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诺拉霉素

诺拉霉素用途

诺加霉素是蒽环素类抗生素。诺加霉素是一种有效的抗革兰氏阳性菌抗生素,对某些肿瘤细胞也有细胞毒性。诺加拉霉素由诺加拉链霉菌诺加拉变种产生。诺加霉素在与DNA模板结合后选择性抑制RNA合成。诺加霉素可用于研究抗癌药物[1][2]。

诺拉霉素名称

[ CAS 号 ]:
1404-15-5

[ 中文名 ]:
诺拉霉素

[ 英文名 ]:
Nogalamycin

[英文别名 ]:

antibiotic205t3
nogalomycin
NOGALAMYCIN
NOGALAMYCIN,STREPTOMYCES NOGALATER

诺拉霉素生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 细胞周期/DNA损伤 >> DNA/RNA合成

信号通路 >> 抗感染 >> 细菌

[ 靶点 ]

RNA Synthesis[2]

[体外研究]

诺加霉素(0-10μg/ml；2小时)对CHO、L1210和B16具有致死性,LD50分别为2.74μg/ml、0.25μg/ml和0.15μg/ml【1】。细胞毒性试验细胞系：CHO、L1210和B16细胞【1】浓度：0-10μg/ml孵育时间：2小时结果：LD50s分别为2.74μg/ml、0.25μg/ml和0.15μg/ml,对CHO、L1210和B16具有杀伤力。

[体内研究]

诺加霉素(0-1000μg/kg；IP)可以逆转化学诱导的大鼠纤维肉瘤肿瘤和自发性肿瘤[3]。动物模型：大鼠【1】剂量：0-1000μg/kg给药：IP结果：化学诱导的大鼠纤维肉瘤肿瘤和自发性肿瘤消退,最有效浓度为556μg/kg。

[参考文献]

[1]. Bhuyan BK, et al. Cell kill kinetics of several nogalamycin analogs and adriamycin for Chinese hamster ovary, L1210 leukemia, and B16 melanoma cells in culture. Cancer Res. 1981;41(1):18-24.

[2]. Bhuyan BK, et al. Differential interaction of nogalamycin with DNA of varying base composition. Proc Natl Acad Sci U S A. 1965;54(2):566-572.

[3]. Bempong MA. Cytological effect of nogalamycin in mammals and regression of methylcholanthrene-induced and spontaneous tumors in rats. Int J Clin Pharmacol Biopharm. 1976;14(1):6-14.

诺拉霉素物理化学性质

[ 密度 ]:
1.49g/cm3

[ 沸点 ]:
899.9ºC at 760mmHg

[ 分子式 ]:
C₃₉H₄₉NO₁₆

[ 分子量 ]:
787.80

[ 闪点 ]:
498.1ºC

[ 精确质量 ]:
787.30500

[ PSA ]:
229.44000

[ LogP ]:
1.13800

[ 外观性状 ]:
固体

[ 蒸汽压 ]:
7.49E-35mmHg at 25°C

[ 折射率 ]:
1.648

[ 储存条件 ]:
-20°C，密封，干燥

诺拉霉素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: RA4550000

CHEMICAL NAME :: Nogalamycin

CAS REGISTRY NUMBER :: 1404-15-5

LAST UPDATED :: 199806

DATA ITEMS CITED :: 22

MOLECULAR FORMULA :: C39-H49-N-O16

MOLECULAR WEIGHT :: 787.89

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 500 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 :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 4600 ug/kg

TOXIC EFFECTS :: Gastrointestinal - hypermotility, diarrhea Gastrointestinal - other changes Nutritional and Gross Metabolic - weight loss or decreased weight gain

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >300 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 :: 13750 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 :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 8500 ug/kg

TOXIC EFFECTS :: Skin and Appendages - other glands Nutritional and Gross Metabolic - weight loss or decreased weight gain

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 250 ug/kg

TOXIC EFFECTS :: Behavioral - muscle weakness Lungs, Thorax, or Respiration - acute pulmonary edema Lungs, Thorax, or Respiration - respiratory depression

MUTATION DATA

TYPE OF TEST :: Mutation test systems - not otherwise specified

TEST SYSTEM :: Mammal - species unspecified Lymphocyte

DOSE/DURATION :: 12 umol/L

REFERENCE :: CBINA8 Chemico-Biological Interactions. (Elsevier Scientific Pub. Ireland Ltd., POB 85, Limerick, Ireland) V.1- 1969- Volume(issue)/page/year: 36,1,1981 *** REVIEWS *** TOXICOLOGY REVIEW CRTXB2 CRC Critical Reviews in Toxicology. (CRC Press, Inc., 2000 Corporate Blvd., NW, Boca Raton, FL 33431) V.1- 1971- Volume(issue)/page/year: 2,159,1973

诺拉霉素安全信息

[ 符号 ]:

GHS07, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H302-H312-H332-H350-H360

[ 警示性声明 ]:
P201-P280-P308 + P313

[ 个人防护装备 ]:
Eyeshields;Faceshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T: Toxic;

[ 风险声明 (欧洲) ]:
45-46-61-20/21/22

[ 安全声明 (欧洲) ]:
53-22-36/37/39-45

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

[ RTECS号 ]:
RA4550000

诺拉霉素文献

Kinetic characterization of small DNA-binding molecules interacting with a DNA strand on a quartz crystal microbalance.

Anal. Biochem. 492 , 34-42, (2015)

Quantitative studies of the binding of various DNA-binding antibiotics with dsDNA are useful for drug design, not only for effective antibiotics, but also for antitumor drugs. We studied the binding k...

The intercalation of DNA double helices with doxorubicin and nogalamycin.

J. Mol. Graph. Model. 26(1) , 14-9, (2007)

A variety of molecules bind to DNA in its major and minor grooves, and some, like the anthraquinoids, are known to form intercalates in which these molecules are inserted directly into the double heli...

Engineering anthracycline biosynthesis toward angucyclines.

Antimicrob. Agents Chemother. 47(4) , 1291-6, (2003)

The biosynthesis pathways of two anthracyclines, nogalamycin and aclacinomycin, were directed toward angucyclines by using an angucycline-specific cyclase, pgaF, isolated from a silent antibiotic bios...

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