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Compound with motoneuron growth promoting effect, preparation method and use thereof

A technology of motor neurons and compounds, applied in the field of natural medicine and drug therapy, to achieve the effect of promoting functional recovery and promoting the growth of motor neuron protrusions

Inactive Publication Date: 2017-12-22
佛山市第五人民医院 +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Motor neuron disease is a chronic, fatal degenerative disease of the nervous system for which there is currently no cure

Method used

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  • Compound with motoneuron growth promoting effect, preparation method and use thereof
  • Compound with motoneuron growth promoting effect, preparation method and use thereof
  • Compound with motoneuron growth promoting effect, preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Embodiment 1: compound synthesis

[0028] Oleanolic acid (1.1 mmole) and nicotinic acid (1.3 eq) were dissolved in anhydrous dichloromethane (30 ml), under the catalysis of pyridine (0.5 g) and 4-dimethylaminopyridine (0.5 g), at room temperature React overnight at 25-30°C, filter, pass through a silica gel chromatographic column (the elution solvent used is ethyl acetate and petroleum ether with a volume ratio (3-9): 7), rotary evaporation, and dry to obtain the white solid target compound. Through liquid chromatography mass spectrometry and NMR analysis, the newly prepared white solid target compound is a conjugate with the structure shown in formula (I):

[0029]

Embodiment 2

[0030] Example 2: Drug function verification at the cellular level

[0031] After the drugs (PSB, nicotinic acid, oleanolic acid and the target compound obtained in Example 1) were applied to the primary cultured motor neurons for 24 hours, the axonal growth of the neurons was observed under an inverted microscope, with 3 wells in each group. A number of fields of view were randomly selected in each well to take pictures, and the statistical process length was measured by IPP software. The values ​​of each group were compared with those of the PBS control group to evaluate the effect of drugs on the process length of motor neurons. Next, the lengths of motor neuron axons were counted at different concentrations, and it was found that the five drugs can all promote the growth of neuron processes at a certain concentration, and there are significant differences compared with PBS ( figure 1 ).

Embodiment 3

[0032] Embodiment 3 animal level is carried out drug function verification

[0033] Wistar rats were subjected to sciatic nerve and femoral nerve clamping operations, and drugs (niacin, oleanolic acid and the target compound obtained in Example 1) were administered by intraperitoneal injection for 28 days after the operation. By detecting the exercise ability and histological changes of the experimental animals before the administration, 14 days after the administration, and 28 days after the administration, the effect of the drug on the recovery of the exercise ability of the experimental animals was evaluated. The experimental animals of different groups were counted respectively in behavioral detection: SFI value ( figure 2 ), foot tail angle ( image 3 ), plantar angle ( Figure 4 ), outstretched leg length ratio ( Figure 5 ) and other detection indicators, it is confirmed that the drugs can promote the recovery of the exercise ability of experimental animals at a cer...

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Abstract

Belonging to the field of natural drugs and drug therapy, the invention discloses a compound with motoneuron growth promoting effect, a preparation method and use thereof. The compound is formed by coupling of oleanolic acid and niacin, and the structural formula is shown as (I). The preparation steps include: dissolving oleanolic acid and niacin in anhydrous dichloromethane, carrying out room temperature reaction overnight under the catalysis of pyridine and 4-dimethylamiopryidine, performing filtering, passing the filtrate through a silica gel chromatographic column, and carrying out rotary evaporation and drying, thus obtaining the target compound. On an in-vitro cell level, the compound can significantly promote motoneuron neurite outgrowth; on a whole animal level, the compound can significantly promote the functional recovery of impaired sciatic nerve and femoral nerve, and can be used for development of drugs treating amyotrophic lateral sclerosis and related motoneuron diseases.

Description

technical field [0001] The invention belongs to the field of natural medicine and medicine treatment, and particularly relates to a compound capable of promoting the growth of motor neurons, a preparation method and application thereof. Background technique [0002] Motor neuron disease is a chronic fatal degenerative disease of the nervous system, and there is currently no cure for it. But since motor neurone disease was discovered more than 100 years ago, people have been fighting it and tried nearly 100 drug treatments. With the development of neuroscience and the in-depth understanding of the etiology and pathophysiology of MND, people have made a series of remarkable achievements in the challenge of this intractable disease. The current main treatment includes etiological treatment, symptomatic treatment and a variety of non-drug supportive treatment. The development direction of treatment research at this stage includes neuroprotective agents, anti-excitotoxic drugs,...

Claims

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Application Information

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IPC IPC(8): C07J63/00A61K31/58A61P25/00
CPCC07J63/008
Inventor 黄文柱王志军刘连刘腾彭咏波严文
Owner 佛山市第五人民医院
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