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In vitro toxicity of latex, its terpenoidal fractions and isolated phorbol esters from Euphorbia umbellata (Pax) Bruyns on monocytic and melanoma cells.
de Souza, Gabriela R; Mazzei, José L; Tostes, João B F; de Carvalho, Andressa de L D; Costa, Thadeu E M M; Penido, Carmen; Siani, Antonio C.
Afiliação
  • de Souza GR; Laboratory of Technology for Biodiversity in Health, Institute of Drug Technology, Oswaldo Cruz Foundation, Rua Sizenando Nabuco 100, Manguinhos, Rio de Janeiro 21041-250, RJ, Brazil.
  • Mazzei JL; Laboratory of Technology for Biodiversity in Health, Institute of Drug Technology, Oswaldo Cruz Foundation, Rua Sizenando Nabuco 100, Manguinhos, Rio de Janeiro 21041-250, RJ, Brazil.
  • Tostes JBF; Laboratory of Technology for Biodiversity in Health, Institute of Drug Technology, Oswaldo Cruz Foundation, Rua Sizenando Nabuco 100, Manguinhos, Rio de Janeiro 21041-250, RJ, Brazil.
  • de Carvalho ALD; Laboratory of Technology for Biodiversity in Health, Institute of Drug Technology, Oswaldo Cruz Foundation, Rua Sizenando Nabuco 100, Manguinhos, Rio de Janeiro 21041-250, RJ, Brazil.
  • Costa TEMM; Laboratory of Applied Pharmacology, Institute of Drug Technology, Oswaldo Cruz Foundation, Rua Sizenando Nabuco 100, Manguinhos, Rio de Janeiro 21041-250, RJ, Brazil; Center for Technological Development in Health (CDTS), Oswaldo Cruz Foundation, Rio de Janeiro, Brazil. Avenida Brasil 4036, room 814
  • Penido C; Laboratory of Applied Pharmacology, Institute of Drug Technology, Oswaldo Cruz Foundation, Rua Sizenando Nabuco 100, Manguinhos, Rio de Janeiro 21041-250, RJ, Brazil; Center for Technological Development in Health (CDTS), Oswaldo Cruz Foundation, Rio de Janeiro, Brazil. Avenida Brasil 4036, room 814
  • Siani AC; Laboratory of Technology for Biodiversity in Health, Institute of Drug Technology, Oswaldo Cruz Foundation, Rua Sizenando Nabuco 100, Manguinhos, Rio de Janeiro 21041-250, RJ, Brazil. Electronic address: antonio.siani@fiocruz.br.
Fitoterapia ; 176: 105987, 2024 Jul.
Article em En | MEDLINE | ID: mdl-38703916
ABSTRACT
In Brazil, latex from Euphorbia umbellata (African milk tree) has been increasingly used in folk medicine to treat several types of cancer, including melanoma. The effect of lyophilized latex (LL), its hydroethanolic extract (E80), triterpene (F-TRI)- and diterpene (F-DIT)-enriched fractions, along with six isolated phorbol esters from LL and phorbol 12-myristate 13-acetate (PMA) on J774A.1, THP-1, SK-MEL-28, and B16-F10 cell line viability were evaluated by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) method. The compounds were identified by 2D-NMR and HRESIMS. The effect of the LL, extract and fractions on cell viability was also assessed through a resazurin reduction assay. At 100 µg/ml, LL, and its fractions moderately inhibited J774A.1 (37.5-59.5%) and THP-1 (12.6-43.6%) metabolism. LL (IC50 70 µg/ml) and F-TRI (IC50 68 µg/ml) were barely more effective against B16-F10 cells, and only F-TRI exerted an inhibitory effect on SK-MEL-28 cells (IC50 66-75 µg/ml). The samples did not effectively inhibit THP-1 growth (IC50 69-87 µg/ml, assessed by MTT). B16-F10 was susceptible to PMA (IC50 53 µM) and two 12-phenylacetate esters (IC50 56-60 µM), while SK-MEL-28 growth was inhibited (IC50 58 µM) by one of these kinds of esters with an additional 4ß-deoxy structure. Synagrantol A (IC50 39 µM) was as effective as PMA (IC50 47 µM) in inhibiting J774A.1 growth in a dose-dependent manner. Furthermore, an in silico study with target receptors indicated a high interaction of the compounds with the PKC proteins. These results provide useful knowledge on the effect of tigliane-type diterpenes on tumor cell from the perspective of medicinal chemistry.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Ésteres de Forbol / Euphorbia / Látex Limite: Animals / Humans País/Região como assunto: America do sul / Brasil Idioma: En Revista: Fitoterapia Ano de publicação: 2024 Tipo de documento: Article País de afiliação: Brasil País de publicação: Holanda
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Ésteres de Forbol / Euphorbia / Látex Limite: Animals / Humans País/Região como assunto: America do sul / Brasil Idioma: En Revista: Fitoterapia Ano de publicação: 2024 Tipo de documento: Article País de afiliação: Brasil País de publicação: Holanda