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Application of goniolactones C to suppressing proliferation and migration of vascular smooth muscle cells

A technology of cornalactone and smooth muscle cells, which is applied to cardiovascular system diseases, medical preparations containing active ingredients, organic active ingredients, etc., to achieve the effect of inhibiting the proliferation and migration of vascular smooth muscle cells and reducing the proliferation of smooth muscle cells

Active Publication Date: 2016-04-27
INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Styryl pyrone has strong antifungal activity and tumor cell cycle inhibitory effect, but there are few reports of such compounds on cell models of cardiovascular and cerebrovascular diseases

Method used

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  • Application of goniolactones C to suppressing proliferation and migration of vascular smooth muscle cells
  • Application of goniolactones C to suppressing proliferation and migration of vascular smooth muscle cells
  • Application of goniolactones C to suppressing proliferation and migration of vascular smooth muscle cells

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1. Cornalide C inhibits serum-induced proliferation of rat vascular smooth muscle cells

[0027] Experimental method: After male SD rats were decapitated, the thoracic aorta blood vessel was quickly taken out under aseptic condition, the fat layer was separated, placed in digestive solution (0.06% trypsin + 0.06% type I collagenase), and kept in the incubator Digest in medium for 20-30min; take it out, completely remove the adventitia, use tweezers to pull the blood vessel to destroy its intima, take the smooth muscle layer, cut it into pieces, and place it in a petri dish; culture it with DMEM / F12 medium + 20% FBS; Digest with 0.125% trypsin; transfer to the second generation and change the medium: DMEM+10% FBS; unless otherwise specified, the smooth muscle referred to in the present invention is P3-P5 generation. Rat vascular smooth muscle cells (VascularSmoothMuscleCell, VSMC) with 10 4 The density of each well was planted in a 96-well plate until 50% conflu...

Embodiment 2

[0033] Example 2. Cornalide C inhibits PDGF-BB-induced proliferation of rat vascular smooth muscle cells

[0034] Experimental method: the cell culture method is the same as in Example 1. Rat vascular smooth muscle cells with 10 4 The density of each hole was planted in a 96-well plate until 50% confluence, the serum was withdrawn and incubated for 24 hours, and then according to the experimental design, 0, 1.25, 2.5, 5, 10 and 20 μM cornacinolide C was added for pre-incubation for 24 hours, and then Add different concentrations of growth factors (bFGF100ng / ml, EGF10μg / ml and PDGF-BB40ng / ml) to continue incubation, discard the cell supernatant after 24h, use crystal violet staining method, observe the OD value of each group, and calculate the OD value of each dose group inhibition rate. Inhibition rate=1-[(model group OD value-blank control value)-(each dose group OD value-blank control value)] / [(model group OD value-blank control value)-(normal control group OD value-blank ...

Embodiment 3

[0039] Example 3. Cornalide C inhibits PDGF-BB-induced DNA synthesis in rat vascular smooth muscle cells

[0040] Experimental method: the cell culture method is the same as in Example 1. Rat vascular smooth muscle cells with 10 4 The density of each well was planted in a 96-well plate until 50% confluence, and the serum was withdrawn to continue incubation for 24 hours. Then, according to the experimental design, 0, 0.25, 0.5, 1, 2 and 4 μM cornacinolide C was added for pre-incubation, and after 24 hours Add PDGF-BB to a final concentration of 40ng / ml, continue to incubate for 24h, and add 10nMBrdu (sterile treatment) to each well 5 hours before the end of the experiment, continue to incubate for 24h, discard the cell supernatant, and rinse the cells with PBS. Triton-100 penetrated the cells, fixed with paraformaldehyde, blocked with BSA overnight, incubated with mouse anti-Brdu primary antibody for 4 hours, rinsed with PBST, incubated with FITC-labeled rabbit anti-mouse IgG...

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Abstract

The invention relates to application of a treatment effective dose of goniolactones C, a medicine composition with the goniolactones C, a medicine box with the goniolactones C and / or an apparatus such as a strut with the goniolactones C and a method for treating or preventing disease states by means of suppressing proliferation and / or migration of smooth muscle cells. Diseases can be selectively blood vessel wall thickening and narrow vessel lumen type cardiovascular and cerebrovascular diseases due to endothelial injury, proliferation of the vascular smooth muscle cells and deposition of matrixes and include diseases due to atherosclerosis, restenosis after angioplasty, hypertension, pulmonary hypertension and diabetic angiopathies.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a new application of cornalactone C for inhibiting the proliferation and migration of vascular smooth muscle cells, more specifically, the invention relates to a method for inhibiting the proliferation and migration of smooth muscle cells, comprising administering therapeutic An effective amount of cornalide C, and pharmaceutical compositions and kits containing cornalactone C, or a method of treating or preventing a disease state by inhibiting smooth muscle cell proliferation and / or migration, including breastfeeding in need Administering a therapeutically effective amount of cornalide C to the animal selected from the group consisting of vessel wall thickening and lumen narrowing cardiovascular disease due to endothelial injury, vascular smooth muscle cell proliferation, matrix deposition, including atherosclerosis , Restenosis after angioplasty, hypertension, pulmonary hypert...

Claims

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Application Information

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IPC IPC(8): A61K31/366A61P9/14A61P9/10A61P9/12
Inventor 杜冠华孙岚陈若芸于德泉王嗣蓝希赵睿
Owner INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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