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A kind of active ingredient extracted and isolated from egg-leaf spider brooding plant and its application

一种用途、化合物的技术，应用在药学领域，能够解决尚未有药物等问题

Inactive Publication Date: 2017-07-04
SICHUAN AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The study found that the benzocoumarin-containing compounds and plant-derived xanthone compounds have good antibacterial activity, but there is no report on the structure and antibacterial activity of the new benzocoumarin compounds, nor Plant-derived xanthone compounds have been reported to be active against Gram-negative bacteria, so there are no related drugs on the market

Method used

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  • A kind of active ingredient extracted and isolated from egg-leaf spider brooding plant and its application
  • A kind of active ingredient extracted and isolated from egg-leaf spider brooding plant and its application
  • A kind of active ingredient extracted and isolated from egg-leaf spider brooding plant and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1: The structural formula of Compound I referred to in the following examples:

[0033] Compound I

[0034] 1 Preparation of extract

[0035] 5.55Kg dried slices of the rhizomes of the egg-leaf spider, 70% ethanol were ultrasonically extracted 3 times (mass volume ratio 1:30), each time for 1 hour. Filter out the medicinal residues, combine the filtrates and concentrate under reduced pressure to an extract without alcohol smell; then disperse the concentrate in water, and extract it with petroleum ether (boiling range 30~60°C), chloroform, ethyl acetate and n-butanol in sequence for 3 times, respectively concentrated under reduced pressure at 50°C to obtain extracts of various parts. The combined chloroform parts were concentrated and dried to give 21.14 g, and the ethyl acetate parts 13.43 g (see figure 1 ).

[0036] 2 Separation and purification of compounds

[0037] 21.14 g of the chloroform part of the ovale spider's brood egg was detected by silica ...

Embodiment 2

[0040]Example 2: The structural formula of compound II referred to in the following examples:

[0041] Compound II

[0042] 1 Preparation of extract

[0043] With embodiment 1.

[0044] 2 Separation and purification of compounds

[0045] 21.14 g of the chloroform part of the ovale spider's brood egg was detected by silica gel column chromatography (silica gel H, 200-300 mesh, 420 g, eluted with chloroform:methanol 500:1-10:1), detected by thin-layer chromatography (TLC), and eluted The solution was concentrated and combined to obtain five parts Fr.A1 ~ Fr.A5.

[0046] The Fr.A2 part is light yellow powder, about 5.4g, mixed with silica gel (100-200 mesh), air-dried for H silica gel column chromatography, and gradient washing with chloroform:methanol (300:1~10:1) system Take off, take one bottle per 75ml. Three fractions were obtained, and Fr.A2-1 was subjected to H silica gel column chromatography again, and after the purity was checked by TLC, compound I ovale xanthone...

Embodiment 3

[0048] Embodiment 3: the synthesis of ovariocoumarin methyl acetylated derivatives

[0049]

[0050] 1

[0051] Put coumarin A I (10 mg, 0.03 mmol) and DMAP (3 g, 0.02 mmol) in a 25 ml round bottom flask, dissolve them in 5 ml THF, then add two drops of acetic anhydride (about 10 mg , 0.06 mmol), reacted at 40°C for 5 h, evaporated the solvent under reduced pressure to obtain residue 1a. The residue 1a was separated by silica gel (0.1 g) column chromatography and eluted with chloroform-methanol (220:1) to obtain compound 1 (white amorphous powder, 4.3 mg, yield 43%). Compound 1: ESIMS m / z 285 [M+H] + .

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PUM

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Abstract

The invention relates to a preparation method and an application of benzocoumarin compounds and simple plant source xanthone compounds. Aspidistra typica baill is adopted to produce the benzocoumarin compounds and the simple plant source xanthone compounds which are novel in structure. According to experiments, the compounds can be used as medical bacteriostatic preparations.

Description

technical field [0001] The present invention relates to egg-laying spider with egg leaf ( Aspidistra typica Baill.) (preservation number: No.20140316-1) method for producing simple plant-derived xanthone compounds and novel benzocoumarin compounds; the present invention also relates to the use of these two types of compounds in the preparation of antibacterial preparations The use belongs to the field of pharmacy. Background technique [0002] Egg leaf spider brooding eggs (scientific name: Aspidistra typica Baill.) is a plant of the family Asparagaceae, with thicker rhizomes and nearly cylindrical. Leaves 2-3 clustered, ovoid-lanceolate to ovate; petiole obvious, hard. The total pedicel is often pulled out in clusters, slender; bracts 3-5, ovate; perianth is urn-shaped, with purple dots outside and dark purple inside; lobes ovate, shorter; stamens 6, few filaments; ovary Short, stubby style, no joints; stigma large, round, shield-shaped expansion. Berries spherical. ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D311/80C07D311/86A61P31/04
CPCC07D311/80C07D311/86Y02A50/30
Inventor 梁晓霞费文波孔令茜贺常亮殷中琼吕程林居纯尹力子邹元峰何敏
Owner SICHUAN AGRI UNIV
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