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半夏白术天麻汤加减的降压和血管舒张作用。

Anti-hypertensive and vasodilatory effects of amended Banxia Baizhu Tianma Tang.

机构信息

School of Pharmaceutical Sciences, Universiti Sains Malaysia, USM 11800 Minden, Pulau Pinang, Malaysia.

School of Pharmaceutical Sciences, Universiti Sains Malaysia, USM 11800 Minden, Pulau Pinang, Malaysia; College of Pharmacy, Fujian University of Traditional Chinese Medicine, 1 Qiuyang Road, Shangjie, Minhou, Fuzhou 350122, Fujian, China.

出版信息

Biomed Pharmacother. 2018 Jan;97:985-994. doi: 10.1016/j.biopha.2017.11.021. Epub 2017 Nov 8.

Abstract

Although Banxia Baizhu Tianma Tang (BBT) has been long administered for hypertensive treatment in Traditional Chinese Medicine (TCM), the ratio of the herbal components that makes up the formulation has not been optimized with respect to the anti-hypertensive effect that it inherently possesses. A newly amended BBT (ABBT) formulation was developed using the evidence-based approach of orthogonal stimulus-response compatibility model. The ABBT showed enhanced therapeutic effect while maintaining its traditional theoretical approach rooted in TCM. This study was designed to investigate the possible mechanism of actions involved in the vasodilatory activity of ABBT-50 by evaluating its vasodilative effect on isolated Sprague Dawley rats in the presence of absence of various antagonists. When pre-contracted with phenylephrine, relaxation was observed in endothelium intact (EC=0.027±0.003mg/ml, R=109.8±2.12%) and denuded aortic rings (EC=0.409±0.073mg/ml, R=63.15±1.78%), as well as in endothelium intact aortic rings pre-contracted with potassium chloride (EC=32.7±12.16mg/ml, R=34.02±3.82%). Significant decrease in the vasodilative effect of ABBT-50 was observed in the presence of Nω-nitro-l-arginine methyl ester (EC=0.12±0.021mg/ml, R=75.33±3.28%), 1H-[1,2,4] Oxadiazolo[4,3-a]quinoxalin-1-one (EC=0.463±0.18mg/ml, R=54.48±2.02%), methylene blue (EC=0.19±0.037mg/ml, R=83.69±3.19%), indomethacin (EC=0.313±0.046mg/ml, R=71.33±4.12%), atropine (EC=0.146±0.013mg/ml, R=77.2±3.41%), and 4-aminopyridine (EC=0.045±0.008mg/ml, R=95.55±2.36%). ABBT-50 was also suppressing Ca release from sarcoplasmic reticulum and inhibiting calcium channels. Vasodilatory effects of ABBT-50 are mediated through NO/sGC/cGMP cascade and PGI, followed by muscarinic pathways and calcium channels.

摘要

尽管半夏白术天麻汤(BBT)在中医中已长期用于高血压治疗,但对于其固有的降压作用,其草药成分的比例尚未得到优化。一种新的改良 BBT(ABBT)配方是使用基于证据的正交刺激-反应相容性模型方法开发的。ABBT 在保持其传统中医理论基础的同时,显示出增强的治疗效果。本研究旨在通过评估其对 Sprague Dawley 大鼠离体血管的舒张作用,探讨 ABBT-50 血管舒张活性的可能作用机制,在存在或不存在各种拮抗剂的情况下。当用苯肾上腺素预收缩时,在完整内皮(EC=0.027±0.003mg/ml,R=109.8±2.12%)和去内皮主动脉环(EC=0.409±0.073mg/ml,R=63.15±1.78%)中观察到舒张,以及在氯化钾预收缩的完整内皮主动脉环中(EC=32.7±12.16mg/ml,R=34.02±3.82%)。当存在 Nω-硝基-L-精氨酸甲酯(EC=0.12±0.021mg/ml,R=75.33±3.28%)、1H-[1,2,4]恶二唑[4,3-a]喹喔啉-1-酮(EC=0.463±0.18mg/ml,R=54.48±2.02%)、亚甲蓝(EC=0.19±0.037mg/ml,R=83.69±3.19%)、吲哚美辛(EC=0.313±0.046mg/ml,R=71.33±4.12%)、阿托品(EC=0.146±0.013mg/ml,R=77.2±3.41%)和 4-氨基吡啶(EC=0.045±0.008mg/ml,R=95.55±2.36%)时,ABBT-50 的舒张作用明显减弱。ABBT-50 还抑制肌浆网钙释放并抑制钙通道。ABBT-50 的血管舒张作用是通过 NO/sGC/cGMP 级联和 PGI 介导的,随后是毒蕈碱途径和钙通道。

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