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Dual HIV-1 reverse transcriptase and integrase inhibitors from Limonium morisianum Arrigoni, an endemic species of Sardinia (Italy).
Sanna, Cinzia; Rigano, Daniela; Corona, Angela; Piano, Dario; Formisano, Carmen; Farci, Domenica; Franzini, Genni; Ballero, Mauro; Chianese, Giuseppina; Tramontano, Enzo; Taglialatela-Scafati, Orazio; Esposito, Francesca.
Afiliación
  • Sanna C; a Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy.
  • Rigano D; b Department of Pharmacy, School of Medicine and Surgery , University of Naples Federico II , Naples , Italy.
  • Corona A; a Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy.
  • Piano D; a Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy.
  • Formisano C; b Department of Pharmacy, School of Medicine and Surgery , University of Naples Federico II , Naples , Italy.
  • Farci D; a Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy.
  • Franzini G; a Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy.
  • Ballero M; c Cosmese, Consorzio per lo Studio dei Metaboliti Secondari , University of Cagliari , Cagliari , Italy.
  • Chianese G; b Department of Pharmacy, School of Medicine and Surgery , University of Naples Federico II , Naples , Italy.
  • Tramontano E; a Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy.
  • Taglialatela-Scafati O; d Genetics and Biomedical Research Institute , National Research Council (CNR) , Cagliari , Italy.
  • Esposito F; b Department of Pharmacy, School of Medicine and Surgery , University of Naples Federico II , Naples , Italy.
Nat Prod Res ; 33(12): 1798-1803, 2019 Jun.
Article en En | MEDLINE | ID: mdl-29397771
During our search for potential templates of HIV-1 reverse transcriptase (RT) and integrase (IN) dual inhibitors, the methanolic extract obtained from aerial parts of Limonium morisianum was investigated. Repeated bioassay-guided chromatographic purifications led to the isolation of the following secondary metabolites: myricetin, myricetin 3-O-rutinoside, myricetin-3-O-(6″-O-galloyl)-ß-d-galactopyranoside, (-)-epigallocatechin 3-O-gallate, tryptamine, ferulic and phloretic acids. The isolated compounds were tested on both HIV-1 RT-associated RNase H and IN activities. Interestingly, (-)-epigallocatechin-3-O-gallate and myricetin-3-O-(6″-O-galloyl)-ß-d-galactopyranoside potently inhibited both enzyme activities with IC50 values ranging from 0.21 to 10.9 µM. Differently, tryptamine and ferulic acid exhibited a significant inhibition only on the IN strand transfer reaction, showing a selectivity for this viral enzyme. Taken together these results strongly support the potential of this plant as a valuable anti HIV-1 drugs source worthy of further investigations.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Inhibidores de Integrasa VIH / Fármacos Anti-VIH / Plumbaginaceae / Transcriptasa Inversa del VIH País/Región como asunto: Europa Idioma: En Revista: Nat Prod Res Año: 2019 Tipo del documento: Article País de afiliación: Italia Pais de publicación: Reino Unido
Texto completo
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XML
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Inhibidores de Integrasa VIH / Fármacos Anti-VIH / Plumbaginaceae / Transcriptasa Inversa del VIH País/Región como asunto: Europa Idioma: En Revista: Nat Prod Res Año: 2019 Tipo del documento: Article País de afiliación: Italia Pais de publicación: Reino Unido