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20(S)-人参皂苷Rg3通过环磷酸腺苷依赖性方式对人血小板聚集和细胞内钙水平的抑制作用。

Inhibitory Effect of 20(S)-Ginsenoside Rg3 on Human Platelet Aggregation and Intracellular Ca Levels via Cyclic Adenosine Monophosphate Dependent Manner.

作者信息

Kwon Hyuk-Woo

机构信息

Department of Biomedical Laboratory Science, Far East University, Chungbuk 27601, Korea.

出版信息

Prev Nutr Food Sci. 2018 Dec;23(4):317-325. doi: 10.3746/pnf.2018.23.4.317. Epub 2018 Dec 31.

Abstract

Intracellular Ca ([Ca]) induces platelet aggregation, and influences the activation of aggregation associated-molecules. The increased [Ca] activates both the Ca/calmodulin-dependent phosphorylation of the myosin light chain and the diacylglycerol-dependent phosphorylation of pleckstrin to trigger granule secretion (i.e., dense body and α-granule) and platelet aggregation. This study was carried out to elucidate the antagonistic effect of 20(S)-ginsenoside Rg3 (G-Rg3) present in Mayer on Ca. G-Rg3 inhibited thrombin-induced human platelet aggregation in a dose-dependent manner and suppressed thrombin-induced elevation of [Ca] mobilization. G-Rg3 increased the levels of cAMP, and subsequently, elevated the phosphorylation of inositol 1,4,5-triphosphate receptor I (Ser) during thrombin-induced human platelet aggregation. Moreover, G-Rg3 inhibited thapsigargin-induced Ca influx and the thrombin-induced elevation of extracellular signal-regulated kinase 2 phosphorylation. G-Rg3 exhibited an inhibitory effect on [Ca] levels leading to granule release and thus a therapeutic potential against platelet-mediated thrombotic disease is suggested.

摘要

细胞内钙([Ca])诱导血小板聚集,并影响聚集相关分子的激活。[Ca]的增加激活了肌球蛋白轻链的钙/钙调蛋白依赖性磷酸化和普列克底物蛋白的二酰基甘油依赖性磷酸化,从而触发颗粒分泌(即致密体和α颗粒)以及血小板聚集。本研究旨在阐明 Mayer 中存在的 20(S)-人参皂苷 Rg3(G-Rg3)对钙的拮抗作用。G-Rg3 以剂量依赖性方式抑制凝血酶诱导的人血小板聚集,并抑制凝血酶诱导的[Ca]动员升高。在凝血酶诱导的人血小板聚集中,G-Rg3 增加了 cAMP 水平,随后提高了肌醇 1,4,5-三磷酸受体 I(Ser)的磷酸化水平。此外,G-Rg3 抑制了毒胡萝卜素诱导的钙内流以及凝血酶诱导的细胞外信号调节激酶 2 磷酸化的升高。G-Rg3 对导致颗粒释放的[Ca]水平具有抑制作用,因此提示其对血小板介导的血栓性疾病具有治疗潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/22ab/6342537/3a704a66c881/pnfs-23-317f1.jpg

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