Abu-Salah K M
Department of Biochemistry, King Saud University, Riyadh, Saudi Arabia.
Br J Biomed Sci. 1996 Jun;53(2):122-33.
Amphotericin B is the most important clinically and best defined chemically of the macrolide heptaene antibiotics. A fermentation product of the soil actinomycetes Streptomyces nodosus, amphotericin B binds selectively to ergosterol in the cell membrane of susceptible fungi, inducing changes in permeability that can produce lethal cell injury. Available since 1960, amphotericin B remains the treatment of choice for most serious systemic fungal infections. This review highlights some important aspects of the physicochemical properties of amphotericin B and their utilisation in its quantitative determination in biological fluids. Its mechanism of action is re-appraised in the light of recent results with regard to its effects on the physical and functional properties of synthetic and natural membranes. Attempts to reduce its toxic effects to host cells and to improve its therapeutic index are evaluated. In addition, the therapeutic values of amphotericin B, apart from its antibiotic activity, are discussed.
两性霉素B是临床上最重要且化学性质最明确的大环内酯类七烯抗生素。它是土壤放线菌结节链霉菌的发酵产物，能选择性地与易感真菌细胞膜中的麦角固醇结合，引起通透性改变，从而导致致命的细胞损伤。自1960年上市以来，两性霉素B仍然是大多数严重全身性真菌感染的首选治疗药物。本综述重点介绍了两性霉素B的一些重要物理化学性质，以及它们在生物体液定量测定中的应用。根据其对合成膜和天然膜的物理及功能特性影响的最新研究结果，对其作用机制进行了重新评估。评估了降低其对宿主细胞毒性作用并提高其治疗指数的尝试。此外，还讨论了两性霉素B除抗生素活性外的治疗价值。
