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Mobola plum seed methanolic extracts exhibit mixed type inhibition of angiotensin Ⅰ-converting enzyme in vitro
Article in Chinese | WPRIM (Western Pacific) | ID: wpr-700079
Responsible library: WPRO
ABSTRACT

Objective:

To explore the possible inhibitory potentials and mechanism by Mobola plum (Parinari curatellifolia) seeds crude methanol (CE) and flavonoid-rich (FE) extracts on angiotensin-1-converting enzyme (ACE I).

Methods:

The sensitivity and kinetic model of inhibition of CE and FE on ACE I using N-[3-(2-furyl)-acryloyl]-Phe-Gly-Gly as enzyme substrate for ACE I was evaluated by Michealis Menten approach.The inhibition mechanism was explored from LineweaverBurk model and IC50 was determined from Cheng-Prusoff empirical analysis.

Results:

The IC50 of CE and FE were 13.54 and 39.38 μg/mL,respectively.Both extracts exhibited mixed type inhibition with the inhibitory constant (Ki) of CE was between 0.38 and 0.37 μg/mL while that of FE showed a two-fold increase (1.62 μg/mL and 0.28 μg/mL).FE on ACE I demonstrated positive cooperativity with a Hill's coefficient of 1.89.

Conclusions:

The study reveals the superior ACE I inhibitory potential of CE over FE and suggest that mixed inhibition pattern of the enzyme might be the underlying mechanism of antihypertensive activity.

Full text: Available Database: WPRIM (Western Pacific) Language: Chinese Journal: Asian Pacific Journal of Tropical Biomedicine Year: 2017 Document type: Article
Full text: Available Database: WPRIM (Western Pacific) Language: Chinese Journal: Asian Pacific Journal of Tropical Biomedicine Year: 2017 Document type: Article
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