Evidence map›Paper›PMID 33467709›Full record

ArticleBiomolecules2021

Derivatives of Tenuazonic Acid as Potential New Multi-Target Anti-Alzheimer's Disease Agents.

Viviana Poliseno, Sílvia Chaves, Leonardo Brunetti, Fulvio Loiodice, Antonio Carrieri, Antonio Laghezza, Paolo Tortorella, João D Magalhães, Sandra M Cardoso, M Amélia Santos and 1 more

Abstract read
In one paragraph

Article in Biomolecules, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.

0numbers the graph read from it
0cells of the map it votes in
13citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

13 citing papers in PubMed.

  1. Review
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  12. Entomotoxic Activity of the Extracts from the Fungus,Journal of fungi (Basel, Switzerland) · 2021
    Article
  13. Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

11 authors.

Viviana PolisenoDepartment of Pharmacy and Pharmaceutical Sciences, University of Bari "A. Moro", via E. Orabona 4, 70125 Bari, Italy.ORCID 0000-0002-6010-2098
Sílvia ChavesCentro de Química Estrutural and Departamento de Engenharia Química, Instituto Superior Técnico, Universidade de Lisboa, Av. Rovisco Pais, 1049-001 Lisboa, Portugal.
Leonardo BrunettiDepartment of Pharmacy and Pharmaceutical Sciences, University of Bari "A. Moro", via E. Orabona 4, 70125 Bari, Italy.ORCID 0000-0002-7787-6639
Fulvio LoiodiceDepartment of Pharmacy and Pharmaceutical Sciences, University of Bari "A. Moro", via E. Orabona 4, 70125 Bari, Italy.
Antonio CarrieriDepartment of Pharmacy and Pharmaceutical Sciences, University of Bari "A. Moro", via E. Orabona 4, 70125 Bari, Italy.ORCID 0000-0002-7725-6667
Antonio LaghezzaDepartment of Pharmacy and Pharmaceutical Sciences, University of Bari "A. Moro", via E. Orabona 4, 70125 Bari, Italy.ORCID 0000-0001-6221-6155
Paolo TortorellaDepartment of Pharmacy and Pharmaceutical Sciences, University of Bari "A. Moro", via E. Orabona 4, 70125 Bari, Italy.ORCID 0000-0003-1358-7376
João D MagalhãesCNC-Center for Neuroscience and Cell Biology, University of Coimbra, 3004-504 Coimbra, Portugal.
Sandra M CardosoCNC-Center for Neuroscience and Cell Biology, University of Coimbra, 3004-504 Coimbra, Portugal.
M Amélia SantosCentro de Química Estrutural and Departamento de Engenharia Química, Instituto Superior Técnico, Universidade de Lisboa, Av. Rovisco Pais, 1049-001 Lisboa, Portugal.ORCID 0000-0002-4069-9368
Luca PiemonteseDepartment of Pharmacy and Pharmaceutical Sciences, University of Bari "A. Moro", via E. Orabona 4, 70125 Bari, Italy.ORCID 0000-0002-7980-5818

Funding

Fundação para a Ciência e Tecnologia (FCT) POCI-01-0145-FEDER-030712Portuguese Fundação para a Ciência e Tecnologia (FCT) UID/QUI/00100/2019University of Bari "Aldo Moro" Contributo ordinario di supporto alla ricerca 2017-18 (Luca Piemontese)
6 · The paper itself

Abstract

Alzheimer's disease (AD) is generally recognized as a multifactorial neurodegenerative pathology with an increasing impact on society. Tenuazonic acid (TA) is a natural compound that was recently identified as a potential multitarget ligand with anti-cholinesterase, anti-amyloidogenic and antioxidant activities. Using its structure as a chemical scaffold, we synthesized and evaluated new derivatives (1-5), including tenuazonic-donepezil (TA-DNP) hybrids (4 and 5) due to the clinical importance of the anti-AD drug donepezil. These novel compounds all achieved activity in the micromolar range towards all selected targets and demonstrated to be potentially orally absorbed. Moreover, a selected compound (1) was further investigated as a chelating agent towards copper (II), zinc (II) and iron (III) and showed good chelating ability (pFe = 16.6, pCu = 11.6, pZn = 6.0 at pH 7.4). Therefore, the TA motif can be considered an interesting building block in the search for innovative multi-functional anti-neurodegenerative drugs, as exemplified by hybrid 5, a promising non-cytotoxic lead compound adequate for the early stages of AD, and capable of ameliorating the oxidative status of SH-SY5Y human neuroblastoma cells.

Indexed as

Alzheimer DiseaseAmyloid beta-PeptidesCell Line, TumorCell SurvivalCholinesterase InhibitorsDonepezilFree Radical ScavengersHumansHydrogen-Ion ConcentrationMetalsMolecular Docking SimulationNeuroprotectionNeuroprotective AgentsProtein AggregatesSpectrophotometryTenuazonic AcidAmyloid beta-PeptidesCholinesterase InhibitorsDonepezilFree Radical ScavengersMetalsNeuroprotective AgentsProtein AggregatesTenuazonic AcidacetylcholinesteraseAlzheimer’s diseaseamyloidantioxidantdonepezilmetal chelationmultifunctional drugsneurodegenerativetenuazonic acid

Identifiers

PMID33467709
PMCPMC7830597

What OpenQuestion holds

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Registered trials

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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.