Patterson J, Holland J, Bieber L L
J Antibiot (Tokyo). 1979 Jun;32(6):646-53. doi: 10.7164/antibiotics.32.646.
The fractional change in the corrected fluorescence of pimaricin or filipin in the presence of a limiting amount of sterol and a competing polyene antibiotic has been used to estimate the relative affinity of amphotericin B, nystatin, filipin, and pimaricin for stigmasterol and for cholesterol. The relative affinities for cholesterol were filipin greater than amphotericin B greater than pimaricin greater than nystatin, while the relative affinities for stigmasterol were filipin greater than pimaricin greater than amphotericin B greater than nystatin. The data indicate that pimaricin and filipin can both interact simultaneously with about 30% of the cholesterol or stigmasterol. However, the stoichiometry of filipin and pimaricin alone for cholesterol and for stigmasterol in dilute aqueous solutions is 1 : 1. In the experiments which indicated both pimaricin and filipin interact with the same sterol molecule changes in corrected fluorescence and the absorbance spectra were monitored; and these criteria indicated that both pimaricin and filipin had interacted with the sterols. Light-scattering measurements indicate large aggregates were not formed. Although the data shows in dilute aqueous solutions the stoichiometry of filipin and/or pimaricin for sterols is 1 : 1, in more complex solutions, other combinations or interactions are indicated especially for pimaricin.
在存在限量甾醇和竞争性多烯抗生素的情况下，制霉菌素或菲律宾菌素校正荧光的分数变化已被用于估计两性霉素B、制霉菌素、菲律宾菌素和匹马菌素对豆甾醇和胆固醇的相对亲和力。对胆固醇的相对亲和力为：菲律宾菌素大于两性霉素B大于匹马菌素大于制霉菌素，而对豆甾醇的相对亲和力为：菲律宾菌素大于匹马菌素大于两性霉素B大于制霉菌素。数据表明，匹马菌素和菲律宾菌素都能与约30%的胆固醇或豆甾醇同时相互作用。然而，在稀水溶液中，仅菲律宾菌素和匹马菌素与胆固醇和豆甾醇的化学计量比为1:1。在表明匹马菌素和菲律宾菌素都与同一甾醇分子相互作用的实验中，监测了校正荧光和吸收光谱的变化；这些标准表明匹马菌素和菲律宾菌素都与甾醇相互作用。光散射测量表明没有形成大聚集体。尽管数据显示在稀水溶液中菲律宾菌素和/或匹马菌素与甾醇的化学计量比为1:1，但在更复杂的溶液中，特别是对于匹马菌素，表明存在其他组合或相互作用。
