BmKn-2 Scorpion Venom Peptide for Killing Oral Cancer Cells by Apoptosis

Abstract

Scorpion venom peptides recently have attracted attention as alternative chemotherapeutic agents thatmay overcome the limitations of current drugs, providing specific cytotoxicity for cancer cells with an abilityto bypass multidrug-resistance mechanisms, additive effects in combination therapy and safety. In the presentstudy, BmKn-2 scorpion venom peptide and its derivatives were chosen for assessment of anticancer activities.BmKn-2 was identified as the most effective against human oral squamous cells carcinoma cell line (HSC-4) byscreening assays with an IC50 value of 29 μg/ml. The BmKn-2 peptide killed HSC-4 cells through induction ofapoptosis, as confirmed by phase contrast microscopy and RT-PCR techniques. Typical morphological featuresof apoptosis including cell shrinkage and rounding characteristics were observed in treated HSC-4 cells. Theresults were further confirmed by increased expression of pro-apoptotic genes such as caspase-3, -7, and -9but decrease mRNA level of anti-apoptotic BCL-2 in BmKn-2 treated cells, as determined by RT-PCR assay.In summary, the BmKn-2 scorpion venom peptide demonstrates specific membrane binding, growth inhibitionand apoptogenic activity against human oral cancer cells.