title: O-naphthoquinone isolated from Capraria biflora L. induces selective cytotoxicity in tumor cell lines.
abstract: Biflorin is an o-naphthoquinone isolated from the roots of the plant Capraria biflora L. (Scrophulariaceae). In this study, the cytotoxic effects of biflorin were verified, and late apoptosis was detected in various cancer cell lines by in situ analysis. The cytotoxicity was further evaluated exclusively for 48 h of treatment in different tumor and non-tumor cell lines (Hep-2, HeLa, HT-29, A-375, and A-549, and HEK-293, respectively). The results indicated that biflorin induced selective cytotoxicity in tumor cells. HeLa cells were more susceptible to biflorin, followed by HT-29, A-549, A-375, and Hep-2 at all concentrations (range 5-50 μg/mL), and the highest half-maximal inhibitory concentration IC50 (56.01 ± 1.17 μg/mL) was observed in HEK-293 cells. Late apoptotic/necrotic events, observed by in situ immunostaining with Annexin V, varied with each cell line; an increase in late apoptotic events was observed corresponding to the increase in biflorin dosage. Hep-2 cells showed a greater percentage of late apoptotic events among the tumor cell lines when treated with higher concentrations of biflorin (69.63 ± 2.28%). The non-tumor HEK-293 line showed greater resistance to late apoptotic events, as well as a lower level of cytotoxicity (77.69 ± 6.68%) than the tested tumor lines. The data presented indicate that biflorin showed an important, possibly selective, cytotoxicity against tumor cell lines, thereby revealing a promising novel substance with potential anticancer activity for tumor therapy.
authors.affiliation: Laboratório de Genômica, Proteômica e Reparo de DNA, Universidade de Caxias do Sul, RS, Brasil.
authors.forename: G G N
authors.initials: GG
authors.lastname: de S Wisintainer
authors.affiliation: University of Toronto and Centre for Addiciton and Mental Health, ON, Canada.
authors.forename: G
authors.initials: G
authors.lastname: Scola
authors.affiliation: Laboratório de Biotecnologia de Produtos Naturais e Sintéticos, Universidade de Caxias do Sul, RS, Brasil.
authors.forename: S
authors.initials: S
authors.lastname: Moura
authors.affiliation: Departamento de Química Orgânica e Inorgânica da Universidade Federal do Ceará, Fortaleza, CE, Brasil.
authors.forename: T L G
authors.initials: TL
authors.lastname: Lemos
authors.affiliation: Laboratório de Oncologia Experimental, Departamento de Fisiologia e Farmacologia, Faculdade de Medicina, Universidade Federal do Ceará, Fortaleza, CE, Brasil.|Fundação Oswaldo Cruz-Ceará, Fortaleza, CE, Brasil.
authors.forename: C
authors.initials: C
authors.lastname: Pessoa
authors.affiliation: Laboratório de Oncologia Experimental, Departamento de Fisiologia e Farmacologia, Faculdade de Medicina, Universidade Federal do Ceará, Fortaleza, CE, Brasil.
authors.forename: M O
authors.initials: MO
authors.lastname: de Moraes
authors.affiliation: Departamento de Química Orgânica e Inorgânica da Universidade Federal do Ceará, Fortaleza, CE, Brasil.
authors.forename: L G S
authors.initials: LG
authors.lastname: Souza
authors.affiliation: Laboratório de Genômica, Proteômica e Reparo de DNA, Universidade de Caxias do Sul, RS, Brasil.
authors.forename: M
authors.initials: M
authors.lastname: Roesch-Ely
authors.affiliation: Laboratório de Genômica, Proteômica e Reparo de DNA, Universidade de Caxias do Sul, RS, Brasil.
authors.forename: J A P
authors.initials: JA
authors.lastname: Henriques
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage* / Q000737:chemistry; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D057809:HEK293 Cells; D006801:Humans; D009285:Naphthoquinones / Q000008:administration & dosage* / Q000737:chemistry; D009369:Neoplasms / Q000188:drug therapy* / Q000473:pathology; D028083:Scrophulariaceae / Q000737:chemistry
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D009285:Naphthoquinones; C040756:1,2-naphthoquinone