keyword
https://read.qxmd.com/read/38239143/advances-in-the-study-of-endocannabinoid-receptors-in-experimental-acupuncture-analgesia
#21
JOURNAL ARTICLE
Wen-Hao Liu, Jun-Shang Wu, Li-Bo Hua, Zhi-Feng Pan, Hai-Bo Zhang, Neng-Gui Xu, Yi-Han He
The endocannabinoid system, an important biological network for maintaining and balancing various functions of the human body, is involved in many physiological functions such as pain, emotion, learning and memory, etc. Among which the endocannabinoid receptors [including type I (CB1) and type II (CB2) receptors] play an important role in the regulation of pain and have become an important target in the mechanism research of acupuncture analgesia. CB1 is mainly distributed in the central nervous system, including the spinal cord, cerebral cortex, amygdala, insular cortex, and basal ganglia, etc...
January 25, 2024: Zhen Ci Yan Jiu, Acupuncture Research
https://read.qxmd.com/read/38232863/discovery-and-preclinical-evaluation-of-a-novel-inhibitor-of-fabp5-art26-12-effective-in-oxaliplatin-induced-peripheral-neuropathy
#22
JOURNAL ARTICLE
George Warren, Myles Osborn, Christopher Tsantoulas, Ana David-Pereira, Daniel Cohn, Paul Duffy, Linette Ruston, Clare Johnson, Heather Bradshaw, Martin Kaczocha, Iwao Ojima, Andrew Yates, Saoirse E O'Sullivan
Oxaliplatin-induced peripheral neuropathy (OIPN) is a dose-limiting toxicity characterised by mechanical allodynia and thermal hyperalgesia, without any licensed medications. ART26.12 is a fatty acid-binding protein (FABP) 5 inhibitor with antinociceptive properties, characterised here for the prevention and treatment of OIPN. ART26.12 binds selectively to FABP5 compared to FABP3, FABP4, and FABP7, with minimal off-target liabilities, high oral bioavailability, and a NOAEL of 1,000 mg/kg/day in rats and dogs...
January 15, 2024: Journal of Pain
https://read.qxmd.com/read/38218067/the-progress-of-small-molecules-against-cannabinoid-2-receptor-cb-2-r
#23
REVIEW
Qinying Zhang, Ying Zhao, Jianan Wu, Wanting Zhong, Wenhai Huang, Youlu Pan
The two subtypes of cannabinoid receptors (CBR), namely CB1 R and CB2 R, belong to the G protein-coupled receptor (GPCR) superfamily and are confirmed as potential therapeutic targets for a variety of diseases such as inflammation, neuropathic pain, and immune-related disorders. Since CB1 R is mainly distributed in the central nervous system (CNS), it could produce severe psychiatric adverse reactions and addiction. In contrast, CB2 R are predominantly distributed in the peripheral immune system with minimal CNS-related side effects...
January 8, 2024: Bioorganic Chemistry
https://read.qxmd.com/read/38215394/structure-based-identification-of-organoruthenium-compounds-as-nanomolar-antagonists-of-cannabinoid-receptors
#24
JOURNAL ARTICLE
Qing Wang, Xuegang Fu, Yuting Yan, Tao Liu, Yuting Xie, Xiaoqing Song, Yu Zhou, Min Xu, Ping Wang, Peng Fu, Jianhui Huang, Niu Huang
Metal complexes exhibit a diverse range of coordination geometries, representing novel privileged scaffolds with convenient click types of preparation inaccessible for typical carbon-centered organic compounds. Herein, we explored the opportunity to identify biologically active organometallic complexes by reverse docking of a rigid, minimum-size octahedral organoruthenium scaffold against thousands of protein-binding pockets. Interestingly, cannabinoid receptor type 1 (CB1) was identified based on the docking scores and the degree of overlap between the docked organoruthenium scaffold and the hydrophobic scaffold of the cocrystallized ligand...
January 12, 2024: Journal of Chemical Information and Modeling
https://read.qxmd.com/read/38200874/agroecological-zone-specific-diet-optimization-for-water-buffalo-bubalus-bubalis-through-nutritional-and-in-vitro-fermentation-studies
#25
JOURNAL ARTICLE
Sultan Singh, Pushpendra Koli, B P Kushwaha, Uchenna Y Anele, Sumana Bhattacharya, Yonglin Ren
The water buffalo faces challenges in optimizing nutrition due to varying local feed resources. In response to this challenge, the current study introduces originality by addressing the lack of region-specific feeding strategies for water buffaloes. This is achieved through the formulation of 30 different diets based on locally available resources, offering a tailored approach to enhance nutritional optimization in diverse agroecological contexts. These diets were segmented into three groups of ten, each catering to the maintenance (MD1 to MD10 ), growth (GD1 to GD10 ), and lactation/production (PD1 to PD10 ) needs of buffaloes...
December 31, 2023: Animals: An Open Access Journal From MDPI
https://read.qxmd.com/read/38195158/-%C3%AE-caryophyllene-inhibits-monoacylglycerol-lipase-activity-and-increases-2-arachidonoyl-glycerol-levels-in-vivo-a-new-mechanism-of-endocannabinoid-mediated-analgesia
#26
JOURNAL ARTICLE
Jost Klawitter, Wiebke Weissenborn, Iuliia Gvon, Mackenzie Walz, Jelena Klawitter, Matthew Jackson, Cristina Sempio, Sonja L Joksimovic, Touraj Shokati, Ingo Just, Uwe Christians, Slobodan M Todorovic
The mechanisms of β -caryophyllene (BCP)-induced analgesia are not well studied. Here, we tested the efficacy of BCP in an acute postsurgical pain model and evaluated its effect on the endocannabinoid system. Rats were treated with vehicle and 10, 25, 50, and 75 mg/kg BCP. Paw withdrawal responses to mechanical stimuli were evaluated using an electronic von Frey anesthesiometer. Endocannabinoids, including 2-arachidonoylglycerol (2-AG), were also evaluated in plasma and tissues using high-performance liquid chromatography-tandem mass spectrometry...
January 10, 2024: Molecular Pharmacology
https://read.qxmd.com/read/38193034/sesquiterpene-evoked-phytochemical-toxicity-in-pc12-neuronal-cells-reveals-a-variable-degree-of-oxidative-stress-and-alpha-tocopherol-and-glutathione-dependent-protection
#27
JOURNAL ARTICLE
John Staton Laws Iii, Scott D Smid
Phytochemicals are often promoted generally as antioxidants and demonstrate variable levels of reactive oxygen species (ROS) sequestration in vitro, which attributes to their neuroprotective bioactivity. Sesquiterpenes from cannabis and essential oils may demonstrate bifunctional properties towards cellular oxidative stress, possessing pro-oxidant activities by generating ROS or scavenging ROS directly. Sesquiterpenes can also oxidize forming sesquiterpene oxides, however the relative contribution they make to the bioactivity or cytotoxicity of complex botanical extracts more generally is unclear, while selected cannabis-prevalent terpenes such as β-caryophyllene may also activate cannabinoid receptors as part of their biological activity...
2024: Current research in toxicology
https://read.qxmd.com/read/38190933/distant-neuroinflammation-acutely-induced-by-focal-brain-injury-and-its-control-by-endocannabinoid-system
#28
JOURNAL ARTICLE
Anna A Karan, Yulia S Spivak, Elena M Suleymanova, Konstantin A Gerasimov, Alex P Bolshakov, Lyudmila V Vinogradova
INTRODUCTION: We studied spatiotemporal features of acute transcriptional inflammatory response induced by a focal brain injury in distant uninjured neuronal tissue and a role of endocannabinoid (eCB) system in its control. MATERIALS AND METHODS: A focal excitotoxic lesion was induced by a unilateral injection of kainate in the dorsal hippocampus of awake Wistar rats. During acute post-injury period (3 h and 24 h post-injection), mRNA levels of genes associated with neuroinflammation (Il1b, Il6, Tnf, Ccl2; Cx3cl1, Zc3 h12a, Tgfb1) and eCB receptors of CB1 and CB2 types (Cnr1 and Cnr2) in intact regions of the hippocampus and neocortex were measured using qPCR...
January 6, 2024: Experimental Neurology
https://read.qxmd.com/read/38186742/dataset-of-amplicon-metagenomic-assessment-of-barley-rhizosphere-bacteria-under-different-fertilization-regimes
#29
JOURNAL ARTICLE
Olubukola Oluranti Babalola, Ben Jesuorsemwen Enagbonma
The metagenomic dataset profiled in this research is built on bacterial 16S rRNA gene amplicon of DNA mined from barley rhizosphere under chemical (CB) and organic (OB) fertilization. Amplicon-based sequencing was prepared by the Illumina platform, and the raw sequence dataset was examined using Metagenomic Rast Server (MG-RAST). The metagenome comprised sixteen samples that include CB1 (494,583 bp), CB2 (586,532 bp), CB3 (706,685 bp), CB4 (574,606 bp), CB5 (395,460 bp), CB6 (520,822 bp), CB7 (511,729 bp), CB8 (548,074 bp), OB1 (642,794 bp), OB2 (513,767 bp), OB3 (461,293 bp), OB4 (498,241 bp), OB5 (689,497 bp), OB6 (423,436 bp), OB7 (478,657 bp) and OB8 (279,186 bp)...
February 2024: Data in Brief
https://read.qxmd.com/read/38150961/discovery-of-a-cb-2-and-5-ht-1a-receptor-dual-agonist-for-the-treatment-of-depression-and-anxiety
#30
JOURNAL ARTICLE
Wenjiao Yang, Xudong Gong, Haiguo Sun, Chunhui Wu, Jin Suo, Jing Ji, Xiangrui Jiang, Jingshan Shen, Yang He, Haji Akber Aisa
Cannabinoid CB2 R agonists have gained considerable attention as potential novel therapies for psychiatric disorders due to their non-psychoactive nature, in contrast to CB1 R agonists. In this study, we employed molecular docking to design and synthesize 23 derivatives of cannabidiol (CBD) with the aim of discovering potent CB2 R agonists rather than CB2 R antagonists or inverse agonists. Structure-activity relationship (SAR) investigations highlighted the critical importance of the amide group at the C-3' site and the cycloalkyl group at the C-4' site for CB2 R activation...
December 14, 2023: European Journal of Medicinal Chemistry
https://read.qxmd.com/read/38132757/solid-state-fermentation-with-white-rot-fungi-pleurotus-species-improves-the-chemical-composition-of-highland-barley-straw-as-a-ruminant-feed-and-enhances-in-vitro-rumen-digestibility
#31
JOURNAL ARTICLE
Yuqiong Wang, Changlong Gou, Liming Chen, Yangci Liao, Hang Zhang, Lilong Luo, Jiahang Ji, Yu Qi
Lignin degradation is important for enhancing the digestibility and improving the nutritive quality of ruminant feeds. White rot fungi are well known for their bioconversion of lignocellulosic biomass. The objective of this paper was to evaluate whether Lentinus sajor-caju , Pleurotus ostreatus , Phyllotopsis rhodophylla , Pleurotus djamor , Pleurotus eryngii , and Pleurotus citrinopileatus treatments altered the chemical compositions of highland barley straw constituents and enhanced their nutritional value as a ruminant feed...
November 30, 2023: Journal of Fungi (Basel, Switzerland)
https://read.qxmd.com/read/38116770/the-endocannabinoid-system-and-its-relationship-to-human-reproduction
#32
REVIEW
A Pařízek, J Suchopár, Z Laštůvka, M Alblová, M Hill, M Dušková
The endocannabinoid system is among the most important regulators of human reproduction. It already applies at the level of the sperm and the egg, plays an important role in the fertilization of the egg, its implantation, regulates the function of the placenta and participates in childbirth. The aim of this work is to summarize the knowledge accumulated so far and to show that the endocannabinoid system must be perfectly regulated in order to maintain a physiological pregnancy from implantation to delivery...
December 17, 2023: Physiological Research
https://read.qxmd.com/read/38113964/activation-of-the-cannabinoid-type-2-cb2-receptor-improves-cardiac-contractile-performance-in-fish-brycon-amazonicus
#33
JOURNAL ARTICLE
Yan Costa Gonçalves, Karina Carla de Francisco Campos, Eliton da Silva Vasconcelos, Beatriz Micucci D'Almeida Eça, Francisco Tadeu Rantin, Ana Lúcia Kalinin, Diana Amaral Monteiro
In addition to their well-known classical effects, cannabinoid CB1 and CB2 receptors have also been involvement in both deleterious and protective actions on the heart under various pathological conditions. While the potential therapeutic applications of the endocannabinoid system in the context of cardiovascular function are indeed a viable prospect, significant debate exists within the literature regarding whether CB1, CB2, or a combination of both receptors exert a favorable influence on cardiac function...
December 17, 2023: Comparative Biochemistry and Physiology. Toxicology & Pharmacology: CBP
https://read.qxmd.com/read/38100640/investigation-of-the-cytotoxicity-induced-by-cannabinoids-on-human-ovarian-carcinoma-cells
#34
JOURNAL ARTICLE
Kartheek Sooda, Simon J Allison, Farideh A Javid
Cannabinoids have been shown to induce anti-tumor activity in a variety of carcinoma cells such as breast, prostate, and brain. The aim of the present study is to investigate the anti-tumor activity of cannabinoids, CBD (cannbidiol), and CBG (cannabigerol) in ovarian carcinoma cells sensitive and resistant to chemotherapeutic drugs. Sensitive A2780 cells and resistant A2780/CP70 carcinoma cells and non-carcinoma cells were exposed to varying concentrations of CBD, CBG, carboplatin or CB1 and CB2 receptor antagonists, AM251 and AM630, respectively, alone or in combination, at different exposure times and cytotoxicity was measured by MTT assay...
December 2023: Pharmacology Research & Perspectives
https://read.qxmd.com/read/38074691/cannabinoids-and-the-endocannabinoid-system-in-immunotherapy-helpful-or-harmful
#35
REVIEW
Arailym Sarsembayeva, Rudolf Schicho
Numerous studies in various cancer models have demonstrated that ingredients of cannabis can influence tumor growth through the endocannabinoid system (ECS), a network of molecules (mediators, receptors, transporters, enzymes) that maintains homeostasis and protection in many tissues. The main constituents of the ECS are the classical cannabinoid (CB) receptors, such as CB1 and CB2 , their endogenous ligands (endocannabinoids), and the endocannabinoids' synthesizing and degrading enzymes. The role of the ECS in cancer is still unclear and its effects often depend on the tumor entity and the expression levels of CB receptors...
2023: Frontiers in Oncology
https://read.qxmd.com/read/38069049/neuroprotection-and-beyond-the-central-role-of-cb1-and-cb2-receptors-in-stroke-recovery
#36
REVIEW
Bashir Bietar, Sophie Tanner, Christian Lehmann
The endocannabinoid system, with its intricate presence in numerous cells, tissues, and organs, offers a compelling avenue for therapeutic interventions. Central to this system are the cannabinoid receptors 1 and 2 (CB1R and CB2R), whose ubiquity can introduce complexities in targeted treatments due to their wide-ranging physiological influence. Injuries to the central nervous system (CNS), including strokes and traumatic brain injuries, induce localized pro-inflammatory immune responses, termed neuroinflammation...
November 24, 2023: International Journal of Molecular Sciences
https://read.qxmd.com/read/38059783/cannabidiol-inhibits-ige-mediated-mast-cell-degranulation-and-anaphylaxis-in-mice
#37
JOURNAL ARTICLE
Xiaohui Yang, Dohyeon Lee, Hyun-Woo Kim, Byung-Hyun Park, Changjin Lim, Eun Ju Bae
SCOPE: Cannabidiol (CBD), the most abundant non-psychoactive constituent of the plant Cannabis sativa, is known to possess immune modulatory properties. This study investigates the effects of CBD on mast cell degranulation in human and mouse primary mast cells and passive cutaneous anaphylaxis in mice. METHODS AND RESULTS: Mouse bone marrow-derived mast cells and human cord-blood derived mast cells are generated. CBD suppressed antigen-stimulated mast cell degranulation in a concentration-dependent manner...
December 7, 2023: Molecular Nutrition & Food Research
https://read.qxmd.com/read/38059442/effects-of-cannabinoid-agonists-and-antagonists-in-male-rats-discriminating-the-synthetic-cannabinoid-am2201
#38
JOURNAL ARTICLE
Dalal AlKhelb, Emily L Burke, Alexander Zvonok, Christos Iliopoulos-Tsoutsouvas, Markos-Orestis Georgiadis, Shan Jiang, Thanh C Ho, Spyros P Nikas, Alexandros Makriyannis, Rajeev I Desai
The synthetic forms of delta-9-tetrahydrocannabinol (Δ9 -THC), dronabinol or nabilone, have been approved to treat several indications. However, due to safety concerns their clinical utility remains limited. Consequently, there is a need for developing cannabinoid (CB) ligands that display better behavioral pharmacological profiles than Δ9 -THC. Here, we utilized drug discrimination methods to compare the interoceptive effects of CB ligands that vary in potency, efficacy, and selectivity at the CB receptors, including two ligands, AM411 and AM4089, that show CB1 partial agonist-like actions in vitro...
December 5, 2023: European Journal of Pharmacology
https://read.qxmd.com/read/38052772/a-monoacylglycerol-lipase-inhibitor-showing-therapeutic-efficacy-in-mice-without-central-side-effects-or-dependence
#39
JOURNAL ARTICLE
Ming Jiang, Mirjam C W Huizenga, Jonah L Wirt, Janos Paloczi, Avand Amedi, Richard J B H N van den Berg, Joerg Benz, Ludovic Collin, Hui Deng, Xinyu Di, Wouter F Driever, Bogdan I Florea, Uwe Grether, Antonius P A Janssen, Thomas Hankemeier, Laura H Heitman, Tsang-Wai Lam, Florian Mohr, Anto Pavlovic, Iris Ruf, Helma van den Hurk, Anna F Stevens, Daan van der Vliet, Tom van der Wel, Matthias B Wittwer, Constant A A van Boeckel, Pal Pacher, Andrea G Hohmann, Mario van der Stelt
Monoacylglycerol lipase (MAGL) regulates endocannabinoid 2-arachidonoylglycerol (2-AG) and eicosanoid signalling. MAGL inhibition provides therapeutic opportunities but clinical potential is limited by central nervous system (CNS)-mediated side effects. Here, we report the discovery of LEI-515, a peripherally restricted, reversible MAGL inhibitor, using high throughput screening and a medicinal chemistry programme. LEI-515 increased 2-AG levels in peripheral organs, but not mouse brain. LEI-515 attenuated liver necrosis, oxidative stress and inflammation in a CCl4 -induced acute liver injury model...
December 5, 2023: Nature Communications
https://read.qxmd.com/read/38004445/cancer-cachexia-induced-human-skeletal-muscle-myotube-degeneration-is-prevented-via-cannabinoid-receptor-2-agonism-in-vitro
#40
JOURNAL ARTICLE
John Noone, Mary F Rooney, Marilena Karavyraki, Andrew Yates, Saoirse E O'Sullivan, Richard K Porter
Cachexia syndrome, leading to reduced skeletal muscle and fat mass, is highly prevalent in cancer patients, resulting in further negative implications for these patients. To date, there is no approved therapy for cachexia syndrome. The objective of this study was to establish an in vitro model of cancer cachexia in mature human skeletal muscle myotubes, with the intention of exploiting the cell model to assess potential cachexia therapeutics, specifically cannabinoid related drugs. Having cultured and differentiated primary human muscle myoblasts to mature myotubes, we successfully established two cancer cachexia models using conditioned media (CM) from human colon adenocarcinoma (SW480) and from non-small-cell lung carcinoma (H1299) cultured cells...
November 8, 2023: Pharmaceuticals
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