Ultrapotent effects of salvinorin A, a hallucinogenic compound from Salvia divinorum, on LPS-stimulated murine macrophages and its anti-inflammatory action in vivo.
Journal of molecular medicine (Berlin, Germany) September 1, 2011 Gabriella Aviello, Francesca Borrelli, Francesca Guida et al. 70 citations
Salvinorin A, a hallucinogenic compound, reduces inflammation in immune cells and in animal models of inflammation. At extremely low concentrations (0.1-10 pM), it lowers levels of inflammatory markers nitrite, TNF-α, and IL-10 (but not IL-1β) and reduces expression of iNOS (but not COX-2) in stimulated macrophages. These effects are blocked by antagonists of both κ-opioid receptors (KOR) and cannabinoid CB1 receptors, and salvinorin A prevents the overproduction of these receptors induced by inflammation. In living animals, salvinorin A reduces paw swelling caused by LPS or carrageenan and pain from formalin injection, with these effects also blocked by KOR and CB1 antagonists. The compound acts through both KOR and CB1 receptors to produce potent anti-inflammatory actions on macrophages and moderate anti-inflammatory effects in vivo.