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1.
Chem Biodivers ; 20(7): e202300536, 2023 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-37335297

RESUMO

In this study, twelve campesterol derivatives (2-13) were prepared by esterification reaction at the hydroxy group in C-3 and catalytic hydrogenation at the carbon-carbon double bond in C-5(6). All obtained compounds were characterized by IR, 1 H-NMR, 13 C-NMR, and MS spectra. Campesterol (1) and its derivatives (2-13) were evaluated in vitro against Staphylococcus aureus (ATCC 6538), Streptococcus mutans (ATCC 0046), Escherichia coli (ATCC 10536), Pseudomonas aeruginosa (ATCC 15442), and Klebsiella pneumoniae (ATCC 10031) using the microdilution method. Among tested compounds, 4, 6, 9, 11, 12, and 13 displayed the best antibacterial activity. Moreover, to support the antibacterial activity experiments, the investigation of molecular interactions of more active compounds, and also compound 1 and neomycin, used as starting material and positive control, respectively, at the binding site of the target proteins was performed using molecular docking simulations. Four compounds (7, 9, 10 and 11) are herein described for the first time.


Assuntos
Antibacterianos , Fitosteróis , Simulação de Acoplamento Molecular , Testes de Sensibilidade Microbiana , Antibacterianos/farmacologia , Antibacterianos/química
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 ; 35(24): 6117-6121, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-33030053

RESUMO

Leishmania amazonensis is a species causative of cutaneous and anergic diffuse cutaneous leishmaniasis, treatment-resistant form, in the New World. Plants essential oils exhibit great potential as microbicide agents. We described the composition of the essential oils of two plants native from Brazil, Myrcia ovata, with geranial and neral as major constituents, and Eremanthus erythropappus, with α-bisabolol. In vitro effects of these essential oils on L. amazonensis promastigotes growth and ultrastructure were analysed as well as their cytotoxicity to murine macrophages. Both oils were highly active with IC50/96 h of 8.69 and 9.53 µg/mL for M. ovata and E. erythropappus against promastigotes and caused ultrastructural alterations including mitochondrial enlargement. Cytotoxicity for murine macrophages varied with the oil concentrations. The IC50 low values of both M. ovata and E. erythropappus oils against L. amazonensis and their relative low cytotoxicity to mammal host cells support their potential use against cutaneous leishmaniasis.


Assuntos
Antiprotozoários , Asteraceae , Leishmania mexicana , Óleos Voláteis , Parasitos , Animais , Antiprotozoários/farmacologia , Camundongos , Camundongos Endogâmicos BALB C , Óleos Voláteis/farmacologia
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