Cannabinoids delta 1-tetrahydrocannabinol, cannabinol, cannabidiol and cannabigerol have been shown to affect directly the activity of phospholipase A2 in a cell-free assay. The compounds produced a biphasic activation of the enzyme, with EC50 values in the range 6.0-20.0 X 10(-6) M and IC50 values in the range 50.0-150.0 X 10(-6) M. These results correlated well with the relative potencies reported for the stimulation of prostaglandin release from human synovial cells in vitro, confirming that activation of phospholipase A2 is the predominant action of cannabinoids on arachidonate metabolism in tissue culture. However, since delta 1-tetrahydrocannabinol is unique among these compounds in possessing cataleptic activity, it is unlikely that phospholipase A2 is the major receptor mediating the psychotropic effects of cannabis.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/0014-5793(87)81420-5 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Exogenous dopamine application ameliorates chilling injury and preserves quality of kiwifruit during cold storage.
Sci Rep
January 2025
Department of Horticulture, Faculty of Agriculture, University of Zanjan, Zanjan, Iran.
This study investigated the mechanisms employed by exogenous dopamine application in alleviating chilling injury in kiwifruits during storage at 1 °C for 120 days. Our results indicated that dopamine treatment at 150 µM alleviated chilling injury in kiwifruits during storage at 1 °C for 120 days. By 150 µM dopamine application, higher SUMO E3 ligase (SIZ1) and target of rapamycin (TOR) genes expression accompanied by lower poly(ADP-Ribose) polymerase 1 (PARP1) and sucrose non-fermenting 1-related kinase 1 (SnRK1) genes expression was associated with higher salicylic acid, ATP, NADPH and proline accumulation in kiwifruits during storage at 1 °C for 120 days.
View Article and Find Full Text PDFClsC protein encoded by a stress-responsive operon in Escherichia coli functions as a trans-acting activator of RNase III.
Int J Biol Macromol
January 2025
Department of Chemistry and Chemistry, Institute for Functional Materials, Pusan National University, Busan 46241, Republic of Korea.
RNase III, an endoribonuclease that cleaves double-stranded RNAs (dsRNAs), significantly impacts Escherichia coli (E. coli) adaptation by regulating global RNA gene expression. YmdB from E.
View Article and Find Full Text PDFSimplifying Traditional Approaches for Accessible Analysis of Snake Venom Enzymes.
Toxicon
January 2025
Department of BioMolecular Sciences, School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, 14040-903, Ribeirão Preto, SP, Brazil. Electronic address:
Snake venoms enzymes affect diverse physiological mechanisms leading to effects such as inflammation, edema, hemolysis, and blood clotting disorders. In this report, we describe modifications to classical assays for assessing the enzymatic activity of snake venom phospholipase A (PLA) and phosphodiesterase (PDE), including the adaptation of the PDE assay to an agar plate. A final staining step, using Stains-all®, was added to the PLA activity assay on an egg yolk-containing agar plate.
View Article and Find Full Text PDFMetabolic pathways of eicosanoids-derivatives of arachidonic acid and their significance in skin.
Cell Mol Biol Lett
January 2025
Department of Analytical Chemistry, Medical University of Bialystok, Kilinskiego 1, 15-069, Bialystok, Poland.
The skin is a barrier that protects the human body against environmental factors (physical, including solar radiation, chemicals, and pathogens). The integrity and, consequently, the effective metabolic activity of skin cells is ensured by the cell membrane, the important structural and metabolic elements of which are phospholipids. Phospholipids are subject to continuous transformation, including enzymatic hydrolysis (with the participation of phospholipases A, C, and D) to free polyunsaturated fatty acids (PUFAs), which under the influence of cyclooxygenases (COX1/2), lipoxygenases (LOXs), and cytochrome P450 (CYPs P450) are metabolized to various classes of oxylipins, depending on the type of PUFA being metabolized and the enzyme acting.
View Article and Find Full Text PDFStructure-activity relationship expansion and microsomal stability assessment of the 2-morpholinobenzoic acid scaffold as antiproliferative phosphatidylcholine-specific phospholipase C inhibitors.
RSC Med Chem
January 2025
School of Chemical Sciences, University of Auckland Auckland 1010 New Zealand
Dysregulation of choline phospholipid metabolism and overexpression of phosphatidylcholine-specific phospholipase C (PC-PLC) is implicated in various cancers. Current known enzyme inhibitors include compounds based on a 2-morpholino-5--benzylamino benzoic acid, or hydroxamic acid, scaffold. In this work, 81 compounds were made by modifying this core structure to explore the pharmacophore.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!