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Composition and application thereof as TR3 receptor inducer

A technology of composition and inducer, applied in application, food preparation, drug combination, etc.

Inactive Publication Date: 2010-11-24
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In addition, the high expression of members of the TR3 subfamily in the blood vessel wall may promote the pathogenesis of atherosclerosis, and the transcriptional activation of Nur77-regulated genes is involved in the inflammatory response of macrophages and the proliferation of vascular smooth muscle cells; it can be speculated that Nur77 located in the nucleus may promote atherosclerosis, Repression of transcriptional activation when located outside the nucleus may inhibit atherosclerotic lesion progression

Method used

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  • Composition and application thereof as TR3 receptor inducer
  • Composition and application thereof as TR3 receptor inducer
  • Composition and application thereof as TR3 receptor inducer

Examples

Experimental program
Comparison scheme
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Embodiment 1

[0026] Example 1: Extracting and separating biliprazone compounds from Red Bud Wood

[0027] Get 5.0kg of dry stems of Cratoxylum formosum subsp.pruniflorum, after coarse crushing, use 8 times the amount of 60% (V / V) ethanol-water reflux to extract twice, each two hours, combine the extracts, reduce After concentrating under pressure, the total extract (675.0 g) was obtained. Take the total extract (600g) of Red Yamwood and dissolve it in an appropriate amount of water, filter it, and take the filtrate and subject it to macroporous resin HP-20 open column chromatography, ethanol-water gradient elution. Respectively recover under reduced pressure to obtain water elution fraction (157.3g), 40% (v / v) ethanol-water elution fraction (257.0g), and 90% (v / v) ethanol-water elution fraction, this fraction It is the total bivapirox fraction of Red Yamwood (CF, 157.0g).

[0028]Take 90% (v / v) ethanol-water elution fraction CF (117.0 g), adopt silica gel open column chromatography, cycl...

Embodiment 2

[0103] Embodiment 2: Extraction and separation of bivapirox compounds from oxwood

[0104] Extract the dry stem (6Kg) of Cratoxylum cochinchinense (Cratoxylum cochinchinense) with 60% (V / V) ethanol-water under reflux, concentrate the extract, and use ethyl acetate, n-butanol, etc. The volume was extracted 3 times, and the ethyl acetate extraction part, that is, the total bivapidone part (142.5g) of oxwood, was subjected to silica gel column chromatography and gradient elution with cyclohexane-acetone (98:2-0:100) to obtain 10 sub-fraction (Fr.1 ~ Fr.10). Crystals were precipitated from sub-fraction Fr.2 (95:5 fraction, 1.9 g), and compound CC-5 (187 mg) was obtained by recrystallization from cyclohexane-acetone after filtration. Insolubles in subfractions Fr.4 (9:1 eluted fraction, 17.5 g), Fr.5 (85:15 eluted fraction, 9.6 g) and Fr.6 were recrystallized in methanol to give compound CC-3 ( 210mg), CC-4 (830mg) and CC-2 (145mg). Sub-fraction Fr.3 (9:1 elution fraction, 14.7g...

Embodiment 3

[0131] Embodiment 3: the effect of the bivapirox compound obtained in embodiment 1 on the expression of TR3mRNA

[0132] In this example, RT-PCR was used for analysis. NIH-H460 lung cancer cells were seeded in 6-well plates (5×10 5 cells / well), adhere to the wall for overnight culture, and after starvation for 12 hours, add drugs for culture. Total RNA was extracted and purified according to the instructions of the total RNA extraction kit. According to the instructions of the reverse transcription kit, the mRNA of the total cellular RNA was transcribed into cDNA. PCR conditions: cDNA 4μL in 20μL system, 10×PCR buffer, 25mmol / L MgCl 2 , 10mmol / L dNTPs, 10μmol / L TR3 primer and 1U Taq enzyme were added each time, and the reaction was carried out in a PCR machine. 94°C for 4min, 94°C for 30sec, 56°C for 30sec, 72°C for 30sec, 35 cycles. PCR primer sequence: TR3 upstream 5′-TCA TGGACG GCT ACA CAG-3′, downstream 5′-GTA GGC ATG GAA TAG CTC-3′; β-actin upstream 5′-CTGGAG AAG AGC...

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Abstract

The invention discloses a composition, a preparation method and application thereof as a TR3 receptor inducer, and belongs to the field of medicaments and foods. The composition serving as the TR3 receptor inducer is applied to preparing the foods or medicaments for preventing or treating cancer, hepatitis or atherosclerosis, and can be prepared into powder, tablets, capsules, pills, suppositories, dropping pills, enteric-coated preparations, injection, syrups, emulsion, suspension, tinctures, plaster or spray. Based on the mechanism that TR3 can be an ideal molecule target spot for screening medicaments for resisting tumors and cardiovascular and cerebrovascular diseases, the composition has practical significance for the discovery and development of compounds which can selectively regulate the expression way of the TR3 or medicinal compositions with the advanced treatment characteristic.

Description

technical field [0001] The invention belongs to the field of medicine and food, in particular to a composition and its application in preparing TR3 receptor inducer. Background technique [0002] TR3(Nur77) is a nuclear receptor encoded by the immediate early gene NR4A1. After being synthesized in the cytoplasm, it enters the nucleus as a transcription factor, and interacts with a specific DNA octamer sequence - Nur77 / NGFI-B binding response element through its central DNA binding domain, or with the retinol receptor RXR Form heterodimers, bind to DNA response elements, regulate the transcriptional activity of target genes, and play an important role in cell growth, differentiation and apoptosis. The structures of TR3 family members all have the typical characteristics of nuclear receptors: the N-terminal transcription activation region AF1, the highly conserved DNA binding region, and the C-terminal ligand-binding region. Many external signals, including various growth fa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61P35/00A61P1/16A61P9/10A61P9/00A61P3/10A23L1/30A23L33/105
Inventor 姚新生张晓坤戴毅王光辉张雪陈海峰段营辉陈杰波靳三林
Owner JINAN UNIVERSITY
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