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大观霉素

大观霉素用途

大观霉素是一种广谱抗生素,可抑制多种革兰氏阳性和革兰氏阴性微生物的生长。大观霉素通过选择性靶向细菌核糖体并中断蛋白质合成发挥作用。大观霉素也是td内含子RNA的非竞争性抑制剂[1][2][3][4][5]。

大观霉素名称

[ CAS 号 ]:
1695-77-8

[ 中文名 ]:
大观霉素

[ 英文名 ]:
Spectinomycin

[中文别名 ]:

[英文别名 ]:

antibiotic2233wp
EINECS 216-911-3
togamycin
spectinomicina
Spectinomycin
Spectacin
espectinomicina
spectam
trobicin
actinospectacin

大观霉素生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 感染

信号通路 >> 抗感染 >> 细菌

[ 靶点 ]

bacterial ribosomal subunit[5]

[体外研究]

大观霉素选择性抑制细胞和大肠杆菌提取物中的蛋白质合成。大观霉素(50μg/mL)可快速可逆地抑制大肠杆菌生长,并立即抑制氨基酸掺入[1]。大观霉素(1μg/mL或3μM)抑制内源性信使RNA或MS-2噬菌体RNA指导的多肽合成,在大肠杆菌提取物中最大抑制率为70-80%[1]。大观霉素通过抑制延伸因子G与核糖体的结合,阻断肽基tRNA从A位点向P位点的移位[2]。大观霉素与16S rRNA中的残基G1064和01192特异性相互作用,并可能使其失活[2]。大观霉素表现出剪接抑制作用,并依赖于pH变化和Mg2+浓度,这表明它和内含子RNA之间存在静电相互作用[3]。

[体内研究]

大观霉素(20 mg/kg；i.m.；20-100 mg/kg；9 d)在健康雏鸡中显示出安全性[4]。大观霉素(10 mg/kg；静脉注射；单剂量)主要通过肾脏排泄清除,约55%以不变形式排泄到尿液中[5]。大鼠体内大观霉素的药代动力学[5]参数C0(μg/mL)AUC0-∞ (μg•h/mL)Vd(L/kg)CL(L/h/kg)MRT,100 mg/kg给药：肌肉注射(胸肌)；9天结果：通过全血计数、生化参数、组织病理学、临床症状、体重增加和饲料转化率(FCR),显示20 mg/kg的生物安全性。产生的轻微毒性为60 mg/kg。

[参考文献]

[1]. Davies J, et al. Inhibition of protein synthesis by spectinomycin. Science. 1965 Sep 3;149(3688):1096-8.

[2]. Brink MF, et al. Spectinomycin interacts specifically with the residues G1064 and C1192 in 16S rRNA, thereby potentially freezing this molecule into an inactive conformation. Nucleic Acids Res. 1994 Feb 11;22(3):325-31.

[3]. Park IK, et al. Spectinomycin inhibits the self-splicing of the group 1 intron RNA. Biochem Biophys Res Commun. 2000 Mar 16;269(2):574-9.

[4]. Khan EA, et al. Safety evaluation study of lincomycin and spectinomycin hydrochloride intramuscular injection in chickens. Toxicol Rep. 2022 Jan 29;9:204-209.

[5]. Madhura DB, et al. Pharmacokinetic profile of spectinomycin in rats. Pharmazie. 2013 Aug;68(8):675-6.

大观霉素物理化学性质

[ 密度 ]:
1.43 g/cm3

[ 沸点 ]:
583.1ºC at 760 mmHg

[ 熔点 ]:
185ºC

[ 分子式 ]:
C₁₄H₂₄N₂O₇

[ 分子量 ]:
332.35000

[ 精确质量 ]:
332.15800

[ PSA ]:
129.51000

[ 外观性状 ]:
一种白色至淡浅黄色结晶盐酸盐五水化物粉末

[ 蒸汽压 ]:
5.05E-16mmHg at 25°C

[ 储存条件 ]:
室温

大观霉素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UQ0332500

CHEMICAL NAME :: 4H-Pyrano(2,3-b)(1,4)benzodioxin-4-one, decahydro-4a,7,9-trihydroxy-2-methyl-6,8- bis(methylamino)-

CAS REGISTRY NUMBER :: 1695-77-8

LAST UPDATED :: 199706

DATA ITEMS CITED :: 10

MOLECULAR FORMULA :: C14-H24-N2-O7

MOLECULAR WEIGHT :: 332.40

WISWESSER LINE NOTATION :: T C666 BO DO GV IOTJ E1 HQ KM1 LQ MM1 NQ

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 :: >5 gm/kg

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

REFERENCE :: BCFAAI Bollettino Chimico Farmaceutico. (Societa Editoriale Farmaceutica, Via Ausonio 12, 20123 Milan, Italy) V.33- 1894- Volume(issue)/page/year: 111,265,1972

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 5724 mg/kg

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

REFERENCE :: BCFAAI Bollettino Chimico Farmaceutico. (Societa Editoriale Farmaceutica, Via Ausonio 12, 20123 Milan, Italy) V.33- 1894- Volume(issue)/page/year: 111,265,1972

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 20 gm/kg

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

REFERENCE :: AACHAX Antimicrobial Agents and Chemotherapy (1961-70). (Ann Arbor, MI) 1961-70. For publisher information, see AMACCQ. Volume(issue)/page/year: -,507,1961

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2 gm/kg

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

REFERENCE :: 85FZAT "Index of Antibiotics from Actinomycetes," Umezawa, H. et al., eds., Tokyo, Univ. of Tokyo Press, 1967 Volume(issue)/page/year: -,105,1967

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >1 gm/kg

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

REFERENCE :: AACHAX Antimicrobial Agents and Chemotherapy (1961-70). (Ann Arbor, MI) 1961-70. For publisher information, see AMACCQ. Volume(issue)/page/year: -,507,1961

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >2 gm/kg

TOXIC EFFECTS :: Behavioral - muscle weakness Behavioral - ataxia Gastrointestinal - nausea or vomiting

REFERENCE :: AACHAX Antimicrobial Agents and Chemotherapy (1961-70). (Ann Arbor, MI) 1961-70. For publisher information, see AMACCQ. Volume(issue)/page/year: -,507,1961

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: >500 mg/kg

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

REFERENCE :: AACHAX Antimicrobial Agents and Chemotherapy (1961-70). (Ann Arbor, MI) 1961-70. For publisher information, see AMACCQ. Volume(issue)/page/year: -,507,1961

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - cat

DOSE/DURATION :: >800 mg/kg

TOXIC EFFECTS :: Behavioral - ataxia

REFERENCE :: AACHAX Antimicrobial Agents and Chemotherapy (1961-70). (Ann Arbor, MI) 1961-70. For publisher information, see AMACCQ. Volume(issue)/page/year: -,507,1961

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: >40 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - other changes

REFERENCE :: AACHAX Antimicrobial Agents and Chemotherapy (1961-70). (Ann Arbor, MI) 1961-70. For publisher information, see AMACCQ. Volume(issue)/page/year: -,507,1961 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X7549 No. of Facilities: 14 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 432 (estimated) No. of Female Employees: 203 (estimated)

大观霉素安全信息

[ 危害码 (欧洲) ]:
Xn

[ 海关编码 ]:
3003209000

大观霉素合成路线

详细合成路线

大观霉素上下游产品

大观霉素上游产品

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大观霉素海关

[ 海关编码 ]: 3003209000