Acetone extract of faba bean (Vicia faba L.) was found to be highest total phenol and flavonoid content among all extracts. Antioxidant activity for inhibition percentage (free radical scavenging activity) had 86.47% for acetone extract, and 97.36% for ascorbic acid respectively. IC value of ascorbic acid and acetone extact were found to be 9 μg/mL ± 0.20 and 30 μg/mL ± 0.21. Faba bean seeds had catechin, epicatechin, gallic acid and ellagic acid which on molecular docking study revealed that it binds effectively with xanthine oxidase by binding energy of -7.78, -6.11, -6.39, -5.78 kcal/mol respectively compared to allopurinol drug having binding energy of -4.94 kcal/mol. Gallic acid, ellagic acid, catechin, epicatechin (polyphenols) and allopurinol bind other than catalytic residues (Glu-1261) of xanthine oxidase. In vitro and in silico analysis recommended that mode of enzyme inhibition was mixed type.
Diabetes mellitus is a group of metabolic disorder of glucose metabolism. The proper management of blood glucose level is an indicator in the treatment of this complex pathology. The aim of the present study was to evaluate the inhibitory potential of Vicia faba crude seed extracts on the activities of a-amylase. Phytochemical screening, FTIR and HPLC analysis confirmed the presence of a phenolic compound with percentage yield of 9.87% in the acetone extract. Acetone extract of seed had highest inhibitory potential against porcine a-amylase (IC 50 value of 2.94 mg/mL). Kinetic analysis revealed that the acetone and methanol extract displayed mixed mode of inhibition toward a-amylase. In-silico analysis was agreement with in-vitro studies in which phenolic compounds (catechin, epicatechin, gallic acid, and proanthocyanidin) showed more negative free energy against standard drug (acarbose) and bound with catalytic residues of a-amylase. These results might be due to the synergistic action of constituents present in seed extract or acting separately.
AbstractHypoglycemic potential and xanthine-oxidase (XO) activity of polyphenols from faba bean were evaluated in the 3T3-L1 cell line, and an interaction study in silico with XO was performed with considerable bioactive components of acetone extract of faba beans. The protonated and fragmented behavior of acetone seed extract revealed the presence of gallic acid (MS/MS, m/z 169) and catechin (MSn, m/z 288.3). Flow cytometry study explained the effect of hydrogen peroxide (H2O2) on cell line as cell death was increased from 9.72 to 41.66% as compared to the control (without H2O2). The atomic force microscopy (AFM), scanning electron microscopy and reactive oxygen species measurement also confirmed the protective effect of polyphenols in the 3T3-L1 cell lines. Oxidative stress through propidium iodide and 4′,6-diamidino-2-phenylindole staining demonstrated that the apoptotic ratio was 0.35 ± 2.62 (P < 0.05) and 30 ± 2.54% in H2O2-treated cells, respectively, as compared to control. The observations of flow cytometry and confocal microscopy marked the effect of seed extract (0.86 ± 0.031, 3.52 ± 0.52, P < 0.05), on glucose uptake in cells through the better relative fluorescence intensity than that of the control. Moreover, molecular docking and molecular dynamics simulation studies gave an insight into the predicted residues that hold favorable polyphenolic-specific interactions. The probable binding modes of the gallic acid and catechin from this study may extend the knowledge of the XO-polyphenol interactions and offered the way to design the analogs of acetone seed extract with reduced toxicity.
Multiple drug resistance is a key limitation for the clinical administration of chemotherapeutic drugs, apart from this their major limitations with free drugs are poor solubility, physiochemical and pharmaceutical behavior. These limitations with free drugs can be overcome by nanoformulations using natural biopolymer. In this study, successful utilization of P-glycoprotein receptor for the delivery of anticancer drug quercetin (Q), encapsulated inside the lipid nanocarriers (LNs) was introduced for the treatment of breast cancer. Bovine serum albumin (BSA) was conjugated on the Q-loaded LNs( BSA-Q-LNs) for targeting to receptor. Q-loaded LNs were prepared using a single emulsion solvent evaporation method, followed by surface modification of Q-loaded LNs using charge interaction. Finally, surface modified Q-loaded LNs were conjugated with BSA using thiol reaction. The formulated nano construct was a spherical structure with a shell size of 530 nm. Encapsulation of Q inside the matrix of LNs is confirmed from shift in FT-IR, XRD peak. The release kinetic of Q-loaded LNs formulation was best fitted in a first-order kinetic model suggesting early burst of Q followed by slow release. The entrapment efficiency and drug loading efficiency were found to be 76±0.3% and 15.72±0.7% respectively. The Q-loaded LNs and BSA-Q-LNs displayed the improved cytotoxicity in drug resistance human breast cancer cell line (MCF-7) as compared to free Q.
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