The current landscape of the antimicrobial peptide melittin and its therapeutic potential

Abstract

Melittin, a main component of bee venom, is a cationic amphiphilic peptide with a linear α-helix structure. It has been reported that melittin can exert pharmacological effects, such as antitumor, antiviral and anti-inflammatory effects in vitro and in vivo. In particular, melittin may be beneficial for the treatment of diseases for which no specific clinical therapeutic agents exist. Melittin can effectively enhance the therapeutic properties of some first-line drugs. Elucidating the mechanism underlying melittin-mediated biological function can provide valuable insights for the application of melittin in disease intervention. However, in melittin, the positively charged amino acids enables it to directly punching holes in cell membranes. The hemolysis in red cells and the cytotoxicity triggered by melittin limit its applications. Melittin-based nanomodification, immuno-conjugation, structural regulation and gene technology strategies have been demonstrated to enhance the specificity, reduce the cytotoxicity and limit the off-target cytolysis of melittin, which suggests the potential of melittin to be used clinically. This article summarizes research progress on antiviral, antitumor and anti-inflammatory properties of melittin, and discusses the strategies of melittin-modification for its future potential clinical applications in preventing drug resistance, enhancing the selectivity to target cells and alleviating cytotoxic effects to normal cells.

Clickable tryptophan modification for late-stage diversification of native peptides

“…Melittin is a short bioactive peptide containing 26 amino acids (sequence H -GIGAVLKVLTTGLPALISWIKRKRQQ- NH 2 ) found from the venom of honeybee, which accounts for 40 to 60% dry weight of the venom ( 72 , 73 ). Apart from causing pain sensation, the bioactivity of melittin includes antibacterial, antiviral, antifungal, antiparasitic, and anticancer effects ( 74 ). The anticancer activities of melittin have been demonstrated in melanoma, non–small cell lung cancer, leukemia, ovarian cancer, cervical cancer, glioblastoma, and pancreatic cancer ( 75 ).…”

Bioactive Peptides and Protein Hydrolysates Used in Meat and Meat Products’ Preservation─A Review

“…69 Melittin, another interesting peptide, is a 26-residue peptide and the major component of bee (Apis mellifera) venom. 70 It is known for its antibacterial activity and other biological properties, such as antiviral and anticancer activity. Melittin exerts its antibacterial activity by forming pores in the bacterial cell membrane, disrupting cellular homeostasis and, eventually, bacterial death.…”

“…Melittin, another interesting peptide, is a 26-residue peptide and the major component of bee ( Apis mellifera ) venom . It is known for its antibacterial activity and other biological properties, such as antiviral and anticancer activity.…”

Emerging Cationic Nanovaccines

“…Interestingly, the self-assembly of the antimicrobial peptide α-melittin yielding NPs evolved as a simple and effective approach against tumor cells; tumor cells were sensitive to α-melittin-NPs, which killed them and promoted the release of whole tumor-cell antigens in situ; furthermore, αmelittin-NPs drained into LNs and activated macrophages and DC after subcutaneous injection; thereafter, the activated effector T cells went to the circulation reaching the tumor and killing their target cancer cells; these NPs also induced the infiltration of innate immune cells such as NK cells and monocytes [206]. Melittin, a main component of bee venom, is a cationic amphiphilic peptide with a linear α-helix structure with antitumor, antiviral and anti-inflammatory effects in vitro and in vivo as comprehensively reviewed recently [207]. In fact, the potential of antimicrobial peptides and their assemblies shaped as NPs requires further investigations for the benefit of cancer immunotherapy [208,209].…”