Application of ferulic acid derivative as neuroprotective drug

A technology of ferulic acid and its derivatives, applied in the field of medicine, can solve the problems of difficult to penetrate the blood-brain barrier, limit the clinical application of neuroprotective drugs, and low bioavailability, so as to reduce cell free radical damage and achieve significant neuroprotective effects , reduce the effect of cell inflammation damage

Inactive Publication Date: 2015-10-07
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Due to the poor lipophilicity of ferulic acid and its sodium salt, it is difficult to penetrate the blood-brain barrier, and there are problems such as low bioavailability and short maintenance time of effective drug concentration in the body, these defects severely limit its clinical application as a neuroprotective drug

Method used

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  • Application of ferulic acid derivative as neuroprotective drug
  • Application of ferulic acid derivative as neuroprotective drug
  • Application of ferulic acid derivative as neuroprotective drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1: Effect of ferulic acid derivatives on NO.

[0025] Count the RAW264.7 macrophages in the growth phase, and adjust the cell density to 5×10 5 cells / ml, seeded in 96-well plate, 100 μl / well, placed at 37 ℃, 5% CO 2 cultured in an incubator. 20 h after the cells adhered to the wall, the medium in the well was discarded, and 80 μl / well basal medium was added, and 10 μl / well of different concentrations of the test compound was added for treatment, and LPS was added after 1 h, with a final concentration of 1 μg / ml, and the cell supernatant was collected after 20 h. Colorimetric method with NaNO 2 Color development, NO content was detected at a wavelength of 550 nm.

[0026] The results showed that after LPS stimulated RAW264.7 macrophages for 20 h, the NO content increased significantly. Ferulic acid derivatives can inhibit NO production in a dose-dependent manner, but ferulic acid has no inhibitory effect on the increase of NO secretion induced by LPS. se...

Embodiment 2

[0027] Example 2: Effects of ferulic acid derivatives on the production of the pro-inflammatory cytokine IL-6.

[0028] Take the RAW264.7 macrophages in the logarithmic growth phase, and adjust the cell density to 5×10 5 cells / ml, seeded in 96-well plate, 100 μl / well, placed at 37 ℃, 5% CO 2 cultured in an incubator. After 20 h of cell attachment, the medium in the well was discarded, and 80 μl / well of basal medium was added, and 10 μl / well of different test compounds (final concentration 10 μM) were added for treatment, and LPS was added after 1 h. The final concentration was 1 μg / ml, and the cell supernatant was collected after 20 h. The concentration of IL-6 was determined by double antibody sandwich ABC-ELISA method.

[0029] The results showed that, compared with the normal group, the content of IL-6 in the culture supernatant of RAW264.7 macrophages only treated with LPS was significantly increased. However, after 1 h of drug pretreatment, 10 μM of ferulic acid der...

Embodiment 3

[0030] Example 3: Ferulic acid derivatives on H 2 o 2 Protection against induced neuronal injury.

[0031] Take PC12 cells in the logarithmic growth phase and adjust the cell density to 1 × 10 6cells / ml, seeded in 96-well plate, 100 μL / well, set at 37 ℃, 5% CO 2 Incubate for 24 h in the incubator. The culture medium was replaced, and different test compounds (final concentration 10 μM) were added to the administration group for pretreatment for 1 h, except for the normal group, H 2 o 2 (final concentration 200 μM) caused free radical damage to cells, and cultured for another 24 h. Then, the cell viability of each group was detected according to the MTT method, that is, 15 μL of 5 mg / mL MTT was added to each well, and the culture was continued for 4 h. The supernatant was discarded, and 200 μL of DMSO was added to each well, and the cells were shaken repeatedly for 5 min until blue-purple crystals formed. Dissolve completely, and measure the OD value of each well with a...

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Abstract

The invention relates to application of a ferulic acid derivative to preparation of drugs for treating and / or preventing neurodegenerative diseases related to nerve cell injury. The neurodegenerative diseases includes but not limited Alzheimer's disease, vascular dementia, Parkinson's disease, multiple sclerosis, diabetic neuropathy, ischemia stroke and hemorrhagic stroke.

Description

technical field [0001] The invention relates to the use of a ferulic acid derivative in the preparation of medicines for treating and / or preventing neurodegenerative diseases related to nerve cell damage, and belongs to the field of medicine. Background technique [0002] Ferulic acid (ferulic acid), the chemical name is 4-hydroxy-3-methoxyphenylacrylic acid, is a phenolic acid compound commonly found in the plant kingdom, and it is also a traditional Chinese medicine such as Chuanxiong, Angelica, Cimicifuga, and Ligusticum. one of the active ingredients. Ferulic acid has anti-thrombotic, anti-platelet aggregation, anti-atherosclerosis, hypolipidemic, anti-oxidation, anti-inflammatory, analgesic and other pharmacological effects. Ferulic acid and its sodium salt are clinically used in the adjuvant treatment of coronary heart disease, arteriosclerosis, cerebrovascular disease, glomerular disease, pulmonary hypertension, diabetic vascular disease, vasculitis and other vascula...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/216A61P25/28A61P25/16A61P25/00
Inventor 杜俊蓉陈雏周红静
Owner SICHUAN UNIV
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