In Vitro and in Vivo Studies on the Angiotensin-Converting Enzyme Inhibitory Activity Peptides Isolated from Broccoli Protein Hydrolysate

The prevalence of a novel coronavirus (2019-nCoV) in the last few months represents a serious threat as a world health emergency concern. Angiotensin-converting enzyme 2 (ACE2) is the host cellular receptor for the respiratory syndrome of coronavirus epidemic in 2019 (2019-nCoV). In this work, the active site of ACE2 is successfully located by Sitmap prediction tool and validated by different marketed drugs. To design and discover new medical countermeasure drugs, we evaluate a total of 184 molecules of 7-chloro-N-methylquinolin-4-amine derivatives for binding affinity inside the crystal structure of ACE2 located active site. A novel series of N-substituted 2,5-bis[(7-chloroquinolin-4-yl)amino]pentanoic acid derivatives is generated and evaluated for a prospect as a lead compound for (2019-nCoV) medication with a docking score range of (-10.60 to -8.99) kcal/mol for the highest twenty derivatives. Moreover, the ADME pharmaceutical properties were evaluated for further proposed experimental evaluation in vitro or in vivo

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Angiotensin-converting enzyme determination in plasma during therapy with converting enzyme inhibitor: two methods compared

Clinical Chemistry ◽

10.1093/clinchem/37.8.1390 ◽

1991 ◽

Vol 37 (8) ◽

pp. 1390-1393 ◽

Cited By ~ 9

Author(s):

T P Gorski ◽

D J Campbell

Keyword(s):

Angiotensin Converting Enzyme ◽

Spectrophotometric Method ◽

Enzyme Inhibitor ◽

Ang Ii ◽

Converting Enzyme ◽

Fluorometric Method ◽

Converting Enzyme Inhibitor ◽

Ace Activity

Abstract For normal and above-normal concentrations of angiotensin-converting enzyme (ACE; EC 3.4.15.1) activity in plasma, results of a manual fluorometric method [with hippuryl-histidyl-leucine (HHL), 5 mmol/L, as substrate] correlated well with those of an automated spectrophotometric method [with 3-(2-furylacryloyl)-L-phenylalanyl-glycyl-glycine (FAPGG), 2 mmol/L, as substrate]. However, for patients receiving converting enzyme inhibitor (CEI) therapy, the spectrophotometric method showed much greater suppression of plasma ACE activity than did the fluorometric method. To determine which of the two methods provided a more reliable indication of ACE inhibition in vivo, we measured plasma ACE, angiotensin I (ANG I), and angiotensin II (ANG II) in patients receiving the CEI perindopril. During perindopril therapy, changes in the ratio of ANG II:ANG I, an index of ACE activity in vivo, showed a close agreement with changes in plasma ACE activity measured with FAPGG as substrate, but not with HHL as substrate. We conclude that measurement of ACE activity in vitro with FAPGG as substrate provides a reliable measure of changes in conversion of ANG I to ANG II in vivo during CEI therapy.

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Xanthine oxidase inhibitory activity of nicotino/isonicotinohydrazides: A systematic approach from in vitro , in silico to in vivo studies

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2017.02.044 ◽

2017 ◽

Vol 25 (8) ◽

pp. 2351-2371 ◽

Cited By ~ 7

Author(s):

Humaira Zafar ◽

Muhammad Hayat ◽

Sumayya Saied ◽

Momin Khan ◽

Uzma Salar ◽

...

Keyword(s):

Xanthine Oxidase ◽

Inhibitory Activity ◽

In Silico ◽

Systematic Approach ◽

In Vivo Studies

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Inhibitory Activities of Polyphenolic Extracts of Bangladeshi Vegetables against α-Amylase, α-Glucosidase, Pancreatic Lipase, Renin, and Angiotensin-Converting Enzyme

Foods ◽

10.3390/foods9070844 ◽

2020 ◽

Vol 9 (7) ◽

pp. 844

Author(s):

Razia Sultana ◽

Adeola M. Alashi ◽

Khaleda Islam ◽

Md Saifullah ◽

C. Emdad Haque ◽

...

Keyword(s):

Angiotensin Converting Enzyme ◽

Pancreatic Lipase ◽

Lipase Activity ◽

Inhibitory Activity ◽

The Other ◽

Converting Enzyme ◽

Inhibitory Activities ◽

Ash Gourd ◽

Better Than

The aim of the study was to determine the in vitro enzyme inhibition activities of aqueous polyphenolic extracts of nine popular Bangladeshi vegetables, namely ash gourd, bitter gourd, brinjal, Indian spinach, kangkong, okra, ridge gourd, snake gourd, and stem amaranth. Polyphenolic glycosides were the major compounds present in the extracts. Inhibition of α-amylase (up to 100% at 1 mg/mL) was stronger than α-glucosidase inhibition (up to 70.78% at 10 mg/mL). The Indian spinach extract was the strongest inhibitor of pancreatic lipase activity (IC50 = 276.77 µg/mL), which was significantly better than that of orlistat (381.16 µg/mL), a drug. Ash gourd (76.51%), brinjal (72.48%), and snake gourd (66.82%) extracts were the most effective inhibitors of angiotensin-converting enzyme (ACE), an enzyme whose excessive activities have been associated with hypertension. Brinjal also had a significantly higher renin-inhibitory activity than the other vegetable extracts. We conclude that the vegetable extracts may have the ability to reduce enzyme activities that have been associated with hyperglycemia, hyperlipidemia, and hypertension.

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