Department of Life and Environmental Sciences - Unit of Pharmaceutical, Pharmacological and Nutraceutical Sciences, University of Cagliari, Cagliari, Italy. Electronic address:
Published: August 2020
AI Article Synopsis
Article Abstract
In experimental animals, inhibition of fatty acid amide hydrolase (FAAH) reduces the gastrointestinal damage produced by non-steroidal anti-inflammatory agents that act by inhibition of cyclooxygenase (COX). This suggests that compounds able to inhibit both enzymes may be potentially useful therapeutic agents. In the present study, we have investigated eight novel amide analogues of carprofen, ketoprofen and fenoprofen as potential FAAH/COX dual action inhibitors. Carpro-AM1 (2-(6-Chloro-9H-carbazol-2-yl)-N-(3-methylpyridin-2-yl)propenamide) and Carpro-AM6 (2-(6-Chloro-9H-carbazol-2-yl)-N-(3-chloropyridin-2-yl)propenamide) were found to be fully reversible inhibitors of the hydrolysis of 0.5 µM [H]anandamide in rat brain homogenates with IC values of 94 and 23 nM, respectively, i.e. 2-3 orders of magnitude more potent than carprofen in this respect. Both compounds inhibited the cyclooxygenation of arachidonic acid by ovine COX-1, and were more potent inhibitors of human recombinant COX-2 when 2-arachidonoylglycerol was used as substrate than when arachidonic acid was used. It is concluded that Carpro-AM1 and Carpro-AM6 are dual-acting FAAH/substrate-selective COX inhibitors.
Department of Oncology, The First Affiliated Hospital of Shandong First Medical University & Shandong Provincial Qianfoshan Hospital, Shandong Lung Cancer Institute, Jinan, China.
Background: Patients receiving chest radiation therapy, or exposed to high radiation levels due to accidental nuclear leakage are at risk of radiation-induced lung injury (RILI). In innate immunity, macrophages not only exhibit certain radiation tolerance but also play an important regulatory role in the whole pathological process. Nervonic acid (NA), a long-chain unsaturated fatty acid found in nerve tissue, plays a pivotal role in maintaining normal tissue growth and repair.
Introduction: The effects of resveratrol (RES) and β-hydroxy-β-methylbutyric acid (HMB) on phenotype, immunity, digestive enzyme activity and short-chain fatty acids (SCFAs) contents in ileum of Tibetan sheep were investigated.
Methods: A total of 120 two-month-old Tibetan sheep (15.5 ± 0.
Hainan Province Key Laboratory of One Health, Collaborative Innovation Center of One Health, School of Life and Health Sciences, Hainan University, Haikou, Hainan, China.
This study probes into the unique metabolic responses of (), a key player in the gut microbiota, when it metabolizes rhamnose rather than typical carbohydrates. Known for its predominant role in the Bacteroidetes phylum, efficiently breaks down poly- and mono-saccharides into beneficial short-chain fatty acids (SCFAs), crucial for both host health and microbial ecology balance. Our research focused on how this bacterium's SCFA production differ when utilizing various monosaccharides, with an emphasis on the oxidative stress responses triggered by rhamnose consumption.
Trifunctional protein deficiency (TFP) is a disorder of fatty acid beta-oxidation associated with metabolic, cardiac, and liver dysfunction in severe forms. We present two siblings diagnosed by newborn screening and confirmed by biochemical testing at birth. Their clinical course was complicated by recurrent rhabdomyolysis, retinopathy, and hypoparathyroidism.
