Spectinomycin 是一种广谱抗生素，可以抑制多种革兰氏阳性和革兰氏阴性细菌的生长。Spectinomycin 通过特异靶向细菌核糖体，干扰蛋白质合成。Spectinomycin 也是 td 内含子 RNA 的非竞争性抑制剂。
| 生物活性 | Spectinomycin is a broad-spectrumantibioticand inhibits the growth of a variety of gram-positive and gram-negative organisms. Spectinomycin acts by selectively targeting to thebacterialribosome and interrupting protein synthesis. Spectinomycin is also a noncompetitive inhibitor of td intron RNA[1][2][3][4][5]. |
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体外研究
(In Vitro) | Spectinomycin selectively inhibits protein synthesis in cells and in extracts ofEscherichia coli.
Spectinomycin (50 μg/mL) inhibitsEscherichia coligrowth rapidly and reversibly, and suppresses amino acid incorporation immediately[1].
Spectinomycin (1 μg/mL or 3 μM) inhibits polypeptide synthesis directed either by endogenous messenger RNA or by MS-2 bacteriophage RNA, with maximum inhibition of 70-80% in extracts ofEscherichia coli[1].
Spectinomycin blocks the translocation of peptidyl-tRNAs from A-site to P-site by inhibiting the binding of elongation factor G to the ribosome[2].
Spectinomycin interacts specifically with the residues G1064 and 01192 in 16S rRNA and potentially makes it inactive[2].
Spectinomycin exhibits splicing inhibition and dependent on pH changes and Mg2+concentration, indicating electrostatic interactions with the intron RNA[3].
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体内研究
(In Vivo) | Spectinomycin (20 mg/kg; i.m.; 20-100 mg/kg; 9 d) shows the safety in healthy chicks[4].
Spectinomycin (10 mg/kg; i.v.; single dose) has the major elimination pathway by renal excretion, approximately 55% is excreted into the urine in unchanged form[5].
Pharmacokinetics of Spectinomycin in Rat[5]
| Parameter | C0(μg/mL) | AUC0-∞(μgoh/mL) | Vd(L/kg) | CL (L/h/kg) | MRT (h) | T1/2α(h) | T1/2β(h) | T1/2γ(h) | fe | CLrenal(L/h/kg) | Eratio | | Non atrioventricular analysis | 44.3 | 16.8 | 0.756 | 0.602 | 0.757 | / | / | / | 0.553 | 0.359 | 1.00 | | Three-compartment model | 37.8 | 15.7 | 0.747 | 0.649 | 1.11 | / | 0.237 | 0.754 | 19.5 | / | / |
| Animal Model: | Arbor Acres plus broiler chicks (15-day-old)[4] | | Dosage: | 20 mg/kg, 60 mg/kg, 100 mg/kg | | Administration: | Intramuscular injection (chest muscles); 9 days | | Result: | Showed biosecurity of 20 mg/kg by complete blood count, biochemical parameters, histopathological, clinical signs, body weight gain, and feed conversion ratio (FCR).
Resulted minor toxicity of 60 mg/kg. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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