Cholate Conjugated Polymeric Amphiphiles as Efficient Artificial Ionophores

A family of amphiphilic copolymers containing hydrophobic cholate pendants has been prepared by copolymerization of cholic acid-based monomer 2-(methacryloxy)-ethyl cholate (MAECA) with polyethylene glycol methyl ether methacrylate (PEGMA). The polymers differ for the content of MAECA that increases from 0 to 35%. The copolymers partition within liposomes and display potent ionophoric activity forming large pores in the membrane and allowing the leakage of small inorganic ions (H+, Na+) and of large polar organic molecules (calcein). Their activity is strictly correlated to the content of cholic acid subunits, increasing as the fraction of cholate moiety increases.

Automated summary

A family of amphiphilic copolymers containing hydrophobic cholate pendants has been prepared, with potent ionophoric activity forming large pores in liposomes and allowing the leakage of small inorganic ions and large polar organic molecules. The activity is strictly correlated to the content of cholic acid subunits, increasing as the fraction of cholate moiety increases.