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Application of blood vessel inhibiting polypeptides with integrin affinity and bonding capability and MMPs (matrix metalloproteinases) inhibiting capability

A technology of protease inhibition and binding ability, applied in the field of medicine, can solve the problems of poor drug targeting and poor therapeutic effect

Active Publication Date: 2015-08-19
NANJING ANJI BIOLOGICAL TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] Aiming at the problems of poor drug targeting and poor therapeutic effect in the existing treatment of arthritis, inflammation caused by bacteria, tumors, ophthalmic diseases and other blood vessel-related diseases, the present invention provides an integrin affinity and binding ability and The vascular inhibitory polypeptide with matrix metalloproteinase inhibitory ability has good preventive and therapeutic effects on blood vessels and inflammation-related diseases including arthritis, inflammation, tumors, eye diseases, etc., increasing its scope of indications

Method used

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  • Application of blood vessel inhibiting polypeptides with integrin affinity and bonding capability and MMPs (matrix metalloproteinases) inhibiting capability
  • Application of blood vessel inhibiting polypeptides with integrin affinity and bonding capability and MMPs (matrix metalloproteinases) inhibiting capability
  • Application of blood vessel inhibiting polypeptides with integrin affinity and bonding capability and MMPs (matrix metalloproteinases) inhibiting capability

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0088] Preparation and Test of Synthetic Peptide I of Vascular Inhibitory Polypeptide

[0089] The solid-phase synthesis method of polypeptide I Arg-Gly-Asp-Gly-Gly-Gly-Gly-Pro(D-Pyr)-(D-Cys)--Bip-Arg-Gly-Glu, which starts with wang resin As raw materials, one peptide to fourteen peptides are sequentially connected with protected amino acids. After the peptide connection is completed, the peptide is fully washed, and then the peptide is cut and post-processed to obtain the crude product of polypeptide I. The crude product was purified twice with preparative HPLC, and finally concentrated and freeze-dried to obtain the pure product. The purity of the polypeptide was determined by analytical RP-HPLC. The method can not only ensure the synthesis efficiency, but also improve the product purity.

[0090] Specific steps are as follows:

[0091] 1. Synthesis:

[0092] Weigh 13g of Wang resin (Wang resin), pour it into a 1L glass sand core reaction column, add CH 2 Cl 2 130mL to...

Embodiment 2

[0123] Preparation and Testing of Synthetic Peptide II of Vasoinhibitory Polypeptide

[0124] The solid-phase synthesis method of Pro-(D-Pyr)-(D-Cys)-Bip-Arg-Gly-Glu-Gly-Gly-Gly-Gly-Gly-Arg-Gly-Asp, which uses Fmoc-Asp(OtBu)- Wang resin was used as the starting material, and the dipeptide to tetradecapeptide were inoculated sequentially with protected amino acids. After the peptide incorporation was completed, it was fully washed, and then the peptide was cut and post-treated to obtain the crude polypeptide II. The crude product was purified twice with preparative HPLC, and finally concentrated and freeze-dried to obtain the pure product. Specific steps are as follows:

[0125] 1. Synthesis:

[0126] Weigh 14.5g of Fmoc-Asp(OtBu)-wang resin (Wang resin prepacked resin), pour it into a 1L glass sand core reaction column, add CH 2 Cl 2 145mL to fully expand the resin.

[0127] Uncapping: Add 25mL of capping solution, seal it and place it in a shaker for 5min to react, the t...

Embodiment 3

[0156] Vaso-inhibitory polypeptides in vivo immune protection in adjuvanted rat arthritis animal model

[0157]An animal model of adjuvant arthritis in rats was constructed to study the therapeutic effect of angioinhibitory polypeptide on adjuvant arthritis (Adjuvant arthritis, AA) rats. Rats were used as test animals, and 63 clean-grade wistar rats (provided by the Comparative Medicine Center of Yangzhou University, animal production license number: SCXK (Su) 2012-0004), male, with a body weight of 150g-180g, were randomly divided into 9 groups, respectively blank control group, model control group, 3 low, medium and high dose groups of polypeptide I (3, 6, 9 mg / kg), 3 low, medium and high dose groups of polypeptide II (3, 6, 9 mg / kg) and positive Drug control group (methotrexate 1mg / kg). Except for the blank group, rat AA models were established in each experimental group on the 0th day by injecting complete Freund's adjuvant containing inactivated Mycobacterium tuberculosi...

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Abstract

The invention discloses an application of a blocker with integrin affinity and bonding capability and MMPs (matrix metalloproteinases) inhibiting capability, and belongs to the field of medicines. The application comprises a polypeptide I (Arg-Gly-Asp-Gly-Gly-Gly-Gly-Pro-(D-Pyr)-(D-Cys)-Bip-Arg-Gly-Glu) and a polypeptide II (Pro-(D-Pyr)-(D-Cys)-Bip-Arg-Gly-Glu-Gly-Gly-Gly-Gly-Arg-Gly-Asp), wherein the polypeptide I is modified with an integrin ligand sequence (Arg-Gly-Asp-Gly-Gly-Gly-Gly); two types of blood vessel inhibiting polypeptides with integrin affinity and bonding capability are formed. The application has the advantages that because of the targeting property of an RGD (arginine-glycin-aspartate) sequence, the polypeptides can be targeted to the new blood vessel endothelium of the RA (rheumatoid arthritis) pannus forming process, the forming of MMPs (matrix metalloproteinases) and the new blood vessel can be inhibited, and the effect of preventing or treating the blood vessel and inflammatory diseases are realized; the polypeptides can be applied to the treatment of the blood vessel and inflammatory diseases, such as arthritis, inflammation, tumors, and eye diseases.

Description

technical field [0001] The invention belongs to the field of medicine, and more specifically relates to the application of blood vessel inhibiting polypeptide with integrin affinity, binding ability and matrix metalloproteinase inhibitory ability. Background technique [0002] Arthritis, inflammation caused by bacteria, tumors, eye diseases such as AMD are all called vascular-related diseases. [0003] Rheumatoid arthritis (RA) is the most common clinical inflammatory joint disease and one of the main disabling factors. It is about 0.5%-1.0% in the whole world, and the incidence rate of RA is about 0.4% in our country. RA can occur at any age, and the incidence rate increases with age. The high-incidence age of women is 45-55 years old, and gender is closely related to the incidence of RA, with a male-to-female ratio of about 1:3. RA is a chronic systemic inflammatory disease of unknown etiology, with chronic, symmetrical, polysynovial arthritis and extra-articular lesion...

Claims

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Application Information

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IPC IPC(8): A61K38/10C07K7/08C07K1/36C07K1/34C07K1/16A61P29/00A61P19/02A61P35/00A61P27/02
CPCY02P20/55
Inventor 康梦实
Owner NANJING ANJI BIOLOGICAL TECH CO LTD
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