| 名稱 | 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) |
| 細胞實驗 | 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]. |
| 動物實驗 | 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]. |
| 體外活性 | Cedrol在100 μg/ml的濃度下抑制L. sulphureus、G. trabeum、L. betulina和T. versicolor這些木材腐朽真菌的生長[1]。同時，Cedrol還能抑制細胞色素P450 (CYP) 的同型酶CYP2B6和CYP3A4，其半抑制濃度(Kis)分別為0.9和3.4 μM[2]。 |
| 體內(nèi)活性 | 在體內(nèi)，cedrol（200 mg/kg）通過抑制由環(huán)磷酰胺引發(fā)的小鼠脫發(fā)模型中的毛囊萎縮，減少脫發(fā)現(xiàn)象[3]。 |
| 存儲條件 | 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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| 關(guān)鍵字 | α-Cedrol | inhibit | Fungal | Cedrol | (+)-Cedrol | CYPs | Cytochrome P450 | Inhibitor |
| 相關(guān)產(chǎn)品 | Naringin | 2-Butyl-1,2-benzisothiazolin-3-one | Potassium gluconate | Dehydroacetic acid sodium | Geraniol | Paclobutrazol | Veratraldehyde | Lauryl betaine | Methyl 2-amino-5-bromobenzoate | Chlorobutanol hemihydrate | Naringenin | Chitosan (MW 150000) |
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