School Of Basic And Applied Sciences

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    Role of Macromolecular Crowding on Stability and Iron Release Kinetics of Serum Transferrin
    (American Chemical Society, 2017) Kumar, Sandeep; Sharma, Deepak; Kumar, Rajesh
    The macromolecular crowding influences the structural stability and functional properties of transferrin (Tf). The equilibrium as well as kinetic studies of Tf at different concentrations of crowding agents (dextran 40, dextran 70, and ficoll 70) and at a fixed concentration of dextran 40 under different concentrations of NaCl at pH 7.4 and 5.6 (?1) revealed that (i) the crowder environment increases the diferric-Tf (Fe2Tf) stability against iron loss and overall denaturation of the protein, (ii) both in the absence and presence of crowder, the presence of salt promotes the loss of iron and overall denaturation of Fe2Tf which is due to ionic screening of electrostatic interactions, (iii) the crowder environment retards iron release from monoferric N-lobe of Tf (FeNTf) by increasing enthalpic barrier, (iv) the retardation of iron release by crowding is enthalpically dominated than the entropic one, (v) both in the absence and presence of crowder, the presence of salt accelerates the iron release from FeNTf due to ionic screening of electrostatic interactions and anion binding to KISAB sites, and (vi) the crowders environment is unable to diminish (a) the salt-induced destabilization of Fe2Tf against the loss of iron and overall denaturation and (b) the anion effect and ionic screening of diffusive counterions responsible to promote iron release from FeNTf. ? 2017 American Chemical Society.
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    A microRNA switch regulates the rise in hypothalamic GnRH production before puberty
    (Nature Publishing Group, 2016) Messina, Andrea; Langlet, Fanny; Chachlaki, Konstantina; Roa, Juan; Rasika, Sowmyalakshmi; Jouy, Nathalie; Gallet, Sarah; Gaytan, Francisco; Parkash, Jyoti; Tena-Sempere, Manuel; Giacobini, Paolo; Prevot, Vincent; Messina, A.; Langlet, F.; Chachlaki, K.; Roa, J.; Rasika, S.; Jouy, N.; Gallet, S.; Gaytan, F.; Parkash, J.; Tena-Sempere, M.; Giacobini, P.; Prevot, V.
    A sparse population of a few hundred primarily hypothalamic neurons forms the hub of a complex neuroglial network that controls reproduction in mammals by secreting the 'master molecule' gonadotropin-releasing hormone (GnRH). Timely postnatal changes in GnRH expression are essential for puberty and adult fertility. Here we report that a multilayered microRNA-operated switch with built-in feedback governs increased GnRH expression during the infantile-to-juvenile transition and that impairing microRNA synthesis in GnRH neurons leads to hypogonadotropic hypogonadism and infertility in mice. Two essential components of this switch, miR-200 and miR-155, respectively regulate Zeb1, a repressor of Gnrh transcriptional activators and Gnrh itself, and Cebpb, a nitric oxide-mediated repressor of Gnrh that acts both directly and through Zeb1, in GnRH neurons. This alteration in the delicate balance between inductive and repressive signals induces the normal GnRH-fuelled run-up to correct puberty initiation, and interfering with this process disrupts the neuroendocrine control of reproduction. ? 2016 Nature Publishing Group. All rights reserved.
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    Pyrazoloquinazolines: Synthetic strategies and bioactivities
    (2015) Garg, Mansi; Chauhan, Monika; Singh, Pankaj Kumar; Singh, Pankaj Kumar; Alex, Jimi Marin; Kumar, Raj
    Numerous N-heterocycles are indisputably evidenced to exhibit myriad biological activities. In the recent past, attempts made to condense the various heterocycles have resulted in derivatives possessing better bioactivities. Among many such condensed heterocycles, pyrazoloquinazolines have managed to hold the attention of many researchers, owing to the broad spectrum of activities they portray. This review is the first of its kind to congregate the various pyrazoloquinazolines reported until now and categorizes these structurally isomeric classes into eleven different groups based on the fusion pattern of the ring such as [1,5-c], [5,1-b], [4,3-h], etc. Furthermore, this review is a concerted effort to highlight design, synthetic strategies as well as biological activities of each class of this condensed heterocycle. Structure-activity relationship studies and in silico approaches wherever reported have also been discussed. In addition, manuscript also offers scope for design, synthesis and generation of libraries of unreported classes of pyrazoloquinazolines for the biological evaluation. Copyright ? 2014 Elsevier Masson SAS. All rights reserved.
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    Chemical composition and biological effects of artemisia maritima and artemisia nilagirica essential oils from wild plants of Western Himalaya
    (Georg Thieme Verlag, 2014) Stappen, Iris; Wanner, J, rgen; Tabanca, Nurhayat; Wedge, David E.; Ali, Abbas; Khan, Ikhlas A.; Kaul, Vijay K.; Lal, Brij; Jaitak, Vikas; Gochev, Velizar; Girova, Tania; Stoyanova, Albena; Schmidt, Erich; Jirovetz, Leopold; Stappen, I.; Wanner, J.; Tabanca, N.; Wedge, D.E.; Ali, A.; Khan, I.A.; Kaul, V.K.; Lal, B.; Jaitak, V.; Gochev, V.; Girova, T.; Stoyanova, A.; Schmidt, E.; Jirovetz, L.
    Artemisia species possess pharmacological properties that are used for medical purposes worldwide. In this paper, the essential oils from the aerial parts of Artemisia nilagirica and Artemisia maritima from the western Indian Himalaya region are described. The main compounds analyzed by simultaneous GC/MS and GC/FID were camphor and 1,8-cineole from A. maritima, and camphor and artemisia ketone from A. nilagirica. Additionally, the oils were evaluated for their antibacterial, antifungal, mosquito biting deterrent, and larvicidal activities. A. nilagirica essential oil demonstrated nonselective antifungal activity against plant pathogens Colletotrichum acutatum, Colletotrichum fragariae, and Colletotrichum gloeosporioides, whereas A. maritima did not show antifungal activity. Both Artemisia spp. exhibited considerable mosquito biting deterrence, whereas only A. nilagirica showed larvicidal activity against Aedes aegypti. Antibacterial effects assessed by an agar dilution assay demonstrated greater activity of A. maritima essential oil against Staphylococcus aureus and Pseudomonas aeruginosa compared to A. nilagirica.