A kind of antitumor active peptide, synthesis method and application

Abstract

The invention belongs to the field of biotechnology, and discloses an anti-tumor active peptide, a synthesis method and an application. The structure of the active peptide is: Cyclo-(Leu-Pro-Pro-(D-Phe)-Ile-Pro-(D -Phe)-Val). The synthesis method comprises the following steps: 1) using resin and amino acid for coupling reaction, so that linear peptide is coupled on the resin; 2) adding cutting solution to the resin for reaction, collecting the solution after reaction, adding DIEA dropwise to the solution Adjust the pH value to be neutral to obtain a crude product solution of the linear peptide; 3) add the crude product solution of the linear peptide dropwise into the cyclic peptide reaction system to synthesize the cyclic peptide. The present invention replaces the two phenylalanines in the original Samoamide A cyclic peptide by two D-phenylalanines, and obtains Samoamide C based on the derivative of Samoamide A through a suitable solid-phase synthesis method, and the prepared Samoamide C The inhibition rate of DPP-4 enzyme activity and the toxicity to tumor cells are significantly improved, reflecting more excellent anti-tumor activity.

Description

technical field [0001] The invention belongs to the field of biotechnology, and specifically relates to an anti-tumor active peptide, a synthesis method and an application. Background technique [0002] Peptide drugs are widely concerned because of their small molecular weight, high specificity, and low side effects. They are considered to be good drugs for treating malignant tumors. Samoamide A[-(Leu-Pro-Pro-Phe-Ile-Pro-Phe-Val)-] is a cyclic peptide naturally extracted from marine algae, and has a good toxic effect on tumor cells. However, the natural extraction of Samoamide A has low extraction yield and poor activity, and cannot be produced and applied on a large scale. Therefore, it is necessary to invent a method for solid-phase synthesis to improve the yield and simultaneously improve its activity, so that it can be more widely used. application. [0003] After searching, for the synthesis method of Samoamide A, related applications have been published in the prior ...

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Problems solved by technology

[0007] Aiming at the defect of poor antitumor activity of the cyclic peptide Samoamide A naturally extracted from marine algae, the present invention provides a method to replace two phenylalanines in the original Samoamide A cyclic peptide by using two D-phenylalanines. acid, to obtain Samoamide C, a derivative based on Samoamide A. Under the same application concentration, Samoamide C has significantly improved the inhibition rate of DPP-4 enzyme activity and the cytotoxicity of tumor cells, reflecting more excellent anti-tumor activity.

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