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Arbutin

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Chemical Structure| 497-76-7 同义名 : β-Arbutin;NSC 4036;Uvasol;Ursin;HSDB 7661;CCRIS 9273;BRN 0089673;Arbutyne;Arbutoside
CAS号 : 497-76-7
货号 : A309050
分子式 : C12H16O7
纯度 : 98%
分子量 : 272.251
MDL号 : MFCD00016915
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(183.65 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

H2O: 30 mg/mL(110.19 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • tyrosinase

    tyrosinase, IC50:1.09 mM
描述 Arbutin is a competitive inhibitor of tyrosinase in melanocytes, with Kiapp values of 1.42 mM for monophenolase; 0.9 mM for diphenolase. Arbutin is also used as depigmenting agents[3]. Arbutin inhibited the tyrosinase activity of cultured human melanocytes at noncytotoxic concentrations. It did not affect the expression of tyrosinase mRNA[4]. Arbutin (0.3-5.4 mM; 24 hours, 48 hours, 72 hours; B16 murine melanoma cells) inhibites the viability of B16 murine melanoma cells in a time-and dose-dependent manner. Arbutin (1.4-5.4 mM; 24 hours) increases the apoptosis rate of B16 murine melanoma cell of treatment at a dose of 5.4 mM[5]. Arbutin inhibits OS (osteosarcoma) cell proliferation, migration and invasion via miR-338-3p/MTHFD1L and by inactivating the AKT(phosphorylated-protein kinase B)/mTOR (phosphorylated-mammalian target of rapamycin) pathway[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02945891 Cervical Cancer Not Applicable Active, not recruiting December 2018 Norway ... 展开 >> Ostfold Hospital Trust Fredrikstad, Norway Oslo University Hospital, Molecular Pathology Oslo, Norway Oslo University Hospital, Ullevål Oslo, Norway Radiumhospital Oslo, Norway 收起 <<
NCT00781625 Urinary Tract Infections Not Applicable Unknown December 2010 Norway ... 展开 >> Akershus Universitetssykehus HF Recruiting Lørenskog, Akershus, Norway, 1478 Contact: Caroline U Skagemo, MD    +47 02900111    cask@ahus.no    Contact: Gunn Iren Meling, PhD, MD    +47 02900 111    gmel@ahus.no    Principal Investigator: Caroline U Skagemo, MD          St.Olavs Hospital Active, not recruiting Trondheim, Norway, 7006 收起 <<
NCT02130713 Chronic Bacterial Prostatitis Phase 4 Completed - Italy ... 展开 >> policlinico Umberto I - Department of Gynecological-Obstetrics Sciences and Urological Sciences Roma, Italy, 00161 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.67mL

0.73mL

0.37mL

18.37mL

3.67mL

1.84mL

36.73mL

7.35mL

3.67mL
参考文献

[1]Tada M, Kohno M, Niwano Y. Alleviation effect of arbutin on oxidative stress generated through tyrosinase reaction with L-tyrosine and L-DOPA. BMC Biochem. 2014 Oct 9;15:23.

[2]Lee HJ, Kim KW. Anti-inflammatory effects of arbutin in lipopolysaccharide-stimulated BV2 microglial cells. Inflamm Res. 2012 Aug;61(8):817-25.

[3]Garcia-Jimenez A, Teruel-Puche JA, Berna J, Rodriguez-Lopez JN, Tudela J, Garcia-Canovas F. Action of tyrosinase on alpha and beta-arbutin: A kinetic study. PLoS One. 2017 May 11;12(5):e0177330

[4]Maeda K, Fukuda M. Arbutin: mechanism of its depigmenting action in human melanocyte culture. J Pharmacol Exp Ther. 1996 Feb;276(2):765-9

[5]Jiang L, Wang D, Zhang Y, Li J, Wu Z, Wang Z, Wang D. Investigation of the pro-apoptotic effects of arbutin and its acetylated derivative on murine melanoma cells. Int J Mol Med. 2018 Feb;41(2):1048-1054

[6]Wang CQ, Wang XM, Li BL, Zhang YM, Wang L. Arbutin suppresses osteosarcoma progression via miR-338-3p/MTHFD1L and inactivation of the AKT/mTOR pathway. FEBS Open Bio. 2021 Jan;11(1):289-299