Journal Article10.1080/14712598.2022.2088277
Bio-nano scale modifications of melittin for improving therapeutic efficacy
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TL;DR: Melittin-nanoconjugation may be one of the best-optimized strategies for improving peptide delivery, increasing its therapeutic efficacy, and providing minimal nonspecific cellular lytic activity.
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Abstract: ABSTRACT Introduction Melittin (MLT), a natural membrane-active component, is the most prominent cytolytic peptide from bee venom. Remarkable biological properties of MLT, including anti-inflammatory, antimicrobial, anticancer, anti-protozoan, and antiarthritic activities, make it an up-and-coming therapeutic candidate for a wide variety of human diseases. Therapeutic applications of MLT may be hindered due to low stability, high toxicity, and weak tissue penetration. Different bio-nano scale modifications hold promise for improving its functionality and therapeutic efficacy. Areas covered In the current review, we aimed to provide a comprehensive insight into strategies used for MLT conjugations and modifications, cellular delivery of modified forms, and their clinical perspectives by reviewing the published literature on PubMed, Scopus, and Google Scholar databases. We also emphasized the MLT structure modifications, mechanism of action, and cellular toxicity. Expert opinion Developing new analogs and conjugates of MLT as a natural drug with improved functions and fewer side effects is crucial for the clinical translation of this approach worldwide, especially where the chemicals and synthetic drugs are more expensive or unavailable in the healthcare system. MLT-nanoconjugation may be one of the best-optimized strategies for improving peptide delivery, increasing its therapeutic efficacy, and providing minimal nonspecific cellular lytic activity.
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References
Barrel-Stave Model or Toroidal Model? A Case Study on Melittin Pores
TL;DR: It is concluded that, among naturally produced peptides that are investigated, only alamethicin conforms to the barrel-stave model, and other peptides, including magainins, melittin and protegrins, all appear to induce transmembrane pores that conform to the toroidal model.
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TL;DR: Understanding of the characteristics of nanoparticles and their interactions with the biological environment will enable us to establish novel strategies for the treatment, prevention, and diagnosis in many diseases, particularly untreatable ones.
Melittin : a membrane-active peptide with diverse functions
TL;DR: The solution and membrane properties ofmelittin are highlighted, with an emphasis on melittin–membrane interaction using biophysical approaches, and the recent applications of melitt in various cellular processes are discussed.
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Toroidal pores formed by antimicrobial peptides show significant disorder.
TL;DR: It is found that peptide aggregation, either prior or after binding to the membrane surface, is a prerequisite to pore formation, and transmembrane pores spontaneously form above a critical peptide to lipid ratio.
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