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Arginine Modification of Lycosin-I to Improve Inhibitory Activity Against Cancer Cells.


Lycosin-I is a linear amphipathic α-helical anticancer peptide (ACP) extracted from the spider Lycosa singoriensis, which can activate the mitochondrial death pathway to induce apoptosis in tumor cells and up-regulate p27 to inhibit cell proliferation. However, low cellular entry and efficacy in solid tumors limit the applicability of Lycosin-I as a novel anticancer drug. Amino acid substitution presents an effective and modest strategy to improve the anticancer activity and bioavailability of ACPs. We report here that an arginine modified Lycosin-I (named R-lycosin-I) was designed and synthesized by substituting lysine (Lys) with arginine (Arg). This peptide exhibited higher anticancer activity and penetrability against solid tumor cells than Lycosin-I. They displayed noticeable differences in their physicochemical properties, including secondary structure, hydrodynamic size and zeta potential. Fluorescent analyses confirmed R-lycosin-I can increase cellular uptake and improve intracellular distribution. Due to its superior physical and chemical properties and high serum stability, R-lycosin-I could penetrate deeply into tumor spheroids and produce strong toxicity in the 3D tumor model. Taken together, these findings suggest arginine substitution approach might provide an effective strategy for improving the anticancer activity of lycosin-I and R-lycosin-I might be a useful lead for developing anticancer drug.

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Publication details

The article was received on 05 Sep 2017, accepted on 10 Oct 2017 and first published on 12 Oct 2017

Article type: Paper
DOI: 10.1039/C7OB02233F
Citation: Org. Biomol. Chem., 2017, Accepted Manuscript
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    Arginine Modification of Lycosin-I to Improve Inhibitory Activity Against Cancer Cells.

    P. Zhang, J. Ma, Y. Yan, B. Chen, B. Liu, C. Jian, B. Zhu, S. P. Liang, Y. Zeng and Z. Liu, Org. Biomol. Chem., 2017, Accepted Manuscript , DOI: 10.1039/C7OB02233F

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