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丹参酮II-A磺酸钠（DS-201）通过抑制L型钙通道诱导大鼠肠系膜动脉血管舒张。

Sodium Tanshinone II-A Sulfonate (DS-201) Induces Vasorelaxation of Rat Mesenteric Arteries via Inhibition of L-Type Ca Channel.

作者信息

Zhang Xiao-Dong, He Chun-Xia, Cheng Jun, Wen Jing, Li Peng-Yun, Wang Na, Li Guang, Zeng Xiao-Rong, Cao Ji-Min, Yang Yan

机构信息

Key Laboratory of Medical Electrophysiology of Ministry of Education, Collaborative Innovation Center for Prevention and Treatment of Cardiovascular Disease, Institute of Cardiovascular Research, Southwest Medical University, Luzhou, China.

出版信息

Front Pharmacol. 2018 Feb 2;9:62. doi: 10.3389/fphar.2018.00062. eCollection 2018.

DOI:10.3389/fphar.2018.00062
PMID:29456510
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5801295/
Abstract

We previously have proved that sodium tanshinone II-A sulfonate (DS-201), a derivative of traditional Chinese medicinal herb Danshen (Salvia miltiorrhiza), is an opener and vasodilator of BK channel in the vascular smooth muscle cells (VSMCs). Vascular tension is closely associated with Ca dynamics and activation of BK channel may not be the sole mechanism for the relaxation of the vascular tension by DS-201. Therefore, we hypothesized that the vasorelaxing effect of DS-20 may be also related to Ca channel and cytoplasmic Ca level in the VSMCs. Arterial tension was measured by Danish Myo Technology (DMT) myograph system in the mesentery vessels of rats, intracellular Ca level by fluorescence imaging system in the VSMCs of rats, and L-type Ca current by patch clamp technique in Ca channels transfected human embryonic kidney 293 (HEK-293) cells. DS-201 relaxed the endothelium-denuded artery rings pre-constricted with PE or high K and the vasorelaxation was reversible. Blockade of K channel did not totally block the effect of DS-201 on vasorelaxation. DS-201 suppressed [Ca] transient induced by high K in a concentration-dependent manner in the VSMCs, including the amplitude of Ca transient, the time for Ca transient reaching to the [Ca] peak and the time to remove Ca from the cytoplasm. DS-201 inhibited L-type Ca channel with an EC of 59.5 μM and at about 40% efficacy of inhibition. However, DS-201did not significantly affect the kinetics of Ca channel. The effect of DS-201 on L-type Ca channel was rate-independent. The effect of DS-201 on vasorelaxation was not only via activating BK channel, but also blocking Ca channel and inhibiting Ca influx in the VSMCs of rats. The results favor the use of DS-201 and Danshen in the treatment of cardiovascular diseases clinically.

摘要

我们之前已经证明，丹参（Salvia miltiorrhiza）的衍生物丹参酮II-A磺酸钠（DS-201）是血管平滑肌细胞（VSMCs）中BK通道的开放剂和血管舒张剂。血管张力与Ca动力学密切相关，BK通道的激活可能不是DS-201舒张血管张力的唯一机制。因此，我们推测DS-20的血管舒张作用可能也与VSMCs中的Ca通道和细胞质Ca水平有关。通过丹麦Myo Technology（DMT）肌动描记系统测量大鼠肠系膜血管中的动脉张力，通过荧光成像系统测量大鼠VSMCs中的细胞内Ca水平，并通过膜片钳技术测量转染Ca通道的人胚肾293（HEK-293）细胞中的L型Ca电流。DS-201使预先用PE或高K预收缩的去内皮动脉环舒张，且血管舒张是可逆的。阻断K通道并没有完全阻断DS-201对血管舒张的作用。DS-201以浓度依赖性方式抑制高K在VSMCs中诱导的[Ca]瞬变，包括Ca瞬变的幅度、Ca瞬变达到[Ca]峰值的时间以及从细胞质中去除Ca的时间。DS-201以59.5μM的EC抑制L型Ca通道，抑制效率约为40%。然而，DS-201对Ca通道的动力学没有显著影响。DS-201对L型Ca通道的作用与速率无关。DS-201对血管舒张的作用不仅通过激活BK通道，还通过阻断Ca通道和抑制大鼠VSMCs中的Ca内流。这些结果支持临床使用DS-201和丹参治疗心血管疾病。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4b68/5801295/4a61f120cbf7/fphar-09-00062-g008.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4b68/5801295/4a61f120cbf7/fphar-09-00062-g008.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4b68/5801295/45d0522372dc/fphar-09-00062-g002.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4b68/5801295/0e8665c6a308/fphar-09-00062-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4b68/5801295/8ecb7cec6a07/fphar-09-00062-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4b68/5801295/f3b84d091012/fphar-09-00062-g007.jpg
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2
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3
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6
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8
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