ArticleChemical biology & drug design2009
Identification and characterization of kava-derived compounds mediating TNF-alpha suppression.
Article in Chemical biology & drug design, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
17 citing papers in PubMed, 33 citations in OpenAlex.
- Kavain Alleviates Choroidal Neovascularization Via Decreasing the Activity of the HIF-1α/VEGF-A/VEGFR2 Signaling Pathway and Inhibiting Inflammation.Advanced pharmaceutical bulletin · 2024Article
- Opportunities and Challenges of Kava in Lung Cancer Prevention.International journal of molecular sciences · 2023Review
- Kavain ablates the radio-resistance of IDH-wildtype glioblastoma by targeting LITAF/NF-κB pathway.Cellular oncology (Dordrecht, Netherlands) · 2023Article
- Clinical pharmacokinetics of kavalactones after oral dosing of standardized kava extract in healthy volunteers.Journal of ethnopharmacology · 2022Article
- Dietary supplementation of gingerols- and shogaols-enriched ginger root extract attenuate pain-associated behaviors while modulating gut microbiota and metabolites in rats with spinal nerve ligation.The Journal of nutritional biochemistry · 2022Article
- Biological Activity, Hepatotoxicity, and Structure-Activity Relationship of Kavalactones and Flavokavins, the Two Main Bioactive Components in Kava (Evidence-based complementary and alternative medicine : eCAM · 2021Review
- Kava as a Clinical Nutrient: Promises and Challenges.Nutrients · 2020Review
- Synthetic Kavalactone Analogues with Increased Potency and Selective Anthelmintic Activity against Larvae ofMolecules (Basel, Switzerland) · 2020Article
- Phytochemicals against TNFα-Mediated Neuroinflammatory Diseases.International journal of molecular sciences · 2020Review
- Identification of a Kavain Analog with Efficient Anti-inflammatory Effects.Scientific reports · 2019Article
- Kavain ReducesJournal of immunology (Baltimore, Md. : 1950) · 2018Article
- Reduction of Articular and Systemic Inflammation by Kava-241 in a Porphyromonas gingivalis-Induced Arthritis Murine Model.Infection and immunity · 2018Article
- Kava-241 reduced periodontal destruction in a collagen antibody primed Porphyromonas gingivalis model of periodontitis.Journal of clinical periodontology · 2017Article
- Oral administration of methysticin improves cognitive deficits in a mouse model of Alzheimer's disease.Redox biology · 2017Article
- Kavain Inhibition of LPS-Induced TNF-α via ERK/LITAF.Toxicology research · 2016Article
- Whole-body deletion of LPS-induced TNF-α factor (LITAF) markedly improves experimental endotoxic shock and inflammatory arthritis.Proceedings of the National Academy of Sciences of the United States of America · 2011Article
- LITAF mediation of increased TNF-α secretion from inflamed colonic lamina propria macrophages.PloS one · 2011Article
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
Abstract
There is a substantial unmet need for new classes of drugs that block TNF-alpha-mediated inflammation, and particularly for small molecule agents that can be taken orally. We have screened a library of natural products against an assay measuring TNF-alpha secretion in lipopolysaccharide-stimulated THP-1 cells, seeking compounds capable of interfering with the TNF-alpha-inducing transcription factor lipopolysaccharide-induced TNF-alpha factor. Among the active compounds were several produced by the kava plant (Piper mysticum), extracts of which have previously been linked to a range of therapeutic effects. When tested in vivo, a representative of these compounds, kavain, was found to render mice immune to lethal doses of lipopolysaccharide. Kavain displays promising pharmaceutical properties, including good solubility and high cell permeability, but pharmacokinetic experiments in mice showed relatively rapid clearance. A small set of kavain analogs was synthesized, resulting in compounds of similar or greater potency in vitro compared with kavain. Interestingly, a ring-opened analog of kavain inhibited TNF-alpha secretion in the cell-based assay and suppressed lipopolysaccharide-induced TNF-alpha factor expression in the same cells, whereas the other compounds inhibited TNF-alpha secretion without affecting lipopolysaccharide-induced TNF-alpha factor levels, indicating a potential divergence in mechanism of action.
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Registered trials
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.