The invention provides low molecular weight compounds that block the pore formed by protective antigen and inhibit anthrax toxin action. Structures of the compounds are derivatives of β-cyclodextrin. Per-substituted alkylamino derivates displayed inhibitory activity, and they were protective against anthrax lethal toxin action at low micromolar concentrations. Also, the addition of one of the alkylamino derivatives to the bilayer lipid membrane with multiple PA channels caused a significant decrease in membrane conductance. Thus, the invention also provides methods for protection against anthrax toxicity.
本发明提供的低分子量化合物可阻塞保护性抗原形成的孔隙,抑制
炭疽毒素的作用。这些化合物的结构是β-
环糊精的衍
生物。过取代的烷基
氨基衍
生物具有抑制活性,在低微摩尔浓度下对
炭疽致死毒素的作用具有保护作用。此外,在具有多个 PA 通道的双层脂膜中加入一种烷基
氨基衍
生物会显著降低膜传导性。因此,本发明还提供了防止
炭疽毒性的方法。