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Coumarinolignoid and preparation method and application thereof

A technology of coumarin and lignan, which can be used in organic chemical methods, nervous system diseases, non-central analgesics, etc., can solve problems such as poor clinical efficacy and achieve good medicinal value.

Active Publication Date: 2019-01-04
GUANGXI NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Based on the theory of neuroinflammation in the onset of neurodegenerative diseases, the current drugs to reduce the inflammatory response in the brain of patients and delay the progression of the disease are mainly concentrated on non-steroidal anti-inflammatory drugs (NSAIDs) and tetracycline antibiotics, but their clinical efficacy is not optimistic
At present, there are no related reports on the extraction of coumarin and lignans from Sapium sinensis and its anti-neuroinflammatory activity

Method used

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  • Coumarinolignoid and preparation method and application thereof
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  • Coumarinolignoid and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Example 1: Preparation and structural characterization of compounds 1a-3a and 1b-3b

[0049] 1) Take 20 kg of Sapium sinensis stems and leaves, crush them, and reflux extract with 95v / v% ethanol (100L) for 3 times, each time for 3 hours, combine the extracts, concentrate under reduced pressure to obtain 1.6kg of extract;

[0050] 2) Suspend the obtained extract with water (8 L), extract with equal volumes of petroleum ether, ethyl acetate, and n-butanol in sequence, collect the ethyl acetate extract, concentrate under reduced pressure, and obtain 168.3 g of ethyl acetate extract.

[0051] 3) The ethyl acetate extract was subjected to silica gel column chromatography, followed by gradient elution with the first eluent and the second eluent, and the combined fractions were detected by thin layer chromatography, and a total of 7 fractions A-G were obtained respectively ; Wherein, the first eluent is a mixed solvent composed of petroleum ether and acetone at a volume ratio ...

Embodiment 2

[0082] Embodiment 2: the preparation of compound 1a-3a and 1b-3b

[0083] Repeat Example 1, the difference is: in step 1), 80v / v% methanol is used for extraction.

[0084] The finally isolated compounds 1a-3a and 1b-3b were characterized by the same method as in Example 1, and were determined to be the target compounds 1a-3a and 1b-3b of the present invention.

Embodiment 3

[0085] Embodiment 3: the preparation of compound 1a-3a and 1b-3b

[0086] Repeat Example 1, the difference is:

[0087] In step 1), 80v / v% ethanol is used for extraction;

[0088] In step 6), in the composition of the mobile phase, methanol is replaced with acetonitrile;

[0089] In step 7), in the composition of the mobile phase, methanol is used to replace acetonitrile therein.

[0090] The finally isolated compounds 1a-3a and 1b-3b were characterized by the same method as in Example 1, and were determined to be the target compounds 1a-3a and 1b-3b of the present invention.

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Abstract

The invention discloses coumarinolignoid and a preparation method and application thereof. The coumarinolignoid specifically comprises six compounds obtained through separation of Sapium discolor (Champ.ex Benth.)Muell.Arg.). Experiments show that the compounds can remarkably inhibit NO release of BV2 microglial cells stimulated by LPS under the condition that the survival rate of the BV2 microglial cells is not influenced by the compounds. The inhibitory effect of the compound 2a is slightly stronger than that of clinically common medicine, namely minocyline, and the compounds are good in potential medicinal value and are expected to be used for preparing medicines for neurodegenerative diseases.

Description

technical field [0001] The invention relates to active components extracted and separated from plants, in particular to coumarinolignoids extracted and separated from Sapium arvensis and its preparation method and application. Background technique [0002] Neurodegenerative disease is a general term for a class of diseases that affect human health. It is a group of chronic and progressive neurological diseases characterized by neuronal degeneration. Each neurodegenerative disease has its own specific triggers. Although the causes of these diseases are different, the appearance of neuroinflammation is a common feature of these diseases. [0003] Among several types of cells involved in neuroinflammation-mediated neurodegeneration, microglia are the most important one. Microglia are resident immune cells in the central nervous system. Under normal circumstances, resting microglia play an immune surveillance role and maintain the normal function of the nervous system. Under ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/04A61P29/00A61P25/00A61K31/37
CPCA61P25/00A61P29/00C07B2200/07C07D493/04
Inventor 梁东张贵杰潘其明廖海兵
Owner GUANGXI NORMAL UNIV
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