| Description | Cedrol is a cedrane sesquiterpenoid and a tertiary alcohol,Cedrol inhibits the cytochrome P450 (CYP) isoforms CYP2B6 and CYP3A4 (Kis = 0.9 and 3.4 μM, respectively) |
| In vitro | Cedrol inhibits the growth of L. sulphureus, G. trabeum, L. betulina, and T. versicolor wood decay fungi when used at a concentration of 100 μg/ml[1].Cedrol inhibits the cytochrome P450 (CYP) isoforms CYP2B6 and CYP3A4 (Kis = 0.9 and 3.4 μM, respectively)[2]. |
| In vivo | In vivo, cedrol (200 mg/kg) prevents hair follicle dystrophy and reduces hair loss in a mouse model of alopecia induced by cyclophosphamide[3] |
| Cell experiments | The inhibitory potencies (IC50 values) of β-cedrene, cedrol, thujopsene, and a CYP2B6 inhibitor, thioTEPA, of CYP2B6- catalyzed bupropion hydroxylase activity were evaluated in pooled human liver microsomes and cDNA-expressed CYP2B6 using LCMS/MS.?Incubation mixtures were prepared in a total volume of 100 μl, including 1 mM NADPH, 10 mM MgCl2, 50 mM potassium phosphate buffer (pH 7.4), various concentrations of β-cedrene, cedrol, thujopsene, or thioTEPA, pooled human liver microsomes (0.2 mg/ml) or human cDNA-expressed CYP2B6 (0.4 pmol), and a CYP2B6-selective substrate 50 μM bupropion.?After a 3-min preincubation at 37℃, the reactions were initiated by adding NADPH and were incubated for 15 min at 37 C in a shaking water bath.?The reaction was terminated by placing tubes on ice and adding 100 μl icecold d9-1 -hydroxybufuralol (internal standard) in methanol.?Incubation mixtures were then centrifuged at 13,000×g for 4 min at 4℃.?All incubations were performed in triplicate, and average values were used.?To evaluate NADPH-dependent mechanism-based inhibition, various concentrations of β-cedrene, cedrol, thujopsene, and thioTEPA were preincubated for 30 min with pooled human liver microsomes in the presence of NADPH.?The reaction was started by bupropion addition[2]. |
| Animal experiments | Acute toxicity, skin irritation and skin sensitization tests of cedrol were conducted before the experiment, which suggested that cedrol had hardly toxic and side effects.Three different doses of cedrol prepared in 85% ethanol were spread on the dorsal skin of mice 2 days after depilation for several consecutive days until the mice were all sacrificed under an ether atmosphere to evaluate whether topical treatment with cedrol may prevent or alleviate CYP-induced alopecia[3]. |
| Target activity | CYP3A4:0.9μM(ki), CYP2B6:3.4 Μm(ki) |
| molecular weight | 222.37 |
| Molecular formula | C15H26O |
| CAS | 77-53-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 44 mg/mL (197.86 mM) |
| References | 1. CHENG, SenSung, CHUNG, et al. Phytochemicals from Cunninghamia konishii Hayata Act as Antifungal Agents[J]. Journal of Agricultural & Food Chemistry, 2012, 60(1):124-8. 2. Jeong H U , Kwon S S , Kong T Y , et al. Inhibitory Effects of Cedrol, β-Cedrene, and Thujopsene on Cytochrome P450 Enzyme Activities in Human Liver Microsomes[J]. Journal of Toxicology and Environmental Health, Part A, 2014, 77(22-24):1522-1532. 3. Chen S S , Zhang Y , Lu Q L , et al. Preventive effects of cedrol against alopecia in cyclophosphamide-treated mice[J]. Environ Toxicol Pharmacol, 2016, 46:270-276. |