Channels formed by amphotericin B covalent dimers exhibit rectification
Minako Hirano1, Yuko Takeuchi, Nobuaki Matsumori
1Laboratory for Cell Dynamics Observation, Planning Office for the Center for Computational and Quantitative Life Science, RIKEN, 7th Floor, Nanobiology Building, 1-3, Yamadaoka, Suita, Osaka 565-0871, Japan.
Abstract:
Amphotericin B (AmB) is a widely used antifungal antibiotic with high specificity for fungi. We previously synthesized several covalently conjugated AmB dimers to clarify the AmB channel structure. Among these dimers, that with an aminoalkyl linker was found to exhibit potent hemolytic activity. We continue this work by investigating the channel activity of the dimer, finding that all channels comprised of AmB dimers show rectification. The direction of the dimer channel in the membrane depended on the electric potential at which the dimer channel was formed. On the other hand, only about half the monomer channels showed rectification. In addition, these channels were easily switched from a rectified to a nonrectified state following voltage stimulation, indicating instability. We propose a model to describe the AmB channel structure that explains why AmB dimer channels necessarily show rectification.
More Related Videos
Related Concept Videos
Antifungal Agents
Regioselectivity and Stereochemistry of Acid-Catalyzed Hydration
Pore Transport and Ion-Pair Transport
Pore transport, also known as convective transport, is a process where small molecules like urea, water, and sugars rapidly cross cell membranes as though there were channels or pores in the membrane. Although direct microscopic evidence is limited but the concept of pores or channels is widely accepted based on physiological evidence. Despite the lack of direct microscopic...
Basicity of Heterocyclic Aromatic Amines
Stereoisomerism
Isomers are different chemical species that have the same chemical formula.
Transition metal complexes often exist as geometric isomers, in which the same atoms are connected through the same types of bonds but with differences in their orientation in space. Coordination complexes with two different ligands in the cis and trans positions from a ligand of interest form isomers. For example, the octahedral [Co(NH3)4Cl2]+ ion has two isomers (Figure 1) In the cis...
Valence Bond Theory


