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Application of paeonol in the preparation of drugs for activating herg ion channels

An ion channel and paeonol technology, applied in the field of biomedicine, can solve the problems of few drugs or compounds and few drugs, and achieve the effect of avoiding complicated and time-consuming, avoiding preclinical tests, and increasing K+ outflow

Inactive Publication Date: 2017-12-22
GUANGZHOU INST OF BIOMEDICINE & HEALTH CHINESE ACAD OF SCI
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Problems solved by technology

[0004] People have been trying to find drugs that can resist the inhibitory effect of myocardial hERG ion channels, that is, antagonists or activators of myocardial hERG ion channels, but there are very few drugs or compounds that can activate hERG ion channels (since the first report in 2005). Since drugs that can activate hERG ion channels, there are still very few drugs that can activate hERG ion channels)

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  • Application of paeonol in the preparation of drugs for activating herg ion channels
  • Application of paeonol in the preparation of drugs for activating herg ion channels
  • Application of paeonol in the preparation of drugs for activating herg ion channels

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Embodiment 1

[0016] Paeonol can be obtained from pharmaceutical raw materials or reagent companies, and because of its low water solubility, it needs to be dissolved in dimethyl sulfoxide (DMSO). Dissolve 0.0167g paeonol in 1ml DMSO as a mother solution, then take the corresponding amount from the mother solution, and prepare a series of drug concentrations of 10μM, 30μM, 100μM, 300μM, 1000μM in extracellular fluid and store in a 4°C refrigerator for later use. Extracellular fluid formula: NaCl 137mM, KCl 4mM, CaCl 2 1.8mM, MgCl 2 1.0 mM, glucose 10 mM, HEPES 10 mM, pH adjusted to 7.4 with 1 M NaOH. Chinese hamster ovary cells (CHO) stably transfected with hERG ion channels (B.D.Walker,S.M.Valenzuela,C.B.Singleton,S.N.Breit & 1T.J.Campbell.Inhibition of HERGchannels stably expressed in a mammalian cell line by the antianginal agentperhexiline maleate.British Journal of Pharmacology 127, 243-251 (1999)) were prepared with HAMSF-12 in 10% fetal bovine serum (FBS), and routinely cultured ...

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Abstract

The invention discloses application of paeonol to preparation of medicine activating an hERG ion channel, and belongs to secondary development and utilization of traditional Chinese medicine effective components. Paeonol has the function of remarkably activating the hERG ion channel, can increase K+ external flow, has the potential in resisting and treating long QT syndromes and has the prospect that paeonol can be developed into medicine preventing acquired long QT syndromes. At present, paeonol is clinically used for treatment of relevant cardiovascular diseases and inflammation prevention, so that paeonol is applied in the aspect of prevention of the acquired long QT syndromes. Complex and time-consuming pre-clinical tests can be avoided.

Description

Technical field: [0001] The invention belongs to the field of biomedicine, in particular to the application of paeonol in the preparation of a medicine for activating hERG ion channels. Background technique: [0002] Acquired Long QT Syndrome (Aquired Long QT Syndrome), also known as QT prolongation syndrome, is a heart rhythm disorder. The electrocardiogram of patients with this syndrome shows QT interval prolongation, T wave and / or U wave abnormalities, There is a tendency to develop polymorphic ventricular arrhythmias, especially torsades de pointes (TdP). Patients often present with palpitations and dizziness, which can cause fainting and death in severe cases. The syndrome can be congenital or acquired, and the latter is mostly caused by adverse drug reactions (inhibition of myocardial hERG ion channels). It has been reported that many drugs have been forced to withdraw from the market. In addition, quite a few newly developed drugs have the effect of inhibiting hERG i...

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/12A61P9/06
CPCA61K31/12
Inventor 李志远黄荣奇龙雁林佐贤马文波
Owner GUANGZHOU INST OF BIOMEDICINE & HEALTH CHINESE ACAD OF SCI
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