Polymer form of antibacterial peptide
A technology of multimer and peptide trimer, which is applied in the direction of cationic antibacterial peptide, antibacterial drug, peptide preparation method, etc., can solve the problems of limited application and toxicity
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[0271] According to another aspect, the present invention relates to the preparation of formula [(U 1 )(U 2 )] n / 2 (C) n / 2 B m The preparation method of the peptide multimer of Z, wherein, U 1 and U 2 Each includes a peptide, and U 1 ≠ U 2 , n=2 x , wherein x=0 or a positive integer, m=1 or 0; comprising the following steps:
[0272] (i) providing at least one solid phase;
[0273] (ii) coupling at least a first amino acid Z to said solid phase;
[0274] (iii) optionally, linking at least one amino acid B to said coupled Z;
[0275] (iii) linking at least one protected amino acid C to Z or B; wherein C comprises at least two differentially protected groups;
[0276] (iv) removing the first protecting group from the attached amino acid C to expose the first reactive side chain;
[0277] (v) providing a first peptide U to said first reactive side chain of C 1 chain extension;
[0278] (vi) removing a second protecting group from the attached B amino acid to expose ...
Embodiment 1
[0343] The solid-phase peptide synthesis (SPPS) method of embodiment 1 multimer
[0344] (A) Synthesis of homodimer
[0345] The peptide synthesis method was adapted from Krajewski et al., (2004). Fluorenylmethoxycarbonyl (Fmoc) protected L amino acids and resins were purchased from Advanced Automated Peptide Protein TECHNOLOGIES, (AAPPTEC) (KY, US) and used with the following side chain protecting group: Lys (Fmoc) (only incorporated from C at the second residue at the end, for dimer synthesis), Arg(pbf), Lys(Boc), Tyr(But), Trp(Boc) and Fmoc-Lys(Boc)-Wang resins (replacing 0.72 mmol / g). Synthesis of dimers was performed by Fmoc chemistry on an Apex 396 (Advanced ChemTech).
[0346] Commercially available Fmoc-Boc-Lys-Wang resin was used as a starting point. Alternatively, coupling of the first amino acid to Wang resin was performed with 0.5M DIC (N,N'-diisopropylcarbodiimide). The next coupling reaction (or acylation) was performed with 0.5M HBTU / 0.5M HOBT / 2M DIEA in NM...
Embodiment 2
[0363] Example 2 Antibacterial Assay
[0364] The method for testing the antibacterial activity of antimicrobial peptides uses the complete kill procedure described below.
[0365] Preparation of test organisms
[0366] Test organisms were either reference cultures obtained from the American Type Culture Collection (ATCC) or clinical isolates obtained from the Pathology Department of Singapore General Hospital. All cultures used in this study were no more than 5 passages from source. Bacterial cultures were grown on trypticase soy agar (TSA) slants and yeast cultures were grown on Sabouraud dextrose agar (SDA) slants at 35°C for 16 hours. The organisms were harvested by centrifugation and washed twice at 20°C in pH 7.2 phosphate buffer (United States Pharmacopeia, USP).
[0367] Organisms used for detection
[0368] The following organisms were used in this study:
[0369] 1. Bacillus cereus ATCC 11778
[0370] 2. Candida albicans ATCC 10231
[0371] 3. Clinical Pseudom...
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