5-nornobiletin as well as preparation method and application thereof

A technology of nobiletin and nobiletin, applied in the field of 5-nornobiletin and its preparation, can solve the problems of low extraction rate, complex separation and purification process, and inapplicability to industrial production, and achieve simple preparation method and high product purity , the effect of improving production efficiency

Active Publication Date: 2022-05-06
TIANJIN UNIV OF COMMERCE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

There is no relevant research on the correlation between 5-DN and ulcerative colitis in the prior art, and the method for extracting 5-DN from orange peel in the prior art has defects such as low extraction rate and complicated separation and purification process, and is not suitable for industrial use. Production

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  • 5-nornobiletin as well as preparation method and application thereof
  • 5-nornobiletin as well as preparation method and application thereof
  • 5-nornobiletin as well as preparation method and application thereof

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preparation example Construction

[0032] In the present invention, the 5-nornobiletin is preferably prepared according to the following preparation method, which specifically includes the following steps: mixing polymethoxyflavone nobiletin with concentrated hydrochloric acid-absolute ethanol solution, and heating to reflux for reaction , to obtain a reaction solution, the reaction solution was concentrated under reduced pressure, the concentrate was dissolved in ethyl acetate, washed with water, and then concentrated under reduced pressure to obtain 5-nornobiletin.

[0033] In the present invention, the polymethoxyflavone nobiletin is preferably extracted from tangerine peel, and the extraction method preferably includes the following steps: mixing tangerine peel powder with absolute ethanol, soaking, filtering, and concentrating to obtain Concentrate, the concentrate and chloroform-water solution are mixed and extracted, the chloroform layer is taken, and the chloroform layer is separated and purified by sili...

Embodiment 1

[0038] Washing and drying commercially available tangerine peels, directly pulverizing them through a medicine pulverizer, and passing through a 40-mesh sieve to obtain tangerine peel powder. Mix tangerine peel powder and absolute ethanol at a material-to-liquid ratio of 1:10, soak for 48 hours, filter and concentrate to obtain a concentrate. The concentrate and chloroform-water solution were mixed and dissolved at a volume ratio of 1:1, stirred and extracted, and the chloroform layer was taken and concentrated to obtain a flavonoid mixture.

[0039] The obtained flavonoid mixture was separated and purified by silica gel column chromatography, and gradient elution was carried out with ethyl acetate:petroleum ether at a ratio of 1:9-1:3, and the eluent was further separated and purified in the preparative liquid phase to obtain NBT ( Retention time 11.1min), the structure of NBT was confirmed by GC-MS technique.

[0040]The obtained NBT was fully mixed with concentrated hydroc...

Embodiment 2

[0042] 8-10 weeks old male C57 BL / 6 mice weighing 21.5-23.0 g were selected and purchased from Beijing Huafukang Biotechnology Co., Ltd. All the purchased mice were placed in the Animal Experiment Center of the Institute of Radiological Medicine, Chinese Academy of Medical Sciences, raised at a room temperature of 20±1°C, with a light cycle of 12 hours, relative humidity controlled at 50%-70%, and the alternation of light and dark between day and night at 12 / 12 , noise <60dB, ammonia concentration does not exceed 20ppm. After one week of observation, it was used for follow-up experiments without any symptoms. All animal experiments were approved by the Ethics Committee of Tianjin University of Commerce.

[0043] The mice were randomly divided into five groups, 6 in each group, namely: blank control group (gavage olive oil mixed with a small amount of DMSO (DMSO content is not higher than 0.6%)), dextran sodium sulfate (DSS) experimental control group group (3% DSS drinking w...

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Abstract

The invention provides 5-nornobiletin as well as a preparation method and application thereof, and belongs to the technical field of medicines. The invention provides an application of 5-nornobiletin in preparation of a product for preventing and treating ulcerative colitis, and provides a remarkable prevention and treatment effect of 5-nornobiletin on ulcerative colitis for the first time. The conditions of diarrhea degree, shortened colon length, intestinal congestion, edema and ulcer, intestinal epithelium injury, intestinal permeability increase and the like can be obviously improved. And high-throughput screening and PT-qPCR show that the 5-nornobiletin enhances the barrier effect of intestinal mucosa by up-regulating the expression of intestinal mucosa epithelium mucoprotein Muc2, thereby achieving the purpose of preventing and treating ulcerative colitis. In addition, the demethylation of the polymethoxy flavone nobiletin is accelerated by adopting an acid catalysis and heating method, the conversion from the polymethoxy flavone nobiletin to the 5-nornobiletin is successfully realized, and the purity of the obtained 5-nornobiletin can reach 97.5%.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to 5-nornobiletin and its preparation method and application. Background technique [0002] Ulcerative colitis (UC) is a common chronic non-specific inflammatory disease mainly involving the colorectum. The disease is a common disease in developed countries, and its incidence is still increasing in recent years. The disease was originally a low incidence in my country, but with the westernization of the diet structure of Chinese people, its incidence is also showing a significant increasing trend. The course of the disease is long and easy to relapse. About 15% of patients present with acute and catastrophic outbreaks, accompanied by risks such as intestinal perforation, hemorrhage, polyps, and even cancer. For the treatment of UC, traditional drugs such as amino acid salicylic acid preparations, glucocorticoids, and immunosuppressants have limited curative effects, an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61K36/752A61P1/00A61P1/04C07D311/30
CPCA61K31/352A61K36/752A61P1/00A61P1/04C07D311/30Y02A50/30
Inventor 王梅燕孙美娣赵辉杨帆
Owner TIANJIN UNIV OF COMMERCE
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