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Steroid saponin type compound as well as preparation method and application of steroid saponin type compound

A technology for steroidal saponins and compounds is applied in the field of medicine and achieves the effects of novel structure, simple extraction and separation method, and good anti-inflammatory activity

Active Publication Date: 2017-05-31
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Trillium is rich in steroidal saponins, which have anti-inflammatory, blood lipid-lowering, anti-tumor, analgesic and hemostasis, immune regulation and other effects. The steroidal saponin compounds with furan ring and their activities involved in the present invention have not been seen so far. patent or literature report

Method used

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  • Steroid saponin type compound as well as preparation method and application of steroid saponin type compound
  • Steroid saponin type compound as well as preparation method and application of steroid saponin type compound
  • Steroid saponin type compound as well as preparation method and application of steroid saponin type compound

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment 1: the preparation of formula I compound:

[0026] Use 1.7Kg of dried Trillium rhizome as raw material, heat and reflux extraction with 70% ethanol for 3 times, each time for 2 hours, concentrate to obtain extract-like ethanol extract, suspend the ethanol extract in water, add and suspend in turn Extract with petroleum ether, ethyl acetate, and n-butanol with equal volumes, and concentrate each extraction solution to obtain an extract. The n-butanol extract was subjected to silica gel column chromatography, and the dichloromethane-methanol solution with a volume ratio of 100:0-0:100 was used for gradient elution, wherein the elution ratio of dichloromethane-methanol was 100:30 The product was subjected to ODS column chromatography, and was eluted with a methanol-water solvent gradient with a volume ratio of 10:90-100:0, and the eluted part with a volume ratio of methanol-water of 70:30 was subjected to semi-preparative ODS high-performance liquid chromatograp...

Embodiment 2

[0027] Embodiment 2: the pharmacological activity of formula I compound

[0028] Test Method and Results

[0029] 1. The effect of the compound of formula I on the survival rate of RAW264.7 cells was detected by MTT method

[0030] Take the RAW264.7 cells cultured in the logarithmic growth phase, and adjust the cell density to 5×10 with fresh DMEM medium containing 10% fetal bovine serum. 4 Cells / mL were inoculated in 96-well plates, and after overnight growth, different concentrations of test compounds were added. After drug pretreatment for 1 hour, LPS (100 ng / mL) was added to continue culturing for 24 hours, and finally the cell viability was detected. After adding 20 μL of MTT (5 mg / mL) to each well, culture was continued for 4 h in the incubator. Carefully aspirate the upper medium, and add 100 μL of DMSO to each well. Leave it for 10 minutes and shake it for about 40 seconds to completely dissolve the formazan crystals. The 96-well plate was placed in a microplate re...

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PUM

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Abstract

The invention belongs to the technical field of medicines, and relates to a new steroid saponin type compound extracted and separated out from roots and tubers of trillium tschonoskii, and application of the new steroid saponin type compound to preparation of an inflammatory cell inhibitor. The compound has a chemical structural formula shown as a formula I; an experiment result shows that the new steroid saponin type compound can be used for inhibiting generation of an inflammatory mediator NO in mouse monocyte-macrophages RAW264.7 under the stimulation of LPS (Lipopolysaccharide); a preparation method of the compound is simple and easy, and further pharmacological and clinical researches are easy to carry out; the application of the new steroid saponin type compound in anti-inflammatory drugs is developed. (The formula I is shown in the description.).

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a steroidal saponin compound and its preparation method and application, in particular to a new steroidal saponin extracted and separated from trillium rhizomes, its preparation method and its preparation method for anti-inflammatory Uses in medicine. Background technique [0002] Inflammation refers to a very important and common pathological process in which the body uses systemic living tissues to defend against external inflammatory factors in response to external stimuli. Non-steroidal drugs are currently commonly used anti-inflammatory drugs in clinical practice. In my country, their consumption is second only to anti-infective drugs. However, there are many adverse reactions, such as affecting the digestive system, and long-term use can lead to gastric ulcers. In recent years, traditional Chinese medicine has received widespread attention due to its good anti-inflammatory...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J71/00A61K31/7048A61P29/00
CPCC07J71/0005
Inventor 贾景明阎婷胡高升
Owner SHENYANG PHARMA UNIVERSITY
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