玫瑰树碱盐酸盐

中文名称:

玫瑰树碱盐酸盐

中文同义词:

玫瑰树碱盐酸盐;玫瑰树盐酸盐;ELLIPTICINE 盐酸盐

英文名称:

Ellipticine (hydrochloride)

英文同义词:

Ellipticine hydrochloride(NSC 71795 hydrochloride);NSC 71795 (hydrochloride)

CAS号:

5081-48-1

分子式:

C17H15ClN2

分子量:

282.77

EINECS号:

相关类别:

API

Mol文件:

5081-48-1.mol

储存条件 

Inert atmosphere,Store in freezer, under -20°C

生物活性

Ellipticine Hydrochloride (NSC 71795, PZE)是一种有效的 DNA topoisomerase II 的抑制剂，并通过其与 cytochromes P450 (CYP) 和 peroxidases 的氧化作用介导形成共价DNA加合物。Ellipticine Hydrochloride 是从澳大利亚的夹竹桃科常绿乔木中分离出来的具有抗肿瘤活性的天然产物。

靶点

Target Value P450 () peroxidase () Topo II ()

Target

Value

P450 ()

peroxidase ()

Topo II ()

体外研究

Ellipticine (NSC 71795) is a potent antineoplastic agent exhibiting the multimodal mechanism of its action. The mechanisms of Ellipticine (NSC 71795) antitumor, mutagenic and cytotoxic activities are suggested to be intercalation into DNA and inhibition of DNA topoisomerase II activity. Another mode of Ellipticine (NSC 71795) action is the formation of covalent DNA adducts mediated by its oxidation with cytochromes P450 (CYP) and peroxidases. Ellipticine (NSC 71795) can also act as an inhibitor or inducer of biotransformation enzymes, thereby modulating its own metabolism leading to its genotoxic and pharmacological effects. Treatment of cells with Ellipticine (NSC 71795) results in inhibition of cell growth and proliferation. This effect is associated with formation of two covalent Ellipticine (NSC 71795)-derived DNA adducts.

体内研究

Ellipticine (NSC 71795) treatment results in ellipticine-derived DNA adduct generation in several healthy organs (liver, kidney, lung, spleen, breast, heart and brain) and in DNA of mammary adenocarcinoma. The levels of Ellipticine (NSC 71795)-derived DNA adducts generated in these adenocarcinomas are almost 2-fold higher than in normal healthy mammary tissue. The induced expression of cytochrome b 5 protein in liver of rats treated with Ellipticine (NSC 71795) suggests that cytochrome b 5 may modulate the CYP-mediated bioactivation and detoxification of Ellipticine (NSC 71795).