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硫酸庆大霉素

硫酸庆大霉素用途

庆大霉素靠结合到30S核糖体亚单位上引起密码读错,阻断肽酰-tRNA(peptidyl-tRNA)从受体位点到供体点点的转移。庆大霉素对假单胞杆菌的杀菌效果靠结合到细胞膜的外膜部分,置换本来存在的阳离子,使膜不稳定,在细胞表面形成空洞。抗菌谱: 革兰氏阴性细菌,葡萄状球菌和其它的革兰氏阳性细菌。 
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硫酸庆大霉素作用

用于治疗败血症、尿路感染、葡萄球菌感染、心内膜炎及其他疾病。
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硫酸庆大霉素名称

[ CAS 号 ]:
1405-41-0

[ 中文名 ]:
庆大霉素硫酸盐

[ 英文名 ]:
Gentamycin Sulfate

[中文别名 ]:

[英文别名 ]:

硫酸庆大霉素生物活性

[ 描述 ]:

Gentamicin sulfate是一种氨基糖苷类抗生素,抑制革兰氏阳性菌和革兰氏阴性细菌的生长并可抑制组织培养中的多种支原体菌株。抑制DNase I活性的IC50值为0.57 mM。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 细菌
研究领域 >> 感染

[ 靶点 ]

IC50: 0.57 mM (DNase I)[1]


[体外研究]

庆大霉素是一种比联合青霉素-链霉素更有效的体外细菌抑制剂,对组织培养单层无毒,并且不抑制病毒复制。它已被成功地用作商业真菌学培养基中的添加剂以抑制细菌的生长,并且已被证明对于更广泛的生物(铜绿假单胞菌,变形杆菌和粪链球菌)比青霉素和链霉素具有杀菌作用。它不会干扰组织培养中某些埃可病毒和脊髓灰质炎病毒产生的细胞病变效应,对恒河猴肾,HeLa和人羊膜细胞无毒,并且在高压灭菌温度下稳定[2]。庆大霉素是由小单孢菌属(Micromonospora)的各种物种产生的。商品庆大霉素主要由不同的庆大霉素C组分组成。 Yoshizawa阐明了与A位点RNA结合的庆大霉素C1a的3D结构。庆大霉素C1a结合在RNA的A位点的主要沟中[3]。

[体内研究]

庆大霉素目前是用于治疗严重感染的首选氨基糖苷类,替代品为阿米卡星,奈替米星和妥布霉素。庆大霉素制剂可以三种形式商购,即耳,眼和局部,基于治疗耳道,眼睛和皮肤感染的相应功能。发现口服和注射形式的庆大霉素对鼠疫耶尔森氏菌具有有效的抗菌活性,如小鼠感染模型所示[3]。用多达9剂甲氧西林或庆大霉素治疗显示异物上的细菌显着减少[4] 。

[动物实验]

小鼠:细菌攻击小鼠用甲氧西林,庆大霉素,甲氧西林和庆大霉素,或不用抗生素治疗。治疗每天给药三次,持续3天。每剂甲氧西林是每只小鼠75mg(3g / kg体重),并且庆大霉素剂量是每只小鼠0.75mg(0.03g / kg)。在0.1或0.5mL盐水中皮下给予抗生素。处死小鼠并收集血清和抽吸样品[4]。

[参考文献]

[1]. Xu W, et al. A rapid and sensitive method for kinetic study and activity assay of DNase I in vitro based on a GO-quenched hairpin probe. Anal Bioanal Chem. 2016 May;408(14):3801-9.

[2]. Rudin A, et al. Antibacterial activity of gentamicin sulfate in tissue culture. Appl Microbiol. 1970 Dec;20(6):989-90.

[3]. Kumar CG, et al. Microbial biosynthesis and applications of gentamicin: a critical appraisal.

[4]. Espersen F, et al. Effect of treatment with methicillin and gentamicin in a new experimental mouse model of foreignbody infection. Antimicrob Agents Chemother. 1994 Sep;38(9):2047-53.


[相关活性小分子]

嘌呤霉素二盐酸盐 | G-418 硫酸盐 | 衣霉素 | 潮霉素B | 盐霉素 | 阿维巴坦钠 | 硫酸新霉素 | 法硼巴坦 | 甲氧西林钠 | 利福平 | 甲硝唑 | 羧苄青霉素钠 | 头孢他啶 | 盐酸依拉环素 | 头孢噻肟钠

硫酸庆大霉素物理化学性质

[ 沸点 ]:
797.6ºC at 760 mmHg

[ 熔点 ]:
218-237°C

[ 分子式 ]:
C(19-21)H(39-43)N5O7·H2SO4

[ 分子量 ]:
561.65 (Average)

[ 闪点 ]:
436.2ºC

[ PSA ]:
719.38000

[ 外观性状 ]:
白色至浅黄色的粉末无气味的

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
H2O: 50 mg/mL As stock solution, store at −20°C. Stable at 37°C for 5 days.

硫酸庆大霉素MSDS

硫酸庆大霉素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
LY2625000
CHEMICAL NAME :
Gentamicin, sulfate
CAS REGISTRY NUMBER :
1405-41-0
LAST UPDATED :
199512

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
45 mg/kg/1W-I
TOXIC EFFECTS :
Nutritional and Gross Metabolic - changes in metals, not otherwise specified
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
21 mg/kg/6D-I
TOXIC EFFECTS :
Nutritional and Gross Metabolic - changes in metals, not otherwise specified
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>5 gm/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Skin and Appendages - hair
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
630 mg/kg
TOXIC EFFECTS :
Behavioral - muscle contraction or spasticity Lungs, Thorax, or Respiration - other changes
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
873 mg(base)/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 :
96 mg/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory stimulation
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
384 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 :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>11269 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 :
245 mg/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory stimulation
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
478 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 :
Rodent - mouse
DOSE/DURATION :
47 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
250 mg/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex) Lungs, Thorax, or Respiration - respiratory stimulation
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intracerebral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
17300 ug/kg
TOXIC EFFECTS :
Peripheral Nerve and Sensation - sensory change involving peripheral nerve Sense Organs and Special Senses (Eye) - ptosis Behavioral - convulsions or effect on seizure threshold
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - guinea pig
DOSE/DURATION :
600 mg/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 :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
200 mg/kg/5D-I
TOXIC EFFECTS :
Kidney, Ureter, Bladder - other changes in urine composition Nutritional and Gross Metabolic - changes in calcium Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - other Enzymes
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
280 mg(base)/kg/7D-I
TOXIC EFFECTS :
Kidney, Ureter, Bladder - other changes in urine composition Nutritional and Gross Metabolic - changes in calcium Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - dehydrogenases
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
240 mg/kg/6D-I
TOXIC EFFECTS :
Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Nutritional and Gross Metabolic - weight loss or decreased weight gain Nutritional and Gross Metabolic - changes in metals, not otherwise specified
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
3840 mg/kg/4W-I
TOXIC EFFECTS :
Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Related to Chronic Data - death
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
2 gm/kg/50D-I
TOXIC EFFECTS :
Behavioral - ataxia Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Mammal - cat
DOSE/DURATION :
1400 mg/kg/70D-I
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex) Behavioral - ataxia Related to Chronic Data - death
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Mammal - cat
DOSE/DURATION :
1365 mg/kg/91D-I
TOXIC EFFECTS :
Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Related to Chronic Data - death
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Mammal - cat
DOSE/DURATION :
4200 mg/kg/30W-I
TOXIC EFFECTS :
Sense Organs and Special Senses (Ear) - changes in cochlear structure or function Behavioral - altered sleep time (including change in righting reflex) Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Mammal - cat
DOSE/DURATION :
2700 mg/kg/27D-I
TOXIC EFFECTS :
Behavioral - ataxia Related to Chronic Data - death
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - guinea pig
DOSE/DURATION :
6557 mg/kg/77D-I
TOXIC EFFECTS :
Sense Organs and Special Senses (Ear) - change in acuity Sense Organs and Special Senses (Ear) - changes in cochlear structure or function Behavioral - muscle contraction or spasticity
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
660 mg/kg
SEX/DURATION :
female 10-15 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - cardiovascular (circulatory) system Reproductive - Specific Developmental Abnormalities - urogenital system
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
660 mg/kg
SEX/DURATION :
female 15-20 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - biochemical and metabolic
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
375 mg/kg
SEX/DURATION :
female 14-18 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - urogenital system Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)
TYPE OF TEST :
DNA damage

MUTATION DATA

TEST SYSTEM :
Rodent - rat
DOSE/DURATION :
9600 ug/kg/8D
REFERENCE :
JOURAA Journal of Urology. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1917- Volume(issue)/page/year: 112,348,1974 *** REVIEWS *** TOXICOLOGY REVIEW PMMDAE Panminerva Medica. (Edizioni Minerva Medica, Casella Postale 491, Turin, Italy) V.1- 1959- Volume(issue)/page/year: 16,9,1974 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X3126 No. of Facilities: 2125 (estimated) No. of Industries: 7 No. of Occupations: 22 No. of Employees: 46715 (estimated) No. of Female Employees: 34072 (estimated)
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硫酸庆大霉素安全信息

[ 符号 ]:

GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H317-H334

[ 警示性声明 ]:
P261-P280-P342 + P311

[ 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) ]:
R42/43

[ 安全声明 (欧洲) ]:
S23-S36/37-S45-S22

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

[ WGK德国 ]:
2

[ RTECS号 ]:
LY2625000

[ 海关编码 ]:
2941901000

硫酸庆大霉素海关

[ 海关编码 ]: 2941901000

硫酸庆大霉素文献

Enhanced secretion of interferon-gamma by bovine gammadelta T cells induced by coculture with Mycobacterium bovis-infected dendritic cells: evidence for reciprocal activating signals.

Immunology 126(2) , 201-8, (2009)

Evidence suggests that gammadelta T cells form part of the innate immune response to Mycobacterium bovis infection. Dendritic cells (DCs) are capable of secreting high levels of interleukin-12 (IL-12)...

Altered states of telomere deprotection and the two-stage mechanism of replicative aging.

Mol. Cell. Biol. 29(9) , 2390-7, (2009)

The molecular distinctions between mortality stages 1 (M1; senescence) and 2 (M2; crisis) of human replicative aging are ill defined. We demonstrate a qualitative difference between telomeric end asso...

Rett syndrome like phenotypes in the R255X Mecp2 mutant mouse are rescued by MECP2 transgene.

Hum. Mol. Genet. 24 , 2662-72, (2015)

Rett syndrome (RTT) is a severe neurodevelopmental disorder that is usually caused by mutations in Methyl-CpG-binding Protein 2 (MECP2). Four of the eight common disease causing mutations in MECP2 are...


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