七尾霉素

七尾霉素用途

Nanaomycin A 是第一个选择性 DNMT3B 抑制剂,IC50 为 500 nM。Nanaomycin A 是一种醌类抗生素,可重新激活人类癌细胞中沉默的抑癌基因。Nanaomycin A 抑制人疟原虫恶性疟原虫的体外生长,IC80 值为 33.1 nM。

七尾霉素名称

[ CAS 号 ]:
52934-83-5

[ 中文名 ]:
七尾霉素

[ 英文名 ]:
Nanafrocin

[中文别名 ]:

那罗星

[英文别名 ]:

4-deoxykalafunginic acid
dihydrokalafungin
Rosanomycin A
Nanafrocine
Nanafrocinum
nanaomycin A
nanafrocinum [INN_la]
OS 3966-A
Nanafrocin

七尾霉素生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

研究领域 >> 感染

信号通路 >> 表观遗传学 >> DNA甲基转移酶

[ 靶点 ]

DNMT3B:500 nM (IC50)

[体外研究]

纳诺霉素A(10-10000纳米；72小时)对所有三种细胞系都有明显的细胞毒性作用[1]。纳诺霉素A(0.5,5μM；72小时)诱导A549细胞RASSF1A蛋白表达[1]。纳诺霉素A(5μM；72小时)具有18倍的相对诱导率[1]。纳诺霉素A对DNMT1酶活性无影响[1]。细胞毒性试验[1]细胞株：HCT116(结肠)、A549(肺)、HL60(骨髓)人肿瘤细胞株浓度：10、100、1000、10000nm孵育时间：72h结果：三种细胞株均有明显的细胞毒性作用。Western Blot分析[1]细胞株：A549细胞浓度：0.5,5μM孵育时间：72h结果：RASSF1A蛋白表达诱导。RT-PCR[1]细胞株：A549细胞浓度：5μM孵育时间：72h结果：相对诱导率为18倍。

[参考文献]

[1]. Kuck D, et al.Nanaomycin A selectively inhibits DNMT3B and reactivates silenced tumor suppressor genes in human cancer cells.Mol Cancer Ther. 2010 Nov;9(11):3015-23.

[2]. Tanaka Y, et al.Heme-dependent radical generation: possible involvement in antimalarial action of non-peroxide microbial metabolites, nanaomycin A and radicicol.J Antibiot (Tokyo). 1999 Oct;52(10):880-8.

七尾霉素物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 沸点 ]:
601.5±55.0 °C at 760 mmHg

[ 分子式 ]:
C₁₆H₁₄O₆

[ 分子量 ]:
302.279

[ 闪点 ]:
229.0±25.0 °C

[ 精确质量 ]:
302.079041

[ PSA ]:
100.90000

[ LogP ]:
2.60

[ 蒸汽压 ]:
0.0±1.8 mmHg at 25°C

[ 折射率 ]:
1.649

[ 储存条件 ]:
-20°C，干燥，密封

七尾霉素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: QL6127000

CHEMICAL NAME :: 1H-Naphtho(2,3-c)pyran-3-acetic acid, 3,4,5,10-tetrahydro-9-hydroxy-1-methyl-5,10-dioxo-, (1S-E)-

CAS REGISTRY NUMBER :: 52934-83-5

LAST UPDATED :: 199306

DATA ITEMS CITED :: 7

MOLECULAR FORMULA :: C16-H14-O6

MOLECULAR WEIGHT :: 302.30

WISWESSER LINE NOTATION :: T C666 BV EO IVT&&J D1 F1VQ NQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >200 mg/kg

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

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 33,728,1980

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 52 mg/kg

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

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 33,728,1980

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 290 mg/kg

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

REFERENCE :: JANTAJ Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo, 141, Japan) V.2-5, 1948-52; V.21- 1968- Volume(issue)/page/year: 28,860,1975

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

ROUTE OF EXPOSURE :: Administration onto the skin

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 52 mg/kg

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

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 33,728,1980

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 28200 ug/kg

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

REFERENCE :: JANTAJ Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo, 141, Japan) V.2-5, 1948-52; V.21- 1968- Volume(issue)/page/year: 28,860,1975

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 56 mg/kg

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

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 33,728,1980

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 52 mg/kg

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

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 33,728,1980

七尾霉素安全信息

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
22-24

[ 危险品运输编码 ]:
UN 2811 6.1/PG 3