柏木脑 T5594

Product Introduction
Bioactivity


英文名: Cedrol

描述: Cedrol 是一种雪松烷倍半萜类叔醇，抑制细胞色素 P450 (CYP) 异构体 CYP2B6 和 CYP3A4，Kis 分别为 0.9 和 3.4 μM，具有抗炎，抗脓毒，抗痉挛，滋补，收敛，利尿，杀虫和抗真菌活性。

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 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].

体内活性: In vivo, cedrol (200 mg/kg) prevents hair follicle dystrophy and reduces hair loss in a mouse model of alopecia induced by cyclophosphamide[3]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 44 mg/mL (197.86 mM)


关键字: α-Cedrol | inhibit | Fungal | Cedrol | (+)-Cedrol | CYPs | Cytochrome P450 | Inhibitor

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相关库: Marine Natural Product Library | Tobacco Monomer Library | Macrocyclic Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Traditional Chinese Medicine Monomer Library | Miao medicine Compound Library | Food as Medicine Compound Library | Microbial Natural Product Library | Antiparasitic Natural Product Library

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