Design, Synthesis, and Biological Evaluation of Novel Cholesteryl Peptides with Anticancer and Multidrug Resistance-Reversing Activities

Antimicrobial peptides have been suggested as promising chemotherapeutics for cancer therapy due to their efficient antitumor activity and lower toxicity to benign cells. In previous study, we find the peptide B1 presents specific cytotoxicity to cancer cells. As hydrophobicity plays a pivotal role in the anticancer activity of peptide, we introduce cholesterol-like moiety (3β-amino-5-cholestene) to the N-terminus of B1 expect to ameliorate the anticancer activity of B1. Biological evaluations revealed that target peptides show improved anticancer activity. The peptides can also penetrate into the cytoplasm and activating mitochondria-cytochrome c apoptosis pathway. Besides, the peptides acted on multidrug-resistant cells and had multidrug resistance-reversing activity. It is therefore suggested these peptides might be promising candidates for oncotherapy.