Bee Venom Component May Have Anti-Tumor Applications (Cancer)

Acid-activated melittin for targeted and safe antitumor therapy

Bioconjug Chem. 2018 Aug 27

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Melittin (MLT), as a natural active biomolecule, can penetrate the tumor cell membrane to play a role in cancer treatment, will attract more attention in the future development of anti-tumor drugs. The main com-ponent of natural bee venom MLT was modified by introducing pH-sensitive amide bond between the 2,3-dimethyl maleimide (DMMA) and the lysine (Lys) of MLT (MLT-DMMA). MLT and its corresponding modified peptide MLT-DMMA were used to anti-tumor and biocompatibility validation.

The biomaterial characteristics were tested by MALDI-TOF MS, 1H NMR, IUPAC and HPLC, cell viability, hemolytic and animal experiment safety evaluation. Compared with the primary melittin, the modified peptide showed decreased surface charge and low cytotoxicity in physiological conditions. Moreover, cell assays confirmed the acid-activated conversion of amide bond resulting in adequately safe during its delivery and timely antitumor activity in tumor lesions.

Thus, MLT-DMMA provided a feasible platform to improve the targeted and safe antitumor applications.