Melittin, a major component of bee venom, is a water-soluble toxic peptide of which a various
biological effects have been identified to be useful in anti-tumor therapy. In addition, Melittin also
has anti-parasitic, anti-bacterial, anti-viral, and anti-inflammatory activities. Therefore, it is a very attractive
therapeutic candidate for human diseases. However, melittin induces extensive hemolysis, a severe
side effect that dampens its future development and clinical application. Thus, studies of melittin
derivatives and new drug delivery systems have been conducted to explore approaches for optimizing
the efficacy of this compound, while reducing its toxicity. A number of reviews have focused on each
side, respectively. In this review, we summarize the research progress on the anti-tumor effects of melittin
and its derivatives, and discuss its future potential clinical applications.