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Dryopteris fragrans phloroglucinol compound flavaspidic acid BB and antibacterial application thereof

A technology of phloroglucinol and fumaric acid, which is applied in the fields of chemistry and medicine, and can solve the problems of anti-bacteria that have not been reported in technology

Active Publication Date: 2018-03-27
GUANGDONG PHARMA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The applicant's long-term research has concluded that the anti-dermatophyte active ingredients of Trichophyllum chinensis are phloroglucinol compounds and derivatives, in which fumaic acid BB has high anti-fungal drug activity, but its anti-bacteria especially in There is currently no technical report on the preparation of drugs for the treatment of drug-resistant bacteria

Method used

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  • Dryopteris fragrans phloroglucinol compound flavaspidic acid BB and antibacterial application thereof
  • Dryopteris fragrans phloroglucinol compound flavaspidic acid BB and antibacterial application thereof
  • Dryopteris fragrans phloroglucinol compound flavaspidic acid BB and antibacterial application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Example 1 The separation and preparation of phloroglucinol compound fumaric acid BB

[0047]S1. Extraction of total phloroglucinol compounds of Trichophyllum chinensis: extract 10 kg dry coarse powder of Trichomona citrifolia by cold soaking with 10 times the volume of 50% edible ethanol for 2 times, each time for 24 hours, and concentrate under reduced pressure to recover ethanol To obtain the sample aqueous solution without alcohol smell;

[0048] 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.

[0049] S3. After dissolving the precipitated extract sample obtained in S2, mix the sample with silica gel, perform preliminary separation on a silica gel chromatographic column, and use different proportions of petroleum ether-acetone (100:1~1:1) successively to obtain the corresponding component Fr- A~E.

[0050] The silica gel chromatographic column uses silica gel (60-100 mesh) to m...

Embodiment 2

[0054] The chemical synthesis of embodiment 2 phloroglucinol compounds fumaric acid BB

[0055] At present, the way to obtain the compound fumaric acid BB is mainly to separate and purify from plants, and the separation and preparation are cumbersome and the yield is low. This example proposes for the first time the chemical synthesis pathway and design of pentamaic acid BB, which can obtain the compound in large quantities and quickly. In this example, phloroglucinol (compound 1) was used as the starting material for the reaction, and intermediate 4 was obtained through fluorine-gram acylation reaction, methylation of methyl iodide, and monodebutyrylation.

[0056] The environmentally friendly reagent oxalyl chloride was reacted with DMF to generate the vilsmeier reagent, and then reacted with the raw material 1,3,5-trimethoxybenzene (5), using sodium cyanoborohydride as the reducing agent, and the compound 7 was obtained in a yield of 90%. , and then by Friedel-Crafts acyla...

Embodiment 3

[0076] Example 3 In vitro anti-superficial fungus effect experiment of Phloroglucinol compound of Phloroglucinol

[0077] (1) Microsporum canis (CMCC(F)T 5C ), Malassezia furfur (CMCC(F)T 17a ), Microsporum gypsumus (CMCC(F) M2C ), provided by the Institute of Dermatology, Chinese Academy of Medical Sciences (Nanjing). The microdilution method of dermatophyte is carried out according to the M38-A2 scheme formulated by CLSI in the United States, which is briefly described as follows: Scrape the colony on the surface of the SDA medium with an inoculation loop, grind the mycelia with a sterile grinder, and suspend the dermatophyte in In sterile normal saline, adjust the turbidity to 0.5 McFarland turbidity, and count the number of spores and short hyphae with a hemocytometer. 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 hemocytom...

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Abstract

The invention relates to the technical field of medicine and discloses an antibacterial application of a Dryopteris fragrans phloroglucinol compound flavaspidic acid BB. The invention provides the flavaspidic acid BB obtained by the chemical synthesis method. The flavaspidic acid BB has good antibacterial effects, effectively fills in the application deficiency of the antibacterial natural compound and provides an effective antibacterial solution for drug-resistant bacteria. The experimental results show that the compound has a strong antibacterial effect and good curative effects especially on drug-resistant bacteria.

Description

technical field [0001] The present invention relates to chemical and medical technical field, more specifically, relate to a kind of Phloroglucinol compounds of Phloroglucinol of Phyllostachys chinensis BB and application thereof. Background technique [0002] Staphylococcus aureus is a Gram-positive pathogenic bacterium that widely exists in nature. Humans are one of the main carriers of Staphylococcus aureus, and healthy people can carry 20% of them, which are distributed on the skin, upper respiratory tract and other positions. When the body's immunity is insufficient, the invasion of the body turns into an endogenous infection, causing systemic infection and local suppurative infection including meningitis, sepsis, endocarditis, and osteomyelitis. One of the most common pathogens. In recent years, reports from the U.S. Centers for Disease Control and Prevention show that the infection caused by Staphylococcus aureus is second only to Escherichia coli. The research prov...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/122A61P31/04C07C46/00C07C50/38
CPCA61K31/122C07C41/18C07C45/00C07C45/455C07C45/64C07C46/00C07C46/06C07C49/825C07C50/38C07C47/575C07C43/2055C07C49/84
Inventor 沈志滨
Owner GUANGDONG PHARMA UNIV
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