Application of andrographolide derivatives in preparing medicaments for preventing and treating neurodegenerative diseases

A technology of andrographolide and neurodegeneration, which is applied in the field of application of andrographolide derivatives in the preparation of drugs for the prevention and treatment of neurodegenerative diseases, can solve the problems such as the unclear pathogenesis of neurodegenerative diseases, and achieve reduction Effects of oxidative stress injury, reduction of inflammatory response, and inhibition of anti-neuroinflammatory response

Active Publication Date: 2013-12-11
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, the pathogenesis of neurodegenerative diseases is not very clear, and it is believed to be related to oxidative stress, neuroinflammation, excitotoxicity and nerve cell apoptosis

Method used

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  • Application of andrographolide derivatives in preparing medicaments for preventing and treating neurodegenerative diseases
  • Application of andrographolide derivatives in preparing medicaments for preventing and treating neurodegenerative diseases
  • Application of andrographolide derivatives in preparing medicaments for preventing and treating neurodegenerative diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Embodiment 1. Andrographolide derivative AL-1 is respectively to hydroxyl free radical (OH), superoxide anion free radical (O2ˉ ), peroxynitrite ion (ONOOˉ) and 1,1-diphenyl in vitro The Scavenging Effects of Four Free Radicals of Radical-2-Phenylhydrazine Free Radical (DPPH)

[0037] Hydroxyl radical (OH): using o-phenanthroline-metal ion-H2O2, through the Fenton reaction (H 2 o 2 +Fe 2+ →·OH+H 2 O+Fe 3+ ) to generate hydroxyl radicals, prompting o-phenanthroline-Fe 2+ Oxidized to o-phenanthroline-Fe 3+ , causing the maximum disappearance of its aqueous solution at a wavelength of 440nm to measure its clearance rate. The specific steps are: add 300 μL of double-distilled water (blank control) or different concentrations of andrographolide derivative AL-1 (dissolved in DMSO to form a 10 mM stock solution, and then diluted with double-distilled water to 0.01 μM, 0.1μM, 1μM, 10μM), add 50μL of1.0mM o-phenanthroline (dissolve 1.0mM in 50mM NaCl solution), then add 1...

Embodiment 2

[0043] Embodiment 2. andrographolide derivative AL-1 is to MPP in vitro + Protective activity of induced SH-SY5Y cell injury

[0044] SH-SY5Y cells were digested and seeded in 96-well plates (2×10 4per well), 100 μl per well. After the cells were cultured in the incubator for 24 hours, the culture medium was discarded. The culture medium (containing 2% FBS) containing different concentrations of andrographolide derivative AL-1 (0.01 μM, 0.1 μM, 1 μM, 10 μM) was protected for 2 hours, and then 2 mM MPP was added + Incubate for 24 hours, then add a new medium solution containing 5mg / ml MTT after aspirating the old medium. After incubating in the incubator for 4 hours in the dark, the culture medium was sucked off, and 150 μl DMSO was added to each well, shaken in the dark until the precipitate was completely dissolved, and the absorbance value at 570 nm was measured with a microplate reader. Taking the normal cell survival rate as 100%, the cell survival rate of different tr...

Embodiment 3

[0046] Example 3. Andrographolide derivative AL-1 to MPP + Protective effect of induced primary cultured cerebellar granule neurons

[0047] Primary cerebellar granule cells were extracted from 3-day-old neonatal mice (body weight 20-25g) and inoculated in 96-well plates (2×10 5 per well), 100 μl per well, after culturing in the incubator for 24 hours, add 10 μM cytarabine to the medium. After culturing to the eighth day, after adding different concentrations of andrographolide derivative AL-1 (0.01 μM, 0.1 μM, 1 μM, 10 μM) for protection, the absorbance of each group was measured by MTT method after induction with 200 μM MPP+ for 24 hours.

[0048] andrographolide derivative AL-1 on MPP + The experimental data of the neuroprotective effect of the induced cerebellar granule neuron cell injury model are as follows: image 3 shown.

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Abstract

The invention belongs to the technical field of medicines, and discloses an application of andrographolide derivatives in preparing medicaments for preventing and treating neurodegenerative diseases. The andrographolide derivatives are andrographolide derivatives AL-1 prepared from andrographolide and alpha-lipoic acid. In-vivo and in-vitro testing results indicate that the AL-1 has an effect of protecting nerves, and can be used for improving the behavioristics of a Parkinson disease model mouse; the mechanism of an AL-1 nerve protection effect is related to free radical scavenging, oxidation resistance and nuclear transcription factor kB(NF-kB) inactivation inhibition. Therefore, the andrographolide derivative AL-1 can be used as a medicament for preventing and treating neurodegenerative diseases, in particular Parkinson disease, and can be manufactured into various preparations with available medicinal carriers.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to the application of an andrographolide derivative in the preparation of medicines for preventing and treating neurodegenerative diseases. Background technique [0002] Neurodegenerative diseases are diseases caused by central nervous system dysfunction caused by progressive degeneration and necrosis of nerve cells, which are aggravated with the aging of the global population, including Alzheimer's disease, Parkinson's disease (Parkinson's disease) disease, PD), amyotrophic lateral sclerosis (Atrophy lateral sclerosis, ALS), Huntington's disease (Huntington's disease, HD), stroke (Stroke) and cardiovascular dementia (Vascular dementia, VD). It mainly affects the cognitive function and motor function of patients, causing disability and high mortality rate, and brings great psychological and economic burden to patients' families and society. For most neurodegenerative ...

Claims

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Application Information

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IPC IPC(8): A61K31/385A61P25/16A61P25/28A61P21/00A61P25/00
Inventor 王玉强张在军孙业伟于沛张高小徐立朋
Owner JINAN UNIVERSITY
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