Historical and scientific evidence suggests that Cannabis use has immunomodulatory and anti-inflammatory effects. We have here investigated the effect of the non-psychotropic phytocannabinoid delta9-tetrahydrocannabivarin (THCV) and of a Cannabis sativa extract with high (64.8%) content in THCV(THCV-BDS) on nitric oxide (NO) production, and on cannabinoid and transient receptor potential (TRP)channel expression in lipopolysaccharide (LPS)-stimulated murine peritoneal macrophages.THCV-BDS and THCV exhibited similar affinity in radioligand binding assays for CB1and CB2recep-tors, and inhibited, via CB2but not CB1cannabinoid receptors, nitrite production evoked by LPS inperitoneal macrophages. THCV down-regulated the over-expression of inducible nitric oxide synthase(iNOS), cyclooxygenase-2 (COX-2) and interleukin 1beta (IL-1beta) proteins induced by LPS. Furthermore, THCVcounteracted LPS-induced up-regulation of CB1receptors, without affecting the changes in CB2, TRPV2 orTRPV4 mRNA expression caused by LPS. Other TRP channels, namely, TRPA1, TRPV1, TRPV3 and TRPM8were poorly expressed or undetectable in both unstimulated and LPS-challenged macrophages.It is concluded that THCV - via CB2receptor activation - inhibits nitrite production in macrophages.The effect of this phytocannabinoid was associated with a down-regulation of CB1, but not CB2or TRPchannel mRNA expression.
Pure delta9-tetrahydrocannabivarin and a Cannabis sativa extract withhigh content in delta9-tetrahydrocannabivarin inhibit nitrite productionin murine peritoneal macrophages
Pierangelo Orlando;Vincenzo Di Marzo;
2016
Abstract
Historical and scientific evidence suggests that Cannabis use has immunomodulatory and anti-inflammatory effects. We have here investigated the effect of the non-psychotropic phytocannabinoid delta9-tetrahydrocannabivarin (THCV) and of a Cannabis sativa extract with high (64.8%) content in THCV(THCV-BDS) on nitric oxide (NO) production, and on cannabinoid and transient receptor potential (TRP)channel expression in lipopolysaccharide (LPS)-stimulated murine peritoneal macrophages.THCV-BDS and THCV exhibited similar affinity in radioligand binding assays for CB1and CB2recep-tors, and inhibited, via CB2but not CB1cannabinoid receptors, nitrite production evoked by LPS inperitoneal macrophages. THCV down-regulated the over-expression of inducible nitric oxide synthase(iNOS), cyclooxygenase-2 (COX-2) and interleukin 1beta (IL-1beta) proteins induced by LPS. Furthermore, THCVcounteracted LPS-induced up-regulation of CB1receptors, without affecting the changes in CB2, TRPV2 orTRPV4 mRNA expression caused by LPS. Other TRP channels, namely, TRPA1, TRPV1, TRPV3 and TRPM8were poorly expressed or undetectable in both unstimulated and LPS-challenged macrophages.It is concluded that THCV - via CB2receptor activation - inhibits nitrite production in macrophages.The effect of this phytocannabinoid was associated with a down-regulation of CB1, but not CB2or TRPchannel mRNA expression.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
