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Synthesis of Derivatives of Natural Product (+)-Brefeldin A and Study of Their Activities

Abstract

布雷菲徳菌素A((+)-BrefeldinA,简称BFA),是一种大环内酯类抗生素,它具有多种生物活性,如抗真菌、抗病毒、抗线虫和抗肿瘤等。但是作为一种抗癌候选药物,本身却具有一些“先天”不足,如在生物体内的半衰期短,生物利用率低,水溶性脂溶性差等。因此开发和研究(+)-BrefeldinA衍生物的工作具有重要意义。 (+)-BrefeldinA是极其昂贵的生化试剂,从外国公司购买,价格约为1.5万美元/克,这是一般研究项目难以负担的,本论文使用具有自主知识产权,来自福建自产的青霉SHZK-15菌种对(+)-BrefeldinA进行放大量生产实验研究,使其达到“克级”BFA生产技术,为后续研...(+)-Brefeldin A, a macrocyclic lactone antibiotic, possesses various biological activities including antiviral, antifungal, nematocidal and antitumor effects. However, as a potential anti-cancer drug, (+)-Brefeldin A is severely limited by its undesirable pharmacokinetic properties including negligible bioavailability after oral administratio -n and rapid clearance from the blood plasma after int...学位:理学硕士院系专业:化学化工学院_有机化学学号:2052007115102

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