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Application of abelmoschus manihot flower extract as TRPC ion channel inhibitor

A technology of hollyhock flowers and calcium ion channels, which is applied in the field of medicine and can solve problems that have not been shown by research

Inactive Publication Date: 2021-06-18
JIANGSU SUZHONG PHARM GRP CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Currently, no studies have demonstrated the inhibitory effects of protocatechuic acid, quercetin-3-O-acacioside, isoquercitrin, and quercetin-3′-O-β-D-glucoside on TRPC channels, and Use in the preparation of medicines for treating TRPC channel-related cardiovascular disease, coronary heart disease, atherosclerosis, end-stage renal failure, neurological disease, chronic pain, acute pain or inflammatory disease

Method used

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  • Application of abelmoschus manihot flower extract as TRPC ion channel inhibitor
  • Application of abelmoschus manihot flower extract as TRPC ion channel inhibitor
  • Application of abelmoschus manihot flower extract as TRPC ion channel inhibitor

Examples

Experimental program
Comparison scheme
Effect test

preparation example 1

[0064] Preparation example 1: Preparation of hollyhock flower extract

[0065] Take 3000g of the medicinal material hollyhock flower, use 19 times of 95% ethanol for the hollyhock flower, reflux extraction twice, each time for 1 hour, filter, combine the filtrate to recover ethanol, concentrate the filtrate to a specific gravity of 1.20, and let the concentrated solution stand at 0°C-4°C for 48 After a few hours, remove the oil layer of the refrigerated liquid, adjust the pH value to 6.0, concentrate and slowly add it to a vacuum belt dryer, dry it at 100°C, pulverize it, put it into a clean double-layer plastic bag, and obtain the hollyhock flower extract. Among them, it contains quercetin-3-O-lociposide 5.6 (mg / g), isoquercitrin 12.2 (mg / g), quercetin-3'-O-β-D-glucoside 11.2 (mg / g) g).

preparation example 2

[0066] Preparation example 2: preparation of hollyhock flower extract

[0067] Take 3000g of the medicinal material hollyhock flower, use 19 times of 95% ethanol for the hollyhock flower, reflux extraction twice, each time for 1 hour, filter, combine the filtrate to recover ethanol, concentrate the filtrate to a specific gravity of 1.20, and let the concentrated solution stand at 0°C-4°C for 48 After a few hours, remove the oil layer of the refrigerated liquid, adjust the pH value to 6.0, concentrate and slowly add it to a vacuum belt dryer, dry it at 100°C, pulverize it, put it into a clean double-layer plastic bag, and obtain the hollyhock flower extract. Among them, it contains quercetin-3-O-lociposide 5.6 (mg / g), isoquercitrin 10.1 (mg / g), quercetin-3'-O-β-D-glucoside 13.8 (mg / g) g).

Embodiment 1-3

[0069] (1) Transfect the cDNA plasmid vector containing TRPC3, TRPC6 or TRPC7 ion channels into the HERK293 cell line, and then select the corresponding antibiotics to incubate the cells according to the resistance of the plasmid to selectively screen the successfully transfected cells. Functional tests were performed on the surviving cells to confirm the expression and function of the channel protein, and then cloned and purified through the "limited dilution" process to obtain a stable cell line that stably expresses a specific channel.

[0070] (2) Add 10-13×104 cells / mL of the stable cells obtained in step (1), and add 150 μL of cell suspension per well into a 96-well plate with a black wall bottom. After 24 hours of cultivation in the incubator, it can be used for subsequent experiments.

[0071] (3) Observe the cells, and after confirming that the cells are in good condition, load the dye (fluo-4) for 60 min.

[0072] (4) prepare channel activator and inhibitor solution...

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Abstract

The invention provides application of an abelmoschus manihot flower extract in preparation of a medicine for inhibiting calcium channels, belongs to the field of medicines, and further provides application of the abelmoschus manihot flower extract in preparation of medicines for treating cardiovascular diseases, coronary heart diseases, atherosclerosis, advanced renal failure, neurological diseases, chronic pain, acute pain or inflammatory diseases. The extract can selectively inhibit calcium ion channels, especially TRPC ion channels, so that the effects of different channels under physiological and pathophysiological conditions can be illustrated, a thought is developed for cardiovascular and cerebrovascular diseases, coronary heart diseases and other diseases, and the application of the abelmoschus manihot flower extract is expanded.

Description

technical field [0001] The technology of the invention belongs to the field of medicine, and in particular relates to the application of the extract of hollyhock flowers. Background technique [0002] Cardiovascular disease is the most harmful disease to human life and health in modern society. According to the report of the World Health Organization, about 17.9 million people died of cardiovascular disease in the world in 2016, accounting for 31% of the total global deaths. It can be seen that the medical needs of new drugs for the prevention and treatment of cardiovascular diseases are very urgent. Relevant studies have proved that TRPC channels are important pharmacological targets for the development of new drugs for some cardiovascular diseases such as cardiomyopathy, heart failure, hypertension and cerebrovascular diseases. Patent application WO2006 / 074802A1 discloses that TRPC channels are used in the treatment of cardiovascular and cerebrovascular diseases. Its rese...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/185A61K31/7048A61K31/192A61P9/00A61P9/10A61P13/12A61P25/00A61P29/00C12Q1/02A61K133/00
CPCA61K36/185A61K31/7048A61K31/192A61P9/00A61P9/10A61P13/12A61P25/00A61P29/00G01N33/502A61K2236/333A61K2236/39A61K2236/51C12N2503/02G01N2500/10
Inventor 唐海涛曹征宇余伯阳葛海涛王正俊马继梅
Owner JIANGSU SUZHONG PHARM GRP CO LTD
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