Literature DB >> 30216691

Cinnamic acids derived compounds with antileishmanial activity target Leishmania amazonensis arginase.

Edson Roberto da Silva1, Simone Brogi2, Alessandro Grillo2, Giuseppe Campiani2, Sandra Gemma2, Paulo Cezar Vieira3, Claudia do Carmo Maquiaveli4.   

Abstract

This study describes the activity of five natural hydroxycinnamic acids and derived compound: caffeic (1), rosmarinic (2), chlorogenic (3), and cryptochlorogenic (4), acids and isoverbascoside (5). All compounds inhibited Leishmania amazonensis arginase with IC50 -in range of 1.5-11 μM. Compounds 2 and 5 also showed activity against promastigotes of L. amazonensis with IC50  = 61 (28-133) μM and IC50  = 14 (9-24) μM, respectively. Further computational studies applying molecular docking simulations were performed on the competitive inhibitors to gain insight into the molecular basis for arginase inhibition and could be exploited to the development of new antileishmanials drug targeting parasite arginase.
© 2018 John Wiley & Sons A/S.

Entities:  

Keywords:  zzm321990Leishmania amazonensiszzm321990; arginase inhibition; enzyme kinetics; molecular modeling; natural products; polyamines

Mesh:

Substances:

Year:  2018        PMID: 30216691     DOI: 10.1111/cbdd.13391

Source DB:  PubMed          Journal:  Chem Biol Drug Des        ISSN: 1747-0277            Impact factor:   2.817


  5 in total

1.  Alkyl and Aryl Derivatives Based on p-Coumaric Acid Modification and Inhibitory Action against Leishmania braziliensis and Plasmodium falciparum.

Authors:  Susiany P Lopes; Lina M Yepes; Yunierkis Pérez-Castillo; Sara M Robledo; Damião P de Sousa
Journal:  Molecules       Date:  2020-07-11       Impact factor: 4.411

Review 2.  Natural Products That Target the Arginase in Leishmania Parasites Hold Therapeutic Promise.

Authors:  Nicola S Carter; Brendan D Stamper; Fawzy Elbarbry; Vince Nguyen; Samuel Lopez; Yumena Kawasaki; Reyhaneh Poormohamadian; Sigrid C Roberts
Journal:  Microorganisms       Date:  2021-01-28

3.  A Comprehensive QSAR Study on Antileishmanial and Antitrypanosomal Cinnamate Ester Analogues.

Authors:  Freddy A Bernal; Thomas J Schmidt
Journal:  Molecules       Date:  2019-11-28       Impact factor: 4.411

4.  Cinnamides Target Leishmania amazonensis Arginase Selectively.

Authors:  Edson Roberto da Silva; Júlio Abel Alfredo Dos Santos Simone Come; Simone Brogi; Vincenzo Calderone; Giulia Chemi; Giuseppe Campiani; Trícia Maria Ferrreira de Sousa Oliveira; Thanh-Nhat Pham; Marc Pudlo; Corine Girard; Claudia do Carmo Maquiaveli
Journal:  Molecules       Date:  2020-11-12       Impact factor: 4.411

5.  Total Synthesis of the Natural Chalcone Lophirone E, Synthetic Studies toward Benzofuran and Indole-Based Analogues, and Investigation of Anti-Leishmanial Activity.

Authors:  Luca Pozzetti; Roberta Ibba; Sara Rossi; Orazio Taglialatela-Scafati; Donatella Taramelli; Nicoletta Basilico; Sarah D'Alessandro; Silvia Parapini; Stefania Butini; Giuseppe Campiani; Sandra Gemma
Journal:  Molecules       Date:  2022-01-11       Impact factor: 4.411

  5 in total

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