Furofuran lignans display schistosomicidal and trypanocidal activities

Author(s)

Andrade e Silva, Marcio Luis ^{[1, 2]} ; Esperandim, Viviane Rodrigues ^[1] ; Ferreira, Daniele da Silva ^[1] ; Magalhaes, Lizandra Guidi ^[1] ; Lima, Thais Coelho ^[1] ; Cunha, Wilson Roberto ^[1] ; Nanayakkara, Dhammika N. P. ^[3] ; Pereira, Ana Carolina ^{[1, 2]} ; Bastos, Jairo Kenupp ^[2]

Affiliation

^[1] Univ Franca, Nucleo Ciencias Exatas & Tecnol, Grp Pesquisas Prod Nat, BR-14404600 Franca, SP - Brazil

^[2] Univ Sao Paulo, Fac Ciancias Farmacaut Ribeirao Preto, Dept Ciencias Farmacaut, BR-14040903 Ribeirao Preto, SP - Brazil

^[3] Univ Mississippi, Sch Pharm, Pharmaceut Sci Res Inst, Natl Ctr Nat Prod Res, University, MS 38677 - USA

• Document type: Journal article
• Source: Phytochemistry; v. 107, p. 119-125, NOV 2014.
• Web of Science Citations: 2

Abstract

Parasitic diseases continue to be a major worldwide health problem, and there is an urgent need for development of therapeutic drugs. This paper describes synthesis of dehydrodiferulic acid dilactone 1 and dehydrodisinapic acid dilactone 2 furofuran lignans by oxidative coupling of ferulic and sinapic acids, respectively. Their schistosomicidal, trypanocidal, and leishmanicidal activities were evaluated in vitro against Schistosoma mansoni adult worms, trypomastigote and amastigotes forms of Trypanosoma cruzi, and promastigote forms of Leishmania amazonensis. Compound 1 did not display significant schistosomicidal activity, but it presented potent trypanocidal activity, since it induced death of trypomastigotes and amastigotes with IC50/24h of 9.3 mu M and 7.3 mu M, respectively. Compound 2 had slight trypanocidal and schistosomicidal activities. None of the compounds were active against L amazonensis. These results demonstrated that furofuran lignans are potentially useful for anti-parasitic drugs development and should be further investigated. (C) 2014 Elsevier Ltd. All rights reserved. (AU)

• FAPESP's process: 11/10179-2 - Obtaining lignans, neolignans and semisynthetic derivatives through reusable porphyrin systems and evaluation of parasitic activity of the substances obtained
• Grantee: Ana Carolina Pereira
• Support Opportunities: Scholarships in Brazil - Post-Doctoral
• FAPESP's process: 09/05049-2 - Development of polymeric nanaparticles and biodegradable systems containing lignans and evaluation its Chagas disease and schistosomiasis activities in vitro and in vivo
• Grantee: Márcio Luís Andrade e Silva
• Support Opportunities: Regular Research Grants
• FAPESP's process: 09/15207-4 - Evaluation of the effect of lignans and neolignans on Schistosoma mansoni: a proteomic study
• Grantee: Lizandra Guidi Magalhães
• Support Opportunities: Scholarships in Brazil - Post-Doctoral