Polypeptide, polypeptide derivative, medicinal salt of polypeptide and pharmaceutical composition
A technology of peptide derivatives and compositions, applied in the fields of polypeptides and derivatives of the polypeptides, pharmaceutically acceptable salts and pharmaceutical compositions, can solve the problems of short plasma half-life and the like, achieve long plasma half-life, good stability, and improve pancreatic islets effect of function
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Embodiment 1
[0138] The production of embodiment 1 polypeptide
[0139] This example describes the production of polypeptides
[0140] All peptides used in this study were synthesized using 9-fluorenylmethyl chloroformate (Fmoc) solid-phase synthesis. Simply put: Dissolve a weighed amount of 2-chlorotrityl chloride resin (1.6mmol / g) in dichloromethane (DCM). For C-terminally amidated peptides of interest, use Rink amide resin instead of 2-chlorotrityl chloride resin. For coupling reactions in the presence of hydroxybenzotriazole (Sigma Chemicals, Inc., St. Louis, MO, USA) in dimethylformamide (DMF), preactivated Fmoc-amino acids were used. The entire synthesis process uses an excess of amino acids. Deprotection of the Fmoc group in 20% piperidine in DMF leads to chain extension reactions. When the chain extension reaction was completed, the Fmoc protecting group was removed from the N-terminus of the polypeptide using DMF containing 25% piperidine, and then washed four times with DMF s...
Embodiment 2
[0144] Stability experiment of embodiment 2 peptide
[0145] This example describes stability experiments of peptides under various conditions.
[0146] Accurately weigh a certain amount of the selected peptide, dissolve it in distilled water to a concentration of 5 mg / mL, and use it as a stock solution to examine the stability of the peptide in the culture medium. Use F-12K medium (GIBCO-BRL, Gaithersburg, MD, USA) to dilute the stock solution to 0.25 mg / mL as a working solution. Transfer each 100 µL of working solution to a separate vial. After the vials were placed in a 37°C incubator for 0, 24, 48 and 72 hours, quantitative analysis was performed using HPLC.
[0147] Table 5 shows the stability of the compounds in the medium. Table 5 shows a comparison of the stability in culture medium of INGAP-PP (peptide 1) and selected peptides, peptide 12 and peptide 16 (see Table 2). in particular, figure 1 Stability comparisons of the INGAP peptide (peptide 1) and selected homo...
Embodiment 3
[0181] Example 3 Effects of Peptides on Glucose-Stimulated Insulin Secretion
[0182] This example describes the effect of peptides on glucose stimulated insulin secretion (GSIS).
[0183] Pancreatic tissue was extracted from male adult Sprague-Dawley (SD) rats. After 7 days of acclimatization, the animals were sacrificed by cervical dislocation, and the whole pancreas was harvested, and the islets were digested with collagenase. After digestion, store islets at 37 °C in a humidified environment at pH 7.4 containing 10% (v / v) fetal bovine serum, 1% penicillin / streptomycin, 10 mM glucose (5% CO 2 / 95%O 2 ) in RPMI1640 (Carlsbad, California, USA) medium, and divided into the following groups: without adding any compound (control group), adding 100nM glucagon-like peptide-1 (GLP-1 group), Add 10 μg / mL peptide 1 group, peptide 12 group, peptide 16 group, see Table 11 below.
[0184] Table 11
[0185]
[0186] in CO 2 / O 2 (5 / 95%), 37 ℃ environment, in 1.0ml containing 0....
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