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1.
Chem Biodivers ; : e202401207, 2024 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-39088251

RESUMO

Anxiety and epilepsy are common worldwide and represent a primary global health concern. Fisetin, a flavonoid isolated from Bauhinia pentandra, has a wide range of biological activities may be a promising alternative to combat diseases related to the central nervous system (CNS). The present study aimed to investigate the anxiolytic and anticonvulsant effects of fisetin on adult zebrafish. Furthermore, molecular docking simulations were performed to improve the results. Fisetin did not present toxicity and caused anxiolytic behavior and delayed seizures in animals. This effect may occur through serotonin neurotransmission at 5-HT3A and/or 5-HT3B receptors. Molecular docking simulations showed that fisetin interacts with the orthosteric site of the 5-HT3A receptor with strong H-bond interactions with the Trp156 residue, with a strong contribution from the catechol ring, a behavior similar to that of the antagonist co-crystallized inhibitor granisetron (CWB). Fisetin may be a promising alternative to combat diseases related to the central nervous system. Keywords anxiety • Bauhinia pentandra • Danio rerio • epilepsy • fisetin.

2.
J Biomol Struct Dyn ; 41(6): 2274-2288, 2023 04.
Artigo em Inglês | MEDLINE | ID: mdl-35067180

RESUMO

Diabetes mellitus is a chronic metabolic disorder that has been increasing drastically around the worldwide. It is important to emphasize that although many drugs are commercially available to treat diabetes, many of them have shown a number of adverse effects. Therefore, search for new antidiabetic agents is of great interest, and natural products, especially those obtained from plants sources, may be an alternative to available drugs. This study reports the in vivo and in silico evaluation of the hypoglycemic activity of fisetinidol. The conformational analysis confirmed that the fisetinidol compound possesses two valleys in the potential energy curve, showing a stable conformer on the global minimum of the PES defined by the dihedral angle θ (C6-C7-O-H) at 179.9°, whose energy is equal to zero. In addition, fisetinidol has shown promise in glycemic control and oxidative stress caused by hyperglycemia induced by high sucrose concentration, causing hypoglycemic and hepatoprotective effects in adult zebrafish. ADMET studies showed that fisetinidol has high passive permeability, low clearance and low toxic risk by ingestion, and computational studies demonstrated that fisetinidol complexes in the same region as metformin and α-acarbose, which constitutes a strong indication that fisetinidol has the same inhibitory mechanisms of α-acarbose and metformin.Communicated by Ramaswamy H. Sarma.


Assuntos
Bauhinia , Diabetes Mellitus , Metformina , Animais , Hipoglicemiantes/farmacologia , Hipoglicemiantes/uso terapêutico , Peixe-Zebra , Acarbose , Metformina/uso terapêutico , Diabetes Mellitus/tratamento farmacológico
3.
Nat Prod Res ; 36(6): 1604-1609, 2022 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-33586542

RESUMO

Phytochemical investigation of the stems of B. pulchella led to the isolation of the known compounds identified as a mixture of taraxerone (1) and ß-amirenone (2), a mixture of sitosterol (3) and stigmasterol (4), 2-hydroxy-3,5-dimethoxybibenzyl (5), 3',4'-dihydroxyphenyl-chroman-7-ol (6), fisetinidol (7), epicatechin (8), guibourtinidol (9), vanillic acid (10), 6'-O-vanilloylisotachioside (11) and 6'-O-syringoylisotachioside (12). The structures of these compounds were elucidated on the basis of their NMR spectroscopic data. The antioxidant activity of compound 7 has been investigated using DPPH° and ABTS°+ assays and the results showed inhibition in the both models. The compounds 6, 7 and 9 showed strong alpha-glucosidase inhibitory activities, being more active than acarbose, the positive control. In addition, all the compounds were isolated from B. pulchella for the first time, and among them, compounds 11 and 12 have not been reported previously from this genus.


Assuntos
Antioxidantes , Bauhinia , Inibidores de Glicosídeo Hidrolases , Antioxidantes/química , Antioxidantes/farmacologia , Bauhinia/química , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , alfa-Glucosidases
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