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HIV latency-reversing activity of latex from Euphorbia umbellata (Pax) Bruyns and three diterpenes isolated from this species.
das Neves, Gabrielle P; Mazzei, José L; Tostes, João B F; Nakamura, Marcos J; Rocha, Helvécio V A; Mourão, Pedro Junior P; Tanuri, Amilcar; Ribeiro da Silva, Antonio J; Siani, Antonio C.
Afiliação
  • das Neves GP; Department of Natural Products, Institute of Drug Technology, Oswaldo Cruz Foundation, Rio de Janeiro, Brazil.
  • Mazzei JL; Department of Natural Products, Institute of Drug Technology, Oswaldo Cruz Foundation, Rio de Janeiro, Brazil.
  • Tostes JBF; Department of Natural Products, Institute of Drug Technology, Oswaldo Cruz Foundation, Rio de Janeiro, Brazil.
  • Nakamura MJ; Department of Natural Products, Institute of Drug Technology, Oswaldo Cruz Foundation, Rio de Janeiro, Brazil.
  • Rocha HVA; Laboratory of Micro and Nanotecnology, Institute of Drug Technology, Oswaldo Cruz Foundation, Rio de Janeiro, RJ, Brazil.
  • Mourão PJP; Laboratory of Molecular Virology, Institute of Biology, Federal University of Rio de Janeiro, Rio de Janeiro, RJ, Brazil.
  • Tanuri A; Laboratory of Molecular Virology, Institute of Biology, Federal University of Rio de Janeiro, Rio de Janeiro, RJ, Brazil.
  • Ribeiro da Silva AJ; Natural Products Research Institute, Federal University of Rio de Janeiro, Rio de Janeiro, RJ, Brazil.
  • Siani AC; Department of Natural Products, Institute of Drug Technology, Oswaldo Cruz Foundation, Rio de Janeiro, Brazil.
Nat Prod Res ; : 1-8, 2024 Jun 20.
Article em En | MEDLINE | ID: mdl-38902957
ABSTRACT
Two unusual phorbol esters, namely 20-deoxyphorbol-3,4,12-triacetate-13-phenylacetate (1) and phorbol-3,4,12,13-tetraacetate-20-phenylacetate (2) plus ingol-3,8,12-triacetate-7-phenylacetate (3) were isolated from the latex of Euphorbia umbellata and identified by HRESIMS and 2D NMR. Compound 1 is herein described for the first time. Assignment of the phenylacetyl group at C-7 in compound 3 was suggested by the HMBC and NOESY spectra obtained in pyridine-d5. In addition to the latex and its distinct terpenoid fractions, the isolated compounds were tested as latent reversal agents against HIV-1-infected J-Lat cells, with reference to phorbol-12-myristate-13-acetate and ingenol-B. Compound 2 reverted 75-80% the viral latency on the GFP-positive cells, resulting EC50 3.70 µg/mL (SI 6.7), while 1 induced 34-40% reactivation at the same concentration range (4-20 µg/mL). The ingol derivative 3 was ineffective. Phorbol esters were confirmed as effective constituents in the latex since the fraction containing them was 2.4-fold more active than the lyophilised latex at the lowest concentration assayed.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Revista: Nat Prod Res Ano de publicação: 2024 Tipo de documento: Article País de afiliação: Brasil País de publicação: Reino Unido
Texto completo
Adicionar na Minha BVS
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XML
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Revista: Nat Prod Res Ano de publicação: 2024 Tipo de documento: Article País de afiliação: Brasil País de publicação: Reino Unido