A number of synthetic amphiphiles have been prepared and found to form pores in liposomal bilayers or in vital microbial and mammalian membranes. The formation of pores by these structures led to the hypothesis that their effect on the bilayer might permit other molecules to be carried along or otherwise co-transported. We have studied the ability of tris(crown) amphiphiles that we call hydraphiles and shown that they enhance the efficacy of such antibiotics as erythromycin, kanamycin, rifampicin, and tetracycline. The hydraphile family is large and evidence will be presented that only certain representatives of this group are effective. In addition, tetrameric amphiphiles called pyrogallol[4]arenes form pores in bilayers, the sizes of which are controlled at least by the cholesterol content. The pores formed by these molecules are large and could, in principle, assist in the passage of relatively large molecules through membranes. The results of studies involving a family of pyrogallolarenes will be presented.

Enhancement of drug activity by synthetic amphiphilic pore-formers

247th National Meeting (2014)

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