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Fine-tuning the neuroprotective and blood-brain barrier permeability profile of multi-target agents designed to prevent progressive mitochondrial dysfunction

dc.contributor.authorBenfeito S.
dc.contributor.authorOliveira C.
dc.contributor.authorFernandes C.
dc.contributor.authorCagide F.
dc.contributor.authorTeixeira J.
dc.contributor.authorAmorim R.
dc.contributor.authorGarrido J.
dc.contributor.authorMartins C.
dc.contributor.authorSarmento B.
dc.contributor.authorSilva R.
dc.contributor.authorRemião F.
dc.contributor.authorUriarte E.
dc.contributor.authorOliveira P.J.
dc.contributor.authorBorges F.
dc.date.accessioned2020-09-02T22:13:06Z
dc.date.available2020-09-02T22:13:06Z
dc.date.issued2019
dc.identifier10.1016/j.ejmech.2019.01.055
dc.identifier.citation167, , 525-545
dc.identifier.issn02235234
dc.identifier.urihttps://hdl.handle.net/20.500.12728/3730
dc.descriptionAlzheimer's disease is an irreversible, complex and progressive neurodegenerative disorder associated with oxidative stress and mitochondrial dysfunction. Exogenous antioxidants can be beneficial for decreasing oxidative stress, as they are able to reward the lack of efficacy of the endogenous defense systems and raise the overall antioxidant response in a pathological condition. Along our overarching project related with the design and development of potent and safe multi-target mitochondriotropic antioxidants, based on dietary antioxidants, novel derivatives were obtained. Overall, mitochondriotropic antioxidants showed remarkable antioxidant and chelating properties, presenting low cytotoxic effects on human differentiated neuronal (SH-SY5Y) and hepatocarcinoma (HepG2) cells and exhibited neuroprotective properties on SH-SY5Y cells against 6-hydroxydopamine (6-OHDA) or hydrogen peroxide (H2O2) oxidative insults. Moreover, compounds 58, 59, 62, 63, 66 and 67 were able to permeate a layer of hCMEC/D3 cells in a time-dependent manner. Mitochondriotropic antioxidant 67 stands out by its remarkable iron chelating and neuroprotective properties toward both H2O2 and 6-OHDA-induced oxidative damage, drug-like properties and BBB permeability. © 2019 Elsevier Masson SAS
dc.language.isoen
dc.publisherElsevier Masson SAS
dc.subjectAlzheimer's disease
dc.subjectBlood-brain barrier
dc.subjectMitochondriotropic antioxidants
dc.subjectNeuroprotection
dc.subject2 (3,4,5 trihydroxyphenyl)acetic acid
dc.subject3 (3,4 dihydroxyphenyl)propanoic acid
dc.subject3 (3,4,5trihydroxyphenyl)propanoic acid
dc.subject3,4 dihydroxyphenylacetic acid
dc.subject3,4,5 trihydroxycinnamic acid
dc.subjectacetic acid derivative
dc.subjectantioxidant
dc.subjectbromide
dc.subjectcaffeic acid
dc.subjectgallic acid
dc.subjecthydrocinnamic acid derivative
dc.subjecthydrogen peroxide
dc.subjectneuroprotective agent
dc.subjectoxidopamine
dc.subjectpropionic acid derivative
dc.subjectprotocatechuic acid
dc.subjectpyrogallol
dc.subjectreactive oxygen metabolite
dc.subjecttriton x 100
dc.subjecttrolox C
dc.subjectunclassified drug
dc.subject[10 [2 (3,4 dihydroxyphenyl)acetamide]decyl]triphenylphosphonium methanesulfonate
dc.subject[10 [2 (3,4,5 trihydroxyphenyl)acetamide]decyl]triphenylphosphonium methanesulfonate
dc.subject[10 [3 (3,4 dihydroxyphenyl)propanamide]decyl]triphenylphosphonium methanesulfonate
dc.subject[10 [3 (3,4,5 trihydroxyphenyl)propanamide]decyl]triphenylphosphonium methanesulfonate
dc.subject[6 [2 (3,4 dihydroxyphenyl)acetamide]hexyl]triphenylphosphonium methanesulfonate
dc.subject[6 [2 (3,4,5 trihydroxyphenyl)acetamide]hexyl]triphenylphosphonium methanesulfonate
dc.subject[6 [3 (3,4 dihydroxyphenyl)propanamide]hexyl]triphenylphosphonium methanesulfonate
dc.subject[6 [3 (3,4,5 trihydroxyphenyl)propanamide]hexyl]triphenylphosphonium methanesulfonate
dc.subjectantioxidant
dc.subjectneuroprotective agent
dc.subjectABTS radical scavenging assay
dc.subjectantioxidant activity
dc.subjectArticle
dc.subjectblood brain barrier
dc.subjectcell viability
dc.subjectconcentration response
dc.subjectcontrolled study
dc.subjectdisorders of mitochondrial functions
dc.subjectDPPH radical scavenging assay
dc.subjectdrug cytotoxicity
dc.subjectdrug design
dc.subjectdrug targeting
dc.subjectEC50
dc.subjecthCMEC/D3 cell line
dc.subjectHep-G2 cell line
dc.subjecthuman
dc.subjecthuman cell
dc.subjectIC50
dc.subjectiron chelation
dc.subjectlipophilicity
dc.subjectmitochondrion
dc.subjectMTT assay
dc.subjectneuropharmacology
dc.subjectneuroprotection
dc.subjectneurotoxicity
dc.subjectnucleophilicity
dc.subjectoxidation reduction potential
dc.subjectoxidative stress
dc.subjectpartition coefficient
dc.subjectresazurin assay
dc.subjectSH-SY5Y cell line
dc.subjectsubstitution reaction
dc.subjectAlzheimer disease
dc.subjectantagonists and inhibitors
dc.subjectblood brain barrier
dc.subjectcell line
dc.subjectdisorders of mitochondrial functions
dc.subjectdrug effect
dc.subjectmetabolism
dc.subjectpathology
dc.subjectpathophysiology
dc.subjectsynthesis
dc.subjecttumor cell line
dc.subjectAlzheimer Disease
dc.subjectAntioxidants
dc.subjectBlood-Brain Barrier
dc.subjectCell Line
dc.subjectCell Line, Tumor
dc.subjectHumans
dc.subjectHydrogen Peroxide
dc.subjectMitochondrial Diseases
dc.subjectNeuroprotective Agents
dc.subjectOxidative Stress
dc.subjectOxidopamine
dc.titleFine-tuning the neuroprotective and blood-brain barrier permeability profile of multi-target agents designed to prevent progressive mitochondrial dysfunction
dc.typeArticle


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