Spectinomycin (hydrochloride hydrate)
(Synonyms: 奇霉素；大观霉素；盐酸大观霉素五水合物; Spectinomycin hydrochloride hydrate) 目录号 : GC13981
Spectinomycin (hydrochloride hydrate) 是一种由链霉菌（S. spectabilis）产生的广谱氨基环醇类抗生素，能够抑制多种革兰氏阳性和革兰氏阴性菌的生长 。
Cas No.:22189-32-8
Sample solution is provided at 25 µL, 10mM.
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Spectinomycin (hydrochloride hydrate) is a broad-spectrum aminocyclic alcohol antibiotic produced by S. spectabilis and inhibits the growth of a variety of gram-positive and gram-negative organisms[1]. Spectinomycin acts by selectively targeting to the bacterial the 30S ribosomal subunit and interrupting protein synthesis[2]. Spectinomycin is also a noncompetitive inhibitor of TD intron RNA with an Ki value of 7.2mM[3]. Spectinomycin is mainly used in the research of Neisseria gonorrhoeae infection[4][5].
In vitro, Spectinomycin (50μg/mL; 10min) selectively inhibits bacterial growth, and suppresses protein synthesis and amino acid incorporation in cells and extracts of Escherichia coli[1]. Spectinomycin (64μg/mL; 0-60min ) relaxes the stringent control of lipopolysaccharide (LPS) synthesis in amino acid-deprived relA+ cells, but does not inhibit LPS synthesis directly[6].
In vivo, intramuscular injection of Spectinomycin (20mg/kg; i.m.; 9d)has no effects on growth performance, clinical blood parameters, organ coefficient, and histopathological parameters, demonstrating its safety in healthy chicks[3]. In rat experiments, Spectinomycin (10mg/kg; i.v.; single dose) has the major elimination pathway by renal excretion, approximately 55% is excreted into the urine in unchanged form[7].
References:
[1] Davies J, Anderson P, Davis BD. Inhibition of protein synthesis by spectinomycin. Science. 1965;149(3688):1096-1098.
[2] Zimmerman JM, Maher LJ 3rd. In vivo selection of spectinomycin-binding RNAs. Nucleic Acids Res. 2002;30(24):5425-5435.
[3] Khan EA, Ma J, Xiaobin M, et al. Safety evaluation study of lincomycin and spectinomycin hydrochloride intramuscular injection in chickens. Toxicol Rep. 2022;9:204-209. Published 2022 Jan 29.
[4] Ribeiro J, Mathieson SI. Spectinomycin in gonorrhoea. Br J Vener Dis. 1975;51(4):272-273.
[5] Karney WW, Pedersen AH, Nelson M, Adams H, Pfeifer RT, Holmes KK. Spectinomycin versus tetracycline for the treatment of gonorrhea. N Engl J Med. 1977;296(16):889-894.
[6] Kusser WC, Ishiguro EE. Effects of aminoglycosides and spectinomycin on the synthesis and release of lipopolysaccharide by Escherichia coli. Antimicrob Agents Chemother. 1988;32(8):1247-1250.
[7] Madhura DB, Lee R, Meibohm B. Pharmacokinetic profile of spectinomycin in rats. Pharmazie. 2013;68(8):675-676.
Spectinomycin (hydrochloride hydrate) 是一种由链霉菌（S. spectabilis）产生的广谱氨基环醇类抗生素，能够抑制多种革兰氏阳性和革兰氏阴性菌的生长 [1]。Spectinomycin通过选择性靶向细菌的 30S 核糖体亚基，中断蛋白质合成来发挥作用 [2]。此外，Spectinomycin还是一种非竞争性抑制剂，对TD内含子RNA的抑制常数（Ki）为7.2mM [3]。Spectinomycin主要用于淋病奈瑟菌（Neisseria gonorrhoeae）感染的研究 [4][5]。
在体外实验中，Spectinomycin（50μg/mL；10分钟）能够选择性地抑制细菌生长，并抑制 Escherichia coli 细胞及其提取物中的蛋白质合成和氨基酸掺入 [1]。此外，Spectinomycin（64μg/mL；0-60 分钟）能够减轻氨基酸匮乏的relA+细胞中脂多糖（LPS）合成的严格控制，但不直接抑制LPS合成 [6]。
在体内实验中，Spectinomycin（20mg/kg；肌肉注射；9天）对健康雏鸡的生长性能、临床血液参数、器官系数和组织病理学参数均无影响，显示出良好的安全性[3]。在大鼠实验中，Spectinomycin（10mg/kg；静脉注射；单剂量）主要通过肾脏排泄，约55%以原形随尿液排出 [7]。
| Cell experiment [1]: | |
Cell lines | E.coli cells |
Preparation Method | The iso-genic E.coli K-12 strains VC210 and VC21l were grown in M9 minimal medium containing 50mM glycerol as the carbon source and supplemented with thiamine (0.5μg/ml)and L-lysine(50pg/ml). Galactose was added to the medium exactly asdescribed previously in experiments involving the deter-mination of LPS synthesis. Cultures were grown at 37℃ in a gyratory water bath shaker, and growth was followed with a Klett-Summerson colorimeter by using a blue flter. Amino acid deprivation was achieved by either omitting L-lysine from the medium or by adding L-valine to 500μg/ml (to cause isoleucine deprivation). Spectinomycin (64μg/ml) was added into medium and cultured for 1h. To determine the effects of the treatment on LPS synthesis, 0.5ml samples taken from the cultures at were pulse-labeledfor 10min with lμCi of p-[1-3H]galactose(10.4 Ci/mmol), and the amounts of radiolabel incorporated into cold trichloroacetic acid-insoluble fractions were determined. |
Reaction Conditions | 64μg/mL; 0-60min |
Applications | Spectinomycin relaxes the stringent control of lipopolysaccharide (LPS) synthesis in amino acid-deprived relA+ cells, but does not inhibit LPS synthesis directly. |
| Animal experiment [2]: | |
Animal models | Arbor Acres plus chicks |
Preparation Method | A total of 80 healthy Arbor Acres plus broiler chicks were completely randomized and blindly divided into four treatment groups (control, one-time dose, three-time dose, and five-time dose) of 20 chicks each (20 chickens per group). At the age of day 15, all chickens (except the control group) were administered Spectinomycin intramuscularly (chest muscles) at different doses of 20mg/kg.bw, 60mg/kg.bw, and 100mg/kg.bw respectively for 9 consecutive days recommended by veterinary international cooperation on harmonization (VICH) guidelines. The chickens had ad libitum access to antibiotic-free feed and water. Feeding chickens were observed twice a day throughout the study. The drug safety was evaluated by complete blood count, biochemical parameters, histopathological, clinical signs, body weight gain, and feed conversion ratio (FCR). |
Dosage form | 20, 60, 100mg/kg/day for 9 days; i.m. |
Applications | Spectinomycin(20mg/kg/day) has no effects on growth performance, clinical blood parameters, organ coefficient, and histopathological parameters, is safe for healthy chicks. |
References: | |
| Cas No. | 22189-32-8 | SDF | |
| 别名 | 奇霉素；大观霉素；盐酸大观霉素五水合物; Spectinomycin hydrochloride hydrate | ||
| 化学名 | (5aR,9aR,10aS)-decahydro-4aR,7S,9S-trihydroxy-2R-methyl-6S,8R-bis(methylamino)-4H-pyrano[3-b][1,4]benzodioxin-4-one, dihydrochloride pentahydrate | ||
| Canonical SMILES | [H][C@@]12[C@@](C(C[C@@H](C)O2)=O)(O)O[C@]3([H])[C@@H](NC)[C@@H](O)[C@@H](NC)[C@H](O)[C@@]3([H])O1.Cl.Cl.O.O.O.O.O | ||
| 分子式 | C14H24N2O7 • 2HCl [5H2O] | 分子量 | 495.4 |
| 溶解度 | ≥ 49.5mg/mL in H20, ≥ 92 mg/mL in DMSO, ≥ 3.61 mg/mL in EtOH with ultrasonic and warming | 储存条件 | Store at 2-8°C,argon filling away from moisture |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0186 mL | 10.0929 mL | 20.1857 mL |
| 5 mM | 0.4037 mL | 2.0186 mL | 4.0371 mL |
| 10 mM | 0.2019 mL | 1.0093 mL | 2.0186 mL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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2.
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