ArticleBritish journal of pharmacology2008
Inhibition of fatty acid amide hydrolase by kaempferol and related naturally occurring flavonoids.
Article in British journal of pharmacology, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed, 51 citations in OpenAlex.
- Kaempferol Regulates Lipid Homeostasis, Endocannabinoid System, and PPARα in Rat Cerebral Cortex Following BCCAO/R.Biomolecules · 2025Article
- The Endocannabinoid System in the Development and Treatment of Obesity: Searching for New Ideas.International journal of molecular sciences · 2025Review
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- Pharmacology of Non-Psychoactive Phytocannabinoids and Their Potential for Treatment of Cardiometabolic Disease.Handbook of experimental pharmacology · 2025Review
- Antimicrobial, Probiotic, and Immunomodulatory Potential ofAntibiotics (Basel, Switzerland) · 2024Article
- Endocannabinoid Hydrolase Inhibitors: Potential Novel Anxiolytic Drugs.Drug design, development and therapy · 2024Review
- Tart cherry (Prunus cerasus L.) dietary supplement modulates visceral adipose tissue CB1 mRNA levels along with other adipogenesis-related genes in rat models of diet-induced obesity.European journal of nutrition · 2021Article
- Mediterranean Diet and Neurodegenerative Diseases: The Neglected Role of Nutrition in the Modulation of the Endocannabinoid System.Biomolecules · 2021Review
- Lifestyle Interventions Improving Cannabinoid Tone During COVID-19 Lockdowns May Enhance Compliance With Preventive Regulations and Decrease Psychophysical Health Complications.Frontiers in psychiatry · 2021Article
- Network Pharmacology Analysis of the Identification of Phytochemicals and Therapeutic Mechanisms ofJournal of immunology research · 2021Article
- Anti-nociceptive effect of Arbutus andrachne L. methanolic leaf extract mediated by CB1, TRPV1 and PPARs in mouse pain models.Inflammopharmacology · 2020Article
- A Polyphenols-Rich Extract fromMolecules (Basel, Switzerland) · 2020Article
- Kaempferol Facilitated Extinction Learning in Contextual Fear Conditioned Rats via Inhibition of Fatty-Acid Amide Hydrolase.Molecules (Basel, Switzerland) · 2020Article
- Flavonoids and Related Members of the Aromatic Polyketide Group in Human Health and Disease: Do They Really Work?Molecules (Basel, Switzerland) · 2020Review
- Cannabinoid CBFrontiers in physiology · 2019Article
- Cannabimimetic phytochemicals in the diet - an evolutionary link to food selection and metabolic stress adaptation?British journal of pharmacology · 2017Review
- A Genetic Screen Reveals Novel Targets to RenderFrontiers in cellular and infection microbiology · 2017Article
- Broad targeting of angiogenesis for cancer prevention and therapy.Seminars in cancer biology · 2015Review
- Contributions of nonhematopoietic cells and mediators to immune responses: implications for immunotoxicology.Toxicological sciences : an official journal of the Society of Toxicology · 2015Review
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeRecent studies have demonstrated that the naturally occurring isoflavone compounds genistein and daidzein inhibit the hydrolysis of anandamide by fatty acid amide hydrolase (FAAH) in the low micromolar concentration range. The purpose of the present study was to determine whether this property is shared by flavonoids. EXPERIMENTAL APPROACH: The hydrolysis of anandamide in homogenates and intact cells was measured using the substrate labelled in the ethanolamine part of the molecule. KEY
resultsTwenty compounds were tested. Among the commonly occurring flavonoids, kaempferol was the most potent, inhibiting FAAH in a competitive manner with a K(i) value of 5 microM. Among flavonoids with a more restricted distribution in nature, the two most active toward FAAH were 7-hydroxyflavone (IC(50) value of 0.5-1 microM depending on the solvent used) and 3,7-dihydroxyflavone (IC(50) value 2.2 microM). All three compounds reduced the FAAH-dependent uptake of anandamide and its metabolism by intact RBL2H3 basophilic leukaemia cells. CONCLUSIONS AND IMPLICATIONS: Inhibition of FAAH is an additional in vitro biochemical property of flavonoids. Kaempferol, 7-hydroxyflavone and 3,7-dihydroxyflavone may be useful as templates for the synthesis of novel compounds, which target several systems that are involved in the control of inflammation and cancer.
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