Spectinomycin dihydrochloride (Synonyms: 鹽酸奇霉素)
Spectinomycin dihydrochloride 是一種廣譜抗生sheng素，可以抑制多種革蘭氏陽性和革蘭氏陰性細菌的生長。Spectinomycin dihydrochloride 通過特異靶向細菌核糖體，干擾蛋白質合成。Spectinomycin dihydrochloride 也是 td 內含子 RNA 的非競爭性抑制劑，Ki 為 7.2 mM。
生物活性
Spectinomycin dihydrochloride is a broad-spectrum antibiotic and inhibits the growth of a variety of gram-positive and gram-negative organisms. Spectinomycin dihydrochloride acts by selectively targeting to the bacterial ribosome and interrupting protein synthesis. Spectinomycin dihydrochloride is also a noncompetitive inhibitor of td intron RNA with an Ki value of 7.2 mM[1]-[5].
IC50 & Target
bacterial ribosomal subunit[5]
體外研究(In Vitro)
Spectinomycin dihydrochloride selectively inhibits protein synthesis in cells and in extracts of Escherichia coli:
Spectinomycin dihydrochloride (50 μg/mL) inhibits Escherichia coli growth rapidly and reversibly, and suppresses amino acid incorporation immediately[1].
Spectinomycin dihydrochloride (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 of Escherichia coli[1][1].
Spectinomycin dihydrochloride 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 dihydrochloride interacts specifically with the residues G1064 and 01192 in 16S rRNA and potentially makes it inactive[2].
Spectinomycin dihydrochloride exhibits splicing inhibition and dependent on pH changes and Mg2+ concentration, indicating electrostatic interactions with the intron RNA[3].
體內研究(In Vivo)
Spectinomycin dihydrochloride (20 mg/kg; i.m.; 20-100 mg/kg; 9 d) shows the safety in healthy chicks[4].
Spectinomycin dihydrochloride (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 dihydrochloride in Rat[5]
| Parameter | C0 (μg/mL) | AUC0-∞ (μg•h/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. |
分子量：405.27
Formula：C14H26Cl2N2O7
CAS 號：21736-83-4
中文名稱：鹽酸奇霉素；鹽酸壯觀mei素
來源：bacterium Streptomyces spectabilis
運輸條件
Room temperature in continental US; may vary elsewhere.
儲存方式
4°C, sealed storage, away from moisture
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性數據
H2O : ≥ 100 mg/mL (246.75 mM)
* "≥" means soluble, but saturation unknown.
| 濃度溶劑體積質量 | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.4675 mL | 12.3375 mL | 24.6749 mL |
| 5 mM | 0.4935 mL | 2.4675 mL | 4.9350 mL |
| 10 mM | 0.2467 mL | 1.2337 mL | 2.4675 mL |
請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 儲存時，請在 6 個月內使用，-20°C 儲存時，請在 1 個月內使用。
參考文獻
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