Browsing by Author "Shiraishi, Carlos Seiti Hurtado"
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- Evaluation of berberine nanoparticles as a strategy to modulate acetylcholinesterase activityPublication . Leimann, Fernanda Vitória; Souza, Luma Borges de; Oliveira, Byanca Pereira Moreira de; Rossi, Bruna Franzon; Silva, Patricia Sabino da; Shiraishi, Carlos Seiti Hurtado; Kaplum, Vanessa; Abreu, Rui M.V.; Pereira, Carla; Barros, Lillian; Peron, Ana Paula; Ineu, Rafael Porto; Oechsler, Bruno Francisco; Sayer, Claudia; Araujo, Pedro Henrique Hermes de; Gonçalves, Odinei Hess; Shiraishi, Carlos S.H.Researchers have concentrated efforts in the search for natural-based reversible inhibitors for cholinesterase enzymes as they may play a key role in the treatment of degenerative diseases. Diverse plant alkaloids can inhibit the action of acetylcholinesterase and, among them, berberine is a promising bioactive. However, berberine has poor water solubility and low bioavailability, which makes it difficult to use in treatment. The solid dispersion technique can improve the water affinity of hydrophobic substances, but berberine solid dispersions have not been extensively studied. Safety testing is also essential to ensure that the berberine-loaded solid dispersions are safe for use. This study investigated the effectiveness of berberine-loaded solid dispersions (SD) as inhibitors of acetylcholinesterase enzyme (AChE). Docking simulation was used to investigate the influence of berberine on AChE, and in vitro assays were conducted to confirm the enzymatic kinetics of AChE in the presence of berberine. Berberine SD also showed improved cytotoxic effects on tumoral cells when dispersed in aqueous media. In vivo assays using Allium cepa were implemented, and no cytotoxicity/genotoxicity was found for the berberine solid dispersion. These results suggest that berberine SD could be a significant step towards safe nanostructures for use in the treatment of neurodegenerative diseases.
- Fig leaves (Ficus carica L.): source of bioactive ingredients for industrial valorizationPublication . Shiraishi, Carlos Seiti Hurtado; Zbiss, Yosra; Roriz, Custódio Lobo; Dias, Maria Inês; Prieto Lage, Miguel A.; Calhelha, Ricardo C.; Alves, Maria José; Heleno, Sandrina A.; Mendes, Vasco da Cunha; Carocho, Márcio; Abreu, Rui M.V.; Barros, LillianThe fig tree (Ficus carica L.) was one of the first domesticated trees. In 2019, the world's fig fruit production was estimated at 1153 tons. However, fig leaves are not utilized, resulting in copious quantities of bio-waste. To identify promising fig tree varieties, hydroethanolic extracts were prepared from the leaves of five fig tree varieties (Pasteliere-PA, Longue d'Aout-LA, Dauphinie-DA, Boujassote Noire-BN, and Marseille-MA). The variety with the highest concentration of organic acids was BN (146.5 mg/g dw), while glucose, fructose, and sucrose were the predominant sugars across all varieties. All extracts present alpha-tocopherol as the prevalent tocopherol isoform (above 78%), while PUFA fatty acids were predominant, ranging from 53% to 71% of total fatty acids. BN showed moderate antioxidant activity (EC50 0.23 +/- 0.01 mg/mL), while the DA variety presented promising cytotoxicity against the tumor AGS and MCF-7 cell line (GI(50) 158 +/- 13 and 223 +/- 21 mu g/mL) and especially in the inhibition of Nitric Oxide Production evaluation (IC50 20 +/- 5 mu g/mL). The DA activities are probably related to high concentrations of flavonoids, specifically the predominant apigenin-C-hexoside-C-pentoside and quercetin-O-deoxyhexosyl-hexoside. Finally, the BN and DA varieties showed good antimicrobial activity, especially against Yersinia enterocolitica. Fig leaves can be considered sustainable sources of industrially valuable bioactive molecules, and several potential applications were highlighted.