ArticlePloS one2018
Prenylated phloroglucinols from Hypericum scruglii, an endemic species of Sardinia (Italy), as new dual HIV-1 inhibitors effective on HIV-1 replication.
Article in PloS one, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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19 citing papers in PubMed, 52 citations in OpenAlex.
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- Mitochondrial resilience and antioxidant defence against HIV-1: unveiling the power ofFrontiers in microbiology · 2024Article
- Promising inhibition of diabetes-related enzymes and antioxidant properties ofJournal of enzyme inhibition and medicinal chemistry · 2023Article
- HIV-1 Integrase Inhibition Activity by Spiroketals Derived fromPharmaceuticals (Basel, Switzerland) · 2023Article
- Analysis of Biochemical and Antimicrobial Properties of Bioactive Molecules ofMolecules (Basel, Switzerland) · 2023Article
- Bioactive Potential: A Pharmacognostic Definition through the Screening of FourMolecules (Basel, Switzerland) · 2022Article
- Age Assessment in Children and Adolescents by Measuring the Open Apices in Teeth: A New Sardinian Formula.Dentistry journal · 2022Article
- Extraction and Nano-Sized Delivery Systems for Phlorotannins to Improve Its Bioavailability and Bioactivity.Marine drugs · 2021Review
- In Vitro Anti-HIV-1 Reverse Transcriptase and Integrase Properties ofPlants (Basel, Switzerland) · 2021Article
- Chemical Characterization and Anti-HIV-1 Activity Assessment of Iridoids and Flavonols fromMolecules (Basel, Switzerland) · 2021Article
- An Integrated LC-ESI-MSMolecules (Basel, Switzerland) · 2020Article
- Extraction, Characterization and Incorporation ofPharmaceutics · 2020Article
- So Uncommon and so Singular, but Underexplored: An Updated Overview on Ethnobotanical Uses, Biological Properties and Phytoconstituents of Sardinian Endemic Plants.Plants (Basel, Switzerland) · 2020Review
- Structure-Activity-Relationship and Mechanistic Insights for Anti-HIV Natural Products.Molecules (Basel, Switzerland) · 2020Review
- Antitumor Potential and Phytochemical Profile of Plants from Sardinia (Italy), a Hotspot for Biodiversity in the Mediterranean Basin.Plants (Basel, Switzerland) · 2019Article
- Cytotoxic Xanthones fromMolecules (Basel, Switzerland) · 2019Article
- Article
- Is the third molar maturity index (IInternational journal of legal medicine · 2018Article
Corrections and comments
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Authors and funding
13 authors at 4 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
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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