Synthesis, in vitro and in silico studies of HO-1 inducers and lung antifibrotic agents-Reference-Cited by-同舟云学术

Synthesis, in vitro and in silico studies of HO-1 inducers and lung antifibrotic agents

Published:2019-07 Issue:13 Volume:11 Page:1523-1536
ISSN:1756-8919
Container-title:Future Medicinal Chemistry
language:en
Short-container-title:Future Medicinal Chemistry

Author:

Pittalà Valeria¹,Vanella Luca¹,Maria Platania Chiara Bianca²,Salerno Loredana¹,Raffaele Marco¹,Amata Emanuele¹^ORCID,Marrazzo Agostino¹,Floresta Giuseppe¹,Romeo Giuseppe¹,Greish Khaled³,Intagliata Sebastiano⁴,Bucolo Claudio²,Sorrenti Valeria¹

Affiliation:

1. Department of Drug Sciences, University of Catania, Viale A. Doria 6, Sicily, 95125, Italy

2. Department of Biomedical & Biotechnological Sciences, Section of Pharmacology, School of Medicine, University of Catania, Via Santa Sofia n. 97, Sicily, 95123, Italy

3. College of Medicine and Medical Sciences, Department of Molecular Medicine, and Nanomedicine Unit, Princess Al-Jawhara Center for Molecular Medicine, Arabian Gulf University, Building 61, King Abdulaziz Avenue, Block 328, Manama, Kingdom of Bahrain

4. Department of Medicinal Chemistry, College of Pharmacy, University of Florida, Medical Science Building, 1345 Center Drive, Gainesville, FL 32610, USA

Abstract

Aim: Dimethyl fumarate (DMF) analogs were synthesized to obtain inducers of HO-1 and antifibrotic agents. Methods: HO-1 expression levels were measured on lung fibroblasts (MRC5). NMR and docking studies were performed. Heme oxygenase activity, gene levels and protein expression have been measured for the most active compound 1a. Collagen production by fibroblast after exposure to TGF-β was measured. Results: Compound 1a showed to be a strong HO-1 inducer. Its activity seems to be mediated by activation of nuclear factor erythroid 2 related factor 2 (Nrf2). TGF-β-induced collagen production was significantly decreased on MRC5, pretreated with DMF or 1a. DMF and 1a have a high potential for treatment of lung fibrotic injuries.

Publisher

Future Science Ltd

Subject

Drug Discovery,Pharmacology,Molecular Medicine

Link

https://www.future-science.com/doi/pdf/10.4155/fmc-2018-0448

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