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光辉霉素

光辉霉素用途

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。

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光辉霉素名称

[ CAS 号 ]:
18378-89-7

[ 中文名 ]:
光辉霉素

[ 英文名 ]:
Mithramycin A

[中文别名 ]:

[英文别名 ]:

Antibiotic LA-7017
aurlelicacid
MFCD00135618
EINECS 232-455-8
MITHRAMYCIN
Mithramycin A From Streptomyces Argillaceus
aurelicacid
PlicatoMycin
a-2371
mitramycin

光辉霉素生物活性

[ 描述 ]:

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。

[ 相关类别 ]:

信号通路 >> 细胞周期/DNA损伤 >> DNA/RNA合成

研究领域 >> 癌症

[ 靶点 ]

Sp1 transcription factor[1]

[体外研究]

Sp1是锌指转录因子,其通过控制参与细胞周期,细胞凋亡和DNA损伤的基因的表达来调节多种细胞功能并促进肿瘤进展。 Sp1与启动子的富含GC的基序结合,并与一般转录机制的组分和多种信号传导途径的共激活因子复合物相互作用。 Plicamycin(Mith)通过诱导蛋白酶体依赖性降解来降低Sp1蛋白,从而通过DR5/caspase-8/Bid信号通路抑制宫颈癌生长。为了评估普利霉素对宫颈癌细胞的抗增殖作用,在不同浓度的普利霉素处理或不处理的情况下培养具有不同遗传背景的两种宫颈癌细胞系。 48小时后,Plicamycin以浓度依赖性方式抑制HEp-2和KB细胞生长。通过DAPI染色对核浓缩和片段化定性估计凋亡细胞死亡。与未处理的对照相比,Plicamycin导致显着的DNA片段化[1]。

[体内研究]

在异种移植模型中测定Plicamycin的抗肿瘤活性(0.2mg/kg /天)并观察肿瘤体积和重量的减少。在Plicamycin处理组中未观察到显着的小鼠体重减轻,表明Plicamycin相关的毒性是最小的。 Plicamycin还增加肿瘤异种移植物中的TUNEL阳性细胞。在器官中没有观察到显着的组间差异,表明本研究中使用的Plicamycin剂量没有明显的全身毒性迹象[1]。

[细胞实验]

HEp-2细胞和KB细胞在100μl/ ml的青霉素和链霉素和10％FBS的DMEM中培养，用于HEp-2细胞，5％FBS用于KB，在含有5％CO 2的潮湿气氛中于37℃培养。接种相同数量的细胞并使其附着。在50-60％汇合时，用DMSO或指定浓度的Plicamycin处理细胞（对于HEp-2细胞为50,100和200nM;对于KB细胞为20,40和80nM）。使用CellTiter 96 Aqueous One Solution Cell Proliferation Assay Kits测定细胞活力。简而言之，将细胞接种在96孔板中并与Plicamycin一起孵育。处理后，向每个孔中加入30μLMTS溶液，并将细胞在37℃下孵育2小时。使用酶标仪在490nm和690nm处分析MTS溶液[1]。

[动物实验]

小鼠[1]使用雌性裸鼠。将KB细胞悬浮在无菌PBS中并皮下注射到小鼠的右侧腹中。将小鼠随机分成两组，每组含有5只小鼠，每周三次用0.2mg / kg /天的Plicamycin（ip）处理29天。对照小鼠接受相同体积的载体。 29天后，称重身体，器官和肿瘤并确定肿瘤体积。测量肿瘤[1]。

[参考文献]

[1]. Choi ES, et al. Modulation of specificity protein 1 by mithramycin A as a novel therapeutic strategy for cervical cancer. Sci Rep. 2014 Nov 24;4:7162.

[相关活性小分子]

放线菌酮 | 放线菌素D | Alpha-毒伞肽 | 茴香霉素 | SCR7 | CX-5461 | 布拉扑兰 | COH29 | 曲西立滨 | 叶酸 | 氢溴酸常山酮 | RG7800 | N-[4-氟-3-(三氟甲基)苯基]-N'-[5-(4-吡啶基)-1,3,4-噻二唑-2-基]脲 | 腺嘌呤 | 奈达铂

光辉霉素物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 沸点 ]:
1169.8±65.0 °C at 760 mmHg

[ 熔点 ]:
180-183ºC

[ 分子式 ]:
C₅₂H₇₆O₂₄

[ 分子量 ]:
1085.145

[ 闪点 ]:
327.4±27.8 °C

[ 精确质量 ]:
1084.472656

[ PSA ]:
358.20000

[ LogP ]:
1.29

[ 外观性状 ]:
黄色粉末

[ 蒸汽压 ]:
0.0±0.3 mmHg at 25°C

[ 折射率 ]:
1.640

光辉霉素MSDS

详细MSDS(安全技术说明书)

光辉霉素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: PZ2800000

CHEMICAL NAME :: Mithramycin

CAS REGISTRY NUMBER :: 18378-89-7

LAST UPDATED :: 199609

DATA ITEMS CITED :: 27

MOLECULAR FORMULA :: C52-H76-O24

MOLECULAR WEIGHT :: 1085.28

WISWESSER LINE NOTATION :: L C666 DVT&&J BQ FYO1&VYQYQ1 M1 NQ LO- BT6OTJ EQ F1 DO- BT6OTJ DQ EQ F1&& EO- BT6OTJ EQ F1 DO

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human

DOSE/DURATION :: 50 ug/kg/5D

TOXIC EFFECTS :: Blood - thrombocytopenia

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2500 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 3100 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1741 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 500 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1090 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2810 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 350 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 250 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 250 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 2400 mg/kg/4W-I

TOXIC EFFECTS :: Liver - change in gall bladder structure or function Blood - hemorrhage Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 2400 mg/kg/4W-I

TOXIC EFFECTS :: Blood - hemorrhage Blood - other changes Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

DOSE :: 2 mg/kg

SEX/DURATION :: female 11 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

MUTATION DATA

TEST SYSTEM :: Rodent - hamster

DOSE/DURATION :: 1250 ug/kg/5D (Continuous)

REFERENCE :: ENMUDM Environmental Mutagenesis. (New York, NY) V.1-9, 1979-87. For publisher information, see EMMUEG. Volume(issue)/page/year: 4,231,1982 *** REVIEWS *** TOXICOLOGY REVIEW 32XPAD "Teratology," Berry, C.L., and D.E. Poswillo, eds., New York, Springer, 1975 Volume(issue)/page/year: -,49,1975 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X3731 No. of Facilities: 290 (estimated) No. of Industries: 1 No. of Occupations: 8 No. of Employees: 6594 (estimated) No. of Female Employees: 2796 (estimated)

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光辉霉素安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Faceshields;Gloves

[ 危害码 (欧洲) ]:
Xn: Harmful;

[ 风险声明 (欧洲) ]:
R22

[ 安全声明 (欧洲) ]:
45-38-36/37/39-28A-22

[ 危险品运输编码 ]:
UN 3249

[ WGK德国 ]:
3

[ RTECS号 ]:
PZ2800000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

光辉霉素文献

Regulation of cytochrome P450 2e1 expression by ethanol: role of oxidative stress-mediated pkc/jnk/sp1 pathway.

Cell Death Dis. 4 , e554, (2013)

CYP2E1 metabolizes ethanol leading to production of reactive oxygen species (ROS) and acetaldehyde, which are known to cause not only liver damage but also toxicity to other organs. However, the signa...

Quiescent sox2(+) cells drive hierarchical growth and relapse in sonic hedgehog subgroup medulloblastoma.

Cancer Cell 26(1) , 33-47, (2014)

Functional heterogeneity within tumors presents a significant therapeutic challenge. Here we show that quiescent, therapy-resistant Sox2(+) cells propagate sonic hedgehog subgroup medulloblastoma by a...

Cooling-increased phospho-β-arrestin-1 and β-arrestin-1 expression levels in 3T3-L1 adipocytes.

Cryobiology 65(1) , 12-20, (2012)

Cooling induces several responses that are modulated by molecular inhibitors and activators and receptor signaling. Information regarding potential targets involved in cold response mechanisms is stil...

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