2.B.29 The Tambjamine Derivative Anion Channel (TD-AC) or
Anionophoric Marine Alkaloid Tambjamine (AMAT) Family
Soto-Cerrato et al. 2015 used two potent anionophore analogues of tambjamines to study the effects induced by these compounds at the cellular level. They showed that active anionophores, capable of facilitating the transmembrane transport of chloride and bicarbonate in model phospholipid liposomes, induce acidification of the cytosol and hyperpolarization of plasma cell membranes, the combined effects of which can be used against cancer stem cells (Soto-Cerrato et al. 2015).
The transmembrane anion transport activity of a series of synthetic molecules, based on the structure of tambjamine alkaloids, can be tuned by varying the lipophilicity of the receptor, with carriers within a certain log P value (n-octanol/water partition coefficient) range performing best (Saggiomo et al. 2012). These compounds transport Cl-, OH- and HCO3-, probably using an antiport mechanism; see Figure 10 in Gale et al. 2017 for the structures of effective derivatives.