Compositae cyclopeptide, immunosuppressive medicine using compositae cyclopeptide as active ingredient and preparation method and application of compositae cyclopeptide

A cyclic peptide and type technology, which is applied in the application field of Compositae type cyclic peptides in the preparation of immunosuppressive drugs, can solve the problems of unfavorable mass production, high price, unfavorable solvent recovery and the like

Inactive Publication Date: 2011-09-07
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI +1
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Its disadvantage is that the mixed solvent system of organic solvent and water is repeatedly used in the separation and purification, and the recovery temperature of the mixed solvent is high, which is unfavorable for the recovery of the solvent; all the solvents in the HPLC method are expensive, which makes the extraction cost too high, and the HPLC technology is also expensive. Not conducive to industrial mass production

Method used

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  • Compositae cyclopeptide, immunosuppressive medicine using compositae cyclopeptide as active ingredient and preparation method and application of compositae cyclopeptide
  • Compositae cyclopeptide, immunosuppressive medicine using compositae cyclopeptide as active ingredient and preparation method and application of compositae cyclopeptide
  • Compositae cyclopeptide, immunosuppressive medicine using compositae cyclopeptide as active ingredient and preparation method and application of compositae cyclopeptide

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Experimental program
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Effect test

Embodiment 1

[0044] Preparation of Compositae-type cyclic peptide compounds Astin C (1), Astin B (2), Astin D (3), Astin H (4), Tataricin A (5) and structure identification of Tataricin A (5):

[0045] Take Aster ( Aster tataricus .L) 50 Kg of dried roots and rhizomes, crushed and soaked in 90% industrial methanol for 5 hours, then heated and refluxed for extraction (temperature = 65°C), extracted three times in total, the first time was 3 hours, the second time was 2 hours, After 2 hours for the third time, the extracts were combined, concentrated under reduced pressure to remove the organic solvent to obtain a total of 23 Kg of methanol extract, and the crude extract was distributed in water, followed by full extraction with ethyl acetate and n-butanol, equal volume Extract three times, recover the solvent to obtain ethyl acetate part (2Kg), n-butanol part (5L) and water part; dissolve the ethyl acetate part with methanol, mix 2.5 Kg of 100-200 mesh silica gel sample, after the mixed sa...

Embodiment 2

[0058] Compositae-type cyclic peptide compounds of the present invention, Astin C (1), Astin B (2), Astin D (3), Astin H (4), Tataricin A (5), showed inhibition on the proliferation of activated T cells induced by Con A active. The experimental principles, methods and results are as follows:

[0059] Experimental principle: T lymphocytes in a normal body are stimulated by specific antigens or mitogens during in vitro culture, and a series of changes can occur in the metabolism and morphology of the cells. The main manifestations are changes in charge, increased cell volume, vigorous metabolism, increased synthesis of intracellular proteins and nucleic acids (and the ability to divide), and the transformation of cell morphology into lymphoblasts, which is the phenomenon of lymphocyte transformation. To this end, various stimulants are used to stimulate lymphocytes in vitro, and the response function of T lymphocytes can be measured according to the degree of transformation (th...

Embodiment 3

[0066] Compositae type cyclic peptide compounds Astin C (1), Astin B (2), Astin D (3), Astin H (4), Tataricin A (5) of the present invention caused by p-trinitrobenzenesulfonic acid (TNBS) Therapeutic effects of murine immune colitis. The experimental principles, methods and results are as follows:

[0067] Experimental principle: Inflammatory bowel disease mainly includes ulcerative colitis and Crohn's disease, which is a recurrent chronic non-specific intestinal inflammatory disease. Safe and effective medicines. Trinitrobenzenesulfonic acid-induced colitis in mice is an ideal model for studying the immune mechanism of human inflammatory bowel disease and developing new anti-inflammatory drugs because of its short cycle and simple method.

[0068] Experimental method: 6-8 weeks old, 18-22 g C57BL / 6 female mice were taken, and a 3.5 F flexible tube was carefully inserted into the colon through the anus with a depth of about 4 cm. Use a 1 mL disposable sterile syringe to in...

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Abstract

Compositae cyclopeptide compounds are monocyclic homogeneous pentapeptide compounds which contain beta-phenylalanine in skeleton and are formed by the directly connected normal peptide bonds of amino acids; and generally, one compositae cyclopeptide molecule contains one L-beta-phenylalanine molecule, one L-serine molecule, one L-proline derivative molecule and two other amino acid derivative molecules. The composite cyclopeptide shown in the structural formula AstinC (1) is a new immunosuppressive agent with plant source. The invention provides a preparation method of the compounds and an application of the compounds in the preparation of the immunosuppressive medicine. In the formula, R1 and R2 represent aryl or alkyl respectively; R3, R4 and R5 represent hydroxyl or halogen atom respectively; and X and Y represent unsaturated bond or saturated bond respectively.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a class of Compositae-type cyclic peptides as an immunosuppressant, a pharmaceutical composition using it as an active ingredient, its preparation method and its application in the preparation of immunosuppressive medicines. Background technique [0002] Immunomodulation is a key factor for the body to maintain a stable internal environment. If the immune system is dysfunctional, the body will produce an excessive immune response to self-antigens and cause tissue damage, which will lead to autoimmune diseases or allergic reactions. Immunosuppressants refer to a class of substances that can reduce tissue damage by inhibiting cellular and humoral immune responses. It has an inhibitory effect on the body's immune response, can inhibit the proliferation and function of cells related to the immune response (macrophages such as T cells and B cells), and reduce the body's...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/56C07K1/22C07K1/16C07K1/14A61K38/12A61P37/06
Inventor 谭宁华徐会敏徐强沈燕曾广智罗琼周文兵范君婷吴雪丰
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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