硫酸小诺霉素

硫酸小诺霉素用途

Micronomicin sulfate (Gentamicin C2b sulfate) 是从 Micromonospora 中分离出来的氨基糖苷抗生素 (antibiotic)。Micronomicin sulfate 是一种接近庆大霉素类抗生素的广谱抗生素,对假单胞菌、变形杆菌、肺炎克雷伯菌、沙雷菌等具有高的抑制活性 (MIC=0.001-8.3 μg/ml)。

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硫酸小诺霉素名称

[ CAS 号 ]:
66803-19-8

[ 中文名 ]:
硫酸小诺霉素

[ 英文名 ]:
Micronomicin sulfate

[中文别名 ]:

沙加霉素

[英文别名 ]:

Micronomycin sulfate
micronomicin sulfate
Sagamacin

硫酸小诺霉素生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 感染

信号通路 >> 抗感染 >> 细菌

[ 靶点 ]

MIC: 0.001-8.3 μg/ml (Pseudomonas, Proteus, Klebsiella pneumoniae, Serratia)[2]

[体外研究]

小诺霉素具有很强的抗菌活性,对金黄色葡萄球菌FDA 209 P、金黄色葡萄球菌最低抑菌值为0.01μg/ml,对大肠杆菌St.M.589、Baker 2、F 14-BK和R5/W677也有活性,最小抑菌值为0.75μg/ml、0.3μg/ml、0.03μg/ml和0.03μg/ml它对铜绿假单胞菌株和肺炎列巴耶拉菌株(MICs=0.03-17.5μg/ml)具有活性[1]。

[体内研究]

硫酸小诺霉素对小鼠的各种细菌感染具有高度的活性,在小鼠体内的急性LD50为93 mg/kg[1]。注射硫酸小诺霉素(静脉注射；4-100 mg/kg；30天)用于亚急性毒性研究。wistar大鼠在100 mg/kg的剂量水平下死亡(30只动物中有10只)：肾脏疾病和共济失调。肾组织学紊乱主要发生在25mg/kg及以上的剂量水平[3]。动物模型：Wistar大鼠[3]剂量：4,10,25,63mg/kg和100mg/kg给药：静脉注射；30天结果：100mg/kg导致大鼠死亡。

[参考文献]

[1]. R Okachi,et al. A New Antibiotic XK-62-2 (Sagamicin). I. Isolation, Physicochemical and Antibacterial Properties. J Antibiot (Tokyo)

[2]. P J Daniels, The Gentamicin Antibiotics. 6. Gentamicin C2b, an Aminoglycoside Antibiotic Produced by Micromonospora Purpurea Mutant JI-33. J Antibiot (Tokyo)

[3]. T Hara, et al. Safety Evaluation of Micronomicin V. Subacute Toxicity in Rats After Intravenous Injection. Jpn J Antibiot. 1983 Nov;36(11):3208-25.

硫酸小诺霉素物理化学性质

[ 密度 ]:
1.32g/cm3

[ 沸点 ]:
667.2ºC at 760mmHg

[ 分子式 ]:
C₂₀H₄₁N₅O_7.xH₂O₄S

[ 分子量 ]:
561.647

[ 闪点 ]:
357.3ºC

[ 精确质量 ]:
561.268005

[ PSA ]:
282.71000

[ 储存条件 ]:
2-8°C，干燥

硫酸小诺霉素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: WK2196000

CHEMICAL NAME :: Streptamine, O-2-amino-2,3,4,6-tetradeoxy-6-(methylamino)-alpha-D- erythro-hexopyranosyl- (1-4)-O-(3-deoxy-4-C-methyl-3-(methylamino)-beta-L-ar abinopyranosyl-(1-6)) -2-deoxy-, sulfate, D-

CAS REGISTRY NUMBER :: 66803-19-8

LAST UPDATED :: 199806

DATA ITEMS CITED :: 9

MOLECULAR FORMULA :: C21-H43-N5-O6.H2-O4-S

MOLECULAR WEIGHT :: 559.77

WISWESSER LINE NOTATION :: T6OTJ CZ F1M1 BO- BL6TJ AZ CQ EZ DO- BT6OTJ CQ DM1 EQ E1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >10 gm/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,1323,1995

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1223 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,APP-18,1982

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 104 mg/kg

TOXIC EFFECTS :: Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea Lungs, Thorax, or Respiration - cyanosis

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: 36,3204,1983

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

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 625 mg/kg

TOXIC EFFECTS :: Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea Lungs, Thorax, or Respiration - cyanosis

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: 36,3204,1983

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 15600 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,1323,1995

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 350 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,APP-18,1982

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 245 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,APP-18,1982

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 459 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,APP-18,1982

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

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 459 mg/kg

TOXIC EFFECTS :: Behavioral - ataxia Lungs, Thorax, or Respiration - respiratory stimulation Gastrointestinal - changes in structure or function of salivary glands

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: 36,3204,1983

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硫酸小诺霉素安全信息

[ 危害码 (欧洲) ]:
Xi