Article
Chemistry, Physical
Moonhyuk Kwon, Joseph C. Utomo, Keunwan Park, Cameron A. Pascoe, Sorina Chiorean, Iris Ngo, Kyle A. Pelot, Cheol-Ho Pan, Seon-Won Kim, Philipp Zerbe, John C. Vederas, Dae-Kyun Ro
Summary: Research has shown that the hallucinogenic plant Salvia divinorum synthesizes neoclerodane diterpenes with regulatory effects on opioid receptors. The discovery of crotonolide G synthase (SdCS) provides a unique lead structure for drug development.
Article
Veterinary Sciences
Vikram Thakur, Mohammad Bashashati, Josue Enriquez, Munmun Chattopadhyay
Summary: This study assessed specific gastrointestinal symptoms in Type 1 diabetic mice and evaluated treatment options for this condition. The results showed that inhibiting endocannabinoid degradation may have a therapeutic effect on gastrointestinal dysmotility.
VETERINARY SCIENCES
(2022)
Review
Neurosciences
Andrea S. Heimann, Camila S. Dale, Francisco S. Guimaraes, Ricardo A. M. Reis, Ami Navon, Michal A. Shmuelov, Vanessa Rioli, Ivone Gomes, Lakshmi L. Devi, Emer S. Ferro
Summary: Hemopressin, derived from hemoglobin alpha-chain, exhibits diverse cannabinoid receptor activities and may have pharmacological effects by interacting with intracellular mitochondrial cannabinoid receptors. The peptide influences physiological processes such as pain, inflammation, appetite, learning, and memory, and shows potential applications in drug delivery systems.
Review
Biochemistry & Molecular Biology
Kangtai Xu, Yifei Wu, Zhuangzhuang Tian, Yuanfan Xu, Chaoran Wu, Zilong Wang
Summary: Pain, especially chronic pain, has a significant impact on patients' quality of life. Cannabinoids have shown potent analgesic effects in preclinical pain models by acting as agonists of CB1 and CB2 receptors. While the activation of CB1 receptors is associated with psychotropic adverse effects, the promising target for pain treatment is the CB2 receptors primarily expressed in immune cells. Microglia, as resident immune cells in the central nervous system, play a critical role in chronic pain, and CB2 receptors regulate their activity and function. This review focuses on the role of microglial CB2 receptors in spinal nociceptive circuitry and their implications for selective CB2 receptor agonist-mediated analgesia.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Sanela Rajlic, Luise Surmann, Pia Zimmermann, Christina Katharina Weisheit, Laura Bindila, Hendrik Treede, Markus Velten, Andreas Daiber, Georg Daniel Duerr
Summary: Ischemic cardiomyopathy leads to inflammation and left ventricular dysfunction. Animal studies suggest that the endocannabinoid system may have cardioprotective effects, including cardiomyocyte adaptation, inflammation, and remodeling. This study investigates the potential cardioprotective effect of the endocannabinoid anandamide (AEA) after ischemia and reperfusion using FAAH (-/-) mice and suggests that increased endocannabinoids may have detrimental effects on cardiomyocyte survival due to PPAR-alpha activation.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Biochemistry & Molecular Biology
Chaoling Chen, Weili Wang, Justin L. Poklis, Aron H. Lichtman, Joseph K. Ritter, Gaizun Hu, Dengpiao Xie, Ningjun Li
Summary: The study suggests that FAAH activation and the consequent reduction of AEA contribute to renal fibrogenesis, while FAAH inhibition protects against fibrogenesis in renal cells independently of CB receptors via the AEA-COX-2 pathway.
BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE
(2022)
Review
Biochemistry & Molecular Biology
Barbara Vuic, Tina Milos, Lucija Tudor, Marcela Konjevod, Matea Nikolac Perkovic, Maja Jazvinscak Jembrek, Gordana Nedic Erjavec, Dubravka Svob Strac
Summary: Neurodegenerative diseases, characterized by protein aggregation in the brain, can be influenced by the activation of CB2 receptors in the endocannabinoid system. Studies suggest that activating CB2 receptors has potential benefits in reducing protein aggregation-based pathology, attenuating inflammation, and alleviating dementia-related symptoms.
Article
Chemistry, Medicinal
Daniel Gundel, Winnie Deuther-Conrad, Lea Ueberham, Sarandeep Kaur, Elina Otikova, Rodrigo Teodoro, Magali Toussaint, Thu Hang Lai, Oliver Clauss, Matthias Scheunemann, Guy Bormans, Michael Bachmann, Klaus Kopka, Peter Brust, Rares-Petru Moldovan
Summary: The cannabinoid receptor type 2 (CB2R) is an ideal target for the diagnosis and therapy of neurodegenerative diseases and cancer. This study introduces a novel F-18-labeled radioligand that can efficiently image upregulated CB2R expression.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Cell Biology
Nuchjira Takheaw, Kanyaruck Jindaphun, Supansa Pata, Witida Laopajon, Watchara Kasinrerk
Summary: Cannabinoid receptor 1 (CB1) and cannabinoid receptor 2 (CB2) are important components of the endocannabinoid system, which regulate immune responses. This study investigated the effects of CB1 selective agonist ACEA and CB2 selective agonist GW833972A on T cell responses. The results showed that both agonists inhibited T cell proliferation and down-regulated activation markers and co-stimulatory molecules on T cells, B cells, and monocytes in different ways. GW833972A also suppressed the cytotoxic activities of CD8(+) T cells without affecting CD4(+) T cells and NK cells. Moreover, only the CB2 agonist caused a reduction in Th1 cytokine production. These findings suggest that the CB1 and CB2 agonists may have therapeutic potential in modulating T cell function in inflammatory and autoimmune diseases.
Editorial Material
Neurosciences
Arnau Busquets-Garcia, Miriam Melis, Luigi Bellocchio, Giovanni Marsicano
Summary: This article introduces the wide expression and regulatory functions of the endocannabinoid system in both the brain and the periphery. It discusses the distribution of cannabinoid receptors in different cell types and compartments, and highlights the different cellular or molecular effects mediated by these receptors. The article also mentions the expression of the endocannabinoid system throughout the body and its role in modulating the connection between the brain and the periphery. Lastly, it emphasizes the importance of understanding the cannabinoid receptors structure and pharmacology for the development of novel allosteric modulators.
EUROPEAN JOURNAL OF NEUROSCIENCE
(2022)
Review
Medicine, Research & Experimental
Hebaallah Mamdouh Hashiesh, Charu Sharma, Sameer N. Goyal, Bassem Sadek, Niraj Kumar Jha, Juma Al Kaabi, Shreesh Ojha
Summary: BCP is a natural compound with selective agonist properties that activate CB2R and have various pharmacological effects. BCP shows protective effects in the heart, liver, nervous system, kidneys, gastrointestinal tract, cancer, with antioxidant, anti-inflammatory, and immunomodulatory actions.
BIOMEDICINE & PHARMACOTHERAPY
(2021)
Article
Neurosciences
Priscila Vazquez-Leon, Ulises Arenas-Martinez, Dafne Cordova-Maqueda, Tomas Fregoso-Aguilar, Eduardo Ramirez-San Juan, Abraham Miranda-Paez
Summary: The KOP system plays a key role in drug abuse, with Sal-A being the predominant compound isolated from Salvia divinorum. This study aimed to investigate the effects of SDE and Sal-A on alcohol intake, food consumption, and anxiety-like behavior in Wistar rats.
ACTA NEUROBIOLOGIAE EXPERIMENTALIS
(2021)
Article
Chemistry, Medicinal
Florian Mohr, Thomas Hurrle, Lindsey Burggraaff, Lukas Langer, Martijn P. Bemelmans, Maximilian Knab, Martin Nieger, Gerard J. P. van Westen, Laura H. Heitman, Stefan Braese
Summary: The study reports the development and evaluation of structure-activity relationship of a series of modified coumarins as cannabinoid receptor ligands. The most potent coumarins showed a CB2 selective agonistic profile with low nanomolar affinities, and several crucial structural requirements were identified through the research.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Pharmacology & Pharmacy
Jun-Fan Xie, Lin-Xin Wang, Wen-Ting Ren, Can Wang, Jin-Xian Gao, Hai-Lin Chen, Xue-Qi Zhao, Yan-Li Ren, Yu-Ping Xie, Yu-Feng Shao, Yi-Ping Hou
Summary: Hemopressin and related peptides act as endogenous ligands or regulators of cannabinoid receptors. This study investigates the effects of mVD-HPa on the sleep-wake cycle and cortical EEG in rats, and identifies the brain neurons activated by mVD-HPa. The results show that mVD-HPa promotes NREM sleep through CB1 receptors and activates VLPO GABAergic neurons, while inhibiting the activity of LH, LC, and TMN neurons.
FRONTIERS IN PHARMACOLOGY
(2023)
Article
Medicine, Research & Experimental
Andrea L. Johnson, Ryan Verbitsky, James Hudson, Rachel Dean, Trevor J. Hamilton
Summary: Terpenes are a diverse group of compounds found in plants, including cannabis, and may have therapeutic benefits. This study found that terpinolene, a type of terpene, has anxiolytic effects in zebrafish, mediated through CB2 receptors. The study also showed that CB2 pathways involved in the anxiolytic response are different from those altering locomotion.
BIOMEDICINE & PHARMACOTHERAPY
(2023)
Article
Pharmacology & Pharmacy
Antonio Inserra, Giada Giorgini, Sebastien Lacroix, Antonella Bertazzo, Jocelyn Choo, Athanasios Markopolous, Emily Grant, Armita Abolghasemi, Danilo De Gregorio, Nicolas Flamand, Geraint Rogers, Stefano Comai, Cristoforo Silvestri, Gabriella Gobbi, Vincenzo Di Marzo
Summary: This study found that repeated administration of lysergic acid diethylamide (LSD) induces prosocial effects in mice and affects the composition of the hippocampal endocannabinoidome and gut microbiota.
BRITISH JOURNAL OF PHARMACOLOGY
(2023)
Article
Pharmacology & Pharmacy
Ester Pagano, Barbara Romano, Donatella Cicia, Fabio A. Iannotti, Tommaso Venneri, Giuseppe Lucariello, Maria Francesca Nani, Fabio Cattaneo, Paola De Cicco, Maria D'Armiento, Marcello De Luca, Ruggiero Lionetti, Stefania Lama, Paola Stiuso, Pietro Zoppoli, Geppino Falco, Silvia Marchiano, Stefano Fiorucci, Raffaele Capasso, Vincenzo Di Marzo, Francesca Borrelli, Angelo A. Izzo
Summary: TRPM8 is overexpressed in colorectal cancer and its high expression is associated with lower survival rate of patients and hyperactivation of related signaling pathways. TRPM8 may serve as a prognostic marker and potential drug target for colorectal cancer.
BRITISH JOURNAL OF PHARMACOLOGY
(2023)
Article
Obstetrics & Gynecology
Camille Dugas, Laurence Laberee, Julie Perron, Gabrielle St-Arnaud, Veronique Richard, Veronique Perreault, Nadine Leblanc, Isabelle Marc, Vincenzo Di Marzo, Alain Doyen, Alain Veilleux, Julie Robitaille
Summary: This study compared the macronutrient and energy content of human milk between women with and without GDM. The results showed that protein, lactose, and energy content were similar between the two groups, but the concentration of TG was higher in women with GDM. Maternal age and fasting glucose level were associated with the composition of human milk, and TG in human milk was associated with infant growth in children without GDM.
BREASTFEEDING MEDICINE
(2023)
Article
Medicine, Research & Experimental
Hilal Kalkan, Ester Pagano, Debora Paris, Elisabetta Panza, Mariarosaria Cuozzo, Claudia Moriello, Fabiana Piscitelli, Armita Abolghasemi, Elisabetta Gazzerro, Cristoforo Silvestri, Raffaele Capasso, Andrea Motta, Roberto Russo, Vincenzo Di Marzo, Fabio Arturo Iannotti
Summary: This study found that there are changes in the gut microbiota composition, short-chain fatty acids (SCFAs) levels, and related metabolites in the mdx mouse model of Duchenne muscular dystrophy (DMD) compared to healthy controls. Supplementation with sodium butyrate (NaB) in mdx mice showed similar benefits as deflazacort (DFZ) in terms of muscle strength, autophagy, and inflammation. In LPS-stimulated C2C12 myoblasts, NaB reduced inflammation, promoted autophagy, and prevented dysregulation of microRNAs targeting the endocannabinoid CB1 receptor gene through the activation of GPR109A and PPAR gamma receptors. This suggests a potential disease-modifying approach for DMD and other muscular dystrophies.
EMBO MOLECULAR MEDICINE
(2023)
Article
Biochemistry & Molecular Biology
Pietro Marini, Philip Cowie, Ahmet Ayar, Guy S. S. Bewick, John Barrow, Roger G. G. Pertwee, Alasdair MacKenzie, Paolo Tucci
Summary: In this study, the researchers investigated the mechanism of CB1/M-3 receptor cross-talk using SH-SY5Y cells as a model system. They found that M-3 receptor activation upregulates the CNR1 gene, leading to a more potent CB1 receptor response. Calcium homeostasis plays a crucial role in this cross-talk. The co-expression of M-3 and CB1 receptors in specific brain areas suggests their involvement in altered synaptic plasticity after exposure to cannabinoids, and highlights the potential of targeting the M-3 receptor in drug development and understanding response variation to cannabinoids.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Review
Pediatrics
Fatma Nur Keskin, Teslime Ozge Sahin, Raffaele Capasso, Duygu Agagunduz
Summary: Phenylketonuria (PKU) is a genetic disorder caused by a mutation in the PAH gene, resulting in elevated blood phenylalanine levels that can harm the brain. Lifelong medical nutrition therapy is recommended to maintain blood phenylalanine levels. Natural protein sources may be limited, so Phe-free amino acid mixtures are used to meet daily protein requirements. Newer treatments like casein glycomacropeptide and pegvaliase are being explored. This review discusses the efficacy and safety of medical nutrition approaches and new protein substitutes in PKU treatment.
CLINICAL AND EXPERIMENTAL PEDIATRICS
(2023)
Article
Biochemistry & Molecular Biology
Paolo Tucci, Iain Brown, Guy S. S. Bewick, Roger G. G. Pertwee, Pietro Marini
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Martina Di Bartolomeo, Tibor Stark, Serena Di Martino, Fabio Arturo Iannotti, Jana Ruda-Kucerova, Giovanni Luca Romano, Martin Kuchar, Samuele Laudani, Petr Palivec, Fabiana Piscitelli, Carsten T. Wotjak, Claudio Bucolo, Filippo Drago, Vincenzo Di Marzo, Claudio D'Addario, Vincenzo Micale
Summary: Adolescent exposure to cannabinoids, such as THC, may increase the risk of psychosis in individuals exposed to perinatal insult. In this study, the researchers examined the effects of peripubertal THC exposure on rats that were also exposed to prenatal methylazoxymethanol acetate (MAM) or perinatal THC (pTHC). They found that the rats exposed to MAM or pTHC exhibited adult phenotypes relevant to schizophrenia, including social withdrawal and cognitive impairment. The researchers also observed changes in gene expression and DNA methylation, suggesting potential molecular mechanisms underlying these effects.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Danilo D'Avino, Ida Cerqua, Hammad Ullah, Michele Spinelli, Rita Di Matteo, Elisabetta Granato, Raffaele Capasso, Lucianna Maruccio, Armando Ialenti, Maria Daglia, Fiorentina Roviezzo, Antonietta Rossi
Summary: The root of Astragalus membranaceus (Fisch.) Bunge is used in Chinese medicine for its immunomodulating activities. Recent studies have shown that it has beneficial effects on allergic diseases. This study investigated the anti-inflammatory properties of a commercial extract of A. membranaceus and its therapeutic application in asthma. The extract was found to inhibit inflammation and improve lung function, making it a potential treatment option for asthma.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Endocrinology & Metabolism
Hayatte-Dounia Mir, Giada Giorgini, Vincenzo Di Marzo
Summary: This review article focuses on the expanded endocannabinoid system (eCBome) and the gut microbiome, which are increasingly attracting attention as sources of chemical signals regulating food intake, energy metabolism, and body weight. The article describes the mechanisms through which these two systems, in interactions with other signaling systems, intervene in eating disorders, based on studies in experimental models or patients. Furthermore, the article discusses the possibility of the involvement of the eCBome-gut microbiome axis in eating disorders, considering the emerging multi-faceted cross-talk mechanisms between these complex systems.
PSYCHONEUROENDOCRINOLOGY
(2023)
Article
Cell Biology
Hilal Kalkan, Elisabetta Panza, Ester Pagano, Giuseppe Ercolano, Claudia Moriello, Fabiana Piscitelli, Monika Sztretye, Raffaele Capasso, Vincenzo Di Marzo, Fabio Arturo Iannotti
Summary: In this study, the researchers investigated the role of the endocannabinoid system in simvastatin-induced muscle toxicity. They found that the expression of endocannabinoids and specific miRNAs targeting the endocannabinoid CB1 gene increased in myoblasts exposed to simvastatin. Moreover, they discovered that the dysregulation of the CB1 receptor and its downstream signaling pathways contributed to statin-induced myopathy.
CELL DEATH & DISEASE
(2023)
Article
Microbiology
Thomas Deschenes, Fred Wilfried Elom Tohoundjona, Pier-Luc Plante, Vincenzo Di Marzo, Frederic Raymond
Summary: This study compared the performance of machine learning approaches according to different types of data representations derived from shotgun metagenomics. Gene-based approaches provided similar or improved classification performances compared to taxonomic and functional profiles. Feature selection based on biological function also improved classification performance for some pathologies. This study proposes new approaches to represent microbiome data for machine learning.
Review
Chemistry, Applied
Duygu Agagunduz, Gizem Ozata-Uyar, Betul Kocaadam-Bozkurt, Aycil Ozturan-Sirin, Raffaele Capasso, Saphwan Al -Assaf, Fatih Ozogul
Summary: Food hydrocolloids are versatile natural food ingredients that can be naturally present or added as functional food ingredients or additives. Recent research suggests that certain hydrocolloids can significantly alter the gut microbiota and have positive effects on health. Therefore, investigating the benefits and side effects on the gut may be useful when exploring the health and safety effects of using hydrocolloids as food additives.
FOOD HYDROCOLLOIDS
(2023)
Article
Medicine, Research & Experimental
Yasemin Acar, Duygu Agagunduz, Paola De Cicco, Raffaele Capasso
Summary: This paper provides a literature review on the neurological roles of flavonoids, one of the most abundant phytochemical families, in Parkinson's disease (PD). Flavonoids have been shown to have beneficial effects on PD, such as protecting dopaminergic neurons, improving motor and cognitive abilities, regulating signaling pathways, and modulating oxidative stress and neuroinflammation. In addition, flavonoids can also promote the growth of beneficial strains and reduce pathogenic strains by changing the composition of bacteria in gut microbiota.
BIOMEDICINE & PHARMACOTHERAPY
(2023)
Article
Pharmacology & Pharmacy
Tangui Barre, Vincenzo Di Marzo, Fabienne Marcellin, Patrizia Burra, Patrizia Carrieri
Summary: Obesity and nonalcoholic fatty liver disease (NAFLD) are global epidemics. The endocannabinoid system is seen as a key target for treating NAFLD. Although clinical trials are lacking, research suggests potential benefits of phytocannabinoids in treating liver steatosis. Cannabis plant should be considered a major prospect for NAFLD treatment. Overcoming scientific and non-scientific barriers is necessary for further research.
CANNABIS AND CANNABINOID RESEARCH
(2023)