ArticleBritish journal of pharmacology2012
The antinociceptive triterpene β-amyrin inhibits 2-arachidonoylglycerol (2-AG) hydrolysis without directly targeting cannabinoid receptors.
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 31 papers, 1 of them a synthesis that pooled it.
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Who cites it
31 citing papers in PubMed, 1 synthesis or guideline pooled it, 78 citations in OpenAlex.
- Endocannabinoid System as a Promising Therapeutic Target in Inflammatory Bowel Disease - A Systematic Review.Frontiers in immunology · 2021Pooled it
- Recent Progress in the Development of Selective MAGL Modulators (2020-2026).Molecules (Basel, Switzerland) · 2026Review
- The Diminished Availability of 2-AG in Aged Synaptic Terminals is Ameliorated by a Full-Spectrum Cannabis Extract with a High THC Content.Neurochemical research · 2026Article
- Development of Glycoconjugated MAGL Inhibitors with Glucose-Dependent Antiproliferative Activity.International journal of molecular sciences · 2026Article
- Synthesis, characterization, antioxidant and anticancer potential of Kalanchoe pinnata green synthesized silver nanoparticles targeting p53/MDM2 nexus in hepatic cancer: integrated in vitro and in silico study.Scientific reports · 2026Article
- Topical β-Caryophyllene for Dermatologic Disorders: Mechanisms, Human Evidence, and Clinical Translation.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Methods for Assessing MAGL Enzymatic Activity: An Extensive Review of Past and Emerging Approaches.International journal of molecular sciences · 2025Review
- Correlation Between In Silico Docking/Simulation Results and In Vitro MAGL Inhibition Potency of Selected Triterpenes.Current issues in molecular biology · 2025Article
- Guayusa (Molecules (Basel, Switzerland) · 2025Review
- Identification of a Possible Endocannabinoid-Mediated Mechanism of Action of Cetylated Fatty Acids.Biomolecules · 2025Article
- Endocannabinoid Hydrolase Inhibitors: Potential Novel Anxiolytic Drugs.Drug design, development and therapy · 2024Review
- Cetirizine and Levetiracetam as Inhibitors of Monoacylglycerol Lipase: Investigating Their Repurposing Potential as Novel Osteoarthritic Pain Therapies.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Pristimerin, a triterpene that inhibits monoacylglycerol lipase activity, prevents the development of paclitaxel-induced allodynia in mice.Frontiers in pharmacology · 2022Article
- On the Biomedical Properties of Endocannabinoid Degradation and Reuptake Inhibitors: Pre-clinical and Clinical Evidence.Neurotoxicity research · 2021Review
- Triterpenoids fromPlants (Basel, Switzerland) · 2021Article
- β-Amyrin Ameliorates Alzheimer's Disease-Like Aberrant Synaptic Plasticity in the Mouse Hippocampus.Biomolecules & therapeutics · 2020Article
- Establishment and Phytochemical Analysis of a Callus Culture fromMolecules (Basel, Switzerland) · 2018Article
- Arctium minus crude extract presents antinociceptive effect in a mice acute gout attack model.Inflammopharmacology · 2018Article
- Tingenone, a pentacyclic triterpene, induces peripheral antinociception due to cannabinoid receptors activation in mice.Inflammopharmacology · 2018Article
- Cannabimimetic phytochemicals in the diet - an evolutionary link to food selection and metabolic stress adaptation?British journal of pharmacology · 2017Review
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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 purposePharmacological activation of cannabinoid CB(1) and CB(2) receptors is a therapeutic strategy to treat chronic and inflammatory pain. It was recently reported that a mixture of natural triterpenes α- and β-amyrin bound selectively to CB(1) receptors with a subnanomolar K(i) value (133 pM). Orally administered α/β-amyrin inhibited inflammatory and persistent neuropathic pain in mice through both CB(1) and CB(2) receptors. Here, we investigated effects of amyrins on the major components of the endocannabinoid system. EXPERIMENTAL APPROACH: We measured CB receptor binding interactions of α- and β-amyrin in validated binding assays using hCB(1) and hCB(2) transfected CHO-K1 cells. Effects on endocannabinoid transport in U937 cells and breakdown using homogenates of BV2 cells and pig brain, as well as purified enzymes, were also studied. KEY
resultsThere was no binding of either α- or β-amyrin to hCB receptors in our assays (K(i) > 10 µM). The triterpene β-amyrin potently inhibited 2-arachidonoyl glycerol (2-AG) hydrolysis in pig brain homogenates, but not that of anandamide. Although β-amyrin only weakly inhibited purified human monoacylglycerol lipase (MAGL), it also inhibited α,β-hydrolases and more potently inhibited 2-AG breakdown than α-amyrin and the MAGL inhibitor pristimerin in BV2 cell and pig brain homogenates. CONCLUSIONS AND IMPLICATIONS: We propose that β-amyrin exerts its analgesic and anti-inflammatory pharmacological effects via indirect cannabimimetic mechanisms by inhibiting the degradation of the endocannabinoid 2-AG without interacting directly with CB receptors. Triterpenoids appear to offer a very broad and largely unexplored scaffold for inhibitors of the enzymic degradation of 2-AG. LINKED ARTICLES: This article is part of a themed section on Cannabinoids. To view the other articles in this section visit http://dx.doi.org/10.1111/bph.2012.167.issue-8.
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