Antimicrobial activity and stability of the D-amino acid substituted derivatives of antimicrobial peptide polybia-MPI.
Antimicrobial activity and stability of the D-amino acid substituted derivatives of antimicrobial peptide polybia-MPI.
复制标题
抗菌肽polybia-MPI D-氨基酸取代衍生物的抗菌活性和稳定性
DOI:
10.1186/s13568-016-0295-8
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发表时间:
2016-12
期刊:
影响因子:
3.7
通讯作者:
Wang R
中科院分区:
文献类型:
--
作者:
Zhao Y;Zhang M;Qiu S;Wang J;Peng J;Zhao P;Zhu R;Wang H;Li Y;Wang K;Yan W;Wang R
Antimicrobial peptide has the potential to be developed as new kind of antimicrobial agents with novel action mechanism. However, the susceptibility to protease is a drawback for potential peptides to be clinical used. d-amino acid substitution can be one way to increase the proteolytic stability of peptides. In the present study, we synthesized the d-lysines substituted analog (d-lys-MPI) and the d-enantiomer of polybia-MPI (D-MPI) to improve the proteolytic resistance of polybia-MPI. Our results showed that, the stability of its d-amino acid partially substituted analog d-lys-MPI was increased. However, it lost antimicrobial activity at the tested concentration with the loss of α-helix content. As shown in the CD spectra, after substitution, the spectra of D-MPI is symmetrical to MPI, indicated it turned into left hand α-helical conformation. Excitingly, the stability of D-MPI toward the tested protease was improved greatly. Notably, the antimicrobial activity of D-MPI was comparable to its L-counterpart MPI, even improved. In addition, the hemolytic activity of D-MPI was lowered. This also indicated that the action target of antimicrobial peptide polybia-MPI was not chiral specific. So,
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影响因子:
3
作者:
Wang, Kai-rong;Zhang, Bang-zhi;Wang, Rui
通讯作者:
Wang, Rui
影响因子:
4.9
作者:
Wang, Kairong;Yan, Jiexi;Wang, Rui
通讯作者:
Wang, Rui
影响因子:
4
作者:
Marr, Alexandra K.;Gooderham, William J.;Hancock, Robert E. W.
通讯作者:
Hancock, Robert E. W.
影响因子:
4.9
作者:
Arnusch, Christopher J.;Ulm, Hannah;Shai, Yechiel
通讯作者:
Shai, Yechiel
DOI:
10.1016/j.bbrc.2013.09.021
发表时间:
2013-10-11
影响因子:
3.1
作者:
Choi, Hyemin;Hwang, Jae-Sam;Lee, Dong Gun
通讯作者:
Lee, Dong Gun