Metal complexes with biological activity are of increasing importance in medicine as potential alternatives for biologically active organic compounds, which often show severe side effects. Metal complexes of amphiphilic character (metallosurfactants) exhibit very interesting properties, however, their potential for biological and medicinal applications have not yet been brought into effective action. The use of metallosurfactants in the field of materials science has been recently reviewed [1,2], but there is no such summary in the field of bioinorganic chemistry, biology or medicine. Here we provide an overview of the interactions of amphiphilic metal complexes with DNA and proteins, comprising binding and cleavage of these biomolecules, as well as antibacterial, antifungal, anthelmintic and antitumor properties. The structural motifs that metallosurfactants usually have in common are long alkyl chains (hydrophobic part) and metal ions coordinating mostly to ligands with nitrogen donors (hydrophilic part). The investigation of amphiphilic metal complexes for biological applications is a new and current research field, suggested by the fact that publication activity for this topic started as recently as in the 2000s with the exception of only a few earlier publications.