Matsumori, Nobuaki published the artcileAmphotericin B Covalent Dimers Forming Sterol-Dependent Ion-Permeable Membrane Channels, Name: Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, the publication is Journal of the American Chemical Society (2002), 124(16), 4180-4181, database is CAplus and MEDLINE.
Polyenemacrolides such as amphotericin B (AmB) are thought to assemble together and form an ion channel across plasma membranes. Their antimicrobial activity has been attributed to this assemblage, whose stability and activity are dependent on sterol constituents of lipid bilayer membranes. The structure of this channel-like assemblage formed in biomembranes has been the target of extensive investigations for a long time. As the first step toward this goal, we prepared several AmB dimers with various linkers and tested their channel-forming activity. Among these, AmB dimers that bore an aminoalkyl-dicarboxylate tether covalently linked between amino groups of AmB showed potent hemolytic activity. Furthermore, K+ influx actions monitored by measuring the pH of the liposome lumen by 31P NMR revealed that the dimers formed a mol. assemblage similar to that of AmB in phospholipid membrane. Judging from changes in 31P NMR spectra, the dimers appeared to induce “all-or-none”-type ion flux across the liposome membrane in the presence of ergosterol, which suggests that the ion channel formed by ergosterol/dimer is similar to that of AmB. On the basis of this data, we are now trying to elucidate the structure of the ion-channel complex by making the labeled conjugates of AmB for NMR measurements.
Journal of the American Chemical Society published new progress about 70539-42-3. 70539-42-3 belongs to alcohols-buliding-blocks, auxiliary class pyrrolidine,Ester,Amide,Inhibitor,Inhibitor, name is Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, and the molecular formula is C18H20N2O12, Name: Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate.
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