Fan Zhuo, Wen Ting, Chen Yaoxu, Huang Lijie, Lin Wei, Yin Chunxia, Tan Wen
School of Bioscience and Bioengineering, South China University of Technology, Guangzhou 510006, China; Pre-Incubator for Innovative Drugs and Medicine, South China University of Technology, Guangzhou 510006, China; Guangdong Provincial Key Laboratory of Fermentation and Enzyme Engineering, South China University of Technology, Guangzhou 510006, China.
School of Bioscience and Bioengineering, South China University of Technology, Guangzhou 510006, China; Pre-Incubator for Innovative Drugs and Medicine, South China University of Technology, Guangzhou 510006, China.
Oxid Med Cell Longev. 2016;2016:6362812. doi: 10.1155/2016/6362812. Epub 2016 Feb 2.
KATP channel is an important mediator or factor in physiological and pathological metabolic pathway. Activation of KATP channel has been identified to be a critical step in the cardioprotective mechanism against IR injury. On the other hand, desensitization of the channel to its opener or the metabolic ligand ATP in pathological conditions, like cardiac hypertrophy, would decrease the adaption of myocardium to metabolic stress and is a disadvantage for drug therapy. Isosteviol, obtained by acid hydrolysis of stevioside, has been demonstrated to play a cardioprotective role against diseases of cardiovascular system, like anti-IR injury, antihypertension, antihyperglycemia, and so forth. The present study investigated the effect of isosteviol (STV) on sarcKATP channel current induced by pinacidil and mitochondrial flavoprotein oxidation induced by diazoxide. Our results showed that preincubating cells with STV not only increased the current amplitude and activating rate of sarcKATP channels induced by pinacidil but also potentiated diazoxide-elicited oxidation of flavoprotein in mitochondria.
KATP通道是生理和病理代谢途径中的重要介质或因素。KATP通道的激活已被确定为抗缺血再灌注(IR)损伤心脏保护机制中的关键步骤。另一方面,在病理状态下,如心肌肥大时,该通道对其开放剂或代谢配体ATP的脱敏作用会降低心肌对代谢应激的适应性,对药物治疗不利。通过甜菊糖苷酸水解获得的异甜菊醇已被证明对心血管系统疾病具有心脏保护作用,如抗IR损伤、抗高血压、抗高血糖等。本研究调查了异甜菊醇(STV)对吡那地尔诱导的肌膜KATP通道电流以及二氮嗪诱导的线粒体黄素蛋白氧化的影响。我们的结果表明,用STV预孵育细胞不仅增加了吡那地尔诱导的肌膜KATP通道的电流幅度和激活速率,还增强了二氮嗪引起的线粒体黄素蛋白氧化。