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Gentiopicroside derivative and preparation and application thereof

A technology of gentiopicroside derivatives and biropicroside derivatives, which is applied in the field of medicine, can solve the problems of limited application and high polarity, and achieve the effect of improving bioavailability

Active Publication Date: 2021-12-21
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, due to the high polarity of NGF, it is difficult to penetrate the blood-brain barrier, which limits its application in the treatment of AD.

Method used

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  • Gentiopicroside derivative and preparation and application thereof
  • Gentiopicroside derivative and preparation and application thereof
  • Gentiopicroside derivative and preparation and application thereof

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Embodiment Construction

[0043] The present invention will be further described below in conjunction with the accompanying drawings and specific embodiments. It should be understood that these examples are only used to illustrate the present invention and are not intended to limit the scope of the present invention. The operating methods not indicated in the following examples are generally in accordance with conventional conditions, or in accordance with the conditions suggested by the manufacturer.

[0044] The dried and powdered traditional Chinese medicine gentian (100 g) was extracted in methanol (gentian / methanol=1 / 10, w / v, g / mL) for 24 hours at room temperature. The methanol extract was filtered, and the filtrate was concentrated, dissolved in water, and distributed with n-hexane, ethyl acetate and n-butanol in sequence to obtain an active n-butanol layer (7.5 g). The n-butanol fraction was separated with an ODS open chromatographic column, and the n-butanol fraction was separated with MeOH / H ...

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Abstract

The invention discloses a preparation method of gentiana rigescens-derived gentiopicroside, a gentiopicroside derivative synthesized on the basis of the gentiopicroside and a synthesis method of the gentiopicroside derivative. According to the invention, it is found by evaluation of a PC12 cell biological activity system that the compounds have relatively good quasi-nerve growth factor activity, and can be applied to preparation of anti-Alzheimer's disease drugs and health-care products. The invention provides a basis for research and development and basic research of new drugs for resisting Alzheimer's disease, and has important practical significance.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a class of gentiopicroside derivatives and their preparation and application. Background technique [0002] With the improvement of medical and health level in modern society, the average life expectancy of human beings is prolonged, and the phenomenon of social aging is becoming more and more serious. Relevant statistical reports predict that by 2050, the population over the age of 60 will reach 2 billion, accounting for about 22% of the world's total population. With the intensification of aging, the incidence of age-related diseases is also increasing year by year. Alzheimer's disease (AD), commonly known as senile dementia, is one of the diseases with the highest incidence. Related reports show that 11.2% of the elderly aged 60 and above are caused by Alzheimer's disease, which is higher than the incidence of stroke, cardiovascular disease and cancer. Therefore, in-depth r...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H17/04C07H1/08C07H1/00A61P25/00A61P25/28A61K31/7048
CPCC07H17/04C07H1/08C07H1/00A61P25/00A61P25/28Y02P20/55
Inventor 戚建华王颖陈丹妮向兰刘倩
Owner ZHEJIANG UNIV