2-Hydroxyestrone(Synonyms: Catecholestrone)

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2-Hydroxyestrone (Synonyms: Catecholestrone)

2-Hydroxyestrone (Catecholestrone) 是一种特异性受体介导的抗雌激素剂。2-Hydroxyestrone 具有抗癌作用。

2-Hydroxyestrone(Synonyms: Catecholestrone)

2-Hydroxyestrone Chemical Structure

CAS No. : 362-06-1

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生物活性

2-Hydroxyestrone (Catecholestrone) is a specific receptor-mediated antiestrogenic agent. 2-Hydroxyestrone is anticarcinogenic[1][2].

IC50 & Target[1]

Human Endogenous Metabolite

 

Estrogen receptor

 

体外研究
(In Vitro)

2-Hydroxyestrone exhibits antiestrogen action on MCF-7 human breast cancer cells. Addition of 2-Hydroxyestrone to the cell cultures in concentration of 1-1000 nM has no effect on cell growth and proliferation because of rapid O-methylation of the catechol estrogen by catechol O-methyltransferase which is highly active in these cells. In the presence of quinalizarin, a potent catechol O-methyltransferase inhibitor which reduces the O-methylation of the steroid, 10 and 100 nM 2-Hydroxyestrone markedly suppresses the growth and proliferation of the cells[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[2]

Cell Line: Human breast cancer cell lines MCF-7, MDA-MB-231, and MDA-MB-330
Concentration: 1-1000 nM
Incubation Time: 6 days
Result: 10 and 100 nM markedly suppressed the growth and proliferation of the cells in the presence of quinalizarin. The tumor cell growth-inhibitory action of the catechol estrogen was neutralized by the presence of 1 nM estradiol.

体内研究
(In Vivo)

Levels of both 2-Hydroxyestrone (2-OHE1; 2 mg/kg; administered ip.) and  2-Hydroxyestrone 4-N-acetylcysteine thioether (2-OHE1 4SR) in rats treated with 2-Hydroxyestrone were significantly different between the induced and noninduced groups[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female and male Sprague-Dawley rats (6 weeks old)[3]
Dosage: 2 mg/kg
Administration: Administered i.p.
Result: Levels of both 2-OHE1 and  2-OHE1 4SR in rats treated with 2-OHE1 were significantly different between the induced and noninduced groups.

分子量

286.37

Formula

C18H22O3
CAS 号

362-06-1
中文名称

2-羟雌甾酮
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
溶解性数据
In Vivo:
  • 1.

    2-Hydroxyestrone is suspended in corn oil by sonication[3].
参考文献

  • [1]. H L Bradlow, et al. 2-Hydroxyestrone: the ‘good’ estrogen. J Endocrinol. 1996 Sep;150 Suppl:S259-65.

    [2]. J Schneider, et al. Antiestrogen action of 2-Hydroxyestrone on MCF-7 human breast cancer cells. J Biol Chem. 1984 Apr 25;259(8):4840-5.

    [3]. M Nakagomi, et al. Quantitation of catechol estrogens and their N-acetylcysteine conjugates in urine of rats and hamsters. Chem Res Toxicol. 2000 Dec;13(12):1208-13.

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