Please use this identifier to cite or link to this item: http://hdl.handle.net/10397/10500
Title: A novel analog of antimicrobial peptide Polybia-MPI, with thioamide bond substitution, exhibits increased therapeutic efficacy against cancer and diminished toxicity in mice
Authors: Zhang, W
Li, J
Liu, LW
Wang, KR
Song, JJ
Yan, JX
Li, ZY
Zhang, BZ
Wang, R
Keywords: Anticancer
Antimicrobial peptide
Enzymatic stability
Thioamide
Toxicity
Issue Date: 2010
Publisher: Elsevier Science Inc
Source: Peptides, 2010, v. 31, no. 10, p. 1832-1838 How to cite?
Journal: Peptides 
Abstract: Polybia-MPI (MPI), a short cationic α-helical antimicrobial peptide, exhibited excellent anticancer activity and selectivity in vitro in our previous studies. To improve its in vivo application, we synthesized an analog (MPI-1) of MPI by replacing the C terminal amide -[CO-NH2] with thioamide -ψ[CS-NH2]. Although there is just one atom difference, the MPI-1 exhibited some surprising properties. In vitro studies revealed that MPI-1 exhibited relatively high lytic activity over MPI, whereas its stability to enzymatic degradation in serum was improved remarkably. Despite the enhanced toxicity in vitro, MPI-1 exhibited significantly lower mortality to mice than MPI at 75 mg/kg. Importantly, in vivo anticancer activity study indicated that MPI-1 could remarkably suppress the growth of sarcoma xenograft tumors more efficiently than MPI. Therefore, the significantly improved anticancer activity and predominantly lower in vivo toxicity might allow MPI-1 to be a good candidate for future anticancer treatment.
URI: http://hdl.handle.net/10397/10500
DOI: 10.1016/j.peptides.2010.06.019
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