Jordan G W, Seet E C
Antimicrob Agents Chemother. 1978 Feb;13(2):199-204. doi: 10.1128/AAC.13.2.199.
The methyl ester of amphotericin B (AME) is water soluble, retains antifungal activity, and is significantly less toxic in mammals than amphotericin B. In contrast to amphotericin B, which is not water soluble, AME exhibits antiviral effects against vesicular stomatitis virus, herpes simplex virus types 1 and 2, Sindbis virus, and vaccinia virus in a plaque reduction assay. No antiviral effects could be demonstrated against the unenveloped adenovirus type 4 or echovirus type 11. The extent of virus inactivation was found to be dependent upon the AME concentration, contact time, and temperature. No consistent effect of the virus concentration on the probability of plaque-forming unit inactivation could be determined. The antiviral effects of AME were partially antagonized by the presence of serum. Binding of AME to vesicular stomatitis virus was demonstrated by the comigration of drug and virus in linear sucrose gradients. AME represents a new class of antiviral agents with activity at concentrations relevant to therapeutics. Sterol components of the host cell membrane that become incorporated into the viral envelope are postulated as the site of reaction with AME.
两性霉素B甲酯(AME)可溶于水,保留抗真菌活性,并且在哺乳动物中的毒性明显低于两性霉素B。与不溶于水的两性霉素B不同,AME在蚀斑减少试验中对水泡性口炎病毒、1型和2型单纯疱疹病毒、辛德毕斯病毒和痘苗病毒具有抗病毒作用。对无包膜的4型腺病毒或11型艾柯病毒未显示出抗病毒作用。发现病毒失活程度取决于AME浓度、接触时间和温度。无法确定病毒浓度对蚀斑形成单位失活概率的一致影响。血清的存在部分拮抗了AME的抗病毒作用。通过药物和病毒在线性蔗糖梯度中的共同迁移证明了AME与水泡性口炎病毒的结合。AME代表了一类新的抗病毒药物,在与治疗相关的浓度下具有活性。宿主细胞膜中掺入病毒包膜的甾醇成分被假定为与AME反应的位点。