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Poly-acetylenic acid derivative

A technology of polyalkynoic acid and derivatives, which is applied in the field of medicine and can solve the problem of no active ingredients of thymegrass

Inactive Publication Date: 2017-12-08
SHANGHAI UNIV OF T C M
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are no reports on thyme extract and its active ingredients for the treatment of common oral diseases such as periodontitis and dental caries

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Take 6Kg of the whole herb of Thyme chinensis, crush it, add 30L 95% ethanol to heat and reflux for extraction for 5 hours, repeat 4 times, filter and combine the extracts, recover the ethanol under reduced pressure, and suspend the extract in water.

[0038] Extract the suspension with petroleum ether (60-90°C) several times until the petroleum ether layer is nearly colorless, discard the petroleum ether layer; then extract the water layer with ethyl acetate saturated with water until the ethyl acetate layer is nearly colorless; The ethyl acetate layer was recovered under reduced pressure to obtain the ethyl acetate fraction. Through silica gel column chromatography, petroleum ether-ethyl acetate system was used successively, and the volume ratio was (100:1), (50:1), (20:1), (10:1), (5:1), ( 2:1), (1:1), (0:1) elution, collect (5:1) to (1:1) eluate, recover the solvent under reduced pressure, and obtain the extract. By ODS reverse phase column chromatography, gradient...

Embodiment 2

[0050] Detect the Thymus ethanol extract (EtOH extract) gained in Example 1, and the extracted petroleum ether fraction (PE fraction), the impact of ethyl acetate fraction (EtOAc fraction) on periodontitis pathogenic bacteria Porphyromonasgingivalis, the results show that the ethanol extract And ethyl acetate part has a certain inhibitory activity of periodontitis pathogenic bacteria Porphyromonas gingivalis.

[0051] According to the quality of the drug, 200mg / mL mother solution was formulated with DMSO, and after shaking, it was found that it could be dissolved without precipitation. The dilution test was started from the drug toxicity upper limit of 1000 μg / mL. At the beginning, the concentrations of the three samples were set at 1000, 500, 200, 100, and 50 μg / mL, respectively, and the initial concentration of Porphyromonas gingivalis was 10^7 / mL. They were co-cultured for 48 hours, and the growth of bacteria in each group was observed with the naked eye. Repeat 2 times. ...

Embodiment 3

[0055] Detect the impact of the three polyalkynoic acid components obtained in Example 1 on periodontal disease pathogenic bacteria (Porphyromonas gingivalis, Fusobacterium nucleatum), and the results show that polyalkynoic acid derivatives can inhibit periodontal disease pathogenic bacteria (Porphyromonas gingivalis, Fusobacterium nucleatum) ) growth. At the same time, it has no cytotoxicity to hGFs. It shows that this kind of compound has antibacterial effect and good safety.

[0056] According to the quality and molecular weight of the drug, DMSO was used to make a 10mM mother solution, and after shaking, it was found that it could be dissolved without precipitation. The two-fold dilution assay was started from 200 μM, the upper limit of drug toxicity. At the beginning, the concentrations of the three drugs were set at 200, 100, and 50 μM, respectively, the initial concentration of Porphyromonas gingivalis was 10^7 / mL, and the initial concentration of Fusobacterium nuclea...

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Abstract

The invention belongs to the technical field of medicines, and relates to a poly-acetylenic acid derivative separated from thesium chinensis, a preparation method of the poly-acetylenic acid derivative, and application in preparing medicines for treating common oral diseases.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a class of polyalkynoic acid derivatives isolated from Thymeca officinalis, its preparation method, and its application in the preparation of medicines for common oral diseases Background technique [0002] Thyme officinalis is a commonly used Chinese herbal medicine. It was first recorded in "Bencao Tujing" in the Song Dynasty, and it was originally recorded in the 1977 edition of "Chinese Pharmacopoeia". Department of herbs or shrubs, with parasitic or semi-parasitic as its main biological characteristics. It has the effects of "clearing away heat and detoxifying", "smoothing the Qi veins" and "regulating Qi". It has the reputation of "plant antibiotics". There is no mention of its activity in the treatment of common oral diseases in current literature reports. [0003] The main components in thyme include polysaccharides, glycosides, flavonoids, alkaloids, steroids, organic ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C57/18C07C57/00C07C51/42C07C51/47A61K31/20A61K31/201A61P29/00A61P11/00A61P1/02A61K8/36A61Q11/00A61K9/20A61K47/38
CPCA61K8/361A61K9/0056A61K9/2054A61K36/185A61Q11/00C07C51/42C07C51/47C07C57/00C07C57/18
Inventor 王峥涛刘畅黎万奎韩竹箴杨莉程绒绒
Owner SHANGHAI UNIV OF T C M
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