Evaluation of Angiotensin Converting Enzyme Inhibitors by Spr Biosensor and Theoretical Studies

Evaluation of Angiotensin Converting Enzyme Inhibitors by Spr Biosensor and Theoretical Studies Publisher Pubmed

Salehabadi H¹ ; Khajeh K² ; Dabirmanesh B² ; Biglar M³ ; Amanlou M^{1, 3}

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1. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, 14176-53955, Iran
2. Department of Biochemistry, Faculty of Biological Sciences, Tarbiat Modares University, Tehran, 14115-111, Iran
3. Drug Design and Development Research Center, The Institute of Pharmaceutical Sciences (TIPS), Tehran University of Medical Sciences, Tehran, 14176-53955, Iran

Source: Enzyme and Microbial Technology Published:2019

Abstract

Surface plasmon resonance (SPR) biosensor has been utilized for monitoring analyte-ligand interactions in modern drug discovery processes. SPR biosensors measure the change in refractive indexes over the course of analyte molecules’ binding to a specific immobilized ligand on sensor chip. This effort highlights a comprehensive SPR study besides enzymatic assay for discovery of new Angiotensin Converting Enzyme (ACE) inhibitors via screening of medicinal plants. At first, five medicinal plants were selected as potential sources for developing new ACE inhibitors through hydrolyzing hippuryl-L-histidyl-L-leucine (HHL) assay. The interaction of selected extracts with immobilized ACE on the sensor chip (500D) confirmed that the Onopordum acanthium L. had the greatest ACE inhibition activity among the set of compounds and its active compound (onopordia) was isolated. SPR biosensor used to evaluate binding affinity of onopordia and ACE. Equilibrium constant (KD), and changes in Gibb's free energy of the binding (ΔGbinding) values for the interaction of onopordia with ACE were found to be 10.24 μM and -28.48 kJ/mol, respectively. Computational analysis supported the binding of onopordia to the ACE active site. Kinetic and thermodynamic parameters of binding revealed that onopordia is an acceptable ACE inhibitor and could treat hypertension. SPR biosensor can be used to improve the drug discovery process for many important classes of drug targets due to its great sensitivity. © 2018 Elsevier Inc.

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Experts (# of related papers)

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Massoud Amanlou (10)

Mahmood Biglar (2)

Style	Citing Format
MLA	Salehabadi H, et al.. "Evaluation of Angiotensin Converting Enzyme Inhibitors by Spr Biosensor and Theoretical Studies." Enzyme and Microbial Technology, vol. 120, no. , 2019, pp. 117-123.
APA	Salehabadi H, Khajeh K, Dabirmanesh B, Biglar M, Amanlou M (2019). Evaluation of Angiotensin Converting Enzyme Inhibitors by Spr Biosensor and Theoretical Studies. Enzyme and Microbial Technology, 120(), 117-123.
Chicago	Salehabadi H, Khajeh K, Dabirmanesh B, Biglar M, Amanlou M. "Evaluation of Angiotensin Converting Enzyme Inhibitors by Spr Biosensor and Theoretical Studies." Enzyme and Microbial Technology 120, no. (2019): 117-123.
Harvard	Salehabadi H et al. (2019) 'Evaluation of Angiotensin Converting Enzyme Inhibitors by Spr Biosensor and Theoretical Studies', Enzyme and Microbial Technology, 120(), pp. 117-123.
Vancouver	Salehabadi H, Khajeh K, Dabirmanesh B, Biglar M, Amanlou M. Evaluation of Angiotensin Converting Enzyme Inhibitors by Spr Biosensor and Theoretical Studies. Enzyme and Microbial Technology. 2019;120():117-123.
BibTex	@article{ author = {Salehabadi H and Khajeh K and Dabirmanesh B and Biglar M and Amanlou M}, title = {Evaluation of Angiotensin Converting Enzyme Inhibitors by Spr Biosensor and Theoretical Studies}, journal = {Enzyme and Microbial Technology}, volume = {120}, number = {}, pages = {117-123}, year = {2019} }
RIS	TY - JOUR AU - Salehabadi H AU - Khajeh K AU - Dabirmanesh B AU - Biglar M AU - Amanlou M TI - Evaluation of Angiotensin Converting Enzyme Inhibitors by Spr Biosensor and Theoretical Studies JO - Enzyme and Microbial Technology VL - 120 IS - SP - 117 EP - 123 PY - 2019 ER -

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