Mahmoud Madiha R, Shahien Mona M, Ibrahim Somia, S Alenazi Fahaad, Hussein Weiam, Abdallah Marwa H, Aljadani Ahmed, Alreshidi Fayez, E El-Horany Hemat, M Osman Elhussein Gamal Eldin, Abdeen H Abdalla Rania, H Elhaj Abeer, M Khalifa Amany
Department of Pharmacology, College of Medicine, University of Ha'il, Ha'il 81442, Saudi Arabia.
Department of Pharmacology, TBRI, Ministry of Higher Education and Scientific Research, Giza 12411, Egypt.
ACS Omega. 2024 May 2;9(19):21234-21244. doi: 10.1021/acsomega.4c01319. eCollection 2024 May 14.
Angiotensin receptor blockers (ARBs) are commonly used to treat hypertension that target the hormonal system (renin-angiotensin system (RAS)), which regulates various physiological functions in the body. ARBs work by blocking the binding of angiotensin II to its receptor, thereby preventing a rise in blood pressure. These drugs not only normalize the overactivation of RAS but also provide protective effects against cardiovascular, renal, and type 2 diabetic patients. Inappropriate RAS activity has been linked to insulin resistance of type 2 diabetes. Olmesartan, as an ARB, was found to have a beneficial role in reducing postprandial glucose levels in type 2 diabetes. However, ARBs can cause side effects, prompting a search for new compounds that have fewer adverse effects. This study explores the potential of natural metabolites, specifically eugenol, gallic acid, myricetin, -cymene, quercetin, and kaempferol, as ARB inhibitors compared to the current standard, olmesartan. Using in silico studies, the binding affinity of these natural substances to the ARB receptor was evaluated. The results showed that myricetin and kaempferol had affinities higher than those of olmesartan, suggesting that they could serve as promising ARB inhibitors for hypertension treatment. These natural compounds could provide an alternative approach to conventional antihypertensive drugs, which may have fewer side effects. However, more research is needed to validate the efficacy and safety of these natural compounds as antihypertensive drugs. Further in vitro and in vivo studies are needed to confirm their effectiveness and safety. This study provides a promising starting point for future investigations into the potential of natural metabolites as alternative treatments for hypertension. The findings also highlight the importance of exploring natural alternative treatments for hypertension and the protective effects of ARBs on early stage type-2 diabetics.
血管紧张素受体阻滞剂（ARBs）常用于治疗高血压，其作用靶点是调节身体各种生理功能的激素系统（肾素-血管紧张素系统（RAS））。ARBs通过阻断血管紧张素II与其受体的结合来发挥作用，从而防止血压升高。这些药物不仅能使过度激活的RAS恢复正常，还对心血管疾病、肾脏疾病患者以及2型糖尿病患者具有保护作用。RAS活性异常与2型糖尿病的胰岛素抵抗有关。奥美沙坦作为一种ARBs，被发现对降低2型糖尿病患者的餐后血糖水平具有有益作用。然而，ARBs可能会引起副作用，这促使人们寻找副作用更少的新化合物。本研究探讨了天然代谢产物，特别是丁香酚、没食子酸、杨梅素、对伞花烃、槲皮素和山奈酚，与当前标准药物奥美沙坦相比作为ARB抑制剂的潜力。通过计算机模拟研究，评估了这些天然物质与ARB受体的结合亲和力。结果表明，杨梅素和山奈酚的亲和力高于奥美沙坦，这表明它们有望成为治疗高血压的ARB抑制剂。这些天然化合物可以为传统抗高血压药物提供一种替代方法，可能具有更少的副作用。然而，需要更多的研究来验证这些天然化合物作为抗高血压药物的有效性和安全性。还需要进一步的体外和体内研究来证实它们的有效性和安全性。本研究为未来探索天然代谢产物作为高血压替代治疗方法的潜力提供了一个有希望的起点。研究结果还强调了探索高血压天然替代治疗方法以及ARBs对早期2型糖尿病患者保护作用的重要性。
