Phloroglucinol derivatives and isomers separation and preparation method and application

A technology of phloroglucinol and phloroglucinol, which is applied in the field of chemistry and medicine, and achieves the effects of high purity, convenient operation and good medicinal activity

Active Publication Date: 2018-05-01
GUANGDONG PHARMA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no technical report on how to efficiently separate and prepare new phloroglucinol derivatives with corresponding pharmaceutical activity from D.

Method used

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  • Phloroglucinol derivatives and isomers separation and preparation method and application
  • Phloroglucinol derivatives and isomers separation and preparation method and application
  • Phloroglucinol derivatives and isomers separation and preparation method and application

Examples

Experimental program
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Effect test

Embodiment 1

[0055] The separation and preparation of embodiment 1 phloroglucinol derivatives

[0056] The schematic diagram of the separation and preparation is shown in the appendix figure 1 And attached figure 2 shown.

[0057] S1. Extraction of the total phloroglucinol derivatives of Trichomonas chinensis: extract 10 kg dry coarse powder of Trichomonas 10 times by cold immersion in 50% edible ethanol twice, each time for 24 hours, concentrate and recover under reduced pressure Ethanol to alcohol-free sample aqueous solution;

[0058] S2. Adjust the pH to 1.5-4.5 with hydrochloric acid, let stand for 12-18 hours, and centrifuge to obtain 1.2 kg of precipitated extract.

[0059] S3. After dissolving the precipitated extract sample obtained in S2, mix the sample with silica gel, perform preliminary separation on the silica gel column, and successively use different proportions of petroleum ether: acetone to elute (100:1-1:1) to obtain the corresponding components Fr.A~E.

[0060] Th...

Embodiment 2

[0064] The separation and preparation of embodiment 2 phloroglucinol derivatives

[0065] The schematic diagram of the separation and preparation is shown in the appendix figure 1 And attached figure 2 shown.

[0066] S1. Extraction of the total phloroglucinol derivatives of Trichomonas chinensis: extract 10 kg dry coarse powder of Trichomonas 10 times by cold immersion in 50% edible ethanol twice, each time for 24 hours, concentrate and recover under reduced pressure Ethanol to alcohol-free sample aqueous solution;

[0067] S2. Adjust the pH to 1.5-4.5 with hydrochloric acid, let stand for 12-18 hours, and centrifuge to obtain 1.2 kg of precipitated extract.

[0068] S3. After dissolving the precipitated extract sample obtained in S2, mix the sample with silica gel, perform preliminary separation on the silica gel column, and successively use different proportions of petroleum ether: acetone to elute (100:1-1:1) to obtain the corresponding components Fr. A-E.

[0069] S...

Embodiment 3

[0071] Example 3 In vitro anti-superficial fungus effect of Phloroglucinol 4 pairs of isomer compounds

[0072] (1) Trichophyton rubrum (CMCC(f)T1b) and Microsporum gypsumoidus (CMCC(F)M2C), provided by the Institute of Dermatology, Chinese Academy of Medical Sciences. The microdilution method of dermatophytes was carried out according to the M38-A2 protocol formulated by CLSI in the United States, which is briefly described as follows. Gently scrape the colonies on the surface of the SDA medium with an inoculation loop and grind the mycelium with a sterile grinder, suspend the dermatophyte in sterile saline, adjust the turbidity to 0.5 McFarland turbidity, and count the number of spores with a hemocytometer and short mycelia. Make the bacterial concentration 1×10 3 CFU / ml to 3×10 3 CFU / ml. That is, the 0.5 McFarland turbidity bacteria solution was diluted 1000 times with RPMI-1640 liquid medium, and counted by the hemocytometer to obtain the inoculum solution. Use RPMI-1...

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Abstract

The invention relates to the technical field of medicine, and discloses a separation and preparation method and an application of a phloroglucinol derivative of Phrylloglucinol derivatives and isomers thereof. The present invention is the first to separate and prepare a class of phloroglucinol compounds from Dryopteris fragrans (L.) Schott., a plant of the genus Dryopteris fragrans (L.) Schott., and discover 4 pairs of isomers. The above 4 pairs of isomer compounds have stronger anti-skin superficial fungus effect. Antibacterial experiments in vitro show that this type of compound has good antibacterial effect on two skin pathogenic fungi Trichophyton rubrum and Microsporum gypsumoid, and has the characteristics of low side effects and not easy to produce drug resistance. The fungal infection provides a new natural compound, which provides strong technical support for the preparation of drugs or pharmaceutical compositions against superficial skin fungal infections.

Description

technical field [0001] The invention relates to the technical fields of chemistry and medicine, and more specifically, to a separation and preparation method and application of Phloroglucinol derivatives of Phrylloglucinol and isomers thereof. Background technique [0002] The superficial fungi that parasitize the skin keratin tissue are dermatophytes, which can be divided into three genera: Trichophyton, Microsporum, and Epidermophyton. Dermatophyte infection is relatively common in my country, and the most common pathogenic bacteria are Trichophyton rubrum, Trichophyton mentagrophytes and Microsporum canis, which often cause diseases such as dermatophyte, tinea capitis, jock itch, and onychomycosis, accompanied by Redness, itching and other symptoms. Trichophyton rubrum is the main pathogenic bacterium that causes skin fungus, accounts for 69.5% of dermatophyte infections, can cause tinea manuum, tinea pedis, tinea capitis, etc. [0003] With the widespread use of antibio...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C49/84C07C49/83C07C49/723C07C45/78A61P31/10A61P17/00
CPCC07C45/78C07C49/723C07C49/83C07C49/84
Inventor 沈志滨唐春萍
Owner GUANGDONG PHARMA UNIV
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