Ergosterol compounds with anti-inflammatory activity, and preparation method and application thereof

An ergosterol and compound technology, applied in the preparation of anti-inflammatory drugs, the ergosterol compound and the preparation field thereof, can solve the problems such as no ergosterol compound NO inhibitor, etc.

Inactive Publication Date: 2019-08-20
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are no reports of ergosterol compounds and their use as NO inhibitors in the preparation of anti-inflammatory drugs in the prior art

Method used

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  • Ergosterol compounds with anti-inflammatory activity, and preparation method and application thereof
  • Ergosterol compounds with anti-inflammatory activity, and preparation method and application thereof
  • Ergosterol compounds with anti-inflammatory activity, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Separation and purification of compounds:

[0028] The method for preparing the compound, crushing the fruit body of Zizhi lucidum, extracting with 95% ethanol under reflux for 2 hours, combining the extracts and recovering the crude extract of the solvent under reduced pressure, suspending the crude extract in water, extracting three times with an equal volume of ethyl acetate, combining the extraction The ethyl acetate extract concentrated under reduced pressure, the extract was subjected to silica gel 200-300 mesh column chromatography, chloroform / methanol system (100:1,50:1,20:1,10:1,5:1, 2:1, 1:1 and 0:1 v / v) gradient elution, and 7 fractions were collected. Fraction C6 was subjected to reverse phase RP-18 column chromatography, eluting with 10%-100% methanol / water to obtain 4 sub-fractions. The fraction of C6-3 was analyzed by HPLC (MeCN / H 2 0,20%-60%, 8mL / min) to obtain compound 1 (6mg, t R =12.4min), 2(4mg,t R =18.3min), and 3(2mg,t R = 20.1 min).

[0029]...

Embodiment 2

[0042] Anti-inflammatory activity test

[0043] The monomeric compounds 1-3 acted on lipopolysaccharide (LPS)-induced RAW264.7 mouse macrophages respectively, and the NO level in the culture supernatant was detected by the Griess reagent chromogenic method to determine the ability of the test drugs to inhibit the release of NO As a screening index, the anti-inflammatory activity of the compound was evaluated.

[0044] 1. Preparation of drug solution:

[0045] (1) The monomer compounds 1-3 were respectively prepared into 100 μg / ml solutions with DMSO, and stored at -4°C;

[0046] (2) LPS: E.Coli O111:B4 (Merck Millipore, USA, product number: LPS25), made into a 100 μg / mL solution with redistilled water, and stored at -20°C.

[0047] 2. Cell line: RAW264.7 mouse macrophages, provided by the Shanghai Branch of the Chinese Academy of Sciences.

[0048] 3. Test method:

[0049] (1) A single mouse macrophage suspension was prepared with 10% fetal calf serum culture medium, and t...

Embodiment 3

[0058] Preparation of injection preparations:

[0059] First obtain compounds 1, 2, and 3 of the present invention according to the method of Example 1, take 50 mg of one or several compounds, dissolve it in 2 ml of propylene glycol, filter the resulting solution and pack it into an ampoule under aseptic conditions .

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PUM

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Abstract

The invention discloses ergosterol compounds with anti-inflammatory activity, and the ergosterol compounds are from Ganoderma sinensis and are as shown in a structural formula which is described in the specification. The invention also discloses a preparation method for the compounds and application of the compounds in pharmacy. The compounds can be applied as NO inhibitors to the preparation of anti-inflammatory drugs.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to ergosterol compounds extracted and separated from Zizhi lucidum, a preparation method thereof and their application as NO inhibitors in the preparation of anti-inflammatory drugs. Background technique [0002] Nitric oxide (NO) is a chemical substance with biological regulation function, which has important reference and application value in the research of inflammation. Studies have shown that when macrophages are stimulated by toxins, inflammatory mediators, etc., it will lead to a large amount of nitric oxide synthase (iNOS), and nitric oxide synthase (iNOS) catalyzes the L-arginine in its substrate , produce NO as the main product of the immune response, so the amount of NO produced in the screening of inflammatory activity can be used as an important indicator of the anti-inflammatory activity of the test drug. LPS-induced mouse macrophages (RAW 264.7) were us...

Claims

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Application Information

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IPC IPC(8): C07J9/00A61P29/00A61K31/575
CPCA61P29/00C07J9/00
Inventor 梅任强段晓燕解勇王雅琴许艳勇
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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