Application of urushiol-silicon polymer in preparation of medicine for inhibiting Smad3 phosphorylation

A compound and phosphorylation technology, applied in active ingredients of hydroxyl compounds, drug combinations, organic chemistry, etc.

Inactive Publication Date: 2014-03-05
NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The patent reveals that the above-mentioned urushiol compound has good antitumor activity and has cytotoxic activity against various tumor cell lines

Method used

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  • Application of urushiol-silicon polymer in preparation of medicine for inhibiting Smad3 phosphorylation
  • Application of urushiol-silicon polymer in preparation of medicine for inhibiting Smad3 phosphorylation
  • Application of urushiol-silicon polymer in preparation of medicine for inhibiting Smad3 phosphorylation

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Embodiment one: the preparation of urushiol compound of the present invention

[0025] The present invention refers to the method described in the aforementioned Chinese patent 201010149042.3 to prepare an urushiol compound, code-named GQ-5.

[0026] Preparation method: take dry resin from Anacardiaceae sumac and grind it, soak and extract in 80% ethanol three times, soak and extract in acetone once, concentrate the extract under reduced pressure to form a paste, disperse with appropriate amount of water, extract with an equal amount of ethyl acetate for 3 Second, silica gel column chromatography, chloroform-methanol gradient elution, and thin-layer chromatography (10% sulfuric acid ethanol color development) as a guide to combine components: A1-11 (chloroform-methanol 98:2), B12-17 (chloroform-methanol 96:4), C18-24 (chloroform-methanol 92:8), D25-32 (chloroform-methanol 90:10). Component C was subjected to MCI Gel CHP20P (3.5×40cm, acetone-water, 50%, 60%, 70%, 80%. ...

Embodiment 2

[0028] Embodiment two: the cytotoxicity of urushiol GQ-5

[0029] 1. Experimental cells: Rat normal renal tubular epithelial cell line NRK52E cells were used. Routine culture, grouping, 96-well plates without serum for 12 hours after the intervention began.

[0030] 2. Experimental grouping and processing

[0031] 1) Normal control group: continue to culture without serum for 48 hours.

[0032] 2) Medication group: pre-incubated with 0.25, 0.5, 1.0, 2.0 and 4.0 μM GQ-5 for 1 hour, and cultured without serum for 48 hours. Three replicate wells were set up for each concentration.

[0033] 3. Experimental process

[0034] GQ-5 was dissolved in DMSO to different final concentrations. After stimulation according to the above conditions, 20 μL of MTT (0.01M) was added to each well, incubated for 4 hours, the medium was discarded, 150 μL of dimethyl sulfoxide (DMSO) was added dropwise to each well, shaken at 37°C for 15 minutes, and the microplate reader was Absorbance was measur...

Embodiment 3

[0037] Example 3: Inhibition of urushiol GQ-5 on TGFβ1-mediated phosphorylation of Smad3

[0038] 1. Experimental cells: Rat normal renal tubular epithelial cell line NRK52E cells and rat normal fibroblast cell line NRK49F cells were used respectively. Intervention began after routine culture, grouping, and serum-free resting for 12 hours.

[0039] 2. Experimental grouping and processing

[0040] 1) Normal control group: continue culturing without serum for 2 hours.

[0041] 2) Negative control group: pre-incubated with 2.5 μM GQ-5 for 1 hour, stimulated with TGFβ 110 ng / ml for 1 hour.

[0042] 3) Positive control group: pre-incubated with 0.1% DMSO for 1 hour, stimulated with TGFβ 110ng / ml for 1 hour.

[0043] 4) Medication group: Pre-incubated with 0.1, 0.5 and 2.5 μM GQ-5 for 1 hour, stimulated with TGFβ 110 ng / ml for 1 hour.

[0044] 3. Experimental process

[0045] GQ-5 was dissolved in DMSO to different final concentrations. After stimulation according to the above...

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Abstract

The invention discloses an application of an urushiol-silicon polymer (code: GQ-5) in preparation of a medicine for inhibiting Smad3 phosphorylation. The in-vitro experiment shows that the urushiol-silicon polymer is able to inhibit TGF (Transforming Growth Factor) beta 1 mediated Smad3 phosphorylation and also can inhibit the expression of mRNA (Messenger Ribose Nucleic Acid) of alpha-SMA (Smooth Muscle Actine), type I collagen and fibronectin at downstream. The in-vivo experiment also shows the same result. Therefore, the GQ-5 has the effect of specifically inhibiting Smad3 phosphorylation and also can be used for preparing a medicine for inhibiting Smad3 phosphorylation.

Description

technical field [0001] The invention relates to a new application of a urushiol compound extracted from Rhusverniciflua Stokes, a plant of the Rhus verniciflua Stokes, in particular to the application of the urushiol compound in preparing a drug for inhibiting Smad3 phosphorylation. Background technique [0002] Natural medicines play an important role in health care and drug research. Statistics show that about 80% of antibacterial drugs and 60% of anticancer drugs are directly or indirectly derived from natural products (J Nat Prod, 2003, 66: 1022-1237). Nature has become an important source of human therapeutic drugs. [0003] The name is "Urushiol compound, its pharmaceutical composition and its preparation method and application" Chinese invention patent (patent number: 201010149042.3; application date: April 16, 2010; publication number: CN101805246A; publication date: August 18, 2010 date; authorization date: June 5, 2013) disclosed that researchers from the Kunming ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/05A61P43/00A61P13/12
CPCA61K31/05A61P13/12A61P43/00C07C39/19
Inventor 侯凡凡程永现聂静艾军何江波
Owner NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV
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