Skip to main content
. 2015 Aug 12;12(4):699–730. doi: 10.1007/s13311-015-0377-3

Table 2.

Enzyme targets of cannabidiol

Target Concentration range (μM); (effect) EC50/IC50 (μM) Ki/Km (μM) Preparation or tissue Assay type Reference
ACAT 1–30; (–) <10* ND Fibroblast/human [64]
Arylalkylamine N-acetyltransferase 0.1–10.0; (–) ND ND Pineal gland/rat Radiometric assay [65]
Catalase 10; (–) ND ND Hepatic/mouse [55]
Complex I 2–102; (–)* 8.2 ND Pig cortex High-resolution respirometry in malate and pyruvate [66]
Complex II 2–102 (–)* 19.1 ND Pig cortex High-resolution respirometry in succinate and rotenone
Complex IV 2–102; (–)* 18.8 ND Pig cortex High-resolution respirometry in antimycin, ascorbate and TMPD
Complex I 15–60 mg/kg, single dose (+) ND ND Prefrontal/cerebral cortex [67]
Complex II ND ND Prefrontal/cerebral cortex/hippocampus
Complex II–III ND ND Prefrontal/cerebral cortex/hippocampus
Complex IV ND ND Prefrontal/cerebral cortex/striatum/hippocampus
Complex I 15–60 mg/kg/day for 14 days (+) ND ND Prefrontal/cortex/striatum/hippocampus
Complex II ND ND Prefrontal/cortex/striatum/hippocampus
Complex II–III ND ND Prefrontal/cortex
Complex IV ND ND Prefrontal/cerebral cortex/striatum
COX1 10–103; (–) ND ND Recombinant/ovine Polarography [68]
318; (NSC)* ND ND Recombinant/ovine Scintillation [69]
COX2 10–103; (–) ND ND Recombinant/human Polarography [68]
318; (NSC)* ND ND Recombinant/ovine Scintillation [69]
0.5mg/mouse/day for 23 days; (+) ND ND Tumor/ CD-1 nude mice Polarography
CYP2C19 10–2–10; (–) 2.51 0.793/50.800 Recombinant/ human HPLC/4'-OH-mephenytoin [57]
10–2–10; (–) 1.55 ND/1.26 Recombinant/human HPLC/5-OH-Omeprazole
10–2–10; (–) 1.79 ND/2.32 Recombinant/human FLUOstar OPTIMA‡/ fluorescein, BMG Labtech, Offenburg, Germany
CYP2D6 1–40; (–) 6.52 1.16 Recombinant/human FLUOstar OPTIMA‡/O-demethylated metabolite of AMMC [60]
1–40; (–) 6.01 2.69 Recombinant/human Measuring dextrome-thorphan O-demethylation
CYP3A4 0.1–50.0; (–) 11.7 1 Baculovirus-infected insect cells/human HPLC for N-desmethyl-diltiazem detection [63]
CYP3A5 0.1–50.0; (–) 1.65 0.195 Baculovirus-infected insect cells/human HPLC for N-desmethyl-diltiazem detection
CYP3A7 0.1–50.0; (–) 24.7 12.3 Baculovirus-infected insect cells/human HPLC for N-desmethyl-diltiazem detection
CYP2C9 0.1–10; (–)* 2.7 2.31 Recombinant/human HPLC/ 4-hydroxy-diclofenac [61]
0.1–10; (–)* 2.67 0.964 Recombinant/human HPLC/ 7-hydroxy-warfarin
CYP1A1 0.1–2.5; (–) 0.537 0.155 Recombinant/human FLUOstar OPTIMA for resorufin detection‡ [62, 70]
CYP1A2 1–10; (–) ~3.5* 2.69 Recombinant/human FLUOstar OPTIMA for resorufin detection‡ [62]
CYP1B1 1-–10; (–) ~5* 3.63 Recombinant/human FLUOstar OPTIMA for resorufin detection‡
DAGL-α 1–102; (NSC) ND ND COS-7 cells membrane/human Scintillation counting [14C]-oleic acid [71]
FAAH 1–102; (–)* 27.5 ND N18TG2 cell membrane/mouse Scintillation counting [14C]-ethanolamine [19]
1–50; (–) 15.2 ND Brain tissue membrane/rat Scintillation counting [14C]-ethanolamine [71]
0.5 mg/mouse/day for 23 days; (+) ND ND Tumor/ CD-1 nude mice [3H]-Arachidonic acid detection/RP-HPLC [68]
10–16; (+) ND ND U87 glioma cells [3H]-Arachidonic acid detection/RP-HPLC
Glutathione reductase 102; (+) ND ND Hepatic tissue/mouse [55]
GSH peroxidase 102; (+) ND ND Hepatic tissue/mouse
HMG-CoA Reductase 1–30; (+) ND ND Fibroblast/human [64]
IDO 0.1–10.0; (–) ND ND LPS stimulated-THP-1 cells/human HPLC/kynurenine–tryptophan [72]
LOX-5 2–200; (–) 73.73 ND LOX inhibitor screening assay kit (Cayman Chemical)† Hydroperoxides treated with chromogen spectrophotometry [73]
10–103; (NSC) ND ND Purified from barley Spectropho-tometric detection of hydroperoxides [68]
0.5mg/mouse/day for 23 days; (–) ND ND Tumor/ CD-1 nude mice Detection of arachidonic acid detection/RP-HPLC
LOX-15 0.2–10.0; (–) 2.56 ND LOX inhibitor screening assay kit (Cayman Chemical)† Hydroperoxides treated with chromogen spectropho-tometry [73]
10–103; (NSC) ND ND Purified from soybean Spectropho-tometric detection of hydroperoxi-des [68]
MAGL 1–102; (NSC) ND ND COS-7 cells homogenate/human Scintillation counting [3H]-glycerol [19]
N-acylethanolamine acid amide hydrolase 1–102; (-) >100 ND HEK293 cells membrane/human Scintillation counting [14C]-ethanolamine
NAD(P)H quinone reductase 102; (–) ND ND Hepatic tissue/mouse NADH-dependent reaction [55]
102; (–) ND ND Hepatic tissue/mouse NADPH-dependent reaction
NAPE-PLD 0.5 mg/mouse/day for 23 days; (NSC) ND ND Tumor/ CD-1 nude mice Assaying [3H]-anandamide formation [68]
Phosholipase A2 31.9–159.5; (+, –) 6.4/134.0 ND Naja naja venom Spectroscopy [74]
Progesterone 17α-hydroxylase 10–103; (–) ND ND Testis microsome/rat HPLC [75]
SOD 102; (–) ND ND Hepatic tissue/mouse [55]
Sphingomyelinase 16.00–63.60; (+)* ND ND Nieman pick Fibroblast/human HPLC, kratos detector and rainin Microsorb§ [76]
Testosterone 6α-hydroxylase 10–103; (–) ND ND Hepatic microsome/rat [75]
Testosterone 16β-hydroxylase 10–103; (–) ND ND Hepatic microsome/rat

ACAT = acyl-cholesterol acyltransferase; COX = cyclooxygenase; CYP = cytochrome P; DAGL = diacylglycerol lipase; FAAH = fatty acid amide hydrolase; GSH = Glutathione; HMG-CoA = 3-hydroxy-3-methylglutaryl-coenzyme A; IDO = indoleamine-2,3-dioxygenase; LOX = lipoxygenase; MAGL = monoacylglycerol lipase; NAPE-PLD = N-acyl-phosphatidyl-ethanolamine-selective phospholipase D; SOD = superoxide dismutase; NSC = no significant change; ND = not described; LPS = lipopolysaccharide; HEK = human embryonic kidney; TMPD = trimethyl pentanediol; HPLC = high-performance liquid chromatography; AMMC = 3-[2-(N,N-diethyl-N-methylammonium)-ethyl]-7-methoxy-4-methylcoumarin; RP-HPLC = reverse phase HPLC; NADH = nicotinamide adenine dinucleotide; NADPH = nicotinamide adenine dinucleotide phosphate; (+) = stimulation; (–) = inhibition

*Estimated from plots in cited paper

†Ann Arbor, MI, USA

§Agilent, Santa Clara, CA, USA