Abstract
Scorpion venom peptides recently have attracted attention as alternative chemotherapeutic agents that may overcome the limitations of current drugs, providing specific cytotoxicity for cancer cells with an ability to bypass multidrug-resistance mechanisms, additive effects in combination therapy and safety. In the present study, 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) by screening assays with an IC50 value of 29 μg/ml. The BmKn-2 peptide killed HSC-4 cells through induction of apoptosis, as confirmed by phase contrast microscopy and RT-PCR techniques. Typical morphological features of apoptosis including cell shrinkage and rounding characteristics were observed in treated HSC-4 cells. The results were further confirmed by increased expression of pro-apoptotic genes such as caspase-3, -7, and -9 but 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 inhibition and apoptogenic activity against human oral cancer cells.
Highlights
It is very interesting in the use of natural toxin to develop safe and more effective therapeutic agents for cancer treatment (Possani et al, 1999; Liu et al, 2014)
We first report the effects of BmKn-2 and its eight derivatives peptides on oral cancer and its mechanisms of action
The susceptibility and selectivity of BmKn-2 against normal and cancer cells could be related to the presence of specific molecules on the cell surface
Summary
It is very interesting in the use of natural toxin to develop safe and more effective therapeutic agents for cancer treatment (Possani et al, 1999; Liu et al, 2014). Scorpion venom peptides have a vast variety of biological activities, immune-modulatory activities and pharmacological functions. The list of scorpion peptides have been expanding to display anti-proliferative and cytotoxic effects on tumor and malignant cells, and new substances are being continually added (Wang and Ji, 2005; Das Gupta et al, 2007; Fu et al, 2012). BmKn-2 is a cationic peptide which isolates from the venom of scorpion Mesobuthus martensii Karsch. In our previous study (Arpornsuwan et al, 2014), it has been shown that BmKn-2 inhibits the proliferation of several cancer cell types but has lower cytotoxicity to dental pulp stem cells and red blood cells
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