关键词: 肽类化合物, MIC, 噬菌体肽库, 分子对接, Fmoc固相合成

Abstract: By inhibition experiments to determine the inhibitory effect of peptide compounds under different culture conditions, and measure theirs minimal inhibitory concentration（MIC）. Adding Vc to compare inhibitory effect and future optimize screening H₃₇Ra inhibitors. According to the results of ELISA test screen the phage peptide library, and then uses the Molecular docking software to simulate peptide docking with ICL protein crystal（1F8I）. The successful docking peptide uses the solid-phase synthesis method of Fmoc for synthesis, and tests its biological activity. By preparative reversed phase HPLC purifies the synthesized peptides and detects mass spectrometry. Four peptides were screened, all of which have bacteriostatic effect, and correlated with the dose. The results showed that when the concentration between 800 and 1 500 μg/mL all group were bacteriostat. When the concentration is 500 μg/mL, only one peptide has bacteriostatic effect in the normal medium, while all cannot inhibit in the limit carbon medium. The inhibitory effect of No.2 peptide is best, and its MIC is 200 μg/mL in normal culture, while it is 500 μg/mL in carbon limitations. Positive control group, two media’s inhibitory effect were consistent, RIF’s and INH’s MIC were 0.8 μg/mL and 0.5 μg/mL, respectively. According to MIC results, the inhibitory effects of peptide, RIF and INH were improved when adding Vc to the normal culture, and to be a dose-dependent increase.

Key words: Peptides, MIC, Phage peptide library, Molecular docking, Solid-phase synthesis method of Fmoc