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New application of sesquiterpenoids to uric acid lowering

A technology of sesquiterpenoids and compounds is applied in the field of new uses of sesquiterpenoids in lowering uric acid, which can solve the problems of triggering acute gout attacks, low drug tolerance, and increasing the risk of cardiovascular system diseases.

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

However, the toxic and side effects of the above-mentioned medicines are usually larger, for example: allopurinol can cause severe toxic and side effects such as allergic reactions (10-15% incidence rate), hypersensitivity syndrome, bone marrow suppression; probenecid, benzbroma Longze has side effects such as irritating the gastrointestinal tract, causing renal colic, and triggering acute attacks of gout; febuxostat can increase the risk of cardiovascular system diseases, and in severe cases, Stevens-Johnson syndrome can occur; moreover, the tolerance of the above drugs generally low sex
In summary, these problems limit the clinical application of these drugs to a certain extent

Method used

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  • New application of sesquiterpenoids to uric acid lowering
  • New application of sesquiterpenoids to uric acid lowering
  • New application of sesquiterpenoids to uric acid lowering

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Weigh 50 kg of inula chinensis medicinal material, pulverize the inulin inulin, soak and extract 3 times with 8 times the volume of ethanol solution with a volume fraction of 90%, and concentrate under reduced pressure to remove the organic solvent to obtain concentrated solution A; pass the concentrated solution A over 50 L -D101 column (column diameter 22cm × height 150cm), wash 4 column volumes respectively with volume fraction of 40% and 95% ethanol, collect the eluate with volume fraction of 95% ethanol, and concentrate under reduced pressure to remove the organic solvent to obtain Concentrated solution B (solid content in concentrated solution B is 3.2kg), concentrated solution B was extracted with petroleum ether for 3 times, and the extraction solvent was recovered under reduced pressure to obtain 2 kg of petroleum ether extract. The petroleum ether eluate was separated by silica gel column chromatography, and gradient elution was carried out with a mixed solutio...

experiment example 1

[0052] Experimental example 1 Research on the Uric Acid-lowering Effect of the Compounds of the Invention

[0053] 1. Experimental materials

[0054] 150 healthy male KM mice, weighing 15-18 g, were provided by Beijing Weitong Lihua Biotechnology Co., Ltd.; 5 mice per cage were divided into cages, and then adaptively reared in the barrier system for 4 days.

[0055] 2. Experimental method

[0056] 2.1 Experimental grouping

[0057] Select 120 mice with concentrated body weight from 150 mice and randomly divide them into 12 groups according to body weight, with 10 mice in each group, which are blank control group, model control group, positive control group, and experimental groups 1-9.

[0058] 2.2 Administration method

[0059] Immediately after the adaptation period, the mice were intragastrically administered once a day in the morning for 7 consecutive days.

[0060] Experimental groups 1-9 were given 25 mg / kg of compound 1-9, and compound 1-9 were suspended with 0.5%...

experiment example 2

[0079] Experimental example 2 Research on the effect of the compound of the present invention on promoting uric acid excretion

[0080] 1. Experimental materials

[0081] 150 healthy male KM mice, weighing 15-18 g, were provided by Beijing Weitong Lihua Biotechnology Co., Ltd.; 5 mice per cage were divided into cages, and then adaptively reared in the barrier system for 4 days.

[0082] 2. Experimental method

[0083] 2.1 Experimental grouping

[0084] Select 120 mice with concentrated body weight from 150 mice and randomly divide them into 12 groups according to body weight, with 10 mice in each group, which are blank control group, model control group, positive control group, and experimental groups 1-9.

[0085] 2.2 Administration method

[0086] Immediately after the adaptation period, the mice were intragastrically administered once a day in the morning for 6 consecutive days.

[0087]Experimental group 1-9 groups were given compound 1-9 25mg / kg respectively, suspen...

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PUM

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Abstract

The invention belongs to the field of drugs or health care products, and particularly relates to new application of sesquiterpenoids to uric acid lowering. The sesquiterpenoids include the structure shown in a formula (I) (please see the specification for the formula (I)), wherein R1, R2, R3 and R4 are shown as definitions of a specification of the invention. Through a hyperuricemia animal model,it is found that the sesquiterpenoids promote uric acid excretion in vivo, has the significant uric acid lowering effect, and can serve as a potential drug for lowering uric acid or treating gout.

Description

technical field [0001] The invention belongs to the field of medicines or health care products, and in particular relates to the new application of sesquiterpenoids in reducing uric acid. Background technique [0002] Uric acid is the final metabolite of human purine compounds, and purine metabolism disorders lead to hyperuricemia. Under a normal purine diet, if the blood uric acid level on an empty stomach is higher than 416 μmol / L for men and 360 μmol / L for women on two different days, it is called hyperuricemia. Gout is a crystal-associated arthropathy caused by the deposition of monosodium urate (MSU), which is directly related to hyperuricemia caused by purine metabolic disorders and / or decreased uric acid excretion. The main clinical manifestation is hyperuricemia , 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, gou...

Claims

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Application Information

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IPC IPC(8): A61K31/365A61P19/06
CPCA61K31/365A61P19/06
Inventor 不公告发明人
Owner CATCH BIO SCI & TECH
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