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Application of Thonningianin A in preparation of medicine serving as L-type calcium ion channel activator

A technology of calcium ion channel and activator, applied in the field of new uses of the extract

Pending Publication Date: 2021-07-23
THE AFFILIATED HOSPITAL OF SOUTHWEST MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Previous studies have shown that moderate autophagy can protect vascular calcification, but whether TA can reduce vascular calcification in diabetes by activating autophagy remains unknown

Method used

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  • Application of Thonningianin A in preparation of medicine serving as L-type calcium ion channel activator
  • Application of Thonningianin A in preparation of medicine serving as L-type calcium ion channel activator
  • Application of Thonningianin A in preparation of medicine serving as L-type calcium ion channel activator

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0107] Effects of TA on Calcification of Smooth Muscle Cells

[0108] To study the effect of TA on calcification in mouse aortic smooth muscle cells (MASMCs). The CCK-8 kit was used to determine the half maximal inhibitory concentration (IC) of TA on MASMCs in the early stage. 50 ). According to the routine operation method of the kit, the cells were divided into control group and different concentrations of TA intervention groups (200, 100, 50, 25, 12.5, 6.25, 3.125 μM) and co-incubated with MASMCs, and the cell survival rate was calculated according to the absorbance. Then calculate the IC of TA in MASMCs by GraphPad Prism 5 software 50 . The results showed that the IC of TA on MASMCs 50 was 13.47 μM, so 6 μM and 8 μM TA were chosen as the intervention concentration to study the effect of TA on the calcification of MASMCs.

[0109] (1) Establishment of mouse aortic smooth muscle cell calcification model

[0110] Primary MASMCs were isolated from the thoracic aorta of 8...

Embodiment 2

[0123] The mechanism of TA activating autophagy and its activation effect on L-type calcium channel on cell membrane

[0124] (1) TA promotes autophagy by increasing the intracellular calcium ion concentration through the L-type calcium ion channel on the cell membrane

[0125] Previous studies have shown that TA can induce intracellular Ca 2+ Increased concentration induces the activation of AMPK associated with AMP / ATP, thereby activating autophagy. In order to further verify whether TA increases the intracellular calcium ion concentration and promotes autophagy by which means, GFP-LC3 U87 cells stably expressing autophagy immunofluorescence were used as experimental subjects, and different calcium ion channel inhibitors Nifedipine (cell membrane L- The effect of TA on autophagy was observed under the intervention of 2-APB (endoplasmic reticulum IP3R calcium channel inhibitor) and Dantrolene (endoplasmic reticulum RyR calcium channel inhibitor).

[0126] The results of imm...

Embodiment 3

[0134] Animal experiments verify the effect of TA on vascular calcification

[0135] (1) Establishment of vascular calcification model in diabetic mice

[0136] The aortic blood vessels of the mice after modeling were taken to detect the tissue calcium content / calcium concentration. The results showed that: compared with the Control group, the calcium ion content and concentration in the aorta of the diabetic mice injected with Vit D (DM+VitD) group Significantly increased ( Figure 6 B, **P Figure 7 A, 7B, 7C). These results indicated that the induction of vascular calcification model in diabetic mice was successful.

[0137] (2) TA reduces aortic medial calcification in diabetic mice

[0138] While inducing calcification in diabetic mice, different concentrations of TA (low concentration 0.1mg / kg, high concentration 0.2mg / kg) were injected into the mice respectively. After 7 days of intervention, control group, DM +VitD group, DM+VitD+0.1mg / kg TA group, DM+VitD+0.2mg / kg ...

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Abstract

The invention discloses application of Thonningianin A (TA) in preparation of a medicine serving as an L-type calcium ion channel activator. The medicine can be used for preventing or / and treating vascular calcification of human or animals. The application has the beneficial effects that penthorum chinense pursh extract TA has the effect of preventing and treating the diabetes-related vascular calcification diseases, the action mechanism of the penthorum chinense pursh extract TA is found, and the new application of the penthorum chinense pursh extract TA in preparation of the medicine serving as the cell membrane L-type calcium channel activator is provided; and TA-containing medicine has the application prospect of preventing or / and treating human or animal vascular calcification.

Description

technical field [0001] The invention belongs to the technical field of new drug application of compounds, and relates to a new application of an extract of C. chinensis, in particular to the application of Thonningianin A (TA) in the drug of cell membrane L-type calcium ion channel activator. Background technique [0002] The occurrence of vascular calcification is due to the stimulation of various pathological factors, which breaks the mineralization defense mechanism of the vascular wall and transforms the vascular smooth muscle cells from a contractile phenotype to an osteogenic phenotype. In recent years, many studies on the pathological process of vascular calcification have led researchers to believe that vascular calcification is an actively regulated, complex biological process that is similar to bone formation and can be prevented and reversed (Leopold J A. Vascular calcification: an age-old problem of oldage. Circulation, 2013, 127(24): 2380-82.). Elevated blood s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7034A61P9/14A61P3/10A61P43/00A61K36/185
CPCA61K31/7034A61P9/14A61P3/10A61P43/00A61K36/185
Inventor 孙晓磊马亚蓉
Owner THE AFFILIATED HOSPITAL OF SOUTHWEST MEDICAL UNIV
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