Bafilomycin A1

具有多种生物活性的细菌代谢物；V-ATPases的抑制剂（N.crassa液泡膜中的Ki=0.5nM）；对V-ATPases的选择性是Na+/K+-、Ca2+-和H+-ATPases的1,000倍以上）；在100nM时抑制H-4-II-E细胞中的自噬体成熟和蛋白质降解；抑制氯喹诱导的原代CGN细胞凋亡；在100nM时降低SARS-CoV-2感染的VeroE6和Huh7细胞以及表达人ACE2的HEK293T细胞培养上清液中的病毒产量；在0.1mg/kg时降低感染SARS-CoV-2的ACE2转基因小鼠的肺RNA拷贝数和病毒性肺炎A bacterial metabolite with diverse biological activities; an inhibitor of V-ATPases (Ki = 0.5 nM in N. crassa vacuolar membranes); >1,000-fold selective for V-ATPases over Na+/K+-, Ca2+-, and H+-ATPases); inhibits autophagosome maturation and protein degradation in H-4-II-E cells at 100 nM; inhibits chloroquine-induced apoptosis in primary CGNs; reduces viral yield in the culture supernatant of SARS-CoV-2-infected Vero E6 and Huh7 cells, as well as HEK293T cells expressing human ACE2, at 100 nM; reduces lung RNA copy numbers and viral pneumonia in ACE2 transgenic mice infected with SARS-CoV-2 at 0.1 mg/kg.