Small molecule peptides and their uses
A technology of small molecule polypeptides and amino acids, which can be used in peptides, medical preparations containing active ingredients, depsipeptides, etc., can solve problems such as frequent drug resistance, achieve good antiparasitic activity, obvious application potential, and synthetic methods. easy effect
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Embodiment 1
[0015] A small molecular polypeptide, the amino acid sequence of the small molecular polypeptide is shown in SEQ ID No.1;
[0016] SEQ ID No. 1: RSSTDDDRNKFYQEYVSTWCQT.
[0017] The isoelectric point of the small molecule polypeptide is 4.5.
[0018] The molecular weight of the small molecule polypeptide is 2729.88g / mol.
[0019] The preparation method of the small molecule polypeptide:
[0020] Choose amino acid-King resin as the carrier (resin), fully swell the resin with dichloromethane, add the first Fmoc-protected amino acid, wash it several times with dimethylformamide, and use an appropriate concentration of DBLK to remove the Fmoc-protecting group Then, wash it several times with dimethylformamide, wash away DBLK, weigh the appropriate condensing agent benzotriazole-N,N,N',N'-tetramethyluronium hexafluorophosphate and activate reagent methylmorpholine and the second Fmoc-protected amino acid (Fmoc-Ser-OH) at the C-terminus (Fmoc-Ser-OH) for coupling, and detected by...
Embodiment 2
[0022] 1. Experimental method
[0023] Add 1mL concentration of 1×10 to a sterilized test tube 6 1 mg of the small molecule polypeptide provided by the present invention was added to each / mL bacterial liquid, and after culturing at 37°C for 24 hours, the culture medium was collected and diluted in multiples, the dilution factor was 10 times, and the number of viable bacteria was detected by the coating culture method.
[0024] 2. Experimental results:
[0025] Table 1 The bactericidal rate (%) of the small molecule polypeptide of the present invention
[0026] bacteria ATCC 6538 ATCC 25922 ATCC 10231 ATCC 9372 Sterilization rate 99.8% 99.9% 99.3% 99.5%
[0027] As can be seen from Table 1, the small molecule polypeptide provided by the present invention is effective against Staphylococcus aureus (ATCC 6538), Escherichia coli (ATCC 25922), Candida albicans (ATCC 10231), Bacillus subtilis black variety (ATCC 9372) all have strong bactericidal pro...
Embodiment 3
[0029] The anti-parasitic activity of the products of the present invention was assessed using fluorescent cell sorting analysis (FACS) to quantify parasite cultures of erythrocytes. The polypeptide that embodiment 1 obtains is dissolved in 1ml DMSO, then with 25mmol / L 4-hydroxyethylpiperazineethanesulfonic acid buffer solution, 32mmol / L NaHCO 3 Dilute 200 times with RPMI 1640 cell culture medium prepared with 10% human plasma. The sample solution was subsequently prepared into 11 different concentrations by 2-fold dilution, 1ml, 2×10 6 / ml parasites were added to the solution and placed in 5% CO at 37°C 2 Cultivate in the incubator for 48h. Add 1ml of 3% diamidinophenylindole solution, incubate for another 18 hours, and measure the number of red blood cells with a fluorescent cell differential analyzer. The inhibition rate of different concentrations of samples against parasites can be obtained, and the IC can be calculated. 50 value.
[0030] The half effective concentra...
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