scholarly journals ANTIHYPERTENSIVE EFFECT OF RUTIN: PHARMACOLOGICAL AND COMPUTATIONAL APPROACH

2019 ◽  
pp. 87-92
Author(s):  
GANGA RAJU M ◽  
PREM PRASAD GOUD ◽  
SUVARCHALA REDDY NVL
Keyword(s):  
Antioxidant Activity ◽  
Angiotensin Converting Enzyme ◽  
Binding Affinity ◽  
Antihypertensive Effect ◽  
Antihypertensive Activity ◽  
Angiotensin Converting Enzyme Inhibition ◽  
Converting Enzyme ◽  
Vitro Assay

Objective: Phenolic compounds, such as flavonoids, have aroused great scientific interest due to their diverse pharmacological activities. Several studies suggested that flavonoids act as antihypertensive by inhibiting angiotensin-converting enzyme (ACE). In the present study, rutin, which is a citrus flavonoid, was evaluated for its antihypertensive activity using in vivo and in vitro models. Rutin was screened for in vitro assay procedures such as diphenylpicrylhydrazyl and nitroblue tetrazolium (NBT) for its antioxidant activity. Methods: Its antihypertensive effect was investigated in Nω-Nitro-l-arginine methyl ester hydrochloride-induced hypertensive rats, and various parameters such as blood pressure and heart rate were measured; in vitro ACE inhibitory activity was carried out against ACE, aiming at a better understanding of the interaction of this flavonoid with the enzyme. To understand its binding affinity with the angiotensin-converting enzyme, molecular docking studies were carried out using ligand fit of Maestro 9.1 (Schrodinger Software Inc.). An in silico study of rutin was performed for the prediction of Absorption, distribution, metabolism and elimination (ADME) by utilizing a web-based program (www.swissadme.ch). This software computes physicochemical descriptors as well as predicts pharmacokinetic properties and drug-like nature of one or multiple small molecules (blood–brain barrier, cytochromes P450, and P-glycoproteins). Results: Rutin at different dose levels of 200 and 400 mg/kg was tested, and the results have shown its antihypertensive, hypotensive, and negative chronotropic effects. Its antihypertensive activity might be mediated through angiotensin-converting enzyme inhibition (half maximal inhibitory concentration=66.01 μg/mL). In vitro studies also revealed the antioxidant activity of rutin, thus playing a major role in reducing oxidative stress associated with hypertension. The rutin showed optimum binding affinity with a molecular target (angiotensin-converting-enzyme) with the binding energy of −9.0 kcal/mol as compared to the standard (−6.3 kcal/mol). These results indicated that rutin is one of the potential ligands to treat hypertension. ADME results revealed the three violations of rutin (such as molecular mass, hydrogen donor, and acceptors) of five, and the standard captopril has got zero violations which clearly indicated the probability for its higher oral bioavailability. Conclusion: From the above, it is concluded that rutin possesses antioxidant and antihypertensive activities.

scholarly journals ANGIOTENSIN CONVERTING ENZYME INHIBITION POTENTIAL OF ANNAPAVALA CHENDHURAM FOR THE TREATMENT OF HYPERTENSION - AN IN–VITRO ASSAY

AYUSHDHARA ◽  
2020 ◽  
pp. 2599-2604
Author(s):  
Sabari Girija N ◽  
Sinekha M A ◽  
Guptaj S ◽  
Shanmugapriya P ◽  
Madhavan R
Keyword(s):  
Angiotensin Converting Enzyme ◽  
Ace Inhibition ◽  
In Vitro Assay ◽  
Lifestyle Changes ◽  
Angiotensin Converting Enzyme Inhibition ◽  
Uv Spectrophotometry ◽  
Test Drug ◽  
Converting Enzyme ◽  
Vitro Assay

Hypertension is that the most noteworthy risk factor for cardiovascular diseases and stroke. Dietary and lifestyle changes play the foremost part to decrease the hazard of hypertension and other related wellbeing complications. Angiotensin Converting Enzyme (ACE) inhibitors play a major role in treating hypertension. Annapavala chendhuram is a herbo – mineral Siddha formulation comes under the type of 32 internal medicines of Siddha. Hypolipidemic activity of Annapavala chendhuram has been proven by some research studies. Hence, the purpose of the present study was to evaluate the ACE inhibition activity on Annapavala chendhuram by using an in-vitro assay. The ACE inhibition assay was evaluated by UV Spectrophotometry technique based on the hydrolysis of histidyl-hippuryl-leucine (HHL) by ACE. About 50µL test sample with varying concentration (100- 500 µg/ml) along with standard captopril (100µg/ml) added with 50µL of ACE and some process had continued. The present study indicates that the test drug Annapavala chendhuram was effective in inhibiting the enzyme ACE dose-dependently. Maximum percentage inhibition of about 53.24±8.403% was observed at 500μg/ml when compared to that of the Captopril, a standard ACE enzyme inhibitor agent with the maximum inhibition 86.98 ± 6.375 at the concentration of 100μg/ml. It was concluded that the test drug Annapavala chendhuram possess significant anti-hypertensive property in protein denaturation assay. So, further in-vitro evaluation of ACE inhibitory activity on Siddha herbal preparations and clinical trials will be the need of the hour.

Interaction of mAb to angiotensin-converting enzyme (ACE) with antigen in vitro and in vivo: antibody targeting to the lung induces ACE antigenic modulation

1994 ◽  
Vol 6 (8) ◽  
pp. 1153-1160 ◽  
Author(s):  
Sergei Danilov ◽  
Elena Atochina ◽  
Holger Hiemisch ◽  
Tatiana Churak-ova ◽  
Aygul Moldobayeva ◽  
...  
Keyword(s):  
Angiotensin Converting Enzyme ◽  
Converting Enzyme ◽  
Antigenic Modulation ◽  
Antibody Targeting

DOCKING STUDY OF NOVEL N-SUBSTITUTED 2,5-BIS[(7-CHLOROQUINOLIN-4-YL)AMINO]PENTANOIC DERIVATIVES AS SELECTIVE HIGH-BINDER WITH ANGIOTENSIN CONVERTING ENZYME 2

INDIAN DRUGS ◽  
2020 ◽  
Vol 57 (08) ◽  
pp. 16-24
Author(s):  
Mohammed Oday Ezzat ◽  
Basma M. Abd Razik ◽  
Kutayba F. Dawood
Keyword(s):  
Angiotensin Converting Enzyme ◽  
Active Site ◽  
Docking Study ◽  
World Health ◽  
Converting Enzyme ◽  
Angiotensin Converting Enzyme 2 ◽  
Pharmaceutical Properties ◽  
Novel Coronavirus

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

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

1991 ◽  
Vol 37 (8) ◽  
pp. 1390-1393 ◽  
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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