effectiveness of tryptanthrin was evaluated in the rat model of carrageenan-induced pleurisy. KEY
resultsTryptanthrin potently reduced LT-formation in human neutrophils (IC(50) = 0.6µM). However, tryptanthrin is not a redox-active compound and did not directly interfere with 5-LO activity in cell-free assays. Similarly, tryptanthrin did not inhibit the release of arachidonic acid, the activation of MAPKs, or the increase in [Ca(2+) ](i) , but it modified the subcellular localization of 5-LO. Moreover, tryptanthrin potently suppressed LT formation in human whole blood (IC(50) = 10µM) and reduced LTB(4) levels in the rat pleurisy model after a single oral dose of 10mg·kg(-1) . CONCLUSIONS AND IMPLICATIONS: Our data reveal that tryptanthrin is a potent natural inhibitor of cellular LT biosynthesis with proven efficacy in whole blood and is effective in vivo after oral administration. Its unique pharmacological profile supports further analysis to exploit its pharmacological potential.
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