PUBLICATION

Δ9-tetrahydrocannabivarin impairs epithelial calcium transport through inhibition of TRPV5 and TRPV6.

Authors
Janssens, A., Silvestri, C., Martella, A., Vanoevelen, J.M., Di Marzo, V., Voets, T.
ID
ZDB-PUB-180901-9
Date
2018
Source
Pharmacological research   136: 83-89 (Journal)
Registered Authors
Keywords
TRPV5, TRPV6, epithelial calcium transport, ossification, phytocannabinoids, Δ(9)-tetrahydrocannabivarin
MeSH Terms
  • Cannabinoids/pharmacology*
  • Zebrafish
  • Calcium/physiology*
  • TRPV Cation Channels/antagonists & inhibitors*
  • TRPV Cation Channels/physiology
  • Epithelium/physiology
  • Animals
  • HEK293 Cells
  • Humans
  • Embryo, Nonmammalian
PubMed
30170189 Full text @ Pharmacol. Res.
CTD
30170189
Citation
Janssens, A., Silvestri, C., Martella, A., Vanoevelen, J.M., Di Marzo, V., Voets, T. (2018) Δ9-tetrahydrocannabivarin impairs epithelial calcium transport through inhibition of TRPV5 and TRPV6.. Pharmacological research. 136:83-89.
Abstract
Compounds extracted from the cannabis plant, including the psychoactive Δ9-tetrahydrocannabinol (THC) and related phytocannabinoids, evoke multiple diverse biological actions as ligands of the G protein-coupled cannabinoid receptors CB1 and CB2. In addition, there is increasing evidence that phytocannabinoids also have non-CB targets, including several ion channels of the transient receptor potential superfamily. We investigated the effects of six non-THC phytocannabinoids on the epithelial calcium channels TRPV5 and TRPV6, and found that one of them, Δ9-tetrahydrocannabivarin (THCV), exerted a strong and concentration-dependent inhibitory effect on mammalian TRPV5 and TRPV6 and on the single zebrafish orthologue drTRPV5/6. Moreover, THCV attenuated the drTRPV5/6-dependent ossification in zebrafish embryos in vivo. Oppositely, 11-hydroxy-THCV (THCV-OH), a product of THCV metabolism in mammals, stimulated drTRPV5/6-mediated Ca2+ uptake and ossification. These results identify the epithelial calcium channels TRPV5 and TRPV6 as novel targets of phytocannabinoids, and suggest that THCV-containing products may modulate TRPV5- and TRPV6-dependent epithelial calcium transport.
Genes / Markers
Figures
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Antibodies
Orthology
Engineered Foreign Genes
Mapping
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