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      The effects of deoxyelephantopin on the cardiac delayed rectifier potassium channel current (IKr) and human ether-a-go-go-related gene (hERG) expression.

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          Abstract

          Elephantopus scaber Linn and its major bioactive component, deoxyelephantopin are known for their medicinal properties and are often reported to have various cytotoxic and antitumor activities. This plant is widely used as folk medicine for a plethora of indications although its safety profile remains unknown. Human ether-a-go-go-related gene (hERG) encodes the cardiac IKr current which is a determinant of the duration of ventricular action potentials and QT interval. The hERG potassium channel is an important antitarget in cardiotoxicity evaluation. This study investigated the effects of deoxyelephantopin on the current, mRNA and protein expression of hERG channel in hERG-transfected HEK293 cells. The hERG tail currents following depolarization pulses were insignificantly affected by deoxyelephantopin in the transfected cell line. Current reduction was less than 40% as compared with baseline at the highest concentration of 50 μM. The results were consistent with the molecular docking simulation and hERG surface protein expression. Interestingly, it does not affect the hERG expression at both transcriptional and translational level at most concentrations, although higher concentration at 10 μM caused protein accumulation. In conclusion, deoxyelephantopin is unlikely a clinically significant hERG channel and Ikr blocker.

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          Author and article information

          Journal
          Food Chem. Toxicol.
          Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association
          Elsevier BV
          1873-6351
          0278-6915
          Sep 2017
          : 107
          : Pt A
          Affiliations
          [1 ] Malaysian Institute of Pharmaceuticals & Nutraceuticals, National Institutes of Biotechnology Malaysia (NIBM), Ministry of Science, Technology and Innovation Malaysia, Pulau Pinang, Malaysia.
          [2 ] Advanced Medical & Dental Institute, Universiti Sains Malaysia, Pulau Pinang, Malaysia.
          [3 ] Atta-ur-Rahman Institute for Natural Product Discovery, Universiti Teknologi MARA (UiTM), Selangor Darul Ehsan, Malaysia.
          [4 ] School of Biological Sciences, Universiti Sains Malaysia, Pulau Pinang, Malaysia.
          [5 ] Malaysian Institute of Pharmaceuticals & Nutraceuticals, National Institutes of Biotechnology Malaysia (NIBM), Ministry of Science, Technology and Innovation Malaysia, Pulau Pinang, Malaysia; Advanced Medical & Dental Institute, Universiti Sains Malaysia, Pulau Pinang, Malaysia. Electronic address: tanml@usm.my.
          Article
          S0278-6915(17)30377-0
          10.1016/j.fct.2017.07.011
          28689918
          af410131-c043-455e-add0-393253794f04

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