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Herba unicorn extract, its preparation method and its use in pharmacy

A single root grass and purpose technology, applied in the field of medicine, can solve the problems of difficulty in collection, no report on the biological activity of chemical composition system, and achieve the effect of strong application prospect and significant anti-neuroinflammatory activity.

Active Publication Date: 2019-06-21
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Oresitrophe rupifraga is a plant of the genus Saxifragaceae (Saxifragaceae) (this genus is a single species), mainly distributed in Henan, Hebei, western Liaoning and eastern Shanxi in my country. Its habitat is very unique and it mostly grows in It is very difficult to collect in valleys at an altitude of 600 to 2000 meters, in the damp rock crevices of cliffs, etc.; folks use the whole herb as medicine, which has the effect of clearing away heat and dampness, and can be used for enteritis and diarrhea in children. However, systematic research on its chemical components and related Biological activity has not been reported

Method used

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  • Herba unicorn extract, its preparation method and its use in pharmacy
  • Herba unicorn extract, its preparation method and its use in pharmacy
  • Herba unicorn extract, its preparation method and its use in pharmacy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Use 3kg of the whole herb of unicorn, crush it, soak it with 7L 90% methanol at room temperature for 36 hours, totally 4 times, combine the extracts from 4 times, concentrate under reduced pressure to obtain 383g of extract, and use 1.2L of water to extract the extract Disperse, and then sequentially extract with petroleum ether, ethyl acetate and n-butanol, and carry out preliminary segmentation of 85.9 g of the ethyl acetate part with a large silica gel column (10×80cm; 100-200mesh), and the eluent is petroleum ether, ethyl acetate Ester (from 5:1 to 0:1, v / v) and ethyl acetate, methanol (from 20:1 to 0:1, v / v) to obtain 5 components Fr.1-Fr.5; Fr .2 Use semi-preparative HPLC [MeOH / H 2 O 70:30, v / v; Flow rate: 3.0mL / min] to obtain compound 1 (3.8mg, t R =15.1min); Fr.5 (6.7g) was subjected to MCI column chromatography [MeOH / H 2 O(3:7-1:0, v / v)] and repeated normal phase silica gel column chromatography, by Sephadex LH-20 (CH 2 Cl 2 / MeOH, 2:1) to obtain compound 2...

Embodiment 2

[0025] Example 2: Anti-neuroinflammatory activity test experiment

[0026] Mouse microglial BV-2 cells were purchased from the American Type Culture Collection (Manassas, VA, USA) and cultured in DMEM (Dulbecco's modified Eagle's medium) medium (including 1800 mg / L NaHCO 3 , 10% (v / v) heat-inactivated fetal bovine serum (FBS), 100unit / mL penicillin G sodium salt and 100μg / mL streptomycin), 37°C, 5% CO 2 Environment, incubator; NO production was measured by Griess kit (Beyotime Biotechnology, China), that is, BV-2 cells were pretreated with different concentrations of test compounds for 4h, and then lipopolysaccharide (LPS, 1 μg / ml, Sigma- Aldrich) for 24h (no LPS was added to the blank group). Aspirate the culture supernatant, mix it with an equal amount of Griess reagent, and let it stand in the dark for 10 minutes at room temperature. Use a microplate reader (M200, TECAN, Austria GmbH, Austria) to measure the OD value of each group at a wavelength of 540nm, and use NaNO 2 ...

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Abstract

The invention relates to extracts of Oresitrophe rupifraga and a preparation method thereof, and application of the extracts to pharmacy, belonging to the technical field of medicine. According to the invention, a compound 1 and a compound 2 as shown in a formula 1 and formula 2 respectively are extracted and separated from the rare plant Oresitrophe rupifraga. Pharmacological test results show that the two compounds both have substantial neuroinflammation inhibitory activity, have IC50 values of 7.21[mu]M to 9.39 [mu]M respectively, exert no toxicity influence on cell survival and can be further used for preparation of drugs used for preventing and / or treating neurodegenerative diseases, especially for treating the Alzheimer's disease and the Parkinson's disease.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to an extract of Oresitrophe rupifraga Bunge, a preparation method thereof and a pharmaceutical application, especially an application in preparing medicine for treating neurodegenerative diseases. Background technique [0002] The prior art discloses neurodegenerative diseases (Neuro-degenerative diseases) including Alzheimer's disease (Alzheimer's disease, AD), Parkinson's disease (Parkinson's disease, PD), amyotrophic lateral sclerosis (Amyotrophic lateral sclerosis, ALS) and Huntington's disease (HD) etc. Studies have shown that the neurodegenerative diseases are aggravating with the aging of the global population, which not only seriously affects the quality of life of patients, but also brings a huge economic burden to the society. Although its pathogenesis is not clear at present, a large number of research data show that inflammation plays an important role in central nervou...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/341A61K31/704A61P25/28A61P25/16C07D307/12C07J17/00
Inventor 胡金锋熊娟武喜营刘新华潘礼龙杨国勋
Owner FUDAN UNIV
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