Even after forty years of its discovery by Arima et al, surfactin, a potent lipopeptide biosurfactant, still attracts attention and fancy of the applied microbiologists and biotechnologists worldwide, mainly due to its versatile bioactive properties and potential industrial implications. Starting from its first invented characteristic as an inhibitor of fibrin clot formation coupled with its significant ability to reduce surface tension of water, it has been credited with antifungal, antiviral, antitumor, insecticidal and antimycoplasma activities. These properties of therapeutic and commercial importance and its recent use as an enhanced oil recovery and a bioremediation agent make it a truly versatile biomolecule, the commercial potential of which could not be fully realized, particularly as a therapeutic agent, mainly because of its hemolytic property. This chapter thus addresses the issues related to the versatile nature of the most studied microbial surfactant, surfactin and its potential commercial and health-care applications.