| Description | Spiramycin (Rovamycin) is a macrolide antibiotic produced by Streptomyces ambofaciens. The drug is effective against gram-positive aerobic pathogens, N. gonorrhoeae, and staphylococci. It is used to treat infections caused by bacteria and Toxoplasma gondii. |
| In vivo | Spiramycin通过结合细菌50S 核糖体亚基而抑制易位。Spiramycin在易位过程中主要通过刺激peptidyl-tRNA从核糖体解离而发挥作用。Spiramycin降低潮霉素A对23S rRNA核苷酸的保护作用。Spiramycin对普氏菌属, 消化链球菌, 真细菌, Porphyromonas菌株和多形杆状菌,具有高效的抗菌活性,且甲硝唑可以增强Spiramycin效果。在30℃下Spiramycin足以抑制野生型细胞蛋白合成但不足以杀死突变型或野生型细胞。以Spiramycin和红霉素处理脂多糖刺激的人单核细胞,可增加总IL-6产量而不影响TNFα,IL-1 α或产生IL-1 β。Spiramycin以刺激peptidyl-tRNA从核糖体中解离的方式抑制蛋白合成。Spiramycin以剂量依赖性抑制脉冲宽度调制和聚羟基脂肪酸酯刺激的人单核白细胞增殖反应。Spiramycin还诱导氚化尿嘧啶核苷摄取降低,表明其干扰细胞周期的某个早期过程。 |
| Synonyms | Espiramicin, 螺旋霉素, Sequamycin, Rovamycin, Provamycin, Formacidine |
| molecular weight | 843.07 |
| Molecular formula | C43H74N2O14 |
| CAS | 8025-81-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 93 mg/mL (110.3 mM) Ethanol: 93 mg/mL (110.3 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) |
| References | 1. Poulsen SM, et al. J Mol Biol, 2000, 304(3), 471-481. 2. Brisson-Noël A, et al. J Antimicrob Chemother, 1988, 22, 13-23. 3. Menninger JR, et al. Antimicrob Agents Chemother, 1982, 21(5), 811-818. 4. Roche Y, et al. J Antimicrob Chemother, 1986, 17(2), 195-203. 5. Bailly S, et al. Antimicrob Agents Chemother, 1991, 35(10), 2016-2019. 6. Etewa SE, et al. Assessment of spiramycin-loaded chitosan nanoparticles treatment on acute and chronic toxoplasmosis in mice. J Parasit Dis. 2018 Mar;42(1):102-113. |