Carbohydrates Commons^™

Probing Allosteric, Partial Inhibition Of Thrombin Using Novel Anticoagulants, Stephen S. Verespy Iii

Theses and Dissertations

Thrombin is the key protease that regulates hemostasis; the delicate balance between procoagulation and anticoagulation of blood. In clotting disorders, like deep vein thrombosis or pulmonary embolism, procoagulation is up-regulated, but propagation of clotting can be inhibited with drugs targeting the proteases involved, like thrombin. Such drugs however, have serious side effects (e.g., excessive bleeding) and some require monitoring during the course of treatment. The reason for these side effects is the mechanism by which the drugs’ act. The two major mechanisms are direct orthosteric and indirect allosteric inhibition, which will completely abolish the protease’s activity. Herein we sought an …

Getting To The Root Of Bacterial Hairs: What Is “S”?, Rebecca Gaddis, Samantha O'Conner, Evan Anderson, Terri Camesano, Nancy Burnham

Nancy A. Burnham

An atomic force microscope (AFM) was used to measure the steric forces of lipopolysaccharides (LPS) on the biofilm-forming bacteria, Pseudomonas aeruginosa. It is well known that LPS play a vital role in biofilm formation. These forces were characterized with a modified version of the Alexander and de Gennes (AdG) model for polymers, which is a function of equilibrium brush length, L, probe radius, R, temperature, T, separation distance, D, and an indefinite density variable, s. This last parameter was originally distinguished by de Gennes as the root spacing or mesh spacing depending upon the type of polymer adhesion; however since …

Design And Synthesis Of Novel Nucleoside Analogues: Oxidative And Reductive Approaches Toward Synthesis Of 2'-Fluoro Pyrimidine Nucleosides, Ramanjaneyulu Rayala

FIU Electronic Theses and Dissertations

Fluorinated nucleosides, especially the analogues with fluorine atom(s) in the ribose ring, have been known to exert potent biological activities. The first part of this dissertation was aimed at developing oxidative desulfurization-fluorination and reductive desulfonylation-fluorination methodologies toward the synthesis of 2'-mono and/or 2',2'-difluoro pyrimidine nucleosides from the corresponding 2'-arylthiopyrimidine precursors. Novel oxidative desulfurization-difluorination methodology was developed for the synthesis of α,α-difluorinted esters from the corresponding α-arylthio esters, wherein the arylthio group is present on a secondary internal carbon. For the reductive desulfonylation studies, cyclic voltammetry was utilized to measure the reduction potentials at which the sulfone moiety of substrates can …

Human Anatomy And Physiology Preparatory Course (1st Edition), Carlos Liachovitzky

Open Educational Resources

The overall purpose of this preparatory course textbook is to help students familiarize with some terms and some basic concepts they will find later in the Human Anatomy and Physiology I course.

The organization and functioning of the human organism generally is discussed in terms of different levels of increasing complexity, from the smallest building blocks to the entire body. This Anatomy and Physiology preparatory course covers the foundations on the chemical level, and a basic introduction to cellular level, organ level, and organ system levels. There is also an introduction to homeostasis at the beginning.

Chemoenzymatic Studies To Enhance The Chemical Space Of Natural Products, Jhong-Min Chen

Theses and Dissertations--Pharmacy

Natural products provide some of the most potent anticancer agents and offer a template for new drug design or improvement with the advantage of an enormous chemical space. The overall goal of this thesis research is to enhance the chemical space of two natural products in order to generate novel drugs with better in vivo bioactivities than the original natural products.

Polycarcin V (PV) is a gilvocarcin-type antitumor agent with similar structure and comparable bioactivity with the principle compound of this group, gilvocarcin V (GV). Modest modifications of the polyketide-derived tetracyclic core of GV had been accomplished, but the most …

Polymer Interactions With Nucleic Acids Under Various Physiological Conditions, Matthew S. Obrzut

Williams Honors College, Honors Research Projects

The goal of this project is to improve our understanding of nucleic acid interactions with cationic polymers with the theory that the polymers could protect the nucleic acids from degradation caused by biological enzymes. We seek to understand what the limitations of the cationic polymers are which, in this case, is mainly polymer-DNA compatibility. This experiment utilized peptide-dextran hybrid polymers with differing functionalizations to condense anionic nucleic acids into nanometer-sized polyplexes. Techniques of dynamic light scattering and zeta-potential were utilized to determine the particle sizes and surface charges of polyplexes.

In this experiment, dextran with a molecular weight of 20 …

Synthesis Of Carbohydrate Functionalized Dendrons For Use As Multivalent Scaffold And In Self-Assembled Structures, Namrata Jain

Electronic Thesis and Dissertation Repository

Carbohydrates are implicated in a large number of biological processes ranging from cell-cell interactions to bacterial and viral infection. Lectins are carbohydrate-binding proteins that are generally specific for certain sugars. However, typical carbohydrate–lectin interactions tend to have very low monomeric binding affinities. In many cases, the binding of saccharide ligands by protein receptors can be improved significantly through the attachment of multiple saccharide residues to a common support. Dendronized polymers constitute a class of macromolecules whose nanoscale size, rigidity, and functionality can be controlled with precision by tuning their molecular architecture. It is hypothesized that due to their large size …

Design And Synthesis Of 4-N-Alkanoyl And 4-N-Alkyl Gemcitabine Analogues Suitable For Positron Emission Tomography, Jesse E. Pulido

FIU Electronic Theses and Dissertations

Gemcitabine is a highly potent chemotherapeutic nucleoside agent used in the treatment of several cancers and solid tumors. However, it is therapeutically limitated because of toxicity to normal cells and its rapid intracellular deamination by cytidine deaminase into the inactive uracil derivative. Modification at the 4-(N) position of gemcitabine's exocyclic amine to an -amide functionality is a well reported prodrug strategy which has been that confers a resistance to intracellular deamination while also altering pharmacokinetics of the parent drug. Coupling of gemcitabine to carboxylic acids with varying terminal moieties afforded the 4-N-alkanoylgemcitabines whereas reaction of 4-N …

Carbocyclodipeptides As Modified Nucleosides: Synthesis And Anti- Hiv Activities, Bhupender S. Chhikara, M. Sudershan Rao, V. Kameshwara Rao, Anil Kumar, Karen W. Buckheit, Robert W. Buckheit Jr., Keykavous Parang

Pharmacy Faculty Articles and Research

A new class of nucleoside analogues were synthesized using cyclic dipeptides and modified 2′-deoxyfuranoribose sugars to introduce flexibility by peptides in place of common nucleoside bases and to determine their biological properties. The synthesis was carried out by coupling of a protected ribose sugar with synthesized dipeptides in the presence of hexamethyldisilazane and trimethylsilyltriflate. The final products were characterized by NMR and high-resolution MS-TOF spectroscopy. The compounds were evaluated for anti-HIV activities. 1-(4-Azido-5-(hydroxymethyl)tetrahydrofuran-2-yl)-3,6-diisopropylpiperazine-2,5-dione (compound 14) containing 3- and 6-isopropyl groups in the base and 3′-azide (EC50 = 1.96 μmol/L) was the most potent compound among all of the synthesized analogs.

Parallel Text Immersion, Daniel P. Becker Ph.D.

Daniel P. Becker

A new method of teaching foreign languages to beginning, intermediate, and advancing foreign language students is proposed involving reading out loud passages, chapters, and entire works of literature that are familiar to the student through required pre-reading in the students’ mother tongue. Testing is proposed to evaluate the success of the method.

Lipopolysaccharide Biosynthesis Without The Lipids: Substrate Recognition For Escherichia Coli Heptosyltransferasei, Daniel J. Czyzyk, Cassie Liu, Erika A. Taylor

Erika A. Taylor, Ph.D.

Heptosyltransferase I (HepI) is responsible for the transfer of l-glycero-d-manno-heptose to a 3-deoxy-α-D-oct-2-ulopyranosonic acid (Kdo) of the growing core region of lipopolysaccharide (LPS). The catalytic efficiency of HepI with the fully deacylated analogue of Escherichia coli HepI LipidA is 12-fold greater than with the fully acylated substrate, with a k(cat)/K(m) of 2.7 × 10(6) M(-1) s(-1), compared to a value of 2.2 × 10(5) M(-1) s(-1) for the Kdo(2)-LipidA substrate. Not only is this is the first demonstration that an LPS biosynthetic enzyme is catalytically enhanced by the absence of lipids, this result has significant implications for downstream enzymes that …

Signal Transduction In Bacterial Chemotaxis, Edward Heath Rowsell

Loma Linda University Electronic Theses, Dissertations & Projects

This study investigated the site of ATP utilization in the signal transduction pathway of bacterial chemotaxis and localized the point of convergence of a methylation-independent system of chemotaxis with the methylation-dependent system. The identity of the signal originating from the phosphotransferase system was investigated by substituting the fructose-inducible HPr-like protein FPr for HPr in transport and chemotaxis. In addition, a novel chemoattractant, glycerol, was identified for Salmonella typhimurium. Histidine-auxotrophic S. typhimurium strains ST23 (hisF) and ST171 (hisF cheB) were depleted for ATP. The times required for the bacteria to adapt to a step increase in serine, …

Effect Of Glucose Administration On Hamster Liver S9-Mediated Mutagenesis, Metabolism And Dna-Binding Of Benzo[A]Pyrene And Aflatoxin B1, Daniel C. Rubano

Loma Linda University Electronic Theses, Dissertations & Projects

Hamster liver S9 prepared from control animals and animals given 30% glucose in drinking water 48 h before time of sacrifice was used in studies of benzo[a]pyrene (BaP) and aflatoxin (AFB₁)-induced mutagenesis, metabolism of BaP and AFB₁, and metabolite binding to calf thymus DNA. BaP-induced mutagenesis in Salmonella typhimurium TA100 was reduced 38.5% while AFB₁-induced mutagenesis was increased 36% by S9 from glucose-treated hamsters. The reduction of [³H]BaP metabolite binding to calf thymus DNA in incubations with S9 from glucose-treated hamsters correlated with a decrease in unknown BaP metabolite-deoxyribonucleoside adducts isolated by …

Muscle Catabolism During A Protein Sparing Modified Fast As Measured By Urinary 3-Methylhistidine, Judith D. Nielsen

Loma Linda University Electronic Theses, Dissertations & Projects

The urinary excretion of 3-Methylhistidine was used as an index of muscle catabolism in four groups of obese persons receiving a Protein Sparing Modified Fast (PSMF). The composition of the supplements were as follows: Group I: 75 g protein, 25 g complex carbohydrate (starch) per day; Group II: 25 g protein, 75 g complex carbohydrate (starch) per day; Group III: 75 g protein, 25 g simple carbohydrate (glucose) per day; Group IV: 25 g protein, 75 g simple carbohydrate (glucose) per day. The PSMF lasted for seven days and a 24-hour urine sample was collected at the beginning of the …

The Duration Of The Effect Of Different Carbohydrates On Neutrophilic Phagocytosis, Judy L. Reeser

Loma Linda University Electronic Theses, Dissertations & Projects

In order to determine the duration of the effect of glucose, fructose, sucrose, honey, starch, and orange juice on neutrophilic phagocytosis, 10 subjects underwent a complete series of carbohydrate tolerance tests. Blood samples were drawn at specific time periods following ingestion of 100 grams of each carbohydrate. Blood was then analyzed for glucose and phagocytic index (the mean number of bacteria engulfed per leukocyte); a red blood cell and white blood cell count and differential white cell count were done also on about 1/2 of the samples. In addition, 7 other subjects participated in a fasting study in which no …

Some Aspects Of Carbohydrate Metabolism In The Cercariae Of Schistosoma Mansoni Sambon, 1907, A. Eugene Dunham Jr.

Loma Linda University Electronic Theses, Dissertations & Projects

Cercariac of Schistosoma mansoni were studied for glycogen utilization, uptake of glucose from solution, lactic acid production, and respiration.

Using the anthrone method of determination of carbohydrate, the amount of glycogen used by a single cercaria in 4 hours is determined as 43.2 x 10^-4 μg ± 6.6 x 10^-4 μg.

Glucose was not observed to have been used from solution under the conditions of the experiment, even in the presence of trehalose. The determinations were made by the Glucostat method.

After deproteinization and desugarization, aliquots of supernatant from cercarial suspensions were analyzed for lactic acid using p-phenylphenol …

A Review Of Drug Addiction And A Study Of Its Relation To Carbohydrate Metabolism, Eppie Chung Hartsuiker

Loma Linda University Electronic Theses, Dissertations & Projects

The specter of addiction eventually involves everyone of the community. It is a three-fold problem of socio-economic, psychological, and physiological factors. The least understood is the physiological or biochemical aspect of addiction.

It has been postulated that an upset in carbohydrate metabolism may be a biochemical cause of addiction. Several avenues were employed to investigate this possible cause of addiction.

1. A diet survey was conducted and revealed a greater consumption of refined carbohydrates, confections and alcoholic beverages in addicts.

2. Five-hour oral glucose tolerance tests were performed on 7 addicts and 12 non-addicts. These tests revealed that there were decreased glucose …

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