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  Prenylated phloroglucinols from Hypericum scruglii, an endemic species of Sardinia (Italy), as new dual HIV-1 inhibitors effective on HIV-1 replication

Sanna, C., Scognamiglio, M., Fiorentino, A., Corona, A., Graziani, V., Caredda, A., et al. (2018). Prenylated phloroglucinols from Hypericum scruglii, an endemic species of Sardinia (Italy), as new dual HIV-1 inhibitors effective on HIV-1 replication. PLoS One, 13(3): e0195168. doi:10.1371/journal.pone.0195168.

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http://dx.doi.org/10.1371/journal.pone.0195168 (Publisher version)
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Sanna, Cinzia, Author
Scognamiglio, Monica1, Author              
Fiorentino, Antonio, Author
Corona, Angela, Author
Graziani, Vittoria, Author
Caredda, Alessia, Author
Cortis, Pierluigi, Author
Montisci, Mariofilippo, Author
Ceresola, Elisa Rita, Author
Canducci, Filippo, Author
Poli, Ferruccio, Author
Tramontano, Enzo, Author
Esposito, Francesca, Author
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1External Organizations, ou_persistent22              

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 Abstract: In a search for new potential multitarget anti-HIV compounds from natural products, we have identified in Hypericum scruglii, an endemic and exclusive species of Sardinia (Italy), a potent plant lead. The phytochemical study of the hydroalcoholic extract obtained from its leaves led to the isolation of its most abundant secondary metabolites, belonging to different chemical classes. In particular, three phloroglucinols derivatives were identified, confirming their significance as chemotaxonomic markers of the Hypericum genus. Among them, the 3-(13-hydroxygeranyl)-1-(2'-methylbutanoyl)phloroglucinol was reported here for the first time. All six isolated compounds have been evaluated firstly for the inhibition of both Human Immunodeficiency Virus type 1 (HIV-1) Reverse Transcriptase (RT)-associated DNA Polymerase (RDDP) and Ribonuclease H (RNase H) activities, for the inhibition of HIV-1 integrase (IN) in biochemical assays, and also for their effect on viral replication. Among the isolated metabolites, three phloroglucinol derivatives and quercitrin were effective on both RT-associated RDDP and RNase H activities in biochemical assays. The same active compounds affected also HIV-1 IN strand transfer function, suggesting the involvement of the RNase H active site. Furthermore, phloroglucinols compounds, included the newly identified compound, were able to inhibit the HIV-1 replication in cell based assays.

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 Dates: 2018-03-162018-03-302018-04
 Publication Status: Published in print
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 Identifiers: Other: EXT557
DOI: 10.1371/journal.pone.0195168
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Title: PLoS One
Source Genre: Journal
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Publ. Info: San Francisco, CA : Public Library of Science
Pages: - Volume / Issue: 13 (3) Sequence Number: e0195168 Start / End Page: - Identifier: ISSN: 1932-6203
CoNE: https://pure.mpg.de/cone/journals/resource/1000000000277850