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金松双黄酮 C 增加大鼠心室肌细胞的收缩。

Chrysosplenol C increases contraction in rat ventricular myocytes.

机构信息

College of Pharmacy, IDRD, Chungnam National University, 220 Gungdong, Yuseong-Gu, Daejeon 305-764, South Korea.

出版信息

J Cardiovasc Pharmacol. 2011 Feb;57(2):259-62. doi: 10.1097/FJC.0b013e318201f119.

Abstract

Chrysosplenol C (4',5,6-trihydroxy-3,3',7-trimethoxyflavone) is a flavone contained in several medicinal plants including Miliusa balansae and Pterocaulon sphacelatum. This compound is known to have an antiviral effect and show cytotoxic activity in several cell lines. In the present study, we explored the effect of chrysosplenol C on contractility in isolated adult rat ventricular myocytes. Chrysosplenol C was isolated from M. balansae, and cell shortenings were measured in field-stimulated single myocytes using a video edge detection method at room temperature. Chrysosplenol C was found to increase cell shortenings in a dose-dependent manner with a half-maximal effective concentration of 45 ± 7.8 μM. Maximal effect of chrysosplenol C, approximately 185% of control, was observed at ≥80 μM. The positive inotropic effect caused by chrysosplenol C was reversible. Time-to-peak contraction and time-to-relengthening were significantly increased by chrysosplenol C. The velocity of cell shortening was slightly accelerated, whereas that of relaxation was not altered by chrysosplenol C. The chrysosplenol C–induced positive inotropic effect was not inhibited by propranolol posttreatment or H-89 pretreatment, suggesting that chrysosplenol C increased contraction independently of β-adrenergic receptor stimulation and protein kinase A. Our findings are the first to demonstrate that chrysosplenol C is a positive inotropic agent in cardiac myocytes.

摘要

金丝桃苷 C(4',5,6-三羟基-3,3',7-三甲氧基黄酮)是几种药用植物中含有的一种类黄酮,包括小米草和沟酸浆。已知该化合物具有抗病毒作用,并在几种细胞系中表现出细胞毒性活性。在本研究中,我们探讨了金丝桃苷 C 对分离的成年大鼠心室肌细胞收缩性的影响。金丝桃苷 C 从小米草中分离出来,在室温下使用视频边缘检测方法测量场刺激的单个心肌细胞中的细胞缩短。发现金丝桃苷 C 呈剂量依赖性增加细胞缩短,半数有效浓度为 45±7.8μM。在≥80μM 时观察到金丝桃苷 C 的最大效应,约为对照的 185%。金丝桃苷 C 引起的正性变力作用是可逆的。金丝桃苷 C 使收缩的达峰时间和复极化时间明显延长。细胞缩短的速度略有加快,而松弛速度不受金丝桃苷 C 影响。金丝桃苷 C 诱导的正性变力作用不受普萘洛尔后处理或 H-89 预处理的抑制,表明金丝桃苷 C 增加收缩作用独立于β-肾上腺素能受体刺激和蛋白激酶 A。我们的发现首次证明金丝桃苷 C 是心肌细胞中的正性变力剂。

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