2-methyl-5-(3,4-dihydroxyphenyl)pyridine as well as extraction method and application thereof

A technology of dihydroxyphenyl and extraction method, applied in the directions of antitoxin, organic chemistry, drug combination, etc., can solve the problems such as few beak-tailed beetles, no reports on the use of beak-tailed beetles extract, etc., and the steps are simple. , Excellent antioxidant activity, the effect of scavenging oxygen free radicals

Active Publication Date: 2017-10-10
DALI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] At present, there are very few research reports on the pharmaceutical and clinical applica

Method used

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  • 2-methyl-5-(3,4-dihydroxyphenyl)pyridine as well as extraction method and application thereof
  • 2-methyl-5-(3,4-dihydroxyphenyl)pyridine as well as extraction method and application thereof
  • 2-methyl-5-(3,4-dihydroxyphenyl)pyridine as well as extraction method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] Take 5Kg of dry powder of Rhizoma Rhizome and extract three times with 95% ethanol (the mass ratio of ethanol and Rhizoma Rhizoma dry powder is 3:1, the first extraction time is 48h, the second extraction time is 12h, the third The extraction time is 12h), the filtrates from the three extractions are combined, and the filtrate is distilled under reduced pressure until there is no alcohol to obtain the cold soak extract; the cold soak extract is successively used with petroleum ether (compared to 1:1, and extracted 3 times ), chloroform (comparison ratio is 1:1, extraction 3 times), ethyl acetate (comparison ratio is 1:1, extraction 3 times) extraction, the ethyl acetate extraction phase is combined, and then under reduced pressure distillation, the ethyl acetate The ester was recovered to obtain ethyl acetate extract; the ethyl acetate extract (200g) was separated by silica gel column chromatography, and petroleum ether: acetone (V: V = 10:0, 9:1, 8:2, 7:3) , 6:4, 5:5, 4...

Embodiment 2

[0075] Take 5Kg of dry powder of Rhizoma Rhizome and extract three times with 95% ethanol (the mass ratio of ethanol and Rhizoma Rhizoma dry powder is 3:1, the first extraction time is 48h, the second extraction time is 12h, the third The extraction time is 12h), the filtrates from the three extractions are combined, and the filtrate is distilled under reduced pressure until there is no alcohol to obtain a cold soak extract; the cold soak extract is successively used with petroleum ether (compared to 1.1:1, and extracted 3 times ), dichloromethane (1.1:1 comparison, 3 extractions), ethyl acetate (1:1 comparison, 3 extractions) extraction, the ethyl acetate extraction phases are combined, and then subjected to vacuum distillation, Ethyl acetate was recovered to obtain an ethyl acetate extract; the ethyl acetate extract (200g) was separated by silica gel column chromatography and separated by petroleum ether: chloroform (V: V = 10:0, 9:1, 8:2, 7 :3, 6:4, 5:5, 4:6, 3:7, 2:8, 1:9, ...

Embodiment 3

[0078] 1,1-Diphenyl-Dipicrylhydrazine (DPPH) is a relatively stable lipid free radical. There is a free electron on its N. Its ethanol solution is purple. The full wavelength scan shows that it has a maximum at 517nm. Absorption peak. After adding antioxidants, DPPH captures an electron to pair with free electrons, the purple fades and becomes a colorless substance. The absorption peak at 517nm disappears, and the degree of fading is quantitatively related to the number of electrons it accepts. That is, the absorption value of DPPH decreases when it is redox, and the lower the absorbance, the stronger its antioxidant effect. According to this principle, the ability of the sample to provide hydrogen atoms, scavenge free radicals, and resist oxidation is measured.

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Abstract

The invention provides a compound named as 2-methyl-5-(3,4-dihydroxyphenyl)pyridine. The compound is capable of eliminating oxygen free radicals and has wide application prospects in the treatment of diseases relevant with cell breaking capacity of free radicals of a human body. The invention further provides an extraction method of 2-methyl-5-(3,4-dihydroxyphenyl)pyridine. The extraction method comprises the steps of firstly carrying out cold-soaked extraction on blaps rynehopetera fairmaire powder so as to obtain an extracting solution, and carrying out extraction, first silica gel column chromatography separation, second silica gel column chromatography separation, ODS reversed-phase column chromatography separation, third silica gel column chromatography separation and gel column chromatography separation, so as to obtain 2-methyl-5-(3,4-dihydroxyphenyl)pyridine. The extraction method has the beneficial effects that the steps are simple, the cost is low, the raw material sources are wide, and industrial production is easily realized.

Description

Technical field [0001] The invention relates to the technical field of medicinal compounds, in particular to a 2-methyl-5-(3,4-dihydroxyphenyl)pyridine and an extraction method and application thereof. Background technique [0002] Blaps rynchopetera Fairmaire (Blaps rynchopetera Fairmaire) is commonly known as stinky shell, small black bug, stink bug, tall foot bug, tall stink bug, spanking bug, bed bug, etc. Adult insects can secrete a defensive liquid with medicinal value (ie smelly fart). Beaktail Pipajia is a long-term and widely used insect medicine by the Yi people in Yunnan (the name of the Yi medicine is transliterated as "Han Zhai"). It is used for fever with heat syndrome, food stagnation, malnutrition in children, night terrors, breast addiction, breast phlegm, sore itching Swollen toxin, eczema, itchy skin, etc. According to investigations, more than 80% of prescriptions for treating tumors and cardiovascular diseases by Yi folk doctors contain the insect medicine....

Claims

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Application Information

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IPC IPC(8): C07D213/30A61P39/06
CPCC07D213/30
Inventor 肖怀丁中涛闫爽施贵荣张俊李贵轲刘熙李玥何正春
Owner DALI UNIV
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