Researchers attached a small piece of the human antimicrobial peptide LL-37 to a biodegradable polymer (PLGA) to make tiny micelle particles that get into cancer cells more easily. In lab tests on four aggressive cancer cell lines, this new formulation reduced cell growth, movement, and invasion better than the peptide alone. The work is still at the cell‑culture stage and not ready for any DIY or clinical use.

LL-37, a well-known antimicrobial human peptide, is a cationic peptide that provides an important antimicrobial defense mechanism in damaged skin. Accumulating evidence indicates that LL-37 also displays an anticancer effect in colon cancer, gastric cancer, hematologic malignancy and oral squamous cell carcinoma. However, anticancer activity of LL-37 peptide fragment analogs has not been reported. Poor intercellular translocation may be one of the causes for this lack of observed anticancer activity. In this study, a LL-37 peptide fragment analog with cysteine at the N-terminus was conjugated with the biodegradable polymer, lactic acid/glycolic acid copolymer (PLGA), using the thiol group of cysteine. The purpose of this study was to improve the cell permeability of the peptide using a micellar system and then evaluate the anticancer activity. Cell proliferation, migration, and invasion assays were performed to evaluate the anticancer activity in four cancer cell lines with high metastasis, HM-1, B16/BL6, HeLa, and HepG2. The LL-37 fragment peptide analog-linked PLGA conjugate was shown to effectively inhibit cell proliferation, migration, and invasion and had increased cell permeability in all the cancer cell lines, compared with the peptide alone. These results suggested that LL-37 fragment peptide analog (CKR12)-linked PLGA conjugate micelles could be useful in the development of cancer therapeutics.