光辉霉素

中文名称:

光辉霉素

中文同义词:

光辉霉素;光辉霉素 A 来源于褶皱链霉菌;普卡霉素(光辉霉素);光神霉素、金霉酸、光辉霉素;普卡酶素, BC;光神霉素A;光辉酶素,光神霉素,普芳拉星,金霉酸;光神霉素,光辉霉素A

英文名称:

MITHRAMYCIN A

英文同义词:

AUREOLIC ACID;METHRAMYCIN A;MITHRAMYCIN A, FOR FLUORESCENCE;MITHRAMYCIN A FROM STREPTOMYCES*PLICATUS APPROX. 96;MITHRAMYCIN COMPLEX FROM STREPTOMYCES*PL ICATUS;MITHRAMYCIN FROM STREPTOMYCES PLICATUS;MITHRACIN;MITHRAMYCIN

CAS号:

18378-89-7

分子式:

C52H76O24

分子量:

1085.15

EINECS号:

634-048-4

相关类别:

医药原料药;抗生素类;抗生素、生物碱;抗生素及抗病毒;生化试剂;抗生素;微生物代谢物;医药原料;antibiotic;Antibiotics;Antitumour

Mol文件:

18378-89-7.mol

熔点 

180-183 °C

比旋光度 

D20 -51° (c = 0.4 in ethanol)

沸点 

761.72°C (rough estimate)

密度 

1.1576 (rough estimate)

折射率 

1.6500 (estimate)

储存条件 

2-8°C

酸度系数(pKa)

4.54±0.60(Predicted)

形态

Powder

颜色

Red to brown

Merck 

13,7619

BRN 

5236667

EPA化学物质信息

Plicamycin (18378-89-7)

生物活性

Plicamycin 是一种选择性特 Sp1 转录因子抑制剂。Plicamycin 通过降低 Sp1 蛋白表达来抑制癌细胞生长。

靶点

Sp1 transcription factor

体外研究

Sp1 is a zinc-finger transcription factor that regulates multiple cellular functions and promotes tumor progression by controlling expression of genes involved in cell cycle, apoptosis and DNA damage. Sp1 binds to GC-rich motifs of promoters and interacts with components of the general transcriptional machinery and co-activator complexes of multiple signaling pathways. Plicamycin (Mith) decreases Sp1 protein by inducing proteasome-dependent degradation, thereby suppressing cervical cancer growth through a DR5/caspase-8/Bid signaling pathway. To assess the antiproliferative effects of Plicamycin on cervical cancer cells, two cervical cancer cell lines with different genetic backgrounds are grown with or without treatment with Plicamycin at different concentrations. Plicamycin inhibits HEp-2 and KB cell growth in a concentration-dependent manner after 48 h. Apoptotic cell death is qualitatively estimated by DAPI staining for nuclear condensation and fragmentation. Plicamycin leads to significant DNA fragmentation compared to untreated controls.

体内研究

The antitumorigenic activity of Plicamycin (0.2 mg/kg/day) is determined in a xenograft model and observed reduction in tumor volume and weight. No significant mouse body weight loss is observed in Plicamycin-treatment groups, indicating that Plicamycin-associated toxicity is minimal. Plicamycin also increases TUNEL-positive cells in tumor xenografts. No notable intergroup differences are observed among organs, indicating no marked signs of systemic toxicity at the Plicamycin dose used in this study.

用途 

抗癌抗生素，对多种动物肿瘤有较强的抑制作用，其作用机理是与DNA结合，抑制转录和蛋白合成，抑制RNA的合成，作用于细胞增殖各期。在MDR表现形中是Pgp的底物。 在流式细胞计中用于荧光染色DNA。适合于检测DNA。

危险品标志 

Xn,T+

危险类别码 

22-26/27/28

安全说明 

45-38-36/37/39-28A-22

危险品运输编号 

3249

WGK Germany 

3

RTECS号

PZ2800000

F 

10

HazardClass 

6.1(b)

PackingGroup 

III

海关编码 

29419090

毒性

LD50 in mice, rats (mg/kg): 2.14, 1.74 i.v. (Slavik, Carter)