Malik Abdul, Mehmood Malik Hassan, Channa Hajra, Akhtar Muhammad Shoaib, Gilani Anwarul-Hassan
Natural Product Research Division, Department of Biological and Biomedical Sciences, Faculty of Health Sciences, Medical College, The Aga Khan University, Stadium Road, P.O. Box 3500, Karachi, 74800, Pakistan.
Faculty of Pharmacy, University of Sargodha, Sargodha, 40100, Pakistan.
BMC Complement Altern Med. 2017 Mar 7;17(1):142. doi: 10.1186/s12906-017-1644-0.
A compound herbal formulation (POL) has been used in the indigenous system of medicine to treat cardiometabolic disorders like diabetes and associated hypertension. POL and most of its constituents have not been studied widely for its therapeutic use in hypertension. This study is aimed to determine the efficacy and possible insight into mechanism(s) for the medicinal use of POL and its ingredients in hypertension.
The aqueous methanolic extracts of POL (POL.Cr) and its components [Cichorium intybus (Ci.Cr), Gymnema sylvestre (Gs.Cr), Nigella sativa (Ns.Cr) and Trigonella foenum graecum (Tfg.Cr)] were tested for blood pressure lowering activity in anaesthetized Sprague-Dawley rats. To assess the vasomodulatory effect, isolated tissue experiments were performed on rat aortic strips using isometric force transducer coupled with PowerLab data acquisition system.
Administration of POL to rats caused a dose-dependent (1-100 mg/kg) fall in mean arterial pressure (MAP) with maximum effect of 85.33 ± 1.76% at 100 mg/kg, similar to the effect of verapamil. All ingredients of POL also decreased blood pressure with varying efficacy in following order Ns.Cr ≅ Ci.Cr > Tfg.Cr > Gs.Cr. In rat aortic preparations, POL and its ingredients inhibited K (80 mM)-induced contractions, Ci.Cr was the most potent followed by Ns.Cr > Tfg.Cr > Gs.Cr ≅ POL. Against phenylephrine (P.E) contractions, Ci.Cr and Tfg.Cr exhibited complete relaxation, while POL.Cr, Gs.Cr and Ns.Cr showed vasomodulatory effect. The Ca antagonist activity was confirmed when POL and its ingredients shifted Ca concentrations-response curves to the right in a manner similar to that of verapamil. On baseline of rat aorta, the parent formulation and its ingredients (except Tfg.Cr) exhibited partially phentolamine (1 μM)-sensitive vasoconstriction.
These data show that POL and its constituents possess blood pressure lowering activity mediated through inhibition of Ca influx via membranous Ca channels and receptor (α-adrenergic) operated pathways. Thus, this study provides a rationale to the medicinal use of POL and its constituents in hypertension.
一种复方草药制剂（POL）已被用于传统医学体系中治疗糖尿病及相关高血压等心脏代谢紊乱疾病。POL及其大多数成分在高血压治疗用途方面尚未得到广泛研究。本研究旨在确定POL及其成分在高血压治疗中的疗效，并深入了解其作用机制。
对POL的水甲醇提取物（POL.Cr）及其成分[菊苣（Ci.Cr）、匙羹藤（Gs.Cr）、黑种草（Ns.Cr）和胡芦巴（Tfg.Cr）]在麻醉的Sprague-Dawley大鼠中进行降血压活性测试。为评估血管调节作用，使用与PowerLab数据采集系统相连的等长力传感器对大鼠主动脉条进行离体组织实验。
给大鼠施用POL导致平均动脉压（MAP）呈剂量依赖性（1 - 100 mg/kg）下降，在100 mg/kg时最大降幅为85.33±1.76%，与维拉帕米的效果相似。POL的所有成分也能降低血压，其效果各异，顺序为Ns.Cr≅Ci.Cr>Tfg.Cr>Gs.Cr。在大鼠主动脉制剂中，POL及其成分抑制K⁺（80 mM）诱导的收缩，Ci.Cr最有效，其次是Ns.Cr>Tfg.Cr>Gs.Cr≅POL。对于去氧肾上腺素（P.E）诱导的收缩，Ci.Cr和Tfg.Cr表现出完全舒张，而POL.Cr、Gs.Cr和Ns.Cr表现出血管调节作用。当POL及其成分以与维拉帕米相似的方式将Ca²⁺浓度 - 反应曲线向右移动时，证实了其钙拮抗剂活性。在大鼠主动脉基线水平，母体制剂及其成分（除Tfg.Cr外）表现出对酚妥拉明（1 μM）部分敏感的血管收缩作用。
这些数据表明，POL及其成分具有通过抑制经膜钙通道和受体（α - 肾上腺素能）介导途径的钙内流来降低血压的活性。因此，本研究为POL及其成分在高血压治疗中的药用提供了理论依据。
