Macrolide antibiotics have been widely used in clinic due to their good antibacterial effects and high safety, but the drug-resistant bacteria appear constantly. To solve the problem of drug resistance in pathogens, s...Macrolide antibiotics have been widely used in clinic due to their good antibacterial effects and high safety, but the drug-resistant bacteria appear constantly. To solve the problem of drug resistance in pathogens, scholars obtain the third generation of macrolide antibiotics, ketolide antibiotics, which are developed by modifying the structure of macrolide antibiotics, thereby efficiently solving the problem. Ketolide antibiotics are a type of erythromycin derivatives with macrolide structure, and the typical drugs mainly include telithromycin, cethromycin and solithromycin, etc . This paper briefly introduced the recent progress of ketolide antibiotics, with an attempt to provide help to the research and development of new macrolide antibiotics.展开更多
Our results show that in liver microsomes from erythromycin,acetylspiramycin and dexamethsone pretreated rats,the rate of praziquantel( PQT)disappearence was increased as compared with control rat When microsomes fro...Our results show that in liver microsomes from erythromycin,acetylspiramycin and dexamethsone pretreated rats,the rate of praziquantel( PQT)disappearence was increased as compared with control rat When microsomes from erythromycin-treated rats were exposed to PQT in the presence of potassium ferricyanide which broke down the cytochrome P-450 Fe(Ⅱ)-metabolite complexes and restored the functional cytochrome P-450,PQT metabolism was further increased. Acetylspiramycin did not form the complexes, so potassium ferricyanide showed no effect on the PQT metabolism in microsomes from acetylspiramycin-treated rats. Triacetyloleandomycin,a specific inhibitor of cytochrome P-450ⅢAI, inhibited PQT metabolism by 53% in liver microsomes from dexamethasone-treated rats.These results indicate the cytochrome P-450ⅢA seems to be involved in metabolism of PQT in rat liver microsomes.展开更多
基金Supported by National Sci-tech Support Plant during Twelfth Five-Year Plan(2015BAD1101)Earmarked Fund for China Agriculture Research System(CAR-38)~~
文摘Macrolide antibiotics have been widely used in clinic due to their good antibacterial effects and high safety, but the drug-resistant bacteria appear constantly. To solve the problem of drug resistance in pathogens, scholars obtain the third generation of macrolide antibiotics, ketolide antibiotics, which are developed by modifying the structure of macrolide antibiotics, thereby efficiently solving the problem. Ketolide antibiotics are a type of erythromycin derivatives with macrolide structure, and the typical drugs mainly include telithromycin, cethromycin and solithromycin, etc . This paper briefly introduced the recent progress of ketolide antibiotics, with an attempt to provide help to the research and development of new macrolide antibiotics.
文摘Our results show that in liver microsomes from erythromycin,acetylspiramycin and dexamethsone pretreated rats,the rate of praziquantel( PQT)disappearence was increased as compared with control rat When microsomes from erythromycin-treated rats were exposed to PQT in the presence of potassium ferricyanide which broke down the cytochrome P-450 Fe(Ⅱ)-metabolite complexes and restored the functional cytochrome P-450,PQT metabolism was further increased. Acetylspiramycin did not form the complexes, so potassium ferricyanide showed no effect on the PQT metabolism in microsomes from acetylspiramycin-treated rats. Triacetyloleandomycin,a specific inhibitor of cytochrome P-450ⅢAI, inhibited PQT metabolism by 53% in liver microsomes from dexamethasone-treated rats.These results indicate the cytochrome P-450ⅢA seems to be involved in metabolism of PQT in rat liver microsomes.
