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New application of phthalide compound to lowering of uric acid

A technology of phthalides and compounds, applied in the new application field of phthalide compounds in lowering uric acid, can solve the problems such as the inability to accurately control the quality of chuanxiong

Active Publication Date: 2020-01-03
CATCH BIO SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among them, the 2010 edition of the "Chinese Pharmacopoeia" uses ferulic acid as its quality control index, but the highest mass fraction of ferulic acid is only 0.9mg / g, which also exists in other traditional Chinese medicines, and the quality of Chuanxiong cannot be accurately controlled.

Method used

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  • New application of phthalide compound to lowering of uric acid
  • New application of phthalide compound to lowering of uric acid
  • New application of phthalide compound to lowering of uric acid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] Weigh 50 kg of the dried rhizomes of Chuanxiong, crush the dried rhizomes of Chuanxiong, soak and extract with 8 times the volume of hot water at 80°C for 1 h, discard the filtrate, and extract the residue with 8 times the volume of 80% ethanol solution by slight boiling for 2 h , and concentrated under reduced pressure to remove the organic solvent to obtain concentrated solution A (solid content 7kg in concentrated solution A); Pass concentrated solution A through 50L-D101 column (column diameter 22cm × height 150cm), with volume fractions of 30% and 95% respectively Rinse 4 column volumes with ethanol respectively, collect the eluate whose volume concentration is 95% ethanol, and concentrate under reduced pressure to remove the organic solvent to obtain concentrated solution B (solid content of concentrated solution B is 1.5 kg). Concentrate B was passed through a 25L-LX-20SS column (column diameter 20cm×height 80cm), washed with ethanol solutions with a volume fracti...

Embodiment 2

[0072]Take by weighing 70kg of the dry aerial part of Chaxiong, after the shredding, be 80% ethanol solution immersion extraction 2 times with the volume fraction of 8 times of volume, and concentrate under reduced pressure to remove the organic solvent, obtain concentrated solution A (solid content 4.5 in concentrated solution A). kg); Concentrated solution A was extracted 3 times with petroleum ether, dichloromethane and ethyl acetate successively, and the extraction solvent was recovered under reduced pressure to obtain petroleum ether extract (2kg), dichloromethane extract (1kg) and ethyl acetate respectively. Ester extract (0.8 kg).

[0073] Wherein, the petroleum ether extract was separated by silica gel column chromatography, and gradient elution was carried out with a mixed solution with a volume ratio of petroleum ether: ethyl acetate (initial volume ratio 20:1, final volume ratio 1:1), TLC Detection and merging of the same fractions resulted in 4 fractions: Fr.PE1-PE...

Embodiment 3

[0077] Weigh 50 kg of dried roots of Angelica sinensis, pulverize, soak and extract 2 times with 6 times the volume fraction of 90% ethanol solution, and concentrate under reduced pressure to remove the organic solvent to obtain concentrated solution A; Ethyl ester and n-butanol were extracted, and the extraction solvent was recovered under reduced pressure to obtain petroleum ether extract (2kg), ethyl acetate extract (150g) and n-butanol extract (90g).

[0078] The petroleum ether extract was extracted with 80% methanol solution by volume, and divided into petroleum ether extract (upper layer, 700 g) and 80% methanol solution extract (lower layer, 1.4 kg). The lower layer extract was separated by regular pressure silica gel column chromatography, and gradient elution was carried out with a mixed solution with a volume ratio of n-hexane:acetone (initial volume ratio of 20:1, final volume ratio of 1:1), and TLC detected and merged the same parts, 8 eluates were obtained: Fr.A-...

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Abstract

The invention belongs to the field of drugs or health care products, and particularly relates to new application of a phthalide compound to lowering of uric acid. The phthalide compound has a structure shown in a formula (I) (please see the specification for the formula (I)), wherein R1-R7 are shown in the definition of the specification of the invention. Through an animal model with hyperuricemia, it is found that the phthalide compound promotes uric acid excretion in the body, has a significant effect of lowering the uric acid, and can be used as a potential drug for lowering the uric acid or treating gout.

Description

technical field [0001] The invention belongs to the field of medicines or health products, and in particular relates to a new use of phthalide compounds in reducing uric acid. Background technique [0002] Uric acid is the final metabolite of human purine compounds, and disorders of purine metabolism lead to hyperuricemia. Under a normal purine diet, the fasting blood uric acid level on two different days is higher than 416 μmol / L in men and 360 μmol / L in women, which is called hyperuricemia. Gout is a crystal-related arthropathy caused by the deposition of monosodium urate (MSU), which is directly related to hyperuricemia caused by disturbance of purine metabolism and / or decreased uric acid excretion. , recurrent gouty acute arthritis, gouty chronic arthritis and tophi, gouty nephropathy and renal uric acid stones, etc. In severe cases, joint disability and renal insufficiency may occur. In addition, gout is often accompanied by abdominal obesity, hyperlipidemia, hyperten...

Claims

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Application Information

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IPC IPC(8): A61K31/365A61P19/06A23L33/10
CPCA61K31/365A61P19/06A23L33/10A23V2002/00A23V2200/30A23V2250/30Y02P20/55
Inventor 不公告发明人
Owner CATCH BIO SCI & TECH