Fundamental Toxicological Sciences

Paper Details

Fundamental Toxicological Sciences
Vol. 4 No. 2 May 13, 2017 p.101-103
Phytocannabinoids, Δ9-tetrahydrocannabinol and cannabidiol, as human calpain-1 (CAPN1) activators
  • Hironori Aramaki (Department of Molecular Biology, Daiichi University of Pharmacy /
Shuso Takeda 1) , Kazuhito Watanabe 2) , Hironori Aramaki 3)
1) Laboratory of Xenobiotic Metabolism and Environmental Toxicology, Faculty of Pharmaceutical Sciences, Hiroshima International University (HIU) , 2) Center for Supporting Pharmaceutical Education, Daiichi University of Pharmacy , 3) Department of Molecular Biology, Daiichi University of Pharmacy
Keywords: Δ9-Tetrahydricannabinol, Cannabidiol, Calpain-1, CAPN1, 2-Methyl-2’-fluoro-anandamide

The effects of Δ9-tetrahydricannabinol (Δ9-THC), cannabidiol (CBD), cannabidiolic acid (CBDA), and 2-methyl-2’-fluoro-anandamide (MF-AEA, a stable analog of anandamide) on the enzymatic activity of purified human calpain-1 (CAPN1) were investigated in the present study. Although leupeptin, a calpain inhibitor, reduced calpain-1 activity in a dose-dependent manner (1, 5, and 25 μM), among the four cannabinoids tested, Δ9-THC and CBD exerted stimulatory effects on calpain-1 enzymatic activity in the same concentration range as leupeptin. CBDA and MF-AEA did not modulate calpain-1 activity, indicating that the phenol structure in Δ9-THC/CBD is a key point, and the carboxylic acid moiety appears to be negatively involved. This is the first study to show that the phytocannabinoids, Δ9-THC and CBD have the ability to activate the enzymatic activity of human calpain-1.