Hypoglycemic and hepatoprotective effects in adult zebrafish (Danio rerio) of fisetinidol isolated from Bauhinia pentandra: In vivo and in silico assays.

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.

Hydrogel and membrane scaffold formulations of Frutalin (breadfruit lectin) within a polysaccharide galactomannan matrix have potential for wound healing.

Plant lectins are carbohydrate-binding proteins, which can interact with cell surfaces to initiate anti-inflammatory pathways, as well as immunomodulatory functions. Here, we have extracted, purified and part-characterized the bioactivity of Jacalin, Frutalin, DAL and PNA, before evaluating their potential for wound healing in cultured human skin fibroblasts. Only Frutalin stimulated fibroblast migration in vitro, prompting further studies which established its low cytotoxicity and interaction with TLR4 receptors. Frutalin also increased p-ERK expression and stimulated IL-6 secretion. The in vivo potential of Frutalin for wound healing was then assessed in hybrid combination with the polysaccharide galactomannan, purified from Caesalpinia pulcherrima seeds, using both hydrogel and membrane scaffolds formulations. Physical-chemical characterization of the hybrid showed that lectin-galactomannan interactions increased the pseudoplastic behaviour of solutions, reducing viscosity and increasing Frutalin's concentration. Furthermore, infrared spectroscopy revealed -OH band displacement, likely caused by interaction of Frutalin with galactose residues present on galactomannan chains, while average membrane porosity was 100 µm, sufficient to ensure water vapor permeability. Accelerated angiogenesis and increased fibroblast and keratinocyte proliferation were observed with the optimal hybrid recovering the lesioned area after 11 days. Our findings indicate Frutalin as a biomolecule with potential for tissue repair, regeneration and chronic wound healing.

Cross-linked coacervates of cashew gum and gelatin in the encapsulation of pequi oil / Coacervados reticulados de goma de cajueiro e gelatina no encapsulamento de óleo de pequi

Pequi oil is rich in bioactive compounds which can be encapsulated to increase protection against extrinsic environmental factors. A delayed degradation of pequi oil may occur by using microencapsulation technology, in addition to masking unpleasant flavors and aromas. Complex coacervation is a technique based on the electrostatic interaction between two oppositely charged biopolymers which form a matrix complexed around an agent of interest. However, cross-linking the particles is often necessary in order to make them more rigid. The objective of this research was to produce and characterize pequi oil microparticles in a cashew gum (CG) and gelatin (GE) matrix cross-linked with tannic acid. Cross-linked pequi oil microparticles were produced by varying the concentrations of biopolymers (0.5% to 1.5%) and tannic acid (0.3% to 8.1%) using a rotational central compound design. Ratio of cashew gum, gelatin and oil was 2:1:1 (m/m/m);respectively, at pH 4.5. The cross-linking process was performed with tannic acid for 30 minutes at 40 °C. The optimized formulation by means of the rotational central compound design for microparticle formation was 0.65% biopolymers (CG and GE) and 6.9% tannic acid. Increasing the tannic acid percentage in the cross-linking of the pequi oil particles had a higher yield and encapsulation efficiency. Cross-linking provided an increase in the degradation temperature of material; and consequently, improved the thermal stability of the particles. The cross-linking process was advantageous in producing the microparticles.(AU)

O óleo de pequi é rico em compostos bioativos, os quais podem ser encapsulados para aumentar a proteção a fatores extrínsecos. A tecnologia de microencapsulamento, além de retardar a degradação do composto ativo, possibilita mascarar aromas e sabores indesejáveis. A coacervação complexa é uma técnica baseada na interação eletrostática entre dois biopolímeros com cargas opostas, que formam uma matriz complexada ao redor do agente de interesse. Entretanto, muitas vezes, se faz necessário o uso da reticulação para tornar as partículas mais rígidas. O objetivo deste trabalho foi produzir e caracterizar micropartículas de óleo de pequi em matriz de goma de cajueiro (GC) e gelatina (GE) reticulada com ácido tânico. As micropartículas de óleo de pequi reticuladas foram produzidas variando as concentrações de biopolímeros (0,5% a 1,5% m/v) e do ácido tânico, em relação à massa de biopolímeros (0,3% a 8,1% m/m), a partir de um delineamento de composto central rotacional. A proporção de GC, GE e óleo foi de 2:1:1 (m/m/m), respectivamente, em pH 4,5. O processo de reticulação foi realizado com ácido tânico por 30 minutos a 40 ºC. A formulação otimizada foi de 0,65% (m/v) de biopolímeros (GC e GE) e 6,9% (m/m) de ácido tânico. O aumento do percentual de ácido tânico na reticulação das partículas de óleo de pequi conferiu maior rendimento e eficiência de encapsulamento. A reticulação proporcionou aumento na temperatura de degradação do material, e consequente estabilidade térmica das partículas. O processo de reticulação foi vantajoso para a produção das micropartículas.(AU)

Cross-linked coacervates of cashew gum and gelatin in the encapsulation of pequi oil / Coacervados reticulados de goma de cajueiro e gelatina no encapsulamento de óleo de pequi

Pequi oil is rich in bioactive compounds which can be encapsulated to increase protection against extrinsic environmental factors. A delayed degradation of pequi oil may occur by using microencapsulation technology, in addition to masking unpleasant flavors and aromas. Complex coacervation is a technique based on the electrostatic interaction between two oppositely charged biopolymers which form a matrix complexed around an agent of interest. However, cross-linking the particles is often necessary in order to make them more rigid. The objective of this research was to produce and characterize pequi oil microparticles in a cashew gum (CG) and gelatin (GE) matrix cross-linked with tannic acid. Cross-linked pequi oil microparticles were produced by varying the concentrations of biopolymers (0.5% to 1.5%) and tannic acid (0.3% to 8.1%) using a rotational central compound design. Ratio of cashew gum, gelatin and oil was 2:1:1 (m/m/m);respectively, at pH 4.5. The cross-linking process was performed with tannic acid for 30 minutes at 40 °C. The optimized formulation by means of the rotational central compound design for microparticle formation was 0.65% biopolymers (CG and GE) and 6.9% tannic acid. Increasing the tannic acid percentage in the cross-linking of the pequi oil particles had a higher yield and encapsulation efficiency. Cross-linking provided an increase in the degradation temperature of material; and consequently, improved the thermal stability of the particles. The cross-linking process was advantageous in producing the microparticles.

O óleo de pequi é rico em compostos bioativos, os quais podem ser encapsulados para aumentar a proteção a fatores extrínsecos. A tecnologia de microencapsulamento, além de retardar a degradação do composto ativo, possibilita mascarar aromas e sabores indesejáveis. A coacervação complexa é uma técnica baseada na interação eletrostática entre dois biopolímeros com cargas opostas, que formam uma matriz complexada ao redor do agente de interesse. Entretanto, muitas vezes, se faz necessário o uso da reticulação para tornar as partículas mais rígidas. O objetivo deste trabalho foi produzir e caracterizar micropartículas de óleo de pequi em matriz de goma de cajueiro (GC) e gelatina (GE) reticulada com ácido tânico. As micropartículas de óleo de pequi reticuladas foram produzidas variando as concentrações de biopolímeros (0,5% a 1,5% m/v) e do ácido tânico, em relação à massa de biopolímeros (0,3% a 8,1% m/m), a partir de um delineamento de composto central rotacional. A proporção de GC, GE e óleo foi de 2:1:1 (m/m/m), respectivamente, em pH 4,5. O processo de reticulação foi realizado com ácido tânico por 30 minutos a 40 ºC. A formulação otimizada foi de 0,65% (m/v) de biopolímeros (GC e GE) e 6,9% (m/m) de ácido tânico. O aumento do percentual de ácido tânico na reticulação das partículas de óleo de pequi conferiu maior rendimento e eficiência de encapsulamento. A reticulação proporcionou aumento na temperatura de degradação do material, e consequente estabilidade térmica das partículas. O processo de reticulação foi vantajoso para a produção das micropartículas.