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Application of bisbibenzyl compound to preparation of anti-inflammatory medicament

An anti-inflammatory drug, bisbibenzyl technology, applied in the directions of anti-inflammatory agents, antitumor drugs, drug combinations, etc., can solve problems such as no application of bisbibenzyl compounds, no reports of anti-inflammatory effects of the two compounds, etc.

Active Publication Date: 2011-11-02
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Studies have confirmed that dichanin M and phylloxin D have good antifungal and antitumor activities, but so far, among the many reports retrieved, there is no report on the anti-inflammatory effect of the two compounds, let alone bibenzyl Application of compounds in anti-inflammation, anti-rheumatoid arthritis and treatment of tumors caused by inflammation

Method used

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  • Application of bisbibenzyl compound to preparation of anti-inflammatory medicament
  • Application of bisbibenzyl compound to preparation of anti-inflammatory medicament
  • Application of bisbibenzyl compound to preparation of anti-inflammatory medicament

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1: Determination of the levels of IL-6, CCL2, IL-1b and MCP-1 inhibited by dichantin M

[0032] Methods: (1) Isolation and culture of human umbilical vein endothelial cells (HUVEC)

[0033] Take the umbilical cord of the newborn under aseptic conditions, cut off the clamp mark, hematoma, and clot blocking part in the ultra-clean bench, divide it into a 20cm section, use a No. 5 handle disposable intravenous infusion needle to absorb 36 ℃ preheated double-antibody PBS, and insert The stump of the umbilical vein was ligated and fixed at the same time, the residual blood in the vein was rinsed repeatedly, and then the other end of the umbilical cord was clamped with a vascular clamp, and then the prepared 0.25% trypsin and 0.53mM EDTA digestive solution were injected respectively to fill the lumen. 37°C, act for 15 minutes. Loosen one end of the vascular clamp, collect the digestive fluid in the umbilical vein, and then inject EGM2 culture solution containing 5% n...

Embodiment 2

[0038] Example 2: Dichanin M inhibits the gene expression of inflammatory factors such as IL-6, IL-1b, CCL2, COX-2, Icam and TNF

[0039] Methods: (1) RT-PCR detection of mRNA levels

[0040] Total RNA was extracted with Qiagen RNEasy kit, and the total RNA was reverse-transcribed into cDNA (invitrogen Carlsbad, CA) using random primers and Superscript III reverse transcriptase according to the instructions. The reverse transcription reaction conditions were 60 min at 48°C and 15 min at 70°C. TaqMan Universe PCR Master Mix is ​​used for quantitative PCR amplification using pre-synthesized targeting primers. IL-6(Hs_m1), IL-1b(Hs_m1), TNF alpha(Hs_m1), CCL2 / MPC1(Hs_m1), vEGF(Hs_m1), COX-2(Hs_m1). cDNA amplification was performed in 96-well reaction plates using the ABI PRISM 7700 Sequence Detection System.

[0041] The reaction system is shown in Table 1 below:

[0042] Table 1

[0043]

[0044] Thermal cycle amplification is performed and cDNA will be generated followi...

Embodiment 3

[0049] Example 3: Dichanin M inhibits the expression of NF-kB

[0050] Methods: Nuclear protein extraction was carried out using a nuclear extraction kit (Active Motif Tokyo, Japan) according to the instructions. Wash cells with ice-bathed PBS containing phosphatase inhibitors, resuspend cells in 200μl lysate, add 1% NP-40 12.5μl after ice-bath for 15min, centrifuge for 10s to mix well, then centrifuge at 4℃ 13,000rpm, 5min. The pellet was resuspended in 25 μl of nuclear extraction buffer, placed in an ice bath for 15 minutes and shaken to fully lyse, centrifuged at 13,000 rpm at 4°C for 5 minutes, and the supernatant was collected for 5 minutes and stored at -70°C. Bradford method was used to detect nucleoprotein content.

[0051] Treat HUVEC cells overnight with compounds and LPS as described above, extract nuclear protein and measure protein concentration by Bradford method, take 5ug and add an equal volume of sample buffer to boil together for 5min, load the sample, sepa...

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Abstract

The invention discloses a novel use of a bisbibenzyl compound, in particular application of the bisbibenzyl compound shown as formula (I) or formula (II) in the specifications to preparation of medicaments for resisting inflammation and rheumatic arthritis or treating tumours caused by inflammation. The result of a study shows that the bisbibenzyl compound can be used for significantly inhibiting activities of an inflammatory factor interleukin-6(IL-6), monocyte chemoattractant protein (MCP-1), and a nuclear factor kB (NF-KB), and inhibiting gene expressions of inflammatory factors such as IL-6, interleukin-1b(1L-1b), NG-KB, a chemotactic factor (CCL2), cyclooxygenase 2(COX-2), intercellular adhesion molecule (Icam), a tumour necrosis factor (TNF) and the like, and presents an excellent anti-inflammatory effect; therefore, the bisbibenzyl compound is the medicament for resisting the inflammation and rheumatic arthritis or treating tumours caused by inflammation, has excellent development prospects and can be used as an essential component to prepare relevant oral preparations, injections and the like.

Description

technical field [0001] The present invention relates to the new application of bisbibenzyl compounds, in particular to the application of this type of compound in the preparation of non-steroidal anti-inflammation, anti-rheumatoid arthritis and anti-inflammation-induced medicaments. Background technique [0002] Inflammation is the body's defense response to stimuli. Any factor that can cause tissue damage, such as biological factors, physical factors and chemical factors can induce inflammation. According to the duration, inflammation can be divided into acute inflammation and chronic inflammation. Acute inflammation generally only manifests as vascular response, which is the body's normal defense response to stimuli from the body or outside the body, and is beneficial to the body. However, if the acute inflammatory response cannot eliminate the influence of stimuli, the inflammatory factors related to the acute inflammatory response will continue to exist and continue to...

Claims

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Application Information

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IPC IPC(8): A61K31/357A61K31/335A61P29/00A61P19/02A61P35/00
Inventor 娄红祥孙斌祝芳华刘慧萍薛霞邓景惕曲显俊
Owner SHANDONG UNIV
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