The use of Brazilian propolis for discovery and development of novel anti-inflammatory drugs

Author(s)

Franchin, Marcelo ; Freires, Irlan Almeida ; Lazarini, Josy Goldoni ; Nani, Bruno Dias ; da Cunha, Marcos Guilherme ; Colon, David Fernando ; de Alencar, Severino Matias ; Rosalen, Pedro Luiz

• Document type: Journal article
• Source: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY; v. 153, p. 7-pg., 2018-06-10.

Abstract

Anti-Inflammatory drugs have been routinely used in the management of acute and chronic inflammatory conditions. Nevertheless, their undesirable side and adverse effects have encouraged the development of more selective, tolerable and efficacious drugs able to modulate the inflammatory process through distinct mechanisms than those of drugs currently available in the market, for instance, inhibition of leukocyte recruitment (chemotaxis, rolling, adhesion and transmigration). Natural products, including Brazilian propolis, have been considered a rich source of anti-inflammatory molecules due to a very complex phytochemical diversity. Brazil has at least thirteen distinct types of propolis and many bioactive compounds have been isolated therefrom, such as apigenin, artepillin C, vestitol, neovestitol, among others. These molecules were proven to play a significant immunomodulatory role through (i) inhibition of inflammatory cytokines (e.g. TNF-alpha) and chemokines (CXCL1/KC and CXCL2/MIP2); (ii) inhibition of lam, ERK1/2, JNK and p38MAPK phosphorylation; (iii) inhibition of NF-kappa B activation; and (iv) inhibition of neutrophil adhesion and transmigration (1CAM-1, VCAM-1 and E-selectin expression). In this review, we shed light on the new advances in the research of compounds isolated from Brazilian propolis from Apis mellifera bees as potentially novel anti-inflammatory drugs. The compilation of data and insights presented herein may open further avenues for the pharmacological management of oral and systemic inflammatory conditions. Further research should focus on clinical and acute/chronic toxicological validation of the most promising compounds described in this review. (C) 2017 Elsevier Masson SAS. All rights reserved. (AU)

• FAPESP's process: 15/26864-7 - Bioprospection of active compounds from organic propolis with activity on neutrophil migration in inflammatory process.
• Grantee: Bruno Dias Nani
• Support Opportunities: Scholarships in Brazil - Doctorate
• FAPESP's process: 16/15563-9 - Characterization of new pharmacological targets and study of the activity of a 4-phenyl coumarin in the differentiation of Th17 lymphocytes in the development of periodontal disease
• Grantee: Marcelo Franchin
• Support Opportunities: Scholarships in Brazil - Post-Doctoral
• FAPESP's process: 16/02926-6 - Phytochemistry and bioprospection of antioxidant and anti-inflammatory activities from unexplored Brasilian native fruits.
• Grantee: Josy Goldoni Lazarini
• Support Opportunities: Scholarships in Brazil - Doctorate