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Background <p>Hypertension is a dangerous health condition, since it is responsible for many deaths worldwide. Nowadays, there are different classes of antihypertensives available to treat hypertension. However, these medications can present serious adverse effects that can lead to treatment abandonment, thus resulting in an inefficient treatment. Peptides with bioactive properties present as an alternative for the development of new therapeutic molecules.</p> Purpose <p>In this work, we aimed to evaluate the antihypertensive potential of a new bioactive peptide.</p> Methods <p>A bioactive peptide was identified from a virtual screening of an <i>inhouse</i> peptide library through molecular docking with Angiotensin-Converting Enzyme (ACE). Its ACE-inhibitory potential was evaluated through an ACE inhibition assay. The cytotoxic potential of the peptide was evaluated based on the MTT assay in Vero cells.</p> Results <p>An initial screening to verify the enzyme’s inhibition showed 65.57 ± 15.04% of inhibitory capacity at 100&#xa0;µg/mL. The peptide presented an IC50 value of 6.6&#xa0;µg/mL and presented no cytotoxicity when tested on Vero cells at 5 and 50&#xa0;µg/mL.</p> Conclusion <p>The peptide described here is a potential alternative for the development of new antihypertensive molecules.</p>

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Identification of a Synthetic Peptide with Potential Angiotensin I-Converting Enzyme (ACE-1) Inhibitory Activity

  • 期刊论文

  • 发表日期：

    2025年1月6日

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  • Camila Innocente-Alves,
  • Raul Izidoro Carneiro,
  • Bruna Stedile,
  • Laura Rascovetzki Saciloto-de-Oliveira,
  • Yohana Porto Calegari-Alves,
  • Diogo André Pilger,
  • Lucélia Santi,
  • Hugo Verli,
  • Walter Orlando Beys-da-Silva

摘要

Background

Hypertension is a dangerous health condition, since it is responsible for many deaths worldwide. Nowadays, there are different classes of antihypertensives available to treat hypertension. However, these medications can present serious adverse effects that can lead to treatment abandonment, thus resulting in an inefficient treatment. Peptides with bioactive properties present as an alternative for the development of new therapeutic molecules.

Purpose

In this work, we aimed to evaluate the antihypertensive potential of a new bioactive peptide.

Methods

A bioactive peptide was identified from a virtual screening of an inhouse peptide library through molecular docking with Angiotensin-Converting Enzyme (ACE). Its ACE-inhibitory potential was evaluated through an ACE inhibition assay. The cytotoxic potential of the peptide was evaluated based on the MTT assay in Vero cells.

Results

An initial screening to verify the enzyme’s inhibition showed 65.57 ± 15.04% of inhibitory capacity at 100 µg/mL. The peptide presented an IC50 value of 6.6 µg/mL and presented no cytotoxicity when tested on Vero cells at 5 and 50 µg/mL.

Conclusion

The peptide described here is a potential alternative for the development of new antihypertensive molecules.