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Liposome dimethylcurcumin inhibits activities of dipeptidase I and matrix metalloproteinase-9

A technology of dimethyl curcumin and dipeptide peptidase, applied in organic active ingredients, non-central analgesics, medical preparations containing active ingredients, etc., can solve problems such as unclear mechanism of action

Inactive Publication Date: 2019-01-18
CHANGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Both curcumin and dimethylcurcumin have important medicinal value and have anti-cancer, anti-inflammatory, anti-viral and anti-arthritic effects, but the mechanism of action is still unclear

Method used

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  • Liposome dimethylcurcumin inhibits activities of dipeptidase I and matrix metalloproteinase-9
  • Liposome dimethylcurcumin inhibits activities of dipeptidase I and matrix metalloproteinase-9
  • Liposome dimethylcurcumin inhibits activities of dipeptidase I and matrix metalloproteinase-9

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1: Collagen-induced arthritis (CIA) rat model was established, Lipo-DiMC was injected intra-articularly, and the inhibitory effect of Lipo-DiMC on DPPI activity and MMP-9 overexpression in CIA rats was detected.

[0028] 1.1 Materials:

[0029] SD rats (female, 5-6 weeks old), body weight 132.1±5.5g, provided by Changzhou Cavens Experimental Animal Co., Ltd.; DPPI fluorescent substrate, synthesized by the laboratory (X.Zhou, et al., Serum based fluorescent assay forevaluating dipeptidyl peptidase I activity in collagen induced arthritis ratmodel, Molecular and Cellular Probes(2016), http: / / dx.doi.org / 10.1016 / j.mcp.2016.10.009 ; Thong, B, et al., Development and validation of a simple cell-based fluorescence assay for dipeptidyl peptidase 1 (DPP1) activity, Journal of Biomolecular screening (2011), http: / / dx.doi.org / 10.1177 / 1087057110385228 ).

[0030] 1.2 Method:

[0031] 1.2.1 Grouping

[0032] They were divided into three groups: normal group, CIA model...

Embodiment 2

[0051] Example 2: Establishment of an in vitro lymphocyte model, detecting the effects of Lipo-DiMC on DPPI activity and MMP-9 secretion in rat spleen lymphocytes.

[0052] 2.1. Materials:

[0053] SD rats (female, 5-6 weeks old), body weight 132.1±5.5g; RPMI 1640 cell culture medium; fetal bovine serum; phosphate buffered solution (PBS); cell 96-well culture plate, etc.

[0054] 2.2. Method:

[0055] 2.2.1 Separation, extraction and culture of rat spleen lymphocytes Specific methods:

[0056] Rats were sacrificed by cervical dissection, rats were dissected, spleens were aseptically removed, and rat splenocytes were isolated by grinding and filtering the cell suspension in a 200-mesh cell sieve. 2 Cultivate overnight in an incubator to remove adherent cells and obtain relatively pure splenic lymphocytes. The spleen lymphocyte culture medium is: RPMI 1640 culture medium of 10% fetal bovine serum + 100 U / mL penicillin and 100 μg / mL streptomycin.

[0057] 2.2.2 The effect of ...

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Abstract

The liposome dimethylcurcumin is a liposome-encapsulated dimethylcurcumin (Lipo-DiMC). Dimethyl curcumin is a synthetic curcumin analog with the chemical formula C23H24O6. Compared with curcumin and dimethyl curcumin, Lipo- DiMC has better metabolic stability and is highly water soluble and has a sustained release effect in vivo. In some inflammatory, autoimmune and cancer diseases, Dipeptidyl peptidase (DPPI) and Matrix metalloproteinase (9, MMP-9) are overexpressed, leading to changes in tissue microenvironment and in vivo. Balance disorders and cause cell reproductive disorders. In the ratmodel of collagen induced arthritis (CIA) treated with Lipo-DiMC, Lipo-DiMC alleviated the swelling of the toes of CIA rats and inhibited DPPI and MMP in body fluids, blood and spleen lymphocytes of CIA rats-9 Overexpression of activity. The in vitro rat spleen lymphocyte model further confirmed that Lipo-DiMC inhibited and regulated the DPPI activity and MMP 9 expression and secretion in rat spleen lymphocytes.

Description

technical field [0001] The invention relates to the in vivo and in vitro inhibitory effect of liposomal dimethyl curcumin on dipeptide peptidase I and matrix metalloproteinase 9, which belongs to the invention of pharmaceutical use. Background technique [0002] Dimethyl curcumin (Dimethyl curcumin) is a synthetic curcumin (Curcumin) analogue, the chemical formula is C 23 h 24 o 6 . Curcumin is mainly derived from the rhizomes of Zingiberaceae and Araceae plants. It is a diketone compound with poor water solubility and stability. Dimethyl curcumin replaces the phenolic hydroxyl group in the curcumin structure with a methoxy group. Compared with curcumin, dimethyl curcumin has better metabolic stability, but both are low in water solubility. Liposome-encapsulated dimethyl curcumin (Lipo-DiMC) has high water solubility and has a slow-release effect in vivo. [0003] [0004] Both curcumin and dimethylcurcumin have important medicinal value, and have anti-cancer, anti-i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/122A61P19/02A61P29/00A61P43/00
CPCA61K31/122A61P19/02A61P29/00A61P43/00
Inventor 周晓鹰孙芝源
Owner CHANGZHOU UNIV
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