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Pharmaceutical application of bicyclic cyclic hexapeptide glycoside compound

A technology for peptide glycosides and compounds, applied in the field of medicine, can solve the problems of no bicyclic hexapeptide glycosides, etc., and achieve the effect of being beneficial to research and development, production, controllability and reproducibility

Pending Publication Date: 2020-11-03
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In the prior art, there are no reports of bicyclic cyclohexapeptide glycosides derived from Rubiaceae plants as STAT3 signaling pathway inhibitors and anti-inflammatory and anti-tumor drugs

Method used

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  • Pharmaceutical application of bicyclic cyclic hexapeptide glycoside compound
  • Pharmaceutical application of bicyclic cyclic hexapeptide glycoside compound
  • Pharmaceutical application of bicyclic cyclic hexapeptide glycoside compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026]The preparation method of Rubiaceae bicyclic hexapeptide glycoside cyclic peptide compound RA-XII refers to patent 201410133237.7, specifically: take the rhizome of the Rubiaceae Chinese herbal medicine Rubia yunnanensis Diels, after drying and crushing, use methanol heat reflux to extract 3 times, each time is 3-4 hours, the extract is concentrated under reduced pressure to obtain methanol extract; :3, 1:1, 0:100) gradient elution, combined the fractions by cyclic peptide TLC detection method to obtain the total cyclic peptide site; each of the following steps must be separated and purified in combination with cyclic peptide TLC detection method; the total cyclic peptide The peptide parts were chromatographed on a silica gel column, eluted with a gradient of 70:1-8:2 chloroform / methanol, and combined into three fractions Fr.1-Fr.3 according to the different cyclic peptide points; Silica gel column chromatography, 10:1-8:2 ethyl acetate / methanol for gradient elution, com...

Embodiment 2

[0028] Evaluation of bicyclic cyclohexapeptide glycoside compound RA-XII on human colorectal cancer cell lines (HCT116, HT29) and mouse colorectal cancer cell line (Colon-26) and other three kinds of colorectal cancer tumor cells by MTT colorimetry The cytotoxic activity of strains, found that bicyclic cyclohexapeptide glycosides have cytotoxic activity. The experimental principles, methods and results are as follows:

[0029] Experimental principle: MTT (thiazolium blue), succinate dehydrogenase in the mitochondria of living cells can reduce exogenous MTT to water-insoluble blue-purple crystalline formazan (Formazan) and deposit in cells, while dead cells do not have this function . Dimethyl sulfoxide (DMSO) can dissolve formazan in cells, and its light absorption value is measured at a wavelength of 540nm with a microplate reader. Within a certain range of cell numbers, the amount of MTT crystal formation is proportional to the number of cells. According to the measured ab...

Embodiment 3

[0036] Using the co-culture model of human colorectal cancer cells HCT116 and mouse immune cells RAW264.7, the anti-inflammatory and anti-tumor activities of the bicyclic hexapeptide glycoside compound RA-XII were evaluated in vitro, and the results showed that the bicyclic cyclohexapeptide glycoside compound RA-XII had Good in vitro anti-inflammatory and anti-tumor activity.

[0037] The experimental methods and results are as follows:

[0038] RAW264.7 cells were plated in 6-well plates, 1x 10 per well 6 cells, HCT116 cells were plated in the upper chamber of a transwell 6-well plate, 5x 10 per well 5 cells, 37°C, 5% CO 2 After culturing for 24 hours, place the upper chamber of the transwell in a 6-well plate with RAW264.7, add the medium containing LPS (1 μg / ml) to make the cells produce an acute inflammatory reaction, and add the medium containing LPS (1 μg / ml) to the other groups respectively. ) and RA-XII (50nM, 100nM, 200nM and 400nM) medium, 37°C, 5% CO 2 Incubate ...

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Abstract

The invention discloses a novel pharmaceutical application of a bicyclic cyclic hexapeptide glucoside compound RA-XII separated from a Chinese herbal medicine namely rubia yunnanensis. Experiments prove that the bicyclic cyclic hexapeptide glucoside compound RA-XII has in-vitro and in-vivo anti-tumor and anti-inflammatory related signal channel inhibition activity, can be used for preparing inhibitors of STAT3 signal channels and anti-inflammatory and anti-tumor drugs, and has the advantages of good anti-inflammatory effect, low toxicity, good anti-tumor effect and the like.

Description

technical field [0001] The invention belongs to the technical field of medicines, and specifically relates to the application of bicyclic cyclohexapeptide glycoside compounds as inhibitors of STAT3 signaling pathways in the preparation of medicaments for treating and preventing inflammatory diseases and cancers related to STAT3 signaling pathways. Background technique [0002] A growing body of literature suggests that chronic inflammation of the gut plays a contributing role in colitis-associated cancer (CAC), with an increased incidence of colorectal cancer among patients with inflammatory bowel disease. Inflammatory cytokines trigger cellular effects and functions through activator of transcription (STAT) molecules, and participate in the transformation of inflammatory lesions to tumors, leading to CAC. Serum inflammatory cytokine IL-6 is significantly increased in colorectal cancer patients. IL-6 is a pleiotropic cytokine involved in tumor growth, invasion and metastasis...

Claims

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Application Information

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IPC IPC(8): A61K38/12A61P35/00A61P29/00
CPCA61K38/12A61P35/00A61P29/00
Inventor 谭宁华刘碧珊林倩文余嘉莉
Owner CHINA PHARM UNIV
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