In Vitro Anti-Trypanosoma cruzi Activity of Halophytes from Southern Portugal Reloaded: A Special Focus on Sea Fennel (Crithmum maritimum L.)

Autor(es)

Pereira, Catarina G. ^[1] ; Moraes, Carolina Borsoi ^{[2, 3]} ; Franco, Caio H. ^[2] ; Feltrin, Clarissa ^[2] ; Grougnet, Raphael ^[4] ; Barbosa, Euzebio Guimaraes ^[5] ; Panciera, Michele ^[6] ; Correia, Carlos Roque D. ^[6] ; Rodrigues, Maria Joao ^[1] ; Custodio, Luisa ^[1]

Afiliação do(s) autor(es)

^[1] Univ Algarve, Fac Sci & Technol, Ctr Marine Sci CCMAR, Ed 7, Campus Gambelas, P-8005139 Faro - Portugal

^[2] Univ Sao Paulo, Inst Biomed Sci, Dept Microbiol, BR-05508900 Sao Paulo, SP - Brazil

^[3] Univ Fed Sao Paulo, Dept Pharmaceut Sci, BR-09913030 Diadema, SP - Brazil

^[4] Univ Paris, Fac Pharm, UMR CNRS 8038, Nat Prod, Anal Synth, 4 Ave Observ, F-75006 Paris - France

^[5] Univ Fed Rio Grande do Norte, Dept Pharm, BR-59064720 Natal, RN - Brazil

^[6] Univ Estadual Campinas, Inst Chem, Josue de Castro St, BR-13083970 Campinas, SP - Brazil

• Tipo de documento: Artigo Científico
• Fonte: PLANTS-BASEL; v. 10, n. 11 NOV 2021.
• Citações Web of Science: 0

Resumo

Marine halophytes are an outstanding reservoir of natural products and several species have anti-infectious traditional uses. However, reports about their potential use against neglected tropical ailments, such as Chagas disease, are scarce. This work evaluated for the first time the in vitro anti-Trypanosoma cruzi activity of extracts from the aromatic and medicinal species Helichrysum italicum subsp. picardii (Boiss. \& Reut.) Franco (Asteraceae, everlasting) and Crithmum maritimum L. (Apiaceae, sea fennel). For that purpose, decoctions, tinctures, and essential oils from everlasting's flowers and sea fennel's stems, leaves, and flowers were tested against intracellular amastigotes of two T. cruzi strains. The extract from the sea fennel flower decoction displayed significant anti-trypanosomal activity and no toxicity towards the host cell (EC50 = 17.7 mu g/mL, selectivity index > 5.65). Subsequent fractionation of this extract afforded 5 fractions that were re-tested in the same model of anti-parasitic activity. Fraction 1 was the most active and selective (EC50 = 0.47 mu g/mL, selectivity index = 59.6) and was submitted to preparative thin-layer chromatography. One major compound was identified, falcarindiol, which was likely the one responsible for the observed anti-trypanosomal activity. This was confirmed using a commercially sourced molecule. Target-fishing studies showed falcarindiol as a ligand of T. cruzi spermidine synthase, pointing to a potential enzyme-inhibiting anti-trypanosomal mechanism of action. Overall, this work shows that sea fennel can provide effective anti-parasitic molecule(s) with potential pharmacological applications in the treatment of CD. (AU)

• Processo FAPESP: 13/25613-5 - Síntese de marcadores fluorescentes moleculares diarilmaleimidas a partir das reações de Heck-Matsuda para aplicações biológicas e bioquímicas
• Beneficiário: Michele Panciera
• Modalidade de apoio: Bolsas no Brasil - Pós-Doutorado