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MECHANISM OF ANTIARRHYTHMIC EFFECT OF THE ANTIMALARIAL ARTEMISININ

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Author:
No author available
Journal Title:
ACTA PHARMACEUTICA SINICA
Issue:
8
DOI:
10.3321/j.issn:0513-4870.1999.08.003
Key Word:
青蒿素;钾通道;心律失常;内向整流钾通道(Kir 2.1);非洲蛙卵母细胞

Abstract: 目的:探讨青蒿素抗心律失常的离子电流基础.方法:用全细胞膜片钳技术和双电极电压钳技术.结果:当细胞超极化到-100 mV时,青蒿素以浓度依赖方式明显抑制家兔心室肌细胞Ik1, 50 μmol.L-1青蒿素可使家兔心室肌细胞Ik1从对照组的-2.36±0.39 nA减少到-1.43±0.31 nA.给予非洲蛙卵母细胞注射Kir 2.1 cRNA后,用不同浓度青蒿素灌注,可减低Kir 2.1钾通道电流,此作用呈电压和浓度依赖性.青蒿素对Kir 2.1钾通道的阻断作用呈可逆性.结论:青蒿素能有效抑制离体心肌细胞Ik1,其抗心律失常作用机理与其抑制心肌细胞Ik1及阻断Kir 2.1通道电流有关.

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