The constant demand for new, effective therapeutic agents has triggered intensive research in the field of diverse antimicrobials of natural origin. These compounds are synthesized by all forms of life and have important biomedical and biotechnological properties, and are thus widely considered a potential solution to the growing problem of resistance to conventional antibiotics, fungal infection and life-threatening diseases. Among these molecules, lipopeptides represent a unique class of bioactive secondary metabolites with increasing scientific, therapeutic and biotechnological interest. The principal representative of the anionic lipopeptide family is surfactin, which is produced by bacterium Bacillus subtilis. This most potent known biosurfactant (i.e. surface-active compound of microbial origin), was named surfactin due to its exceptional surface activity. Since its discovery (Arima et al., 1968) and the identification of its molecular structure as a macrolide lipopeptide (Kakinuma et al., 1969) it has been best recognized for its high amhiphilicity and strong tendency for self-aggregation (Ishigami et al., 1995). Due to these characteristics it shows remarkable surface-, interfaceand membrane-active properties, resulting in a number of promising biological activities, which are of great relevance in health care and biotechnology. These properties make surfactin a candidate drug for the resolution of a number of global issues in medicine (Banat et al., 2010; Cao et al., 2010), industry (Nitschke & Costa, 2007; Abdel-Mawgoud et al., 2008) and environmental protection (Mulligan, 2009).