Clerodane diterpene derivative and preparation method thereof and anti-inflammatory drug or inflammatory reaction inhibitor thereof
A technology of Crotane-type diterpene and anti-inflammatory drugs, which is applied in the field of anti-inflammatory drugs or inflammatory response inhibitors, preparation, Crotane-type diterpene derivatives, and can solve the problem of insufficient research on anti-inflammatory drug ingredients, Issues such as no Crotane-type diterpene derivatives, no Crotane-type diterpene derivatives and application reports of their pharmaceutical compositions
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[0032] The preparation method of the above-mentioned Crotane type diterpene derivatives,
[0033] Including pretreatment: the stems and leaves of the whole leaves of Zizhu are dried and pulverized;
[0034] Extraction: extracting the crushed stems and leaves of the whole leaf of Zizhu with 70% acetone / water solution at room temperature;
[0035] Purification: the extracted product is sequentially extracted with petroleum ether, ethyl acetate and n-butanol, and then the obtained extract is concentrated under reduced pressure and decolorized with MCI small-pore resin to obtain an extract;
[0036] Separation:
[0037] 1) Dissolve the extract in chloroform and adsorb it on silica gel, place it at 20-25°C to evaporate the solvent to dry, grind it, and perform silica gel column chromatography, eluting with 1:0 → 0:1 gradient of chloroform / methanol to obtain A-F six fractions;
[0038] 2) Part B obtained in step 1) was sectioned by medium-pressure reversed-phase C-18 column chrom...
Embodiment
[0058] The preparation method of Crotane type diterpene derivatives:
[0059] 1) Take the stem and leaf part of the whole leaf Zizhu, dry and pulverize;
[0060] 2) Using 70% acetone / water at room temperature, extracting the stem and leaf part of the whole-marginal leaves of Aurantia chinensis crushed in step 1) for 3 times, combining the acetone extracts, filtering, and concentrating under reduced pressure;
[0061] 3) suspending the extract obtained in step 2) in an aqueous solution, sequentially extracting with petroleum ether, ethyl acetate and n-butanol, and decolorizing the extracted part of ethyl acetate with MCI to obtain its extract;
[0062] 4) The extract obtained in step 3) was dissolved and adsorbed on silica gel with chloroform, placed at room temperature until the solvent was evaporated to dryness, ground, and subjected to silica gel column chromatography, eluted with a gradient of 1:0→0:1 chloroform / methanol, Get six fractions of A-F;
[0063] 5) Part B obtai...
Embodiment 2
[0081] According to the method of Example 1, the Crotane-type diterpene derivative I was first prepared, and after dissolving with a small amount of DMSO, water for injection was added as usual, finely filtered, potted and sterilized to make an injection.
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