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Application of triterpenoids in the preparation of Parkinson's medicines

A technology of triterpene compounds and triterpenoids, which is applied in the field of Parkinson's medicine and its preparation, can solve the problems of unclear targets of autophagy inducers and poor drug efficacy, and achieve the goal of overcoming the defects of unclear targets and good Drug efficacy and effects with clear targets

Active Publication Date: 2019-11-29
THE HONG KONG POLYTECHNIC UNIV SHENZHEN RES INST +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The purpose of the present invention is to overcome the above-mentioned deficiencies of the prior art, to provide an application of triterpenoids with clear targets and different from classic mTOR inhibitors, and to solve the problem of unclear targets of existing autophagy inducers
[0007] Another object of the present invention is to provide an autophagy inducer for the treatment of Parkinson's disease, which solves the problem that the existing autophagy inducers cannot induce autophagy in the cerebral cortex of animals or only induce mild autophagy in neurons. Technical problems with poor efficacy

Method used

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  • Application of triterpenoids in the preparation of Parkinson's medicines
  • Application of triterpenoids in the preparation of Parkinson's medicines
  • Application of triterpenoids in the preparation of Parkinson's medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Effect of isothermal calorimetry (ITC) maslinic acid (MA) and palinginic acid (TA) on the function of autophagy-related proteins:

[0050] The thermal transformation caused by the interaction between the autophagy scaffold protein Beclin1 and the autophagy inhibitor Bcl-2 was measured with an isothermal calorimeter iTC200 (MicroCal) with or without the addition of maslinic acid or palindromic acid. Before the assay, both Beclin1 and Bcl-2 were dialyzed into 50 mM Tris, pH 8.0, and 150 mM NaCl buffer with or without maslinic acid or palinic acid at a final concentration of 10 μM. During the measurement, load 40 μl Beclin1 (concentration 12 mg / ml) on the titration syringe of the isothermal calorimetric titrator, and load 220 μl Bcl-2 (500 μg / ml) on the sample pool of the isothermal calorimetric titrator. Each injection was 2 μl, equilibrated for 180 seconds between each injection. Data were collected and analyzed by Origin 7.0.

[0051] Present embodiment 1 test analysi...

Embodiment 2

[0054] Pull-down experiments to detect the effects of maslinic acid (MA) and palinginic acid (TA) on the interaction between Beclin1 and autophagy inhibitor Bcl-2:

[0055] GST was used as the fusion tag of the autophagy inhibitor Bcl-2, GST-Bcl-2 was used as bait, and the purified autophagy backbone protein Beclin1 was used as prey to carry out pull-down experiments. Purified GST-Bcl-2 (or GST) 1.0mM and purified Beclin11.0mM (molar concentration 1:1) were mixed in 50mM Tris, pH 8.0, and 150mM NaCl buffer solution, the buffer solution contained or did not contain 10μM final concentration of maslinic acid or palinic acid. The mixture was incubated at room temperature for 30 minutes. The mixture was added to the GST affinity agarose beads equilibrated with the above buffer, and processed by the standard pull-down step. After the protein complex was eluted, the SDS sample buffer was added and separated and detected by SDS-PAGE.

[0056] The result is as Figure 3a , 3b It can...

Embodiment 3

[0058] Light scattering was used to determine the effect of maslinic acid (MA) and palinginic acid (TA) on the interaction between Beclin1 and autophagy inhibitor Bcl-2:

[0059] The protein molecular weight was determined by fast protein liquid chromatography-static light scattering; the protein particle size was detected by dynamic light scattering. Purified GST-Bcl-2 (or GST) 1.0mM and purified Beclin11.0mM (molar concentration 1:1) were mixed in 50mM Tris, pH 8.0, and 150mM NaCl buffer, the buffer contained or did not contain 10μM final concentration of Maslinic acid or Potentinic acid. The mixture was incubated at room temperature for 30 minutes. The mixture is loaded onto a gel chromatography column, separated and purified by fast protein liquid chromatography, and the molecular weights of components with different peak times are detected by a static light scattering instrument; or the particle size of the protein is detected by a dynamic light scattering instrument. T...

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Abstract

The invention provides application of a triterpene compound and a Parkinson's disease treatment medicine. The application comprises blocking of mutual combination between autophagy skeleton protein Beclin1 and an autophagy inhibiting factor Bcl-2 so as to induce nerve cell autophagy, and preparation of a Parkinson's disease treatment medicine. The triterpene compound is any one or a mixture of two of maslinic acid and tormentic acid. The Parkinson's disease treatment medicine provided by the invention comprises a pharmaceutically acceptable auxiliary material as well as an effective dosage of any one or a mixture of two of the maslinic acid and the tormentic acid. The triterpene compounds, namely the maslinic acid and the tormentic acid, are capable of directly blocking mutual combination between the autophagy skeleton protein Beclin1 and the autophagy inhibiting factor Bcl-2, so that the triterpene compounds have the function of promoting autophagy in nerve cells, and have a nerve protection function on Parkinson's disease cells. Therefore, the maslinic acid and the tormentic acid can be directly adopted to prepare the Parkinson's disease treatment medicine, and the Parkinson's disease treatment medicine is endowed with good medicinal effect.

Description

technical field [0001] The invention belongs to the technical field of autophagy-inducing compounds, and in particular relates to the application of a triterpenoid compound capable of inducing nerve cell autophagy, a medicine for treating Parkinson's containing the triterpenoid compound and a preparation method thereof. Background technique [0002] Parkinson's disease (PD), also known as shaking palsy (paralysis agitans), is a neurodegenerative disease commonly seen in middle-aged and elderly people. A total of 6 million people around the world suffer from Parkinson's disease. As the global population ages, the number of patients with Parkinson's disease is increasing year by year. The main pathological change of Parkinson's disease is the degeneration and death of dopamine (DA) neurons in the substantia nigra of the midbrain, which leads to a significant decrease in the content of DA in the striatum and the accumulation of a large number of Lewy bodies in the neurons. The...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/56A61P25/16
Inventor 李小花董晓莉赵清张焕
Owner THE HONG KONG POLYTECHNIC UNIV SHENZHEN RES INST
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