1.Intravaginal administration of metformin hydrochloride loaded cationic niosomes amalgamated with thermosensitive gel for the treatment of polycystic ovary syndrome: In vitro and in vivo studies.
Saini N1, Sodhi RK2, Bajaj L1, Pandey RS3, Jain UK1, Katare OP4, Madan J5. Colloids Surf B Biointerfaces. 2016 Apr 8;144:161-169. doi: 10.1016/j.colsurfb.2016.04.016. [Epub ahead of print]
BACKGROUND AND OBJECTIVE: Metformin hydrochloride (MTF-HCl) is extensively recommended by physicians for the treatment of polycystic ovary syndrome (PCOS). Mechanistically, MTF-HCl activates AMP-dependent kinase-α (AMPK-α) pathway to decrease the glucose production, enhances fatty acid oxidation and elevates the uptake of glucose in tissues. However, despite favourable physicochemical properties, oral administration of MTF-HCl is associated with impaired bioavailability (50-60%), lactic-acidosis and frequent dosing (500mg 2-3 times a day) in PCOS that ultimately influence the patient compliance. Therefore, in present investigation, MTF-HCl loaded unmodified and cationic small unilamellar niosomes were separately amalgamated with thermosensitive gel (MTF-HCl-SUNs-Gel and MTF-HCl-C-SUNs-Gel) for the treatment of PCOS through vaginal route of administration.
2.In vitro immunomodulatory activity and in vivo anti-inflammatory and analgesic potential with gastroprotective effect of the Mediterranean red alga Laurencia obtusa.
Lajili S1,2, Deghrigue M1, Bel Haj Amor H1, Muller CD2, Bouraoui A1. Pharm Biol. 2016 Apr 20:1-10. [Epub ahead of print]
CONTEXT: Red algae have been recognized as a rich natural source of compounds possessing interesting biological and pharmacological activities.
3.Comparing different enamel pretreatment options for resin-infiltration of natural non-cavitated carious lesions.
Abdelaziz M, Rizzini AL, Bortolotto T, Rocca GT, Feilzer AJ, Garcia-Godoy F, Krejci I. Am J Dent. 2016 Feb;29(1):3-9.
PURPOSE: To compare two different enamel pretreatments and their effect on the efficiency of penetration of a one-component adhesive into natural carious lesions.
4.Lower Protein Stability Does Not Necessarily Increase Local Dynamics.
McClelland LJ, Bowler BE. Biochemistry. 2016 Apr 22. [Epub ahead of print]
Overall protein stability is thought to have an important impact on the millisecond timescale dynamics modulating enzyme function. In order to better understand the effects of overall stability on the substructure dynamics of mitochondrial cytochrome c, we test the effect of a destabilizing L85A mutation on the kinetics and equilibrium thermodynamics of the alkaline conformational transition. The alkaline conformational transition replaces the Met80 ligand of the heme with a lysine residue from Ω-loop D, the heme crevice loop, consisting of residues 70-85. Residues 67 to 87 are the most conserved portion of the sequence of mitochondrial cytochrome c, suggesting this region is of prime importance for function. Mutations to Ω-loop D affect the stability of the heme crevice directly, modulating the pKapp of the alkaline transition. Two variants of yeast iso-1-cytochrome c, WT*/L85A and WT*/K73H/L85A, were prepared for these studies. Guanidine-HCl unfolding monitored by circular dichroism and pH titrations at 695 nm, respectively, were used to study the thermodynamics of global and local unfolding of these variants.
