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Application of conferone serving as beta2-adrenergic receptor antagonist

A technology of ferulone and receptor antagonist, which is applied in the field of ferulone as a β2-adrenergic receptor antagonist, can solve the problems of low controllability and achieve high stability and toxicity low effect

Active Publication Date: 2015-04-08
北京北科德源生物医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Recent studies have found that the potency of β2-adrenergic receptor inhibitors varies with the amount, while the above two known compounds are highly active and less controllable in use

Method used

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  • Application of conferone serving as beta2-adrenergic receptor antagonist
  • Application of conferone serving as beta2-adrenergic receptor antagonist
  • Application of conferone serving as beta2-adrenergic receptor antagonist

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Example 1 The effect of ferulone broad leaf on β2 adrenergic receptors

[0017] Materials and methods: HEK / beta-2 cell line was provided by Beijing Institute of Genomics, Chinese Academy of Sciences.

[0018] Isoprenaline (SIGMA, Cat#I2760) was used as a positive control for the β2 adrenergic receptor activator, and ICI118,551hydrocloride (SIGMA, Cat#I127-5MG) was used as a positive control for the β2 adrenergic receptor antagonist. The small molecule of ferulone to be tested was purchased from Shanghai Taosu Biochemical Technology Co., Ltd.

[0019] First seed HEK / beta-2 cells into the wells of a 96-well plate, the number of cells is 4X10 4 / hole. and put in CO 2 Grow in the incubator for one day. On the second day, the calcium flux test method was used to detect the effect of adding small molecular compounds such as ferulone on calcium flow and the effect of adding small molecular compounds such as ferulone on calcium and adding β2 adrenoceptor agonist on the calc...

Embodiment 2

[0020] The influence of embodiment 2 broad-leaf ferulone on hypertension

[0021] The purpose of the test: to detect whether the compound can cause blood pressure and blood sugar changes in the hypertensive animal experimental model SHR rats, and the dose value that causes blood pressure changes by gavage of multiple doses of the test compound to spontaneously hypertensive rats (SHR) for the first time, Preliminary proof of whether the lead compound acts on the Beta adrenergic receptor will also serve as a reference for the next step of fine pharmacodynamic experiments.

[0022] Materials and methods: SHR rats, an animal experimental model of hypertension, were prepared by the method of two kidneys and one clip of 10-week-old male rats. SHR hypertension 161±1.5mmHg is a successful animal model. Broad leaf ferulone was purchased from Shanghai Taosu Biochemical Technology Co., Ltd. Soybean oil is used as the solvent of ferulone. The route of administration is intragastric adm...

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Abstract

The invention relates to new application of compounds, in particular to application of conferone serving as a beta2-adrenergic receptor antagonist.

Description

technical field [0001] The present invention relates to the new application of field compound, in particular, relates to the application of ferulone as β2-adrenoceptor antagonist. Background technique [0002] Conferone was isolated from the fruit of Ferula conocaula, and was subsequently found to be available in most plants of the genus Ferula, so it was considered to be a common small molecule Natural product ingredients. Experimental studies have shown that ferulone can enhance the cytotoxicity of vinblastine, vincristine and cisplatin, but ferulone itself does not show obvious cytotoxicity. [0003] There are currently two known selective β2-adrenergic receptors: ICI-118,551[(±)-1-[2,3-(dihydro-7-methyl-1H-inden-4-yl)oxy] -3-[(1-methylethyl)amino]-2-butanol] and Butoxamine (Butaxamine)[α-[1-(t-butylamino)ethyl]-2,5-dimethoxybenzyl alcohol)hydrochloride]. These two drugs are both used in experimental research, and their main function is to block the activity of β2-adre...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61P3/10A61P9/12A61P9/06A61P9/00
CPCA61K31/352
Inventor 赵勇谢威刘昕陈洁宋新蕊常莉
Owner 北京北科德源生物医药科技有限公司
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