title: CB(2) and TRPV(1) receptors oppositely modulate in vitro human osteoblast activity.
abstract: In the current study, we have investigated the effect of CB2 and TRPV1 receptor ligands on in vitro osteoblasts from bone marrow of human healthy donors. A pivotal role for the endocannabinoid/endovanilloid system in bone metabolism has been highlighted. We have demonstrated a functional cross-talk between CB2 and TRPV1 in human osteoclasts, suggesting these receptors as new pharmacological target for the treatment of bone resorption disease as osteoporosis. Moreover, we have shown the presence of these receptors on human mesenchimal stem cells, hMSCs. Osteoblasts are mononucleated cells originated from hMSCs by the essential transcription factor runt-related transcription factor 2 and involved in bone formation via the synthesis and release of macrophage colony-stimulating factor, receptor activator of nuclear factor kappa-B ligand and osteoprotegerin. For the first time, we show that CB2 and TRPV1 receptors are both expressed on human osteoblasts together with enzymes synthesizing and degrading endocannabinoids/endovanilloids, and oppositely modulate human osteoblast activity in culture in a way that the CB2 receptor stimulation improves the osteogenesis whereas TRPV1 receptor stimulation inhibits it.
authors.affiliation: Department of Woman, Child and of General and Specialist Surgery, Second University of Naples, Naples, Italy. Electronic address: francesca.rossi@unina2.it.
authors.forename: Francesca
authors.initials: F
authors.lastname: Rossi
authors.affiliation: Department of Experimental Medicine, Pharmacology Division, The Second University of Naples, Italy.
authors.forename: Giulia
authors.initials: G
authors.lastname: Bellini
authors.affiliation: Department of Experimental Medicine, Pharmacology Division, The Second University of Naples, Italy.
authors.forename: Chiara
authors.initials: C
authors.lastname: Tortora
authors.affiliation: Department of Onco-Haematology, IRCCS "Bambino Gesù" Children Hospital, Rome, Italy.
authors.forename: Maria Ester
authors.initials: ME
authors.lastname: Bernardo
authors.affiliation: Department of Experimental Medicine, Pharmacology Division, The Second University of Naples, Italy.
authors.forename: Livio
authors.initials: L
authors.lastname: Luongo
authors.affiliation: Department of Onco-Haematology, IRCCS "Bambino Gesù" Children Hospital, Rome, Italy.
authors.forename: Antonella
authors.initials: A
authors.lastname: Conforti
authors.affiliation: Department of Onco-Haematology, IRCCS "Bambino Gesù" Children Hospital, Rome, Italy.
authors.forename: Nadia
authors.initials: N
authors.lastname: Starc
authors.affiliation: Department of Woman, Child and of General and Specialist Surgery, Second University of Naples, Naples, Italy.
authors.forename: Iolanda
authors.initials: I
authors.lastname: Manzo
authors.affiliation: Department of Woman, Child and of General and Specialist Surgery, Second University of Naples, Naples, Italy.
authors.forename: Bruno
authors.initials: B
authors.lastname: Nobili
authors.affiliation: Department of Onco-Haematology, IRCCS "Bambino Gesù" Children Hospital, Rome, Italy.
authors.forename: Franco
authors.initials: F
authors.lastname: Locatelli
authors.affiliation: Department of Experimental Medicine, Pharmacology Division, The Second University of Naples, Italy.
authors.forename: Sabatino
authors.initials: S
authors.lastname: Maione
mesh_terms: D001862:Bone Resorption / Q000378:metabolism; D001842:Bone and Bones / Q000378:metabolism / Q000502:physiology; D002454:Cell Differentiation / Q000502:physiology; D002478:Cells, Cultured; D063388:Endocannabinoids / Q000378:metabolism / Q000502:physiology; D006801:Humans; D016173:Macrophage Colony-Stimulating Factor / Q000378:metabolism; D059630:Mesenchymal Stem Cells / Q000378:metabolism / Q000502:physiology; D016328:NF-kappa B / Q000378:metabolism; D010006:Osteoblasts / Q000378:metabolism* / Q000502:physiology; D010010:Osteoclasts / Q000378:metabolism / Q000502:physiology; D010012:Osteogenesis / Q000502:physiology; D010024:Osteoporosis / Q000378:metabolism; D053244:Osteoprotegerin / Q000378:metabolism / Q000502:physiology; D043885:Receptor, Cannabinoid, CB2 / Q000378:metabolism*; D050916:TRPV Cation Channels / Q000378:metabolism*
chemical_list: D063388:Endocannabinoids; D016328:NF-kappa B; D053244:Osteoprotegerin; D043885:Receptor, Cannabinoid, CB2; D050916:TRPV Cation Channels; C494484:TRPV1 receptor; D016173:Macrophage Colony-Stimulating Factor
keywords: CB(2) receptor; Endocannabinoid/endovanilloid system; Human osteoblast culture; Osteoblast activity markers; TRPV(1) receptor