| 名称 | Cedrol |
| 描述 | 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) |
| 细胞实验 | 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]. |
| 动物实验 | 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]. |
| 体外活性 | Cedrol在100 μg/ml的浓度下抑制L. sulphureus、G. trabeum、L. betulina和T. versicolor这些木材腐朽真菌的生长[1]。同时，Cedrol还能抑制细胞色素P450 (CYP) 的同型酶CYP2B6和CYP3A4，其半抑制浓度(Kis)分别为0.9和3.4 μM[2]。 |
| 体内活性 | 在体内，cedrol（200 mg/kg）通过抑制由环磷酰胺引发的小鼠脱发模型中的毛囊萎缩，减少脱发现象[3]。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 45 mg/mL (202.37 mM), Sonication is recommended.
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| 关键字 | α-Cedrol | inhibit | Fungal | Cedrol | (+)-Cedrol | CYPs | Cytochrome P450 | Inhibitor |
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