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.
)