Uoorakkottil Ilyas, Koottangodan Rashid, Thajudheen Kamal Y, Alsheri Saad Ali, Ahmed Mohammed Muqtader
Department of Pharmacognosy and Phytochemistry, Moulana College of Pharmacy, Perinthalmanna 679321, KL, India.
Department of Pharmacology, Moulana College of Pharmacy, Perinthalmanna 679321, KL, India.
Pharmaceutics. 2024 Dec 23;16(12):1628. doi: 10.3390/pharmaceutics16121628.
Angiotensin-converting enzyme (ACE) is a key regulator of blood pressure, and ACE inhibition is an essential part of the treatment of hypertension. We used a molecular docking approach to find the interaction of ACE with an active flavonoid isolated from Linn, , which leads to potential antihypertensive effects in methyl predenisolone-induced hypertensive rats. Additionally, the pharmacokinetic parameters of this compound are assessed. was isolated from leaves of by sedimentation method. The compound was characterized by UPLC-MSMS, NMR, and UV spectroscopy to confirm the identity of the compound. Hypertension was induced in rats with methyl predenisolone (5 mg/kg/day) for 14 days. Systolic and diastolic blood pressure effects of were assessed using a tail-cuff method. The blood plasma data for oral administration were used to determine various pharmacokinetic parameters from the bioavailability and serum concentration. In methyl predenisolone-induced hypertensive rats, both systolic and diastolic blood pressures were significantly lower than that of the vehicle with treatment from ( < 0.01). The pharmacokinetic process showed the moderate bioavailability of the compound; induces powerful antihypertensive activity in methyl predenisolone-induced hypertensive rats, implying potential clinical application as a new therapeutic drug for hypertension.
血管紧张素转换酶（ACE）是血压的关键调节因子，抑制ACE是高血压治疗的重要组成部分。我们采用分子对接方法来研究ACE与从[植物名称]中分离出的一种活性黄酮类化合物的相互作用，该相互作用在甲基强的松龙诱导的高血压大鼠中产生潜在的降压作用。此外，还评估了该化合物的药代动力学参数。[化合物名称]通过沉淀法从[植物名称]的叶子中分离得到。通过超高效液相色谱-串联质谱（UPLC-MSMS）、核磁共振（NMR）和紫外光谱对该化合物进行表征，以确认其身份。用甲基强的松龙（5毫克/千克/天）诱导大鼠高血压14天。采用尾套法评估[化合物名称]对收缩压和舒张压的影响。口服给药的血浆数据用于从生物利用度和血清浓度确定各种药代动力学参数。在甲基强的松龙诱导的高血压大鼠中，从[具体时间]开始治疗，收缩压和舒张压均显著低于赋形剂组（P<0.01）。药代动力学过程显示该化合物具有中等生物利用度；[化合物名称]在甲基强的松龙诱导的高血压大鼠中诱导出强大的降压活性，这意味着它作为一种治疗高血压的新型治疗药物具有潜在的临床应用价值。
