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德夸菌素

德夸菌素用途

Decoyinine 是 GMP 合成酶的一个选择性抑制剂。

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德夸菌素名称

[ CAS 号 ]:
2004-04-8

[ 中文名 ]:
德夸菌素

[ 英文名 ]:
Decoyinine

[英文别名 ]:

decoyinine
Decoyinin
Antibiotic A 14
U-7984
Angustmycin A
A 14

德夸菌素生物活性

[ 描述 ]:

Decoyinine 是 GMP 合成酶的一个选择性抑制剂。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 癌症

[ 靶点 ]

GMPS[1].

[体外研究]

Decoyinine是腺苷的类似物,其通过抑制GMP合成酶引起细胞内GTP水平的降低。 Decoyinine仅在其中α-淀粉酶调节的分解代谢物抑制组分已被gra-10突变无法操作的菌株中对oaamylase合成发挥刺激作用。由Decoyinine在WLN-11中对α-淀粉酶活性的明显刺激不是在酶活性本身水平上产生的人为效应。观察到嘌呤核苷酸,最值得注意的是GMP,对环状芽孢杆菌F-2淀粉酶的活性表现出显着的抑制作用,对枯草芽孢杆菌α-淀粉酶的抑制作用较小。在实验中使用的浓度(1.07mM)下,Decoyinine对枯草芽孢杆菌WLN-11 oaamylase活性没有体外作用。在相同浓度下,GMP对淀粉酶活性有轻微的抑制作用[2]。

[体内研究]

结果表明,Decoyinine(Angustmycin A)处理阻碍了异种移植小鼠模型中的肿瘤生长。此外,与GMPS活性一样,Decoyinine的作用似乎不是亚型特异性的,因为它损害了携带NRASQ61R(SK-Mel-103)或BRAFV600E(SK-Mel-28)突变的细胞的异种移植物的生长[1]。

[细胞实验]

将等基因菌株WLN-4（sacA321 amyRJ-amyE +）和WLN-11（sacA321 gra-10-amyE +）接种到含有2％（wt / vol）葡萄糖的最小S7培养基中，培养的生长在洗涤的指数期种子培养物中。相同的媒介。在对数生长中期，将每种培养物均匀地分成两个烧瓶，其中含有1/10培养体积的新鲜S7培养基或1/10体积的过滤灭菌的S7培养基，其中每毫升含2.5mg的Decoyinine。溶解（最终Decoyinine浓度，250μg/ mL）。在添加诱饵之前和之后的定期间隔，从培养物中取出样品，并如前所述测定培养物上清液的α-淀粉酶。在添加Decoyinine后16小时，确定每种培养物中耐热孢子的频率[2]。

[动物实验]

将小鼠[1] SK-Mel-103和SK-Mel-28细胞皮下接种在SCID小鼠的两侧（18只小鼠/细胞系）中。一旦肿瘤体积达到约100mm 3，将小鼠随机分配到四组中的一组，并且每天腹膜内注射诱饵（120mg / kg），MMF（30mg / kg）或各自的载体进行治疗。每隔一天用卡尺测量肿瘤大小，一旦肿瘤体积达到1000mm3就杀死小鼠或者动物显示出发病迹象[1]。

[参考文献]

[1]. A Bianchi-Smiraglia, et al. Pharmacological targeting of guanosine monophosphate synthase suppresses melanoma cell invasion and tumorigenicity. Cell Death Differ. 2015 Nov; 22(11): 1858–1864.

[2]. W L Nicholson, et al. Effect of Decoyinine on the regulation of alpha-amylase synthesis in Bacillus subtilis. J Bacteriol. 1987 Dec; 169(12): 5867–5869.

[相关活性小分子]

德夸菌素物理化学性质

[ 密度 ]:
1.9±0.1 g/cm3

[ 沸点 ]:
580.3±60.0 °C at 760 mmHg

[ 分子式 ]:
C₁₁H₁₃N₅O₄

[ 分子量 ]:
279.25

[ 闪点 ]:
304.7±32.9 °C

[ PSA ]:
128.54000

[ LogP ]:
-1.25

[ 蒸汽压 ]:
0.0±1.7 mmHg at 25°C

[ 折射率 ]:
1.837

[ 储存条件 ]:
2-8℃

德夸菌素MSDS

详细MSDS(安全技术说明书)

德夸菌素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: AU6256000

CHEMICAL NAME :: Adenine, 9-(6-deoxy-beta-D-erythro-hex-5-enulofuranosyl)-

CAS REGISTRY NUMBER :: 2004-04-8

LAST UPDATED :: 199106

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C11-H13-N5-O4

MOLECULAR WEIGHT :: 279.29

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >2500 mg/kg

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

REFERENCE :: UPJOH* "Compounds Available for Fundamental Research, Volume II-6, Antibiotics, A Program of Upjohn Company Research Laboratory." (Kalamazoo, MI 49001) Volume(issue)/page/year: 2(6),-,1971

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >1 gm/kg

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

REFERENCE :: UPJOH* "Compounds Available for Fundamental Research, Volume II-6, Antibiotics, A Program of Upjohn Company Research Laboratory." (Kalamazoo, MI 49001) Volume(issue)/page/year: 2(6),-,1971

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2500 mg/kg

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

REFERENCE :: 85GDA2 "CRC Handbook of Antibiotic Compounds," Vols.1- , Berdy, J., Boca Raton, FL, CRC Press, 1980- Volume(issue)/page/year: 5,294,1981

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德夸菌素安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 危险品运输编码 ]:
NONH for all modes of transport

德夸菌素文献

Metabolic initiation of differentiation and secondary metabolism by Streptomyces griseus: significance of the stringent response (ppGpp) and GTP content in relation to A factor.

J. Bacteriol. 169(8) , 3608-16, (1987)

I investigated the significance of the intracellular accumulation of guanosine 5'-diphosphate 3'-diphosphate (ppGpp) and of the coordinated decrease in the GTP pool for initiating morphological and ph...

DegS-DegU and ComP-ComA modulator-effector pairs control expression of the Bacillus subtilis pleiotropic regulatory gene degQ.

J. Bacteriol. 173(7) , 2366-77, (1991)

Production of a class of both secreted and intracellular degradative enzymes in Bacillus subtilis is regulated at the transcriptional level by a signal transduction pathway which includes the DegS-Deg...

Multiple regulatory sites in the Bacillus subtilis citB promoter region.

J. Bacteriol. 172(9) , 5408-15, (1990)

The aconitase (citB) gene of Bacillus subtilis is repressed during growth in a medium that contains a rapidly metabolizable carbon source and a source of 2-ketoglutarate. It is derepressed when either...

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