RESUMO
Phyllanthus emblica Linn. (PE) fresh fruits contain high concentrations of polyphenolics, of which free and bound phenolics are rich in biological activities. In this study, the inhibitory activity and mechanism of PEFP and PEBP on α-glucosidase (α-GLU) were investigated using spectroscopic techniques, kinetic analysis, and molecular docking. The results showed that 13 PEFP and 12 PEBP were identified by UPLC-MS/MS analysis, and Bis-HHDP-hexose and castalagin (vesgalagin) were found for the first time in PE fresh fruits. Kinetic analysis of enzyme inhibition showed that a mixture of free and bound phenolics inhibited α-GLU, and the effect of the conformational relationship of PEFP and PEBP with α-GLU on hypoglycemia was further explored by fluorescence quenching, circular dichroism (CD) spectroscopy, and molecular docking analysis. The findings demonstrated the inhibitory activity and mechanism of free and bound phenolics on α-GLU and provided a theoretical basis for PE polyphenolics as α-GLU inhibitors for hypoglycemia.
Assuntos
Frutas , Inibidores de Glicosídeo Hidrolases , Fenóis , Phyllanthus emblica , Extratos Vegetais , alfa-Glucosidases , alfa-Glucosidases/química , alfa-Glucosidases/metabolismo , Dicroísmo Circular , Frutas/química , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Cinética , Simulação de Acoplamento Molecular , Fenóis/química , Fenóis/farmacologia , Phyllanthus emblica/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Polifenóis/química , Polifenóis/farmacologia , Espectrometria de Massas em TandemRESUMO
In this work, a zein-tamarind seed polysaccharide (TSP) co-delivery system was fabricated using an anti-solvent precipitation method. The formation mechanism, characterization, and effect on alleviating colitis and gut microbiota dysbiosis in mice of zein-TSP-curcumin (Z/T-Cur) nanocomplexes were investigated. Hydrogen bonding and the hydrophobic effect played a key role in the formation of Z/T-Cur nanocomplexes, and the interactions were spontaneous and driven by enthalpy. The encapsulation efficiency, loading capacity, and bioavailability increased from 60.8% (Zein-Cur) to 91.7% (Z/T-Cur1:1), from 6.1% (Zein-Cur) to 18.3% (Z/T-Cur1:1), and from 4.7% (Zein-Cur) to 20.0% (Z/T-Cur1:1), respectively. The Z/T-Cur significantly alleviated colitis symptoms in DSS-treated mice. Additionally, the prepared nanocomplexes rebalanced the gut microbiota composition of colitis mice by increasing the abundance of Akkermansia. Odoribacter and Monoglobus were rich in the Z-T-Cur treatment group, and Turicibacter and Bifidobacterium were rich in the zein-TSP treatment group. This study demonstrated that the TSP could be helpful in the targeted drug delivery system.