Imperatorin

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Chemical Structure| 482-44-0 同义名 : Ammidin; Marmelosin; NSC 402949; 8-Isopentenyloxypsoralene; 8-Isoamylenoxypsoralen; Pentosalen
CAS号 : 482-44-0
货号 : A118402
分子式 : C16H14O4
纯度 : 97%
分子量 : 270.28
MDL号 : MFCD00016881
存储条件:

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Imperatorin is an effective of NO synthesis inhibitor (IC50=9.2 μmol), which also is a BChE inhibitor (IC50=31.4 μmol). Imperatorin is a weak agonist of TRPV1 with EC50 of 12.6±3.2 μM[3]. Imperatorin can activate RUNX2, COL1A1 and osteocalcin by promoting the Ser9 phosphorylation of GSK3β and entry of β-catenin into the nucleus. Intragastric administration of imperatorin promoted osteogenesis and inhibited osteoclast in vivoYan DY, Tang J, Chen L, Wang B, Weng S, Xie Z, Wu ZY, Shen Z, Bai B, Yang L. Imperatorin promotes osteogenesis and suppresses osteoclast by activating AKT/GSK3 β/β-catenin pathways. J Cell Mol Med. 2020 Feb;24(3):2330-2341|https://pubmed.ncbi.nlm.nih.gov/31883297Yan DY, Tang J, Chen L, Wang B, Weng S, Xie Z, Wu ZY, Shen Z, Bai B, Yang L. Imperatorin promotes osteogenesis and suppresses osteoclast by activating AKT/GSK3 β/β-catenin pathways. J Cell Mol Med. 2020 Feb;24(3):2330-2341|https://pubmed.ncbi.nlm.nih.gov/31883297. Imperatorin is a weak agonist of TRPV1, a channel implicated in detecting several noxious stimuli, exhibiting a 50% effective concentration (EC50) of 12.6 ± 3.2 μM[4]. Imperatorin administered acutely at the doses of 5 and 10 mg/kg prior to the injection of scopolamine (1 mg/kg) improved memory acquisition and consolidation impaired by scopolamine. Furthermore, repeatable (7 days, twice daily) administration of the highest dose of imperatorin (10 mg/kg) significantly attenuated the effects of scopolamine on memory acquisition, whereas the doses of 5 and 10 mg/kg of this furanocoumarin were effective when memory consolidation was measured. Imperatorin, administered with scopolamine, increased antioxidant enzymes activity and decreased concentration of malondiamide, an indicator of lipid peroxidation level[5]. Imperatorin inhibited HIF-1α (hypoxia-inducible factor-1) protein synthesis by downregulating the mTOR/p70S6K(ribosomal protein S6 kinase)/4E-BP1 (eIF4E binding protein-1) and MAPK pathways[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.70mL

0.74mL

0.37mL

18.50mL

3.70mL

1.85mL

37.00mL

7.40mL

3.70mL

参考文献

[1]Koziol E, Skalicka-Wozniak K. Imperatorin-pharmacological meaning and analytical clues: profound investigation. Phytochem Rev. 2016;15:627-649.

[2]Kleiner HE, Vulimiri SV, et al. Oral administration of the citrus coumarin, isopimpinellin, blocks DNA adduct formation and skin tumor initiation by 7,12-dimethylbenz[a] anthracene in SENCAR mice. Carcinogenesis. 2002 Oct;23(10):1667-75.

[3]Kozioł E, Skalicka-Woźniak K. Imperatorin-pharmacological meaning and analytical clues: profound investigation. Phytochem Rev. 2016;15:627-649

[4]Chen X, Sun W, Gianaris NG, Riley AM, Cummins TR, Fehrenbacher JC, Obukhov AG. Furanocoumarins are a novel class of modulators for the transient receptor potential vanilloid type 1 (TRPV1) channel. J Biol Chem. 2014 Apr 4;289(14):9600-10

[5]Budzynska B, Boguszewska-Czubara A, Kruk-Slomka M, Skalicka-Wozniak K, Michalak A, Musik I, Biala G. Effects of imperatorin on scopolamine-induced cognitive impairment and oxidative stress in mice. Psychopharmacology (Berl). 2015 Mar;232(5):931-42

[6]Mi C, Ma J, Wang KS, Zuo HX, Wang Z, Li MY, Piao LX, Xu GH, Li X, Quan ZS, Jin X. Imperatorin suppresses proliferation and angiogenesis of human colon cancer cell by targeting HIF-1α via the mTOR/p70S6K/4E-BP1 and MAPK pathways. J Ethnopharmacol. 2017 May 5;203:27-38