Antioxidant Quercetin 3-O-Glycosylated Plant Flavonols Contribute to Transthyretin Stabilization

Ciccone, Lidia; Tonali, Nicolò; Fruchart-Gaillard, Carole; Barlettani, Lucia; Rossello, Armando; Braca, Alessandra; Orlandini, Elisabetta; Nencetti, Susanna

doi:10.3390/cryst12050638

Cited by 6 publications

(4 citation statements)

References 67 publications

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“…The competitive ANS-binding and its displacement by EPA and DHA were performed according to the procedure previously described [ 52 ]. TTR was incubated with ANS at room temperature for 15 min, in 96-well plates.…”

Section: Methodsmentioning

confidence: 99%

Omega-3 PUFAs as a Dietary Supplement in Senile Systemic Amyloidosis

et al. 2023

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Eicosapentaenoic acid (EPA; 20:5) and docosahexaenoic acid (DHA; 22:6), two omega-3 poly-unsaturated fatty acids (PUFAs), are the main components in oil derived from fish and other marine organisms. EPA and DHA are commercially available as dietary supplements and are considered to be very safe and contribute to guaranteeing human health. Studies report that PUFAs have a role in contrasting neurodegenerative processes related to amyloidogenic proteins, such as β-amyloid for AD, α-synuclein in PD, and transthyretin (TTR) in TTR amyloidosis. In this context, we investigated if EPA and DHA can interact directly with TTR, binding inside the thyroxin-binding pockets (T4BP) that contribute to the tetramer stabilization. The data obtained showed that EPA and DHA can contribute to stabilizing the TTR tetramer through interactions with T4BP.

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Section: Methodsmentioning

confidence: 99%

Omega-3 PUFAs as a Dietary Supplement in Senile Systemic Amyloidosis

et al. 2023

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“…As a preliminary explorative investigation, we set up two types of soaking experiments: low concentration of metallodrug (0.5-1 mM) and long soaking experiment (1-4 weeks) or high concentration of metallodrug (10-30 mM) and short soaking (few minutes). Promising and reproducible results have been obtained by soaking the native protein crystals [57][58][59][60] with 5 to 10 mM of metallodrug, for 5-10 minutes, at different pHs.…”

Section: Protein Crystals Soaked With Heavy Metal Ionsmentioning

confidence: 96%

Inorganic Drugs as a Tool for Protein Structure Solving and Studies on Conformational Changes

Tolbatov

Marrone

Shepard

et al. 2023

Chemistry A European J

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Inorganic drugs are capable of tight interactions with proteins through coordination towards aminoacidic residues, and this feature is recognized as a key aspect for their pharmacological action. However, the “protein metalation process” is exploitable for solving the phase problem and structural resolution. In fact, the use of inorganic drugs bearing specific metal centers and ligands capable to drive the binding towards the desired portions of the protein target could represent a very intriguing and fruitful strategy. In this context, a theoretical approach may further contribute to solve protein structures and their refinement. Here, we delineate the main features of a reliable experimental‐theoretical integrated approach, based on the use of metallodrugs, for protein structure solving.

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“…The binding of ANS (8-anilino-1-naphthalenesulfonic acid), Sigma-Aldrich (St. Louis, MO, USA) and its displacement by the three selected compounds 2a-c were studied using Human Plasma TTR (Merck Millipore, Molsheim, France) according to the protocol previously described [68,69]. Briefly, TTR (8 µM) was incubated with ANS (16 µM) at r.t. for 15 min in 96-well plates.…”

Section: Ans Competitive Binding Assaymentioning

confidence: 99%

New Hybrid Compounds Incorporating Natural Products as Multifunctional Agents against Alzheimer’s Disease

Ciccone,

Camodeca,

Tonali

et al. 2023

Pharmaceutics

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A series of new hybrid derivatives 1a–c, 2a–c, 3a–c, 4a–c, 5a–c, inspired by nature, were synthesized and studied as multifunctional agents for the treatment of Alzheimer’s disease (AD). These compounds were designed to merge together the trifluoromethyl benzyloxyaminic bioactive moiety, previously identified, with different acids available in nature. The ability of the synthesized compounds to chelate biometals, such as Cu2+, Zn2+ and Fe2+, was studied by UV–Vis spectrometer, and through a preliminary screening their antioxidant activity was evaluated by DPPH. Then, selected compounds were tested by in vitro ABTS free radical method and ex vivo rat brain TBARS assay. Compounds 2a–c, combining the strongest antioxidant and biometal chelators activities, were studied for their ability to contrast Aβ1-40 fibrillization process. Finally, starting from the promising profile obtained for compound 2a, we evaluated if it could be able to induce a positive cross-interaction between transthyretin (TTR) and Aβ in presence and in absence of Cu2+.

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Antioxidant Quercetin 3-O-Glycosylated Plant Flavonols Contribute to Transthyretin Stabilization

Cited by 6 publications

References 67 publications

Omega-3 PUFAs as a Dietary Supplement in Senile Systemic Amyloidosis

Omega-3 PUFAs as a Dietary Supplement in Senile Systemic Amyloidosis

Inorganic Drugs as a Tool for Protein Structure Solving and Studies on Conformational Changes

New Hybrid Compounds Incorporating Natural Products as Multifunctional Agents against Alzheimer’s Disease

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