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Showing 1 to 20 of 126 for “"Bioactivities"”.
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Synthesis and bioactivities of novel N¹-acylhydrazides
Curcumin, a herbal polyphenol, has demonstrated anticancer activity in vitro as well as in vivo but have limited clinical benefits due to low oral bioavailability. Structural modification such as truncation of the β-diketone moiety of curcumin led to the development of the …
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Design and Application of Probes of Novel Bioactivities
Whilst methods for the isolation and optimisation of bacterial enzymes for preparative biotransformations are well established the use of plant biocatalysts is relatively unexplored. Since the plant kingdom contains a greater diversity of potential biocatalysts this represents an untapped resource. …
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Phytoecdysteroid accumulation in plants and bioactivities in animal models
… steroidal compounds that have valued bioactivities including plant defense against herbivorous insects, and growth and performance-enhancing properties in mammals. In this program of research, phytoecdysteroid accumulation was investigated in Ajuga turkestanica (Regel) Briq., a …
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Syntheses and Bioactivities of Targeted and Conformationally Restrained Taxol Analogs
… conformation, which would result in the loss of bioactivities. It is an indirect evidence to support T-taxol conformation. As for macrocyclic taxol lactones, it is proposed that they would have a close contact between the ester moiety on the C-3' phenyl ring and Phe272 of the β-tubulin protein …
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Syntheses, bioactivities and conformations of peptidomimetics containing 2,3-methanoamino acids
Asymmetric syntheses of E- and Z-2,3-methanomethionine (ie E- and Z-cyclo-Met), protected Z-2,3-methanoarginine, and Z-2,3-methanoaspartic acid derivatives have been developed. These functionalized 2,3-methanoamino acids were prepared from a common intermediate: 1- ((tert-butoxy)carbonyl) …
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Assessment of blue whiting protein hydrolysate bioactivities using cell culture models
… at semi-pilot scale and all of the above bioactivities were reassessed in greater detail. The antioxidant and immunomodulatory activities of the six industrial-scale BWSPHs before simulated gastrointestinal digestion (SGID) (BW-SPH-A to BW-SPH-F) and after SGID (BW-SPH-A-GI to BW-SPH-F-GI) …
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Bioactivities of Antiestrogens and Antiestrogen Metabolites in the Rat and Mouse
Recent studies demonstrate that a number of the triarylethylene-type antiestrogens act as pro-drugs, being converted in vivo to metabolites having greater estrogenic and antiestrogenic potency than their parent compounds. This laboratory has revealed that two potent nonsteroidal antiestrogens,
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Studies on the Biosynthesis and Bioactivities of Nybomycin and Its Derivatives
Made available in DSpace on 2014-12-13T20:10:00Z (GMT). No. of bitstreams: 1 7709115.pdf: 9151042 bytes, checksum: 02dff9acea3fdab80cfb08256c39a1ee (MD5) Previous issue date: 1976
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Design, Syntheses, and Bioactivities of Conformationally Locked Pin1 Ground State Inhibitors
Pin1 (protein interacting with NIMA 1) is a peptidyl-prolyl isomerase involved in mitosis. As a potential anti-cancer drug target, Pin1 interacts and regulates the activity of an increasing number of cell cycle enzymes by an unknown mechanism. These cell cycle enzymes include Cdc25, Cdc27, Cyclin …
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Extractio, purification, characterization and bioactivities of polysaccharides isolated from selected Namibian mushrooms
… study is a preliminary attempt to elucidate the bioactivities of K. pfeilii and T. schimperi PS for potential application in functional food and nutraceuticals. Water and alkali PS extracts of K. pfeilii and T. schimperi were extracted and purified using Freimund’s method. The PS were chemically …
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Exploring new chemical entities from traditional medicine: Docking, synthesis and specific bioactivities
<p>Traditional medical systems contributed significantly to medicine with a number of their phytochemicals found to possess good biological properties. Recently, Dr. Youyou Tu was awarded the Nobel Prize (2015) for her discovery/isolation of Artemisinin from the TCM plant Artemisia annua. Our first …
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Syntheses and Bioactivities of Targeted and Conformationally Restrained Paclitaxel and Discodermolide Analogs
Paclitaxel was isolated from the bark of <i>Taxus brevifolia</i> in the late 1960s. It exerts its biological effect by promoting tubulin polymerization and stabilizing the resulting microtubules. Paclitaxel has become one of the most important current drugs for the treatment of breast and ovarian …
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Characterization of Mycochemicals and Bioactivities of a New Zealand Native Mushroom Hericium novae-zealandiae
… of the identified compounds. In addition, the bioactivities of the extracts and the compounds were evaluated in relation to anti-proliferation of three prostate cancer (PCa) cell lines (DU145, LNCaP, and PC3), AChE inhibition and antioxidant activities. Four nucleoside substitutes, namely …
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In vitro bioactivities of anodised titanium in mixtrue of B-Glycerophosphate and calcium acetate for biomedical application
Anodic oxidation has been widely used to modify the surface properties of titanium in order to improve the biocompatibility after implantation. In this study, high purity titanium foils were exposed in a mixture of β-glycerophosphate disodium salt pentahydrate (β-GP) and calcium acetate monohydrate …
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Design, Syntheses and Bioactivities of Androgen Receptor Targeted Taxane Analogs, Simplified Fluorescently Labeled Discodermolide Analogs, and Conformationally Constrained Discodermolide Analogs
Prostate cancer is the most common non-skin cancer for men in America. The androgen receptor exerts transcriptional activity and plays an important role for the proliferation of prostate cancer cells. Androgen receptor ligands bind the androgen receptor and inhibit its transcriptional activity …
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Synthesis and Properties of ordered Mesoporous SiO2-CaO Bioactive glasses
… surfactant templating route. The formation and bioactivities of the ordered mesoporous bioactive glasses were investigated systematically. In order to investigate the effects of the ordered mesoporous structure on bioactivities, disordered porous bioactive glasses with the same composition were …
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Natural and Synthetic Ligand-Binding Induce Different Pilin Assemblies in vitro and Control P. aeruginosa Bioactivities in vivo, and Development of Bacterial-Motility Enabled Binding Assays
… ligands of pilin that control P. aeruginosa bioactivities. </p> <p>For biochemical and structural studies on pilin protein, we used a common technique of recombinantly expressing truncated pilin in E. coli. The truncation of pilin from the N’-terminal α-helix retains the perceived binding …
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Associating adverse drug effects with protein targets by integrating adverse event, in vitro bioactivity, and pharmacokinetic data
… associations between AEs observed in humans and bioactivities of drugs while taking into account drug plasma concentrations. In the first chapter, post-marketing drug-AE associations are derived from the United States Food and Drug Administration Adverse Event Reporting System using …
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