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Rubiaceae-type cyclopeptide, its pharmaceutical composition and application

A Rubiaceae, type technology, applied in the application field of Rubiaceae type cyclic peptides to prepare anti-herpes simplex virus type I (HSV-1) drugs, can solve the problem of relatively expensive aminopropyl bonds and silica gel materials, heavy methanol The controllability and reproducibility of crystallization technology is not good, and it is not commonly used.

Inactive Publication Date: 2012-12-12
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The disadvantages are that alumina has strong adsorption to samples, aminopropyl bond and silica gel materials are more expensive, and are not commonly used in laboratories and industries, and the controllability and reproducibility of methanol recrystallization technology are not good.

Method used

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  • Rubiaceae-type cyclopeptide, its pharmaceutical composition and application
  • Rubiaceae-type cyclopeptide, its pharmaceutical composition and application
  • Rubiaceae-type cyclopeptide, its pharmaceutical composition and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Rubiaceae type cyclic peptide compounds RA-V (1), RA-I (2), RA-XXIV (3), RA-XII (4), rubiyunnanin D (5), rubiyunnanin C (6), rubiyunnanin E (7 ), rubiyunnanin F (8), rubiyunnanin G (9), rubiyunnanin H (10) and RY-II (11) preparation methods and structural identification:

[0035] Take 100kg of the rhizome of red ginseng, dry and pulverize it, and extract it with methanol reflux for 3 times (100L×3 times), the time is 3h, 3h, 2h, and the extract is concentrated under reduced pressure to obtain 21kg of methanol extract. Add water to the methanol extract and suspend it, then fully extract it with ethyl acetate and n-butanol successively, extract three times in equal volumes (30L x 3 times), recover the solvent to obtain 6.4kg of ethyl acetate, 8kg of n-butanol and water 5kg. The ethyl acetate part was subjected to silica gel column chromatography, eluted with chloroform / methanol gradient (100:0, 95:5, 9:1, 8:2, 0:100), thin layer chromatography, combined with cyclic pepti...

Embodiment 2

[0054] Rubiaceae type cyclic peptide compounds of the present invention RA-V (1), RA-I (2), RA-XXIV (3), RA-XII (4), rubiyunnanin D (5), rubiyunnanin C (6), rubiyunnanin E (7), rubiyunnaninF (8), rubiyunnanin G (9), rubiyunnanin H (10) and RY-II (11) can significantly inhibit the LPS and IFN-γ-induced mouse peritoneal macrophage cell line RAW264.7 model NO generated. The experimental principles, methods and results are as follows:

[0055] Experimental principle: The gene encoding nitric oxide synthase (Nitric Oxide Synthase, NOS) is one of the direct target genes of the NF-κB signaling pathway. When cells are stimulated by microbial endotoxins and inflammatory mediators, the NF-κB signaling pathway will be activated , so as to generate a large amount of inducible NOS. Nitric oxide synthase catalyzes its substrate L-arginine to generate NO and L-citrulline. NO exists in the form of nitrite ions in aqueous solution. In this experiment, LPS and IFN-γ were used to stimulate RAW...

Embodiment 3

[0062] Rubiaceae type cyclic peptide compounds of the present invention RA-V (1), RA-I (2), RA-XXIV (3), RA-XII (4), rubiyunnanin D (5), rubiyunnanin C (6), rubiyunnanin E (7), rubiyunnanin F (8), rubiyunnanin G (9), rubiyunnanin H (10) and RY-II (11) used the luciferase reporter gene method to detect the inhibitory activity of NF-κB pathway, and further confirmed the role of cyclic peptide molecules in the NF-κB pathway. The experimental principles, methods and results are as follows:

[0063] Experimental principle: NF-κB nuclear transcription factor has a conserved DNA-binding sequence, which regulates the expression of downstream genes by binding to it. The pNF-κB-Luc reporter plasmid (Clontech) contains the firefly luciferase reporter gene, whose expression is regulated by a synthetic promoter, which contains the basic promoter element (TATA box), and the NF-κB transcription factor DNA binding sequence, so the expression of the firefly luciferase reporter gene is regula...

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Abstract

The invention provides a rubiaceae-type cyclopeptide compound rubiyunnanin F(8), a pharmaceutical composition with the compound as an active component, as well as a preparation method and application of the compound. The invention provides the preparation method of the compound and application of the compound in preparation of anti-herpes simplex virus type I (HSV-1) medicines.

Description

[0001] This application is a divisional application of the patent application "Cyclic peptide of Rubiaceae type, pharmaceutical composition with it as active ingredient, preparation method and application thereof" (application number: 201010232742.9, filing date: July 21, 2010). Technical field: [0002] The present invention belongs to the technical field of medicines, and in particular, relates to a class of Rubiaceae type cyclic peptides, which are used as NF-κB signaling pathway inhibitors, a pharmaceutical composition using it as an active ingredient, its preparation method and its application in the preparation of anti-herpes simplex virus I Type (HSV-1) drug application. Background technique: [0003] The NF-κB signaling pathway is widely involved in a variety of biological effects, including immune response, inflammatory response, virus infection, cell growth, apoptosis, and tumor development, etc. It is one of the most important signaling pathways in higher biologica...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/64A61K38/12A61P31/22
Inventor 谭宁华范君婷李艳苏佳李佳周宇波彭延敏彭涛朱钦昌曾广智
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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