Computational pharmacokinetics and in vitro-in vivo correlation of anti-diabetic synergistic phyto-composite blend

Despite tremendous strides in modern medicine stringent control over insulin resistance or restoration of normoglycemia has not yet been achieved.With the growth of molecular biology,omics technologies,docking studies,and in silico pharmacology,modulators of enzymes and receptors affecting the molecular pathogenesis of the disease are being considered as the latest targets for anti-diabetic therapy.Therapeutic molecular targets are now being developed basing on the up or down regulation of different signaling pathways affecting the disease.Phytosynergistic antidiabetic therapy is in vogue both with classical and non-classical medicinal systems.However its chemoprofiling,structural and pharmacokinetic validation awaits providing recognition to such formulations for international acceptance.Translational health research with its focus on benchside product development and its sequential transition to patient bedside puts the pharma RDs to a challenge to develop bio-waiver protocols.Pharmacokinetic simulation models and establishment of in vitro-in vivo correlation can help to replace in vivo bioavailability studies and provide means of quality control for scale up and post approval modification.Thisreview attempts to bring different shades highlighting phyto-synergy,molecular targeting of antidiabetic agents via different signaling pathways and bio-waiver studies under a single umbrella.

Phenolic profile and biological potential of Endopleura uchi extracts

Objective:To improve the knowledge on the metabolite composition of Endopleura uchi bark,concerning phenolic compounds,and to evaluate some of its biological capacities for further possible exploitation in food and pharmaceutical industries associated to their healthpromoting qualities.Methods:Two different extracts(infusion and hydroethanolic) were studied concerning phenolic composition and biological potential.Results:Five compounds were determined by HPLC-DAD,being bergenin the major one.In general way,infusion presents a greater richness in these metabolites.The antioxidant,acetylcholinesterase.butyrylcholinesterase,α-glucosidase and antibacterial activity were checked by in vitro assays.A dose-dependent response was noticed against DPPH,superoxide and nitric oxide radicals,acetylcholinesterase,butyrylcholinesterase and against α-glucosidase inhibitory assay.Antibacterial capacity of both extracts was investigated against Gram-positive and Gramnegative bacteria,being more effective against the first one.The concentrations of infusion extract tested here revealed that is non-toxic for intestinal(Caco-2) cells line.Conclusions:The results suggest that the extracts of Endopleura uchi may be interesting for incorporating in pharmaceutical preparations for human health,since it can suppress hyperglycaemia and inhibit cholinesteases,and or as food additive due to its antiradical and antibacterial activities.