New application of polyalkynes in lowering uric acid
A technology for lowering uric acid and polyacetylene, which can be used in medical preparations containing active ingredients, pharmaceutical formulas, bone diseases, etc., and can solve undisclosed problems.
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Embodiment 1
[0044] Example 1 Preparation of Compound 1-15
[0045]
[0046]
[0047] Take 100 kg of the flower heads of the chrysanthemum chrysanthemums of Compositae (Comppositae), crush them, soak and extract them with 15 times the volume of ethanol solution with a volume concentration of 70%, the extraction temperature is 50-100°C, the extraction time is 20min-120min, and concentrated under reduced pressure to Without solvent, the concentrate was obtained; the concentrate was extracted three times by adding 1 volume times of ethyl acetate, the ethyl acetate layers were combined, and concentrated under reduced pressure until there was no solvent to obtain the ethyl acetate extract; the ethyl acetate extract was subjected to ODS Separation by reverse-phase silica gel column chromatography, using methanol as mobile phase A and water as mobile phase B, and carrying out gradient elution at a flow rate of 1 mL / min according to the following procedure: the volume fraction of mobile phas...
Embodiment 2
[0059] Example 2 Preparation of Compound 16-23
[0060]
[0061] Take 100kg of Compositae plant Atractylodes atractylodis, soak and extract with 15 times the volume of ethanol aqueous solution with volume concentration of 70% after crushing, the extraction temperature is 50-100°C, the extraction time is 20min-120min, and concentrated under reduced pressure until there is no solvent, to obtain Concentrate A; the concentrate was separated by a low-pressure D101 column (column diameter 28cm×height 162cm, column volume 100L), ethanol-water (30:70, 4BV; 95:5, 4BV) gradient elution, and 95% of the parts were collected; the After the part is concentrated (solid content about 3kg), it is separated by LX-20SS column (column diameter 20cm×height 78cm, column volume 25L), ethanol-water (70:30, 3BV; 80:20, 3BV; 95:5, 4BV) Gradient elution, 95% of the parts were collected to obtain the crude concentrated solution B (solid content about 1 kg).
[0062] The concentrated solution B was ...
experiment example 1
[0077] Experimental example 1 Research on the Uric Acid-lowering Effect of the Compounds of the Invention
[0078] 1. Experimental method
[0079] 1.1 Experimental animals and grouping
[0080] 300 healthy male KM mice, weighing 15-18g, were provided by Beijing Weitong Lihua Biotechnology Co., Ltd.; after being divided into cages with 5 mice per cage, they were adapted in the barrier system of Suzhou Kaixiang Biotechnology Co., Ltd. Sexually raised for 4 days, selected 260 from 300, divided into 26 groups at random according to body weight, 10 in each group, respectively blank control group, model control group, positive control group, experimental group 1-23 groups (respectively with compound 1-23 is test drug).
[0081] 1.2 Administration method
[0082] After the adaptation period, the mice were given intragastric administration immediately, once a day in the morning, wherein, the experimental groups 1-23 were treated with 0.5% carboxymethyl cellulose sodium (CMC-Na) s...
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