Objective: To study a new type of anti-brucella drug, in order to achieve the functional cure of brucellosis. Methods: In this paper, solid phase peptide synthesis (SPPS) and chemical reaction in liquid phase were used to synthesize and modify three cyclic peptides, namely cyclic OP11 peptide, triazole-butyl peptide and triazole-amyl peptide, according to the linear peptide structure of brucella infection inhibitor OP11. The stability of the target peptide was tested by dithiothreitol (DTT) and the antibacterial activity of the peptide was determined by Brucella ovis. Results: Brucella ovis was used to test the minimum inhibitory concentration (MIC) of the target peptide. The results showed that the MIC values of linear OP11 peptide, cyclic OP11 peptide, triazolamide peptide and triazolamide peptide were 1.281, 0.043, 0.059 and 0.052 μg/mL, respectively. In the presence of DTT, the disulfide bond in cyclic OP11 peptide could be reduced with a half-life of 8 h, while triazolbutaditide and triazolamyl peptide were stable to DTT. Conclusion: The modified cyclic OP11 peptide has the strongest inhibitory effect on Brucella melitensis, and the antibacterial activity of triazole-containing butypeptide and pentapeptide is second only to that of disulfide-containing cyclic OP11 peptide. In addition, peptides containing a triazole ring are more chemically stable than peptides containing a disulfide bond.
LYU Ya'nan
,
DUO Yilun
,
ZHAO Jiawei
,
DONG Zhiqiang
,
GUO Ye
. Synthesis modification and activity of Brucella infection inhibitors[J]. Journal of Baotou Medical College, 2024
, 40(5)
: 1
-5
.
DOI: 10.16833/j.cnki.jbmc.2024.05.001
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