Abstract
Angiotensin converting enzyme (ACE) plays a crucial role in regulating blood pressure in the human body. Identification of potential ACE inhibitors from medicinal plants supported the idea of repurposing these medicinal plants against hypertension. A method based on ultra-performance liquid chromatography (UPLC) coupled with a diode array detector (DAD) was used for the rapid screening of plant extracts and purified compounds to determine their ACE inhibitory activity. Hippuryl-histidiyl-leucine (HHL) was used as a substrate, which is converted into hippuric acid (HA) by the action of ACE. A calibration curve of the substrate HHL was developed with the linear regression 0.999. The limits of detection and quantification of this method were found to be 0.134 and 0.4061 mM, respectively. Different parameters of ACE inhibitory assay were optimized, including concentration, incubation time and temperature. The ACE inhibition potential of Adhatoda vasica (methanolic-aqueous extract) and its isolated pyrroquinazoline alkaloids, vasicinol (1), vasicine (2) and vasicinone (3) was evaluated. Compounds 1–3 were characterized by various spectroscopic techniques. The IC50 values of vasicinol (1), vasicine (2) and vasicinone (3) were found to be 6.45, 2.60 and 13.49 mM, respectively. Molecular docking studies of compounds 1–3 were also performed. Among these compounds, vasicinol (1) binds as effectively as captopril, a standard drug of ACE inhibition.
Highlights
Hypertension is a state in which the blood pressure is continuously elevated [1]
Trifluoracetic acid (TFA) and TEA were added in the mobile phase separately to check the effects on peak separation
Our results showed that the binding energies of vasicine (2) and vasicinone (3) are comparatively lower than those of the known inhibitors, whereas vasicinol (1) showed significant binding energy
Summary
Hypertension is a state in which the blood pressure is continuously elevated [1]. It is a major and common progressive disorder related to cardiovascular and renal diseases, stroke and diabetes [2]. Recent data have shown that one in six people in the world, or about one billion are afflicted by high blood pressure, and it is expected that this number is likely to increase to 1.5 billion by 2025 [3]. The renin angiotensin aldosterone system (RAAS) or renin angiotensin system (RAS) plays a significant role in the regulation of blood pressure. ACE (EC 3.4.15.1) is an important physiological enzyme in the RAS which controls peripheral blood pressure and fluid balance in the body [5]. It converts decapeptide angiotensin I to the potent vasoconstrictor octapeptide angiotensin II by the cleavage of the dipeptide histidylleucine [7]
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