新霉素B

Framycetin (Fradiomycin B; Neomycin B)是一种氨基糖苷类抗生素。抑制锤头核酶的Ki值为13.5 μM。

信号通路 >> 抗感染 >> 细菌

研究领域 >> 感染

Ki: 13.5 μM (hammerhead ribozyme)[1]

临床上使用新霉素B来治疗肝性脑病(通过降低肠道中的铵水平)和肠致病性大肠杆菌感染。新霉素B靶向细菌和人类核糖体并影响翻译。向HCC细胞系添加新霉素B选择性地抑制成熟miRNA的产生,促进下游蛋白质并抑制侵袭[2]。新霉素B与不具有一级序列同源性的各种靶RNA相互作用。这意味着药物结合RNA的结构而不是序列基序。它的主要同源靶标是16S rRNA的解码位点,但它也与HIV-1,I组内含子和锤头状核酶中的Rev-反应元件结合,从而抑制其生物学功能[3]。氨基糖苷类抗生素新霉素B在翻译过程中诱导遗传密码的误读并抑制几种核酶。新霉素B的核糖体靶位点是16S rRNA1400至1500区域,已经通过从27个核苷酸的小RNA解剖该结构域清楚地证明了这一点。这种16 S rRNA的小亚结构域受到新霉素的化学修饰保护,其位置与30 S亚基相同[4]。

[1]. Stage TK, et al. Inhibition of the hammerhead ribozyme by neomycin. RNA. 1995 Mar;1(1):95-101.

[2]. Childs-Disney JL, et al. Small Molecule Targeting of a MicroRNA Associated with Hepatocellular Carcinoma. ACS Chem Biol. 2016 Feb 19;11(2):375-80.

[3]. Stampfl S, et al. Monovalent ion dependence of neomycin B binding to an RNA aptamer characterized by spectroscopic methods. Chembiochem. 2007 Jul 9;8(10):1137-45.

[4]. Hoch I, et al. Antibiotic inhibition of RNA catalysis: neomycin B binds to the catalytic core of the td group I intron displacing essential metal ions. J Mol Biol. 1998 Sep 25;282(3):557-69.

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

DATA ITEMS CITED :

4

MOLECULAR FORMULA :

C23-H46-N6-O13

MOLECULAR WEIGHT :

614.75

WISWESSER LINE NOTATION :

T6OTJ B1Z CQ DQ EZ FO- AL6TJ BZ DZ EQ FO- BT5OTJ CQ E1Q DO- BT6OTJ CZ DQ EQ F1Z

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

1250 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

85GDA2 "CRC Handbook of Antibiotic Compounds," Vols.1- , Berdy, J., Boca Raton, FL, CRC Press, 1980- Volume(issue)/page/year: 1,127,1980

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intraperitoneal

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

250 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

85ERAY "Antibiotics: Origin, Nature, and Properties," Korzyoski, T., et al., eds., Washington, DC, American Soc. for Microbiology, 1978 Volume(issue)/page/year: 1,741,1978

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

220 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

HBTXAC "Handbook of Toxicology," 4 vols., Philadelphia, W.B. Saunders Co., 1956-59 Volume(issue)/page/year: 2,121,1957

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

24 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: 27,677,1974