Application of japonicone A in preparation of tumor necrosis factor (TNF) inhibitor drugs
A technology of tumor necrosis factor and inula lactone, which can be used in anti-tumor drugs, drug combinations, respiratory diseases, etc., can solve problems such as slow progress in applied research, and achieve the effect of great clinical application value.
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Embodiment 1
[0037] Example 1 Preparation of compound bisinulalide A
[0038] Dry inula (I.japonica, grown in Bozhou, Anhui, commercially available) aerial parts including stems, leaves, flowers) 10.0kg powder, room temperature (25 ℃) with 95% ethanol extraction 3 times, each Each time 80L took 24, 12, 12 hours respectively. After diluting 408.7 g of the obtained crude extract with an appropriate amount of water 10 L, it was sequentially extracted with 40 L of petroleum ether for four times, 40 L of dichloromethane for four times, 40 L of ethyl acetate for four times, and 10 L of n-butanol for extraction. The obtained dichloromethane extract 42.3g was separated with 200-300 mesh thin-layer silica gel, and the 2 Cl 2 - MeOH (100:0, 50:1, 20:1, 10:1, 5:1, 2:1,) for gradient elution. Thin-layer chromatography detects, collects and contains diinulalide A therein, adopts Sephadex LH-20 to carry out separation again, uses CH 2 Cl 2 -MeOH (1:1) was used to elute the mixture to obtain a mixtu...
Embodiment 2
[0040] Example 2 Virtual target screening suggests that TNF-α is the target of inulalide A
[0041] Inverse molecular docking calculations were performed using the INVDOCK software package. The software package has been patented by the United States (Patent No. US6519611). In this method, the three-dimensional structure of the drug molecule is input, and the combination of the drug molecule and the protein in the protein three-dimensional structure database is simulated by a computer program, so as to predict the protein to which the drug molecule binds and the binding active site. Using the INVDOCK software package, the potential target proteins of the active ingredients of traditional Chinese medicine can be predicted.
[0042] In this application, the three-dimensional structure of inulalide A was input into the INVDOCK software package for the NF-κB (cell transcription factor) signaling pathway (NF-Kbsignaling pathway) in the Biocarta signaling pathway database, see http:...
Embodiment 3
[0043] Example 3 BIACORE (Biomacromolecule Interaction Analyzer) analysis confirms the interaction between inulalide A and TNF-α
[0044] In order to further verify the direct interaction between inula lactone A and TNF-α, the biomolecular interaction analysis equipment BIACORE 3000 developed by Amersham Bioscience based on the principle of surface plasmon resonance (SPR) was used to analyze the interaction between inula lactone A and TNF-α. Interaction between lactone A and recombinant TNF-α molecule coupled to a sensor chip. The experimental process is as follows: Firstly, recombinantly expressed TNF-α (purchased from GeneTex, Inc., USA, purity>98%) is covalently coupled to the surface of the sensor chip using the amino coupling method in Biacore 3000 control software, and TNF-α is coupled to the surface of the sensor chip. The joint volume is 4000 Response Units (Response Unit, RU) ( image 3 ); the compound was dissolved in phosphate buffer containing 1‰ dimethyl sulfoxid...
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