Natural Product Research Division, Department of Biological and Biomedical Sciences, The Aga Khan University Medical College, Karachi 74800, Pakistan.
BMC Complement Altern Med. 2013 Dec 26;13:371. doi: 10.1186/1472-6882-13-371.
Cardiovascular disorders (CVDs) are the leading cause of disease burden worldwide. Apart from available synthetic drugs used in CVDs, there are many herbal formulations including POL-10 (containing 10 herbs), which have been shown to be effective in animal studies but POL-10 was found to cause tachycardia in rodents as its side effect. This study was designed to modify the composition of POL-10 for better efficacy and/or safety profile in CVDs.
To assess the antidyslipidemic, antihypertensive and endothelial modulatory properties of two herbal formulations, (ZPTO and ZTO) containing Z: Zingiber officinalis, P: Piper nigrum, T: Terminalia belerica and O: Orchis mascula, different animal models including, tyloxapol and high fat diet-induced dyslipidemia and spontaneously hypertensive rats (SHR) were used. Effect on endothelial function was studied using isolated tissue bath set up coupled with PowerLab data acquisition system. The antioxidant activity was carried out using DPPH radical-scavenging assay.
Based on preliminary screening of the ingredients of POL-10 in tyloxapol-induced hyperlipidemic rats, ZPTO and ZTO containing four active ingredients namely; Z, P, T and O were identified for further studies and comparison. In tyloxapol-induced hyperlipidemic rats, both ZPTO and ZTO caused significant reduction in serum triglyceride (TG) and total cholesterol (TC). In high fat diet-fed rats, ZPTO decreased TC, low-density lipoproteins cholesterol (LDL-C) and atherogenic index (AI). ZTO also showed similar effects to those of ZPTO with additional merits being more effective in reducing AI, body weight and more importantly raising high-density lipoproteins. In SHR, both formulations markedly reduced systolic blood pressure, AI and TG levels, ZTO being more potent in reversing endothelial dysfunction while was devoid of cardiac stimulatory effect. In addition, ZTO also reduced LDL-C and improved glucose levels in SHR. In DPPH radical-scavenging activity test, ZTO was also more potent than ZPTO.
The modified formulation, ZTO was not only found more effective in correcting cardiovascular abnormalities than ZPTO or POL-10 but also it was free from tachycardiac side-effect, which might be observed because of the presence of Piper nigrum in ZPTO.
心血管疾病(CVDs)是全球疾病负担的主要原因。除了用于 CVDs 的现有合成药物外,还有许多草药配方,包括 POL-10(含 10 种草药),在动物研究中已证明其有效,但 POL-10 被发现会导致啮齿动物心动过速,这是其副作用。本研究旨在修改 POL-10 的组成,以在 CVDs 中获得更好的疗效和/或安全性。
为了评估两种草药配方(ZPTO 和 ZTO)的抗血脂、抗高血压和内皮调节特性,我们使用了包含 Z:姜黄、P:黑胡椒、T:诃子和 O:玉凤花的不同动物模型,包括 tyloxapol 和高脂饮食诱导的血脂异常和自发性高血压大鼠(SHR)。使用离体组织浴装置和 PowerLab 数据采集系统研究内皮功能。使用 DPPH 自由基清除测定法进行抗氧化活性测定。
基于 POL-10 成分在 tyloxapol 诱导的高脂血症大鼠中的初步筛选,确定了包含四种活性成分 Z、P、T 和 O 的 ZPTO 和 ZTO 进行进一步研究和比较。在 tyloxapol 诱导的高脂血症大鼠中,ZPTO 和 ZTO 均显著降低血清甘油三酯(TG)和总胆固醇(TC)。在高脂饮食喂养的大鼠中,ZPTO 降低了 TC、低密度脂蛋白胆固醇(LDL-C)和致动脉粥样硬化指数(AI)。ZTO 还表现出与 ZPTO 相似的作用,除了更有效地降低 AI、体重外,更重要的是提高了高密度脂蛋白。在 SHR 中,两种配方均显著降低收缩压、AI 和 TG 水平,ZTO 逆转内皮功能障碍的作用更强,而没有心脏刺激作用。此外,ZTO 还降低了 SHR 的 LDL-C 和改善了血糖水平。在 DPPH 自由基清除活性测试中,ZTO 也比 ZPTO 更有效。
与 ZPTO 或 POL-10 相比,修改后的配方 ZTO 不仅在纠正心血管异常方面更有效,而且没有心动过速的副作用,这可能是因为 ZPTO 中含有黑胡椒。