Applications and evolution of melittin, the quintessential membrane active peptide

Guha, Shantanu; Ferrie, Ryan P.; Ghimire, Jenisha; Ventura, Cristina R.; Wu, Eric; Sun, Leisheng; Kim, Sarah Y.; Wiedman, Gregory; Hristova, Kalina; Wimley, Wimley C.

doi:10.1016/j.bcp.2021.114769

Cited by 67 publications

(70 citation statements)

References 265 publications

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“…The hemolysis of MEL decreases after phosphorylation [ 69 ] or modification of amino acid sequences to obtain MEL analogs [ 70 , 71 ] has been proved. The derived MEL peptides have been designed and developed to exert more desirable properties, such as lower hemolysis effects [ 72 , 73 , 74 ], enhanced therapeutic properties [ 75 , 76 ] and even controllable activation providing targeting ability to tumor tissue [ 70 , 77 ]. Substituting alanine for leucine drastically reduces the hemolytic activity on human red blood cells, which is only about 1–2% of the hemolytic activity of MEL, while the antibacterial activity remains equivalent to MEL [ 73 ].…”

Section: Delivery Vehicles For Melittinmentioning

confidence: 99%

Melittin-Based Nano-Delivery Systems for Cancer Therapy

et al. 2022

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Melittin (MEL) is a 26-amino acid polypeptide with a variety of pharmacological and toxicological effects, which include strong surface activity on cell lipid membranes, hemolytic activity, and potential anti-tumor properties. However, the clinical application of melittin is restricted due to its severe hemolytic activity. Different nanocarrier systems have been developed to achieve stable loading, side effects shielding, and tumor-targeted delivery, such as liposomes, cationic polymers, lipodisks, etc. In addition, MEL can be modified on nano drugs as a non-selective cytolytic peptide to enhance cellular uptake and endosomal/lysosomal escape. In this review, we discuss recent advances in MEL’s nano-delivery systems and MEL-modified nano drug carriers for cancer therapy.

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Section: Delivery Vehicles For Melittinmentioning

confidence: 99%

Melittin-Based Nano-Delivery Systems for Cancer Therapy

et al. 2022

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“…Melittin’s primary structure is amphipathic, having a more hydrophobic N -terminal half and a more hydrophilic C-terminal half. Its secondary structure varies according to its concentration in an aqueous solution: at low concentrations, it assumes a monomeric random coiled conformation, while at higher concentrations, it adopts an α-helical tetramer folding [ 75 , 76 ]. The adopted α-helix conformation is a helix-hinge-helix motif, with the first helix formed by residues—a hinge region formed by residues (glycine-X-proline motif), and the second helix formed by residues [ 77 , 78 , 79 , 80 ].…”

Section: Nanosystems and Nanocarriersmentioning

confidence: 99%

“…The adopted α-helix conformation is a helix-hinge-helix motif, with the first helix formed by residues—a hinge region formed by residues (glycine-X-proline motif), and the second helix formed by residues [ 77 , 78 , 79 , 80 ]. These molecular and structural characteristics are directly related to melittin binding and permeabilizing different cellular membranes [ 76 ].…”

Section: Nanosystems and Nanocarriersmentioning

confidence: 99%

Nanobiotechnology with Therapeutically Relevant Macromolecules from Animal Venoms: Venoms, Toxins, and Antimicrobial Peptides

et al. 2022

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Some diseases of uncontrolled proliferation such as cancer, as well as infectious diseases, are the main cause of death in the world, and their causative agents have rapidly developed resistance to the various existing treatments, making them even more dangerous. Thereby, the discovery of new therapeutic agents is a challenge promoted by the World Health Organization (WHO). Biomacromolecules, isolated or synthesized from a natural template, have therapeutic properties which have not yet been fully studied, and represent an unexplored potential in the search for new drugs. These substances, starting from conglomerates of proteins and other substances such as animal venoms, or from minor substances such as bioactive peptides, help fight diseases or counteract harmful effects. The high effectiveness of these biomacromolecules makes them promising substances for obtaining new drugs; however, their low bioavailability or stability in biological systems is a challenge to be overcome in the coming years with the help of nanotechnology. The objective of this review article is to describe the relationship between the structure and function of biomacromolecules of animal origin that have applications already described using nanotechnology and targeted delivery.

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“…Мелиттин образован 26 остатками аминокислот. В водной среде он формирует амфифильный тетрамер, что придает ему свойства катионного детергента с высокой поверхностной активностью [5]. В предыдущих исследованиях описаны противовирусные, антибактериальные, противогрибковые, противопаразитарные и противоопухолевые свойства мелиттина, и на данный момент считается, что главный эффект этого вещества как неселективного цитолитического пептида заключается в физическом и химическом разрушении всех прокариотических и эукариотических клеточных мембран [6][7][8][9][10].…”

Section: Introductionunclassified

Impact of Honeybee Venom Melittin on Cell Viability of Different Prostate Cancer Lineages

Khalikov

Gromenko

Galimova

et al. 2022

Kreativnaâ hirurgiâ i onkologiâ

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Background. Melittin is a major constituent of honeybee venom and comprises a water-soluble surfactant peptide with cytolytic effects potentially applicable in anticancer therapy. We evaluated the impact of melittin from Bashkir honeybee (Apis mellifera mellifera L.) venom on cell viability of various prostate cancer lineages.Materials and methods. MTT assays with cell viability index estimation were used to evaluate the effect of melittin on cell proliferation in various-grade malignancy prostate cancer (PC) lineages, LNCaP, PC-3 and DU145.Results and discussion. Lineage DU145 revealed a low sensitivity to melittin, because a relatively high peptide concentration of 10 μg/mL had a suppressive effect on its proliferation. With PC-3 cells, a 0.1 μg/mL concentration suppressed proliferation significantly to 46.15 %, while melittin at a 10 μg/mL dose had a cytolytic effect on most cells (4.27 % viability). LNCaP cells experienced the lowest toxicity at 10 μg/mL melittin compared to PC-3 and DU145 lineages. The LNCaP, PC-3 and DU145 PC lineages demonstrated suppressed proliferation at melittin levels 0.01–100 μg/mL.Conclusion. The study reveals a significant reduction of the PC lineages viability at a minimal melittin concentration of 0.01 μg/mL, which indicates a high cytolytic activity of this peptide and renders it a candidate agent in antitumour therapy.

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Applications and evolution of melittin, the quintessential membrane active peptide

Cited by 67 publications

References 265 publications

Melittin-Based Nano-Delivery Systems for Cancer Therapy

Melittin-Based Nano-Delivery Systems for Cancer Therapy

Nanobiotechnology with Therapeutically Relevant Macromolecules from Animal Venoms: Venoms, Toxins, and Antimicrobial Peptides

Impact of Honeybee Venom Melittin on Cell Viability of Different Prostate Cancer Lineages

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