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Cinnamyl amino acid compound and application thereof

A technology of cinnamoyl amino acids and compounds, applied in the field of cinnamoyl amino acid compounds, can solve problems such as difficult to pass through the blood-brain barrier, concentration maintenance time period, and limited clinical application, and achieve clear pharmacological effects, small toxic and side effects, and inhibition of iNOS Effect

Inactive Publication Date: 2018-09-04
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the poor lipophilicity of ferulic acid and its sodium salt, it is difficult to pass through the blood-brain barrier, and there are problems such as low bioavailability and effective drug concentration in the body.
These problems severely limit its clinical application as a neuroprotective drug

Method used

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  • Cinnamyl amino acid compound and application thereof
  • Cinnamyl amino acid compound and application thereof
  • Cinnamyl amino acid compound and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] 1. In vitro anti-inflammatory activity of cinnamoyl amino acid compounds

[0025] 1.1 Experimental materials: BV-2 cells, DMEM cell culture medium, Gibico fetal bovine serum, 96-well cell culture plate, DMSO (Sigma), LPS (Sigma), NO detection kit (Beiyuntian), microplate reader.

[0026] 1.2 Experimental method:

[0027] BV-2 cells in 1 × 10 4 Cells / well were seeded in 96-well plates, and then grouped into groups; blank group, LPS model group, LPS+10 μM different test drug groups, and cultured for 24 hours. Then drugs and blank culture solution were added to the corresponding groups to continue culturing for 4 hours. Finally, except the blank group, each group was stimulated with LPS at a final concentration of 500 ng / mL for 24 hours. Finally, draw 50 μL of the supernatant to measure the NO content according to the requirements of the NO detection kit.

[0028] 1.3 Experimental results: such as figure 1 Shown, the amount of NO released. 4-Hydroxycinnamoyl-L-tyrosi...

Embodiment 2

[0031] 2. Cinnamoyl amino acid compounds inhibit iNOS in vitro

[0032] 2.1 Experimental materials: BV-2 cells, DMEM cell culture medium, Gibico fetal bovine serum, 96-well cell culture plate, DMSO (Sigma), LPS (Sigma), iNOS viability detection kit (Beiyuntian), microplate reader.

[0033] 2.2 Experimental method: BV-2 cells were mixed with 1×10 4 Cells / well were inoculated in 96-well plates, and then grouped into groups; blank group, LPS model group, LPS+(0.01-10 μM) different test drug groups, and cultured for 24 hours. Then drugs and blank culture solution were added to the corresponding groups to continue culturing for 4 hours. Finally, except the blank group, each group was stimulated with LPS at a final concentration of 500 ng / mL for 24 hours. Finally, iNOS activity was determined according to the requirements of the iNO detection kit.

[0034] 2.3 Experimental results:

[0035]

[0036] As shown in Table 1, the half inhibition IC of cinnamoyl amino acid compounds o...

Embodiment 3

[0039] 3. Preferred compound 4-hydroxy-3-methoxycinnamoyl-L-tyrosine anti-Parkinson activity in vivo

[0040] 3.1 Experimental materials: 10-week-old C57BL / 6, rotary rod fatigue tester, MPTP (Sigma)

[0041] 3.2 Experimental grouping: Mice were randomly divided into 5 groups, 5 in each group: normal control group, diocortin alone group, model group, 4-hydroxy-3-methoxycinnamoyl-L-tyrosine Low-dose group (10 mg / kg), 4-hydroxy-3-methoxycinnamoyl-L-tyrosine high-dose group (20 mg / kg). Continuous pre-administration for 12 days, the blank group and the model group were given equal doses of PBS, and the model was made on the 13th day, and the model group and the drug group were given intraperitoneal injection of MPTP (20mg / kg) every 2h for a continuous injection of 4 hours. Second-rate. After modeling, conduct behavioral tests. The rotarod performance of mice was tested using the YLS-4C mouse rotarod instrument. 4, 24, 48, and 72 hours after MPTP modeling, the mice were placed o...

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Abstract

The invention discloses a cinnamyl amino acid compound and application thereof, relates to the fields of medicinal chemistry and pharmacotherapeutics and in particular relates to a cinnamyl amino acidcompound with inducible nitric oxide synthase (iNOS) inhibitory activity or pharmaceutically acceptable salts or esters thereof, pharmaceutical compositions containing the compounds and medical application thereof, particularly application in prevention and treatment of neuronal cell damage related neurodegenerative diseases comprising ischemic cerebral apoplexy, Parkinson's disease and other aspects.

Description

technical field [0001] The present invention relates to a cinnamoyl amino acid compound, in particular to a cinnamoyl amino acid compound having inducible nitric oxide synthase (iNOS) inhibitory activity, and its use in the treatment and prevention of ischemic stroke and Parkinson's disease The application in the medicine of the present invention belongs to the technical field of pharmacy. Background technique [0002] Acute ischemic stroke is characterized by high incidence, high disability and high mortality. Epidemiological survey results show that the onset of this type of disease is gradually becoming younger, which has attracted extensive attention. Inflammation plays an important role in the pathological process of ischemia-induced brain injury. One of the important signs of inflammatory response after cerebral ischemia is the activation of glial cells. Glial cells are the most numerous type of immune cells in the central nervous system. They can not only provide nu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C235/34C07C233/51A61K31/198A61P25/00A61P9/10A61P25/16A61P25/28A61P25/24A61P29/00
CPCA61K31/198A61P9/10A61P25/00A61P25/16A61P25/24A61P25/28A61P29/00C07C233/51C07C235/34
Inventor 汪豪胡晓龙吕先宇林俊冯家豪叶文才
Owner CHINA PHARM UNIV
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