Planta Med 2012; 78 - P_92
DOI: 10.1055/s-0032-1307600

In Vitro Activity of Phytocannabinoids from High Potency Cannabis sativa

A Husni 1, S Ross 2, O Dale 1, C Gemelli 1, G Ma 1, SP Manly 2, MA ElSohly 2, S Cutler 1
  • 1Department of Medicinal Chemistry, School of Pharmacy, The University of Mississippi, University, MS 38677
  • 2National Center for Natural Products Research, Thad Cochran Research Center, University, MS 38677

Cannabinoids are a chemical class of agents that represent compounds derived synthetically or naturally from Cannabis. Marijuana is the most widely used drug of abuse all over the world. Tetrahydrocannabinol (THC, pictured below) is pharmacologically and toxicologically the best studied constituent of marijuana, responsible for most of the psychoactive effects of natural Cannabis preparations. There have been over 100 compounds isolated from marijuana.

Cannabinoid receptors CB1 and CB2 are G-protein coupled receptors that are positively coupled to adenylyl cyclase. This has led to the development of selective cannabinoid CB1 and CB2 receptor ligands. Our strategy is to identify selective cannabinoid CB1 and CB2 receptor ligands from natural products or synthetic compounds for pain management, drug abuse, cancer, and diabetes. The first step is to establish stable experimental models for specific receptor binding and functional assays. Through optimization of different buffers, temperatures, and bovine serum albumin (BSA) the receptor specific binding ratio has improved dramatically. These optimizations allowed us to screen novel phytocannabinoids for CB1 and CB2 receptor binding and functional activity.