TY - JOUR
T1 - The effects of metal ions on the cytotoxicity and selectivity of a histidine-containing lytic peptide
AU - Chen, Long
AU - Dong, Sijia
AU - Liang, Jun F.
PY - 2013/9
Y1 - 2013/9
N2 - The histidine-containing peptide L5C (PAWRHAFHWAWHMLHKAA) is a histidine-rich lytic peptide. Interactions of some divalent metal ions with peptide L5C and their effects on the cell lysis activity of the peptide were studied. The presence of Cu2+ caused a secondary structure change (from random coil to α-helix) which resulted in the loss of cell lysis activity in peptide L5C. Binding of Zn2+ to peptide L5C also reduced the lytic activity of the peptide but Zn2+ did not affect the secondary structure of the peptides. Instead, Zn2+ induced peptide L5C aggregation. Unlike Zn2+ and Cu2+, Mg2+ had no significant effect on the activity of peptide L5C. Further experiments revealed that formed ion-peptide L5C complexes were sensitive to pH and dissociated in acidic solutions. Peptide L5C demonstrated improved pH-selectivity in the presence of trace amount of Zn2+. This property of histidine-containing lytic peptides can be used to improve their therapeutic effectiveness in the treatment of cancers.
AB - The histidine-containing peptide L5C (PAWRHAFHWAWHMLHKAA) is a histidine-rich lytic peptide. Interactions of some divalent metal ions with peptide L5C and their effects on the cell lysis activity of the peptide were studied. The presence of Cu2+ caused a secondary structure change (from random coil to α-helix) which resulted in the loss of cell lysis activity in peptide L5C. Binding of Zn2+ to peptide L5C also reduced the lytic activity of the peptide but Zn2+ did not affect the secondary structure of the peptides. Instead, Zn2+ induced peptide L5C aggregation. Unlike Zn2+ and Cu2+, Mg2+ had no significant effect on the activity of peptide L5C. Further experiments revealed that formed ion-peptide L5C complexes were sensitive to pH and dissociated in acidic solutions. Peptide L5C demonstrated improved pH-selectivity in the presence of trace amount of Zn2+. This property of histidine-containing lytic peptides can be used to improve their therapeutic effectiveness in the treatment of cancers.
KW - Cancer treatment
KW - Histidine-rich
KW - Metal ions
KW - Peptide
KW - pH-selectivity
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U2 - 10.1007/s10989-013-9344-1
DO - 10.1007/s10989-013-9344-1
M3 - Article
AN - SCOPUS:84887435972
SN - 1573-3149
VL - 19
SP - 239
EP - 244
JO - International Journal of Peptide Research and Therapeutics
JF - International Journal of Peptide Research and Therapeutics
IS - 3
ER -