Abstract
We present an in-silico-to-in-vitro approach to develop well-defined, self-assembled, rigid-cored polymeric (Polybee) nano-architecture for controlled delivery of a key component of bee venom, melittin. A competitive formulation with lipid-encapsulated (Lipobee) rigid cored micelle is also synthesized. In a series of sequential experiments, we show how nanoscale chemistry influences the delivery of venom toxins for cancer regression and help evade systemic disintegrity and cellular noxiousness. A relatively weaker association of melittin in the case of lipid-based nanoparticles is compared to the polymeric particles revealed by energy minimization and docking studies, which are supported by biophysical studies. For the first time, the authors’ experiment results indicate that melittin can play a significant role in DNA association-dissociation processes, which may be a plausible route for their anticancer activity.
Highlights
Host defense peptides (HDPs) are a class of evolutionarily conserved substances of the innate immune response that are recognized as chief players in the defense system found among all classes of life
In a series of sequential experiments, we studied how nanoscale chemistry influences the delivery of venom toxins for cancer regression and helps evade systemic disintegrity and cellular noxiousness
Our experimental and computational results indicated that Polybees were better cancer cell growth inhibitors than Lipobees in two breast cancer cell lines, presumably due to their stable and tighter association with melittin
Summary
Host defense peptides (HDPs) are a class of evolutionarily conserved substances of the innate immune response that are recognized as chief players in the defense system found among all classes of life. They are usually amphipathic, have a net positive charge (generally +2 to +9) and are short in sequence (10–100 aa); HDPs have recently been explored for their anticancer property [1,2,3,4]. A cationic amphipathic peptide made up of 26 amino acid (aa) residues, has been found to be a potent component of bee venom Apis mellifera [6]. It has PLOS ONE | DOI:10.1371/journal.pone.0125908 June 1, 2015
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