Ellipticine hydrochloride

产品编号: T4614 别名:

NSC 71795 (hydrochloride),玫瑰树碱盐酸盐,Ellipticine HCl

Ellipticine hydrochloride 是一种有效的抗肿瘤剂，抑制 DNA 拓扑异构酶 II 的活性。

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Ellipticine hydrochloride Chemical Structure

CAS：5081-48-1

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生物活性化学信息储存和溶解度信息参考文献引用文献

产品描述

Ellipticine hydrochloride is a potent antineoplastic agent; inhibits DNA topoisomerase II activities.

体外活性

Ellipticine is a potent antineoplastic agent exhibiting the multimodal mechanism of its action. The mechanisms of ellipticine antitumor, mutagenic and cytotoxic activities are suggested to be intercalation into DNA and inhibition of DNA topoisomerase II activity. Another mode of ellipticine action is the formation of covalent DNA adducts mediated by its oxidation with cytochromes P450 (CYP) and peroxidases[1]. Ellipticine 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 results in inhibition of cell growth and proliferation. This effect is associated with formation of two covalent ellipticine-derived DNA adducts[2].

体内活性

Ellipticine 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-derived DNA adducts generated in these adenocarcinomas are almost 2-fold higher than in normal healthy mammary tissue. The induced expression of cytochrome b5?protein in liver of rats treated with ellipticine suggests that cytochrome b5?may modulate the CYP-mediated bioactivation and detoxification of ellipticine[3].

细胞实验

The cytotoxicity of ellipticine is determined by MTT test. Ellipticine is dissolved in DMSO (1 mM) and diluted in culture medium to final concentrations of 0, 0.1, 1, 5 or 10 μM. Cells in exponential growth are seeded at 1×104 per well in a 96-well microplate. After incubation the MTT solution is added, the microplates are incubated for 4 hours and cells lysed in 50% N,N-dimethylformamide containing 20% of sodium dodecyl sulfate (SDS), pH 4.5. The absorbance at 570 nm is measured. The mean absorbance of medium controls is subtracted as a background. The viability of control cells is taken as 100% and the values of treated cells are calculated as a percentage of control. The IC50 values are calculated using linear regression of the dose-log response curves[2] .

Cas No.

5081-48-1

分子式

C17H15ClN2

分子量

282.77

别名

NSC 71795 (hydrochloride);玫瑰树碱盐酸盐;Ellipticine HCl;Ellipticine hydrochloride

参考文献

[1]Stiborova M, et al. Ellipticine cytotoxicity to cancer cell lines - a comparative study. Interdiscip Toxicol. 2011 Jun;4(2):98-105.[2]Stiborova M, et al. Molecular mechanisms of antineoplastic action of an anticancer drug ellipticine. Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2006 Jul;150(1):13-23.[3]Wang W, Shu M, Nie A, et al. Ultrasensitive evaluation of Ribonuclease H activity using a DNAzyme-powered on-particle DNA walker[J]. Sensors and Actuators B: Chemical. 2020, 304: 127380.[4]Stiborova M, et al. The anticancer drug ellipticine activated with cytochrome P450 mediates DNA damage determining its pharmacological efficiencies: studies with rats, Hepatic Cytochrome P450 Reductase Null (HRN™) mice and pure enzymes. Int J Mol Sci. 2014 Dec 25;16(1):284-306.

引用文献

[1]Wang W, Shu M, Nie A, et al. Ultrasensitive evaluation of Ribonuclease H activity using a DNAzyme-powered on-particle DNA walker. Sensors and Actuators B: Chemical. 2020, 304: 127380 [2]Li X, Ye C, Mulati M, et al. Ellipticine blocks synergistic effects of IL-17A and TNF-α in epithelial cells and alleviates severe acute pancreatitis-associated acute lung injury. Biochemical Pharmacology. 2020: 113992.

储存和溶解度

DMSO:5.8 mg/mL (20.51 mM)),Need ultrasonic and warming
Powder: -20°C for 3 years
In solvent: -80°C for 2 years

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Keywords

Inhibitor NSC 71795 (hydrochloride) Ellipticine hydrochloride 玫瑰树碱盐酸盐 Ellipticine NSC71795 NSC 71795 NSC-71795 Topoisomerase Ellipticine HCl inhibit 5081-48-1

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Ellipticine hydrochloride

NSC 71795 (hydrochloride),玫瑰树碱盐酸盐,Ellipticine HCl

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