克林霉素

产品简介

Clindamycin 是一种具有口服活性的广谱抑菌林可酰胺类抗生素 (antibiotic)。Clindamycin 有效抑制细菌蛋白质合成，其具有以亚抑制浓度 (sub-MICs) 在金黄色葡萄球菌中毒力因子表达的能力。Clindamycin 的抗性是由 50S 核糖体亚基 (23S rRNA) 中抗生素结合位点的酶促甲基化产生。Clindamycin 降低杀白细胞毒素 (PVL)，毒性休克-葡萄球菌毒素 (TSST-1) 或 α-溶血素 (Hla) 的产生。Clindamycin 也可用于疟疾的研究。

体外研究：

Clindamycin is a semisynthetic analogue of lincomycin. Clindamycin primarily inhibits the initiation of peptide chain synthesis by deregulating enzyme-catalyzed initiation of peptide bounds. Clindamycin appears to have a modest effect on protein synthesis by certain mammalian cells. Clindamycin is active against most gram-positive aerobic bacteria. Clindamycin is about eight times more active than lincomycin against Staphylococcus aureus and Streptococcus pneumonia. Clindamycin is four times more active than erythromycin against S. aureus and is active even against strains that are resistant to erythromycin, penicillin, and methicillin. Clindamycin is active against gram-positive anaerobes. Clindamycin highly activates against Bacteroides specie. Clindamyci also alters the bacterial surface in such a way that phagocytosis and intracellular killing of the bacteria is greatly facilitated. Clindamycin potentiates opsonization and phagocytosis.

体内研究：

Clindamycin (50 mg/kg daily administrated by intramuscular) increases the survival rate of monkeys infected with penicillin-resistant S. aureu to 87.5% (7/8). [5] Clindamycin (40 mg/kg administrated three times daily) protects 87.5% (7/8) of rabbits from anaerobic pulmonary infections induced by transtracheal inoculation of a mixture of B. fragillis, Streptococcus morbillorm, Fusobacterium nucleatum and Eubacterium lentum. Clindamycin (400 mg/kg treated by mixed in the diet) increases survival rate of mice infected with the Toxoplasma gondii to 100%, while all animals die in untreated group.

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