A kind of guaiacane-type sesquiterpene compound and its preparation method and application
A compound and composition technology, applied in the field of medicine, can solve problems such as potential safety hazards and unclear active ingredients, and achieve strong effects, anti-inflammatory effects, and inhibitory effects
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Embodiment 1
[0033] The preparation of the compound of structure shown in embodiment 1 formula I
[0034] 1) 5,000 sticks of finished Reduning injection were dried under reduced pressure to obtain concentrated Reduning injection;
[0035] 2) Take the concentrated solution of step 1) and add purified water to dilute it, let it stand at room temperature, take the supernatant and separate it through a HP-20 macroporous adsorption resin column, elute with purified water of 4 times the column volume, and discard the eluent , carry out gradient elution with different concentrations of ethanol (10% ethanol, 30% ethanol, 50% ethanol, 70% ethanol, 95% ethanol, each eluent collects 4 column volumes), collects 95% ethanol elution site ;
[0036] 3) Take the 90% ethanol elution part of step 2), and separate through silica gel column (100-200 mesh silica gel) chromatography, and carry out gradient elution with dichloromethane-methanol as eluent (dichloromethane-methanol volume ratio respectively 1:0,...
Embodiment 2
[0049] The preparation of the compound of structure shown in embodiment 2 formula I
[0050] 1) 5,000 sticks of finished Reduning injection were dried under reduced pressure to obtain concentrated Reduning injection;
[0051] 2) Take the concentrated solution of step 1) and add purified water to dilute it, let it stand at room temperature, take the supernatant and separate it through a D101 macroporous adsorption resin column, elute with purified water of 3 times the column volume, discard the eluent, and use Carry out gradient elution with different concentrations of ethanol (5% ethanol, 25% ethanol, 45% ethanol, 65% ethanol, 90% ethanol, each eluent collects 3 column volumes), and collect the elution site of 90% ethanol;
[0052] 3) Take the 90% ethanol elution part of step 2), separate it through silica gel column (100-200 mesh silica gel) chromatography, and carry out gradient elution with dichloromethane-methanol as eluent (dichloromethane-methanol volume ratio respective...
Embodiment 3
[0056] Example 3 The compound of the structure shown in formula I resists PGE in vitro 2 experiment
[0057] 1. Materials
[0058] 1.1 Drug Compound shown in structural formula I;
[0059] 1.2 Cell model Mouse macrophage cell line RAW 264.7, from the Academy of Chinese Medical Sciences, provided by the entrusting party Jiangsu Kangyuan Pharmaceutical Co., Ltd.; culture conditions: DMEM+10% fetal bovine serum (FBS), 37 ° C, 5% CO 2 .
[0060] 2. Principles and methods
[0061] 2.1 Experimental principle
[0062] Lipopolysaccharide (LPS) of the outer membrane of Gram-negative bacteria (Sigma, USA, batch number: 114M4009) is one of the most important pathogenic molecules that mediate infectious inflammatory damage, and many diseases are closely related to the persistent subclinical inflammation induced by LPS. In animal and cell experiments, LPS is widely used to induce inflammation.
[0063]Macrophages play a vital role in the inflammatory response. After being stimulated,...
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