ArticleBritish journal of pharmacology2007
Inhibition of the cellular uptake of anandamide by genistein and its analogue daidzein in cells with different levels of fatty acid amide hydrolase-driven uptake.
Article in British journal of pharmacology, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Who cites it
23 citing papers in PubMed, 46 citations in OpenAlex.
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- Phytocannabinoids as Potential Multitargeting Neuroprotectants in Alzheimer's Disease.Current drug research reviews · 2024Review
- Endocannabinoid Hydrolase Inhibitors: Potential Novel Anxiolytic Drugs.Drug design, development and therapy · 2024Review
- Light controlled self-escape capability of non-cationic carbon nitride-based nanosheets in lysosomes for hepatocellular carcinoma targeting stimulus-responsive gene delivery.Bioengineering & translational medicine · 2023Article
- Fatty acid amide hydrolase inhibition and N-arachidonoylethanolamine modulation by isoflavonoids: A novel target for upcoming antidepressants.Pharmacology research & perspectives · 2022Article
- Mediterranean Diet and Neurodegenerative Diseases: The Neglected Role of Nutrition in the Modulation of the Endocannabinoid System.Biomolecules · 2021Review
- Kaempferol Facilitated Extinction Learning in Contextual Fear Conditioned Rats via Inhibition of Fatty-Acid Amide Hydrolase.Molecules (Basel, Switzerland) · 2020Article
- Effect of Hataedock Treatment on Epidermal Structure Maintenance through Intervention in the Endocannabinoid System.Evidence-based complementary and alternative medicine : eCAM · 2020Article
- Role of pannexin-1 in the cellular uptake, release and hydrolysis of anandamide by T84 colon cancer cells.Scientific reports · 2019Article
- 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
- Effects of tumour necrosis factor α upon the metabolism of the endocannabinoid anandamide in prostate cancer cells.PloS one · 2017Article
- Contributions of nonhematopoietic cells and mediators to immune responses: implications for immunotoxicology.Toxicological sciences : an official journal of the Society of Toxicology · 2015Review
- Potential upstream regulators of cannabinoid receptor 1 signaling in prostate cancer: a Bayesian network analysis of data from a tissue microarray.The Prostate · 2014Article
- Ketoconazole inhibits the cellular uptake of anandamide via inhibition of FAAH at pharmacologically relevant concentrations.PloS one · 2014Article
- Article
- Evidence for bidirectional endocannabinoid transport across cell membranes.The Journal of biological chemistry · 2012Article
- Phytoestrogens enhance the vascular actions of the endocannabinoid anandamide in mesenteric beds of female rats.International journal of hypertension · 2012Article
- Biochanin A, a naturally occurring inhibitor of fatty acid amide hydrolase.British journal of pharmacology · 2010Article
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
background and purposeGenistein, a tyrosine kinase inhibitor used to block caveolae dependent endocytosis, reduces the cellular uptake of anandamide in RBL2H3 basophilic leukaemia cells. However, genistein is also a competitive inhibitor of fatty acid amide hydrolase, the enzyme responsible for anandamide hydrolysis. Here we have investigated whether inhibition of fatty acid amide hydrolase rather than inhibition of endocytosis is the primary determinant of genistein actions upon anandamide uptake. EXPERIMENTAL APPROACH: Cellular uptake of anandamide, labelled in the arachidonoyl part of the molecule was assessed in four different cell lines using a standard method. Fatty acid amide hydrolase activity in homogenates and intact cells was measured using anandamide labelled in the ethanolamine part of the molecule. KEY
resultsThe fatty acid amide hydrolase inhibitor URB597 inhibited anandamide uptake into RBL2H3 cells and R3327 AT-1 prostate cancer cells, but not into 3T3-L1 preadipocytes or PC-3 prostate cancer cells. An identical pattern was seen with genistein. The related compound daidzein inhibited anandamide hydrolysis in homogenates and intact cells, and reduced its uptake into RBL2H3 and R3327 AT-1, but not PC-3 cells. Anandamide hydrolysis by cell homogenates was in the order RBL2H3 > R3327 AT-1 > PC-3 approximately 3T3-L1. CONCLUSIONS AND IMPLICATIONS: The ability of genistein to inhibit anandamide uptake is mimicked by daidzein (which does not affect tyrosine kinase), and is only seen in cells that show sensitivity to URB597. This indicates that blockade of fatty acid amide hydrolase is the primary determinant of the effects of genistein on cellular anandamide uptake.
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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.