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Merck

Defined nanoscale chemistry influences delivery of peptido-toxins for cancer therapy.

PloS one (2015-06-02)
Santosh K Misra, Mao Ye, Sumin Kim, Dipanjan Pan
RESUMEN

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.

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Sigma-Aldrich
Tetrahidrofuran, anhydrous, ≥99.9%, inhibitor-free
Sigma-Aldrich
Tetrahidrofuran, anhydrous, contains 250 ppm BHT as inhibitor, ≥99.9%
Sigma-Aldrich
Melittin from honey bee venom, ≥85% (HPLC)
Supelco
Tetrahidrofuran, HPLC grade, ≥99.9%, inhibitor-free
Sigma-Aldrich
Melittin, ≥97% (HPLC), synthetic
Sigma-Aldrich
Melittin from honey bee venom, ≥65% (HPLC)