Howarth W R, Tewari R P, Solotorovsky M
Antimicrob Agents Chemother. 1975 Jan;7(1):58-63. doi: 10.1128/AAC.7.1.58.
The in vitro antifungal activity of amphotericin B methyl ester (AME), a water-soluble derivative of amphotericin B, was compared to that of the parent compound against a variety of pathogenic and potentially pathogenic fungi. AME has a significant antifungal activity, but the activity of AME was slightly lower than that of amphotericin B. Among the yeast-like organisms, only the yeast cells of Sporothrix schenckii were more resistant than others to both antibiotics, with a minimal fungicidal concentration of 5 to 10 mug/ml. The yeast cells of other fungi were killed at concentrations of 1 mug or less of either antibiotic per ml. The filamentous forms of S. schenckii and Oidiodendron kalrai were more resistant than the filamentous forms of other dimorphic fungi to both drugs. The minimal fungicidal concentration for S. schenckii was 10 mug/ml and for O. kalrai, 50 mug/ml. The dermatophytes, phycomycetes, and dematacious and other potentially pathogenic fungi were inhibited fairly well by both drugs, but up to 50 mug/ml was required for fungicidal action. The water solubility and wide spectrum of antifungal activity of AME warrant evaluation of its chemotherapeutic activity against experimental fungal infections.
两性霉素B甲酯(AME)是两性霉素B的一种水溶性衍生物,其体外抗真菌活性与母体化合物针对多种致病性和潜在致病性真菌的活性进行了比较。AME具有显著的抗真菌活性,但AME的活性略低于两性霉素B。在类酵母生物中,只有申克孢子丝菌的酵母细胞对这两种抗生素的耐药性比其他菌更强,其最低杀菌浓度为5至10微克/毫升。其他真菌的酵母细胞在每毫升1微克或更低浓度的任何一种抗生素作用下都会被杀死。申克孢子丝菌和卡氏帚霉的丝状形态比其他双相真菌的丝状形态对这两种药物的耐药性更强。申克孢子丝菌的最低杀菌浓度为10微克/毫升,卡氏帚霉为50微克/毫升。这两种药物对皮肤癣菌、藻菌、暗色真菌和其他潜在致病性真菌均有较好的抑制作用,但杀菌作用需要高达50微克/毫升的浓度。AME的水溶性和广泛的抗真菌活性谱值得评估其对实验性真菌感染的化疗活性。