Cyclopeptide, preparation method and uses thereof

A cyclic peptide and peptide bond technology, which is used in the application field of cyclic peptide compounds and the preparation of anti-immunosuppressive drugs

Inactive Publication Date: 2008-04-16
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Brachystemin F (brachystemin F) is a class of cyclic octapeptide natural products found in the anti-rheumatic Chinese herbal medicine Brachystemma calycinum (Brachystemma calycinum) with the ability to inhibit T-, B-lymphocyte transformation (clinically used cyclosporine Bacterin is a cyclic undecapeptide derived from fungi), and its structural formula has not yet been reported, so it is a new chemical substance, and its biological activity is the first discovery

Method used

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  • Cyclopeptide, preparation method and uses thereof
  • Cyclopeptide, preparation method and uses thereof
  • Cyclopeptide, preparation method and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Preparation and structure identification of Brachystemin F [Brachystemin F: cyclo(Pro-Pro-Ile-Ser-Phe-Ala-Ser-Tyr)]:

[0022]The root (13kg) of Brachystemma calycinum was collected, dried in the sun, and pulverized. Reflux extraction with 90% ethanol was performed 4 times for 2.0, 1.5, 1.0 and 1.0 hours, respectively. The extracts were combined, concentrated under reduced pressure, and then extracted with petroleum ether, ethyl acetate, and n-butanol. 50 g of the ethyl acetate extract was subjected to silica gel column chromatography (2.3 kg, 200-300 mesh), eluted with a gradient of chloroform-methanol (100:0-70:30), and the collected fractions were developed by thin layer, and then washed with 6 equivalents The tube was sealed with hydrochloric acid, heated and hydrolyzed at 110°C for 1 hour, and ninhydrin reagent was sprayed. By comparing the spots before hydrolysis with no color, and after hydrolysis, the spots showed positive reactions to determine the principle of...

Embodiment 2

[0031] Prepare Brachystemin F (Brachystemin F) according to the method of Example 1, add water for injection according to conventional methods, fine filter, potting and sterilization can be made into injection.

Embodiment 3

[0033] Brachystemin F (Brachystemin F) was prepared according to the method of Example 1, which was dissolved in sterile water for injection, filtered with a sterile funnel, subpackaged, freeze-dried at low temperature and sealed aseptically to obtain a powder injection.

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Abstract

A cyclic peptide is provided, which consists of 3-15 amino acids connected together with each other, wherein the amino acids contained by the cyclic peptide can be the common amino acids or the rare ones, the natural amino acids or the artificial ones, the conformation of any amino acid can be L-type or D-type, and the connection sequence is free among the amino acids. The preferred formula (I) consists of 8 common amino acids connected with each other through peptide linkages to form a cyclic peptide, and the present invention also relates to the method to prepare the cyclic peptide and the application thereof to preparation of immune-suppressive drugs.

Description

Technical field: [0001] The invention relates to the technical field of medicines, in particular to a cyclic peptide compound, its preparation method, and its application in the preparation of anti-immunosuppressive drugs. Background technique: [0002] Immunosuppressant (Immunosuppressant) is a class of immunosuppressive drugs, its main function is to suppress the abnormal immune response of the body, and is used for anti-rejection and autoimmune diseases (auto- immune diseases) treatment. In the 20th century, with the advancement of surgery and immunosuppressive drugs, organ transplantation has become an effective and routine treatment for organ failure. According to statistics, in 2005, China performed about 8,000 cases of kidney transplantation and nearly 4,000 cases of liver transplantation, while the United States completed 14,492 cases of organ transplantation during the same period. At present, the types of organs that can be transplanted in my country and the numb...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K5/12C07K7/64A61K38/12A61P37/06
Inventor 程永现吕青
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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