抗真菌剂两性霉素B的结构修饰

Structural modifi cations of an antifungal agent:amphotericin B

自两性霉素B作为抗真菌剂应用于临床以来,便受到了人们的广泛关注,目前仍为治疗全身或深部真菌病的首选药物。但其毒副作用,水溶性差等缺点存在,使得该抗生素的临床应用受到了一定的限制,因此开发新型两性霉素B衍生物具有重要的研究和应用价值,近年人们对两性霉素B进行了大量的结构修饰研究,并从中获得了一系列有价值的衍生物。本文对两性霉素B结构修饰的最新研究进展作了一个简要的综述,并重点对几个毒副作用明显降低的两性霉素B衍生物作了较为详细的介绍。

Amphotericin B（AMB） is a well-known antifungal agent since it has been used in clinic. However, the drawbacks of amphotericin B, such as toxicity and poor water solublility, limit the clinical application. Therefore, it is necessary to develop new amphotericin B derivatives. In recent years, lots of studies focused on the structural modifications of amphotericin B have been carried out and obtained a series of valuable derivatives. In this paper, the structural modifications of amphotericin B and their antifungal activities were reviewed, especially for some obviously less toxic derivatives.