产品说明书

Bergaptol

Print
Chemical Structure| 486-60-2 同义名 : 5-Hydroxypsoralen;4-Hydroxybergapten;Psoralin, 5-hydroxy-;5-Hydroxyfuranocoumarin
CAS号 : 486-60-2
货号 : A133600
分子式 : C11H6O4
纯度 : 98%
分子量 : 202.163
MDL号 : MFCD00210479
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(247.33 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Bergaptol is a hydroxylated psoralen that acts as a potent inhibitors of debenzylation activity of CYP3A4 enzyme with an IC50 value of 24.92 uM[3]. Bergaptol specifically inhibited VBL (vinblastine) efflux[4]. BER (Bergaptol) treatment significantly inhibited LPS-induced production of nitric oxide (NO), interleukin-6 (IL-6), and tumor necrosis factor-α (TNF-α), and gene expression of inducible nitric oxide synthase (iNOS), IL-6, TNF-α, interleukin-1 beta (IL-1β) and cyclooxygenase-2 (COX-2). BER also potently blocked LPS-induced mitogen-activated protein kinase (MAPK) phosphorylation and nuclear factor-kappa B (NF-κB) activation, as evidenced by the inhibitory effects on c-Jun N-terminal kinase (JNK), P38, P65, IκBα and IκKα/β phosphorylation, and NF-κB nuclear translocation. Furthermore, BER treatment markedly mitigated ox-LDL-induced foam cell formation by inhibiting scavenger receptor class A type I (SRA1) and cluster of differentiation 36 (CD36)-dependent cholesterol uptake[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.95mL

0.99mL

0.49mL

24.73mL

4.95mL

2.47mL

49.47mL

9.89mL

4.95mL
参考文献

[1]Girennavar B, Jayaprakasha GK, et al. Radical scavenging and cytochrome P450 3A4 inhibitory activity of bergaptol and geranylcoumarin from grapefruit. Bioorg Med Chem. 2007 Jun 1;15(11):3684-91.

[2]bou Elzahab M. Photooxygenation of some potentially skin-photosensitizing hydroxyfurocoumarins. Part 2: Xanthotoxol and bergaptol. Pharmazie. 1993 Feb;48(2):144-5.

[3]Girennavar B, Jayaprakasha GK, Jadegoud Y, Nagana Gowda GA, Patil BS. Radical scavenging and cytochrome P450 3A4 inhibitory activity of bergaptol and geranylcoumarin from grapefruit. Bioorg Med Chem. 2007 Jun 1;15(11):3684-91

[4]Ohnishi A, Matsuo H, Yamada S, Takanaga H, Morimoto S, Shoyama Y, Ohtani H, Sawada Y. Effect of furanocoumarin derivatives in grapefruit juice on the uptake of vinblastine by Caco-2 cells and on the activity of cytochrome P450 3A4. Br J Pharmacol. 2000 Jul;130(6):1369-77

[5]Shen CY, Wang TX, Jiang JG, Huang CL, Zhu W. Bergaptol from blossoms of Citrus aurantium L. var. amara Engl inhibits LPS-induced inflammatory responses and ox-LDL-induced lipid deposition. Food Funct. 2020 Jun 24;11(6):4915-4926