9-Hydroxyellipticine hydrochloride

9-Hydroxyellipticine hydrochloride用途

9-Hydroxyellipticine hydrochloride 是 Topo II 和RyR 的抑制剂。9-Hydroxyellipticine hydrochloride 具有抗肿瘤、抗氧化和释放儿茶酚胺的活性。 9-Hydroxyellipticine hydrochloride 对 Hela S-3 和293T 细胞的IC50 值分别为1.6 μM 和1.2μM。

9-Hydroxyellipticine hydrochloride名称

[ CAS 号 ]:
52238-35-4

[ 中文名 ]:
9-羟基玫瑰树碱盐酸盐

[ 英文名 ]:
9-Hydroxyellipticine hydrochloride

[英文别名 ]:

Ellipticine,hydrochloride
ELLIPTICINE ANALOG
9-HE,HCl
9-Hydroxyellipticine HCl
9 OHE HCl

9-Hydroxyellipticine hydrochloride生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

研究领域 >> 心血管疾病

信号通路 >> 细胞周期/DNA损伤 >> 拓扑异构酶

[ 靶点 ]

Topoisomerase II

[体外研究]

9-羟基磷灰石(9HE)在0.1~100μM范围内以浓度依赖的方式选择性抑制Lewis肺癌和SW480(人结肠癌细胞系)p53蛋白磷酸化[4]。

[体内研究]

9-羟基磷灰石(5或10 mg/kg,ip)导致小鼠骨髓细胞染色体聚集和姐妹染色单体交换[1]。动物模型：3～5月龄C57B1/6雄性小鼠[1]。剂量：5或10 mg/kg。管理：IP。结果：导致小鼠骨髓细胞染色体聚集、染色单体畸变和微核形成。

[参考文献]

[1]. Renault G, et al. In vivo exposure to four ellipticine derivatives with topoisomerase inhibitory activity results in chromosome clumping and sister chromatid exchange in murine bone marrow cells. Toxicol Appl Pharmacol. 1987 Jun 30;89(2):281-6.

[2]. Saeki K, et al. Cardioprotective effects of 9-hydroxyellipticine on ischemia and reperfusion in isolated rat heart. Jpn J Pharmacol. 2002 May;89(1):21-8.

[3]. Naoya Sato, et al. Synthesis and in vitro Antitumor Activity of 9-Hydroxyellipticine Derivatives with Glucose Conjugation via Triazolylmethyl Succinate Linker. Heterocycle, Vol. 92, NO 4, 2016.

[4]. Ohashi M, et al. Inhibition of p53 protein phosphorylation by 9-hydroxyellipticine: a possible anticancer mechanism. Jpn J Cancer Res. 1995 Sep;86(9):819-27.

9-Hydroxyellipticine hydrochloride物理化学性质

[ 密度 ]:
1.349g/cm3

[ 沸点 ]:
557.7ºC at 760mmHg

[ 分子式 ]:
C₁₇H₁₅ClN₂O

[ 分子量 ]:
298.76700

[ 闪点 ]:
291.1ºC

[ 精确质量 ]:
298.08700

[ PSA ]:
48.91000

[ LogP ]:
4.99370

[ 储存条件 ]:
-20°C，密封，干燥

9-Hydroxyellipticine hydrochloride

9-Hydroxyellipticine hydrochloride用途

9-Hydroxyellipticine hydrochloride名称

9-Hydroxyellipticine hydrochloride生物活性

9-Hydroxyellipticine hydrochloride物理化学性质

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