2. Academic Validation
  3. A UPLC-DAD-Based Bio-Screening Assay for the Evaluation of the Angiotensin Converting Enzyme Inhibitory Potential of Plant Extracts and Compounds: Pyrroquinazoline Alkaloids from Adhatoda vasica as a Case Study

A UPLC-DAD-Based Bio-Screening Assay for the Evaluation of the Angiotensin Converting Enzyme Inhibitory Potential of Plant Extracts and Compounds: Pyrroquinazoline Alkaloids from Adhatoda vasica as a Case Study

  • Molecules. 2021 Nov 18;26(22):6971. doi: 10.3390/molecules26226971.
Syeda Tehreem 1,  Saeedur Rahman 1,  Muhammad Salman Bhatti 1,  Reaz Uddin 2,  Muhammad Noman Khan 1,  Saba Tauseef 2,  Hesham R El-Seedi 3 4,  Abdullatif Bin Muhsinah 5,  Jalal Uddin 6,  Syed Ghulam Musharraf 1 2 7
Affiliations

Affiliations

  • 1 H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan.
  • 2 Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan.
  • 3 Pharmacognosy Group, Department of Pharmaceutical Biosciences, BMC, Uppsala University, SE-751 24 Uppsala, Sweden.
  • 4 International Research Center for Food Nutrition and Safety, Jiangsu University, Zhenjiang 212013, China.
  • 5 Department of Pharmacognosy, College of Pharmacy, King Khalid University, Abha 62529, Saudi Arabia.
  • 6 Department of Pharmaceutical Chemistry, College of Pharmacy, King Khalid University, Abha 62529, Saudi Arabia.
  • 7 T.C.M. Hospital of Southwest Medical University, Luzhou 646000, China.
PMID: 34834066 DOI: 10.3390/molecules26226971
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.

Keywords

angiotensin converting enzyme; hypertension; pyrroquinazoline alkaloids; vasicine; vasicinol; vasicinone.

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