title: In vitro activity of the hydroethanolic extract and biflavonoids isolated from Selaginella sellowii on Leishmania (Leishmania) amazonensis.
abstract: This study is the first phytochemical investigation of Selaginella sellowii and demonstrates the antileishmanial activity of the hydroethanolic extract from this plant (SSHE), as well as of the biflavonoids amentoflavone and robustaflavone, isolated from this species. The effects of these substances were evaluated on intracellular amastigotes of Leishmania (Leishmania) amazonensis, an aetiological agent of American cutaneous leishmaniasis. SSHE was highly active against intracellular amastigotes [the half maximum inhibitory concentration (IC50) = 20.2 µg/mL]. Fractionation of the extract led to the isolation of the two bioflavonoids with the highest activity: amentoflavone, which was about 200 times more active (IC50 = 0.1 μg/mL) and less cytotoxic than SSHE (IC50 = 2.2 and 3 μg/mL, respectively on NIH/3T3 and J774.A1 cells), with a high selectivity index (SI) (22 and 30), robustaflavone, which was also active against L. amazonensis (IC50 = 2.8 µg/mL), but more cytotoxic, with IC50 = 25.5 µg/mL (SI = 9.1) on NIH/3T3 cells and IC50 = 3.1 µg/mL (SI = 1.1) on J774.A1 cells. The production of nitric oxide (NO) was lower in cells treated with amentoflavone (suggesting that NO does not contribute to the leishmanicidal mechanism in this case), while NO release was higher after treatment with robustaflavone. S. sellowii may be a potential source of biflavonoids that could provide promising compounds for the treatment of cutaneous leishmaniasis.
authors.affiliation: Laboratório de Parasitologia Humana, Centro de Ciências Biológicas e da Saúde, Universidade Federal de Mato Grosso do Sul, Campo Grande, MS, Brasil.
authors.forename: Yasmin Silva
authors.initials: YS
authors.lastname: Rizk
authors.affiliation: Laboratório de Farmacognosia, Centro de Ciências Biológicas e da Saúde, Universidade Federal de Mato Grosso do Sul, Campo Grande, MS, Brasil.
authors.forename: Alice
authors.initials: A
authors.lastname: Fischer
authors.affiliation: Laboratório de Biologia Molecular e Culturas Celulares, Centro de Ciências Biológicas e da Saúde, Universidade Federal de Mato Grosso do Sul, Campo Grande, MS, Brasil.
authors.forename: Marillin de Castro
authors.initials: Mde C
authors.lastname: Cunha
authors.affiliation: Laboratório de Tecnologia Farmacêutica, Centro de Ciências Biológicas e da Saúde, Universidade Federal de Mato Grosso do Sul, Campo Grande, MS, Brasil.
authors.forename: Patrik Oening
authors.initials: PO
authors.lastname: Rodrigues
authors.affiliation: Laboratório de Microbiologia, Centro de Ciências Biológicas e da Saúde, Universidade Federal de Mato Grosso do Sul, Campo Grande, MS, Brasil.
authors.forename: Maria Carolina Silva
authors.initials: MC
authors.lastname: Marques
authors.affiliation: Laboratório de Biologia Molecular e Culturas Celulares, Centro de Ciências Biológicas e da Saúde, Universidade Federal de Mato Grosso do Sul, Campo Grande, MS, Brasil.
authors.forename: Maria de Fátima Cepa
authors.initials: Mde F
authors.lastname: Matos
authors.affiliation: Laboratório de Biofisiofarmacologia, Centro de Ciências Biológicas e da Saúde, Universidade Federal de Mato Grosso do Sul, Campo Grande, MS, Brasil.
authors.forename: Mônica Cristina Toffoli
authors.initials: MC
authors.lastname: Kadri
authors.affiliation: Laboratório de Farmacognosia, Centro de Ciências Biológicas e da Saúde, Universidade Federal de Mato Grosso do Sul, Campo Grande, MS, Brasil.
authors.forename: Carlos Alexandre
authors.initials: CA
authors.lastname: Carollo
authors.affiliation: Laboratório de Parasitologia Humana, Centro de Ciências Biológicas e da Saúde, Universidade Federal de Mato Grosso do Sul, Campo Grande, MS, Brasil.
authors.forename: Carla Cardozo Pinto de
authors.initials: CC
authors.lastname: Arruda
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000627:therapeutic use*; D044946:Biflavonoids / Q000302:isolation & purification / Q000627:therapeutic use*; D005260:Female; D007891:Leishmania / Q000187:drug effects* / Q000378:metabolism; D016773:Leishmaniasis, Cutaneous / Q000188:drug therapy*; D008264:Macrophages / Q000187:drug effects; D051379:Mice; D008807:Mice, Inbred BALB C; D008826:Microbial Sensitivity Tests; D041681:NIH 3T3 Cells; D009569:Nitric Oxide / Q000032:analysis; D008517:Phytotherapy; D010936:Plant Extracts / Q000627:therapeutic use*; D061251:Primary Cell Culture; D032503:Selaginellaceae / Q000737:chemistry*
chemical_list: D000981:Antiprotozoal Agents; D044946:Biflavonoids; D010936:Plant Extracts; C116328:robustaflavone; D009569:Nitric Oxide; C011164:amentoflavone