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Novel limonoid as well as preparation method and medical application thereof

A compound and drug technology, applied in the field of limonoid compounds, can solve the problems of content reduction, content difference, variety and origin, etc.

Inactive Publication Date: 2016-02-24
XINING YIGE INTPROP CONSULTING SERVICE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The content of synephrine decreased significantly with the extension of the picking period, but there was no obvious correlation between the content difference and the variety and production area

Method used

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  • Novel limonoid as well as preparation method and medical application thereof
  • Novel limonoid as well as preparation method and medical application thereof
  • Novel limonoid as well as preparation method and medical application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1: Compound (Ⅰ) isolation preparation and structure confirmation

[0027] (a) Crush the dried Fructus Aurantii (8kg), extract with 75% ethanol under reflux (30L×3 times), combine the extracts, concentrate until there is no alcohol smell (6L), and use petroleum ether (6L×3 times) in turn , Ethyl acetate (6L×3 times) and water-saturated n-butanol (6L×3 times) to obtain petroleum ether extract, ethyl acetate extract (375g) and n-butanol extract respectively; (b) step (a) Use AB-8 macroporous resin to remove impurities from the ethyl acetate extract, first eluting 6 column volumes with 5% ethanol, then eluting 8 column volumes with 70% ethanol, and collect the 70% eluate. Concentrate under reduced pressure to obtain a 70% ethanol elution concentrate (129g); (c) In step (b), the 70% ethanol elution concentrate is separated with normal phase silica gel, and the volume ratio is 50:1 (8 column volumes). , 30:1 (8 column volumes), 15:1 (8 column volumes) and 5:1 (10 column...

Embodiment 2

[0029] Example 2: Compound (I) Pharmacological Action Test

[0030] 1. Materials and Instruments

[0031] Healthy female SD rats were provided by the Experimental Animal Center of Shanghai Second Military Medical University. The preparation method of compound (I) is shown in Example 1, and the HPLC normalized purity is greater than 98%. Dimethyl sulfoxide, ginkgo extract (EGb761, positive drug), MTT, Aβ25-35, and L-polylysine were all purchased from SIGMA, USA. DMEM high glucose medium, Neurobasal, and B27 were purchased from GIBCO, USA. NSE was purchased from ABCOM in the UK. Tunel was purchased from Wuhan Boster Company. The LDH kit was purchased from Nanjing Jiancheng Biochemical Reagent Company.

[0032] Electronic balance, Sartorius, Beijing. 1815TCCO 2 Constant temperature incubator (U.S. Shel-Lab company), TH-2C constant temperature oscillator (Jiangsu Taicang Experimental Equipment Factory), dissecting microscope (Japan OLYMPUS company), desktop centrifuge (German Herae...

Embodiment 3

[0085] Preparation of tablets: According to the method of Example 1, compound (I) is first prepared, and the salt prepared by organic acid such as tartaric acid, or citric acid, formic acid or oxalic acid, etc., and inorganic acid such as hydrochloric acid or sulfuric acid or phosphoric acid, The weight ratio of the excipient to the excipient is 1:7, and the excipient is added for granulation and tableting.

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PUM

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Abstract

The invention discloses a novel limonoid as well as a preparation method and medical application thereof, and belongs to the technical field of medicines. The novel limonoid is reported for the first time, is novel in structure and can be obtained by extraction, separation and purification of dry fructus aurantii immaturus. In-vitro tests show that the novel limonoid has a neuroprotection function on A beta(25-35)-induced hippocampal neuron injuries, also has the function of relieving A beta(25-35)-induced hippocampal neuron toxic injuries and can be used for developing neuroprotection medicines.

Description

Technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a limonin compound isolated from dried Citrus aurantium, a pharmaceutical composition containing the same, and a preparation method and application thereof. Background technique [0002] Citrus aurantium is a commonly used Chinese medicine in clinical practice. It is the dried young fruit of the Rutaceae plant Citrusaurantium L. and its cultivated varieties or the sweet orange Citrussinensis Osbeck. Collect the self-falling fruits from May to June, remove impurities, and cut them into two halves from the middle, sun-dried or low-temperature drying, and the smaller ones are directly sun-dried or low-temperature drying. Citrus aurantium is produced in Sichuan, Jiangxi, Hunan, Fujian and other places. Lime orange from Jiangxi is used as the authentic medicinal material, and Citrus aurantium from Jiangxi has the best quality. Citrus aurantium has the effects of dispelling qi ...

Claims

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Application Information

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IPC IPC(8): C07D407/04A61K31/366A61P25/00
CPCC07D407/04
Inventor 杨辉
Owner XINING YIGE INTPROP CONSULTING SERVICE
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