ArticleActa pharmacologica Sinica2013
Allocryptopine and benzyltetrahydropalmatine block hERG potassium channels expressed in HEK293 cells.
Article in Acta pharmacologica Sinica, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.
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5 citing papers in PubMed, 14 citations in OpenAlex.
- Computational Evaluation of N-Based Transannular Interactions in Some Model Fused Medium-Sized Heterocyclic Systems and Implications for Drug Design.Molecules (Basel, Switzerland) · 2023Article
- Exploring the Anti-inflammatory Effects of Protopine Total Alkaloids ofFrontiers in veterinary science · 2022Article
- Natural products modulating the hERG channel: heartaches and hope.Natural product reports · 2017Review
- Shuyu Capsules Relieve Premenstrual Syndrome Depression by Reducing 5-HTNeural plasticity · 2016Article
- Novel Bayesian classification models for predicting compounds blocking hERG potassium channels.Acta pharmacologica Sinica · 2014Article
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Authors and funding
8 authors.
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No grant is acknowledged in the PubMed record.
Abstract
aimAllocryptopine (ALL) is an alkaloid extracted from Corydalis decumbens (Thunb) Pers. Papaveraceae, whereas benzyltetrahydropalmatine (BTHP) is a derivative of tetrahydropalmatine extracted from Corydalis ambigua (Pall) Cham et Schlecht. The aim of this study was to investigate the effects of ALL and BTHP on the human ether-a-go-go related gene (hERG) current expressed in HEK293 cells.
methodsCultured HEK293 cells were transiently transfected with hERG channel cDNA plasmid pcDNA3.1 using Lipofectamine. The whole-cell current IHERG was evoked and recorded using Axon MultiClamp 700B amplifier. The drugs were applied via supserfusion.
resultsBoth ALL and BTHP reversibly suppressed the amplitude and density of IHERG in concentration- and voltage-dependent manners (the respective IC50 value was 49.65 and 22.38 μmol/L). BTHP (30 μmol/L) caused a significant negative shift of the steady-state inactivation curve of IHERG, while ALL (30 μmol/L) did not affect the steady-state inactivation of IHERG. Furthermore, BTHP, but not ALL, shortened the time constants of fast inactivation and slow time constants of deactivation of IHERG. But both the drugs markedly lengthened the time constants for recovery of IHERG from inactivation. Using action potential waveform pulses, it was found that both the drugs at 30 μmol/L significantly suppressed the current densities in the late phase of action potential, but did not significantly affect the current densities in the early phase of action potential.
conclusionBoth ALL and BTHP derived from Chinese herbs potently block hERG current.
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