Open Access. Powered by Scholars. Published by Universities.®

Chemistry Commons

Open Access. Powered by Scholars. Published by Universities.®

Cleveland State University

Discipline
Keyword
Publication Year
Publication
Publication Type
File Type

Articles 121 - 150 of 397

Full-Text Articles in Chemistry

Sialyltransferase Inhibition And Recent Advances, Libo Wang, Ying Liu, Lijun Wu, Xue-Long Sun Jan 2016

Sialyltransferase Inhibition And Recent Advances, Libo Wang, Ying Liu, Lijun Wu, Xue-Long Sun

Chemistry Faculty Publications

Sialic acids, existing as terminal sugars of glycoconjugates, play important roles in various physiological and pathological processes, such as cell–cell adhesion, immune defense, tumor cell metastasis, and inflammation. Sialyltransferases (STs) catalyze the transfer of sialic acid residues to non-reducing oligosaccharide chains of proteins and lipids, using cytidine monophosphate N-acetylneuraminic acid (CMP-Neu5Ac) as the donor. Elevated sialyltransferase activity leads to overexpression of cell surface sialic acids and contributes to many disease developments, such as cancer and inflammation. Therefore, sialyltransferases are considered as potential drug targets for disease treatment. Inhibitors of sialyltransferases thus are of medicinal interest, especially for the cancer …


Multi-Dimensional Glycan Microarrays With Glyco-Macroligands, Satya Nandana Narla, Huan Nie, Yu Li, Xue-Long Sun Oct 2015

Multi-Dimensional Glycan Microarrays With Glyco-Macroligands, Satya Nandana Narla, Huan Nie, Yu Li, Xue-Long Sun

Chemistry Faculty Publications

Glycan microarray has become a powerful high-throughput tool for examining binding interactions of carbohydrates with the carbohydrate binding biomolecules like proteins, enzymes, antibodies etc. It has shown great potential for biomedical research and applications, such as antibody detection and profiling, vaccine development, biomarker discovery, and drug screening. Most glycan microarrays were made with monovalent glycans immobilized directly onto the array surface via either covalent or non-covalent bond, which afford a multivalent glycans in two dimensional (2D) displaying. A variety of glyco-macroligands have been developed to mimic multivalent carbohydrate-protein interactions for studying carbohydrate-protein interactions and biomedical research and applications. Recently, a …


Effects Of Interferons And Double-Stranded Rna On Human Prostate Cancer Cell Apoptosis, Haiyan Tan, Chun Zeng, Junbo Xie, Norah J. Alghamdi, Ya Song, Hongbing Zhang, Aimin Zhou, Di Jin Sep 2015

Effects Of Interferons And Double-Stranded Rna On Human Prostate Cancer Cell Apoptosis, Haiyan Tan, Chun Zeng, Junbo Xie, Norah J. Alghamdi, Ya Song, Hongbing Zhang, Aimin Zhou, Di Jin

Chemistry Faculty Publications

Prostate cancer is the second most commonly diagnosed cancer among men in the United States. Prostate cancer therapy is severely hampered by lack of response and development of resistance to conventional chemotherapeutic drugs in patients. Therefore, the development and discovery of new drugs have become an urgent clinical need. Interferons (IFNs), a family of pleiotropic cytokines, exert antitumor activities due to their anti-proliferative, immunomodulatory and proapoptotic functions. Here, we report that pretreatment of prostate cancer PC-3 cells with IFNs sensitized these cells to double-stranded RNAs (dsRNAs)-induced apoptosis. The enhancement effect of IFN treatment was dependent on IFN subtypes, in particular, …


Determination Of Triapine, A Ribonucleotide Reductase Inhibitor, In Human Plasma By Liquid Chromatography Tandem Mass Spectrometry, Ye Feng, Charles A. Kunos, Yan Xu Sep 2015

Determination Of Triapine, A Ribonucleotide Reductase Inhibitor, In Human Plasma By Liquid Chromatography Tandem Mass Spectrometry, Ye Feng, Charles A. Kunos, Yan Xu

Chemistry Faculty Publications

Triapine is an inhibitor of ribonucleotide reductase (RNR). Studies have shown that triapine significantly decreases the activity of RNR and enhanced the radiation-mediated cytotoxicity in cervical and colon cancer. In this work, we have developed and validated a selective and sensitive LC-MS/MS method for the determination of triapine in human plasma. In this method, 2-[(3-fluoro-2-pyridinyl)methylene] hydrazinecarbothioamide (NSC 266749) was used as the internal standard (IS); plasma samples were prepared by deproteinization with acetonitrile; tripaine and the IS were separated on a Waters Xbridge Shield RP18 column (3.5 µm; 2.1 × 50 mm) using a mobile phase containing 25.0% methanol and …


Globally Profiling Sialylation Status Of Macrophages Upon Statin Treatment, Dan Wang, Huan Nie, Evgeny Ozhegov, Lin Wang, Aimin Zhou, Yu Li, Xue Long Sun Sep 2015

Globally Profiling Sialylation Status Of Macrophages Upon Statin Treatment, Dan Wang, Huan Nie, Evgeny Ozhegov, Lin Wang, Aimin Zhou, Yu Li, Xue Long Sun

Chemistry Faculty Publications

Sialic acids (SAs) are widely expressed on immune cells and their levels and linkages named as sialylation status vary upon cellular environment changes related to both physiological and pathological processes. In this study, we performed a global profiling of the sialylation status of macrophages and their release of SAs in the cell culture medium by using flow cytometry, confocal microscopy and liquid chromatography tandem mass spectrometry (LC-MS/MS). Both flow cytometry and confocal microscopy results showed that cell surface α-2,3-linked SAs were predominant in the normal culture condition and changed slightly upon treatment with atorvastatin for 24 h, whereas α-2,6-linked SAs …


A Rapid Lc-Ms/Ms Method For Quantification Of Csuoh0901, A Novel Antitumor Agent, In Rat Plasma, Ramakrishna R. Voggu, Ravali Alagandula, Xiang Zhou, Bin Su Ph.D., Bo Zhong, Baochuan Guo May 2015

A Rapid Lc-Ms/Ms Method For Quantification Of Csuoh0901, A Novel Antitumor Agent, In Rat Plasma, Ramakrishna R. Voggu, Ravali Alagandula, Xiang Zhou, Bin Su Ph.D., Bo Zhong, Baochuan Guo

Chemistry Faculty Publications

CSUOH0901, a novel anticancer derivative of nimesulide, exhibits very promising anticancer activities in various cancer cell lines. In order to support further pharmacological and toxicological studies of this promising anticancer drug candidate, an LC-MS/MS method was developed and validated in accordance with the US Food and Drug Administration guidelines. The drug molecules were extracted from plasma samples by protein precipitation and then analyzed with LC-ESI-MS/MS. An excellent analyte separation was achieved using a phenomenex C18 column with a mobile phase of 90% methanol and 5 m m of ammonium formate. The validated linear dynamic range was between 0.5 and 100 …


A Rapid Lc-Ms/Ms Method For Quantification Of Csuoh0901, A Novel Antitumor Agent, In Rat Plasma, Ramakrishna R. Voggu, Ravali Alagandula, Xiang Zhou, Bin Su, Bo Zhong, Baochuan Guo May 2015

A Rapid Lc-Ms/Ms Method For Quantification Of Csuoh0901, A Novel Antitumor Agent, In Rat Plasma, Ramakrishna R. Voggu, Ravali Alagandula, Xiang Zhou, Bin Su, Bo Zhong, Baochuan Guo

Chemistry Faculty Publications

CSUOH0901, a novel anticancer derivative of nimesulide, exhibits very promising anticancer activities in various cancer cell lines. In order to support further pharmacological and toxicological studies of this promising anticancer drug candidate, an LC-MS/MS method was developed and validated in accordance with the US Food and Drug Administration guidelines. The drug molecules were extracted from plasma samples by protein precipitation and then analyzed with LC-ESI-MS/MS. An excellent analyte separation was achieved using a phenomenex C18 column with a mobile phase of 90% methanol and 5 m m of ammonium formate. The validated linear dynamic range was between 0.5 and 100 …


Crystal Structure Of 9-Methacryloylanthracene, Aditya Agrahari, Patrick O. Wagers, Steven M. Schildcrout, John Masnovi, Wiley J. Youngs Apr 2015

Crystal Structure Of 9-Methacryloylanthracene, Aditya Agrahari, Patrick O. Wagers, Steven M. Schildcrout, John Masnovi, Wiley J. Youngs

Chemistry Faculty Publications

In the title compound, C18H14O, with systematic name 1-(anthracen-9-yl)-2-methylprop-2-en-1-one, the ketonic C atom lies 0.2030 (16) angstrom out of the anthrylring-system plane. The dihedral angle between the planes of the anthryl and methacryloyl moieties is 88.30 (3)degrees and the stereochemistry about the Csp(2) - Csp(2) bond in the side chain is transoid. In the crystal, the end rings of the anthryl units in adjacent molecules associate in parallel-planar orientations [shortest centroid-centroid distance = 3.6320 (7) angstrom]. A weak hydrogen bond is observed between an aromatic H atom and the O atom of a molecule displaced by translation in the a-axis …


Addressing The Achievement Gap: Engaging Students In The Chemistry Classroom, Haidy Kamel Dr. Mar 2015

Addressing The Achievement Gap: Engaging Students In The Chemistry Classroom, Haidy Kamel Dr.

Cleveland State University Regional Chemistry Teaching Symposium: March 12 & 13, 2015

No abstract provided.


Magical Science: Chemistry Magic Tricks Just For Fun! (Workshop), Regan L. Silvestri Mar 2015

Magical Science: Chemistry Magic Tricks Just For Fun! (Workshop), Regan L. Silvestri

Cleveland State University Regional Chemistry Teaching Symposium: March 12 & 13, 2015

Chemistry magic tricks are simply chemistry demonstrations cleverly performed, and are highly valuable for engaging and motivating students in the study of chemistry. Our agenda has been to adapt common chemistry demonstrations into presentations with clever twists, essentially turning them into magic tricks. This workshop will show how a science demonstration can be turned into a science magic trick simply by adapting the presentation. Science magic tricks provide a unique forum not only for expanding scientific knowledge, but moreover scientific interest. Our hope is that students will be engaged and motivated in the future study of chemistry.


Working With High School Students, The Pros And Cons", Luciana Aronne Feb 2015

Working With High School Students, The Pros And Cons", Luciana Aronne

Cleveland State University Regional Chemistry Teaching Symposium: March 12 & 13, 2015

No abstract provided.


Csu 4th Annual Regional Chemistry Symposium: March 12 & 13, 2015, Zhihai Li Dr. Feb 2015

Csu 4th Annual Regional Chemistry Symposium: March 12 & 13, 2015, Zhihai Li Dr.

Cleveland State University Regional Chemistry Teaching Symposium: March 12 & 13, 2015

CSU 4th Annual Regional Chemistry Symposium: March 12 & 13, 2015

Register here for the 4th Annual Regional Chemistry Symposium March 12 & 13, 2015 Fee: $100 for two days $50 for one day Limited Time special registration fee! The registration fee for the two-day symposium is $100 and includes breakfast, lunch, an outstanding wine and cheese social hour, and discount rates on lodging. A schedule of events will also include a list of Cleveland's best sights, sounds and tastes.

To pay with credit card, visit CSU's ShopNet page at https://campusnet.csuohio.edu/ShopNet/index.jsp

You may also pay the fee in person on …


Characterization Of Cold Drawn Poly L Lactic Acid By Raman Spectroscopy And Raman Hyperspectral Imaging, Ramya Sudha Muttavarapu Jan 2015

Characterization Of Cold Drawn Poly L Lactic Acid By Raman Spectroscopy And Raman Hyperspectral Imaging, Ramya Sudha Muttavarapu

ETD Archive

Artificial modulation of bone growth and repair processes is an important area of current research. Studies have established that the micro mechanical and bulk physical properties of a polymer implant influence its performance behavior and degradation patterns in the body. One important parameter for the class of polymers known as polylactides is the degree of crystalline character. Hence, studying the bulk and micro crystalline composition of an important polymer implant, Poly-L-Lactic acid is the objective of this study. Poly-L-Lactic acid has elastic properties that can be tailored to resemble natural bone and its reaction to mechanical stress. Varying degrees of …


A Simple And Rapid Lc-Ms/Ms Method For The Determination Of Bmcl26 A Novel Anti-Parasitic Agent In Rat Plasma, Ramakrishna R. Voggu, Xiang Zhou, Bing Su, Baochuan Guo Jan 2015

A Simple And Rapid Lc-Ms/Ms Method For The Determination Of Bmcl26 A Novel Anti-Parasitic Agent In Rat Plasma, Ramakrishna R. Voggu, Xiang Zhou, Bing Su, Baochuan Guo

Chemistry Faculty Publications

BMCL26 is a potential drug derived from nimesulide, which has exhibited the substantial anti-parasitic activity in various cell lines. To conduct various pharmacological and toxicological properties of this drug, we developed and validated a rapid LC-MS/MS method for its quantification in accordance with the FDA guidelines. Protein precipitation with 0.1% formic acid in acetonitrile was used to extract the analytes along with the internal standard (JCC76) from rat plasma. It was found that the calibration curve of the method had an excellent linearity (r2 ≥ 0.9993) for the analyte concentration ranging from 0.5 to 100 ng/mL with acceptable inter- and …


Specific N-Glycans Of Hepatocellular Carcinoma Cell Surface And The Abnormal Increase Of Core-Α-1, 6-Fucosylated Triantennary Glycan Via N-Acetylglucosaminyltransferases-Iva Regulation, Huan Nie, Xia Liu, Yubao Zhang, Tingting Li, Chao Zhan, Wenjuan Huo, Anshun He, Yuanfei Yao, Yu Jin, Youpeng Qu, Xue-Long Sun, Yu Li Jan 2015

Specific N-Glycans Of Hepatocellular Carcinoma Cell Surface And The Abnormal Increase Of Core-Α-1, 6-Fucosylated Triantennary Glycan Via N-Acetylglucosaminyltransferases-Iva Regulation, Huan Nie, Xia Liu, Yubao Zhang, Tingting Li, Chao Zhan, Wenjuan Huo, Anshun He, Yuanfei Yao, Yu Jin, Youpeng Qu, Xue-Long Sun, Yu Li

Chemistry Faculty Publications

Glycosylation alterations of cell surface proteins are often observed during the progression of malignancies. The specific cell surface N-glycans were profiled in hepatocellular carcinoma (HCC) with clinical tissues (88 tumor and adjacent normal tissues) and the corresponding serum samples of HCC patients. The level of core-α-1,6-fucosylated triantennary glycan (NA3Fb) increased both on the cell surface and in the serum samples of HCC patients (p < 0.01). Additionally, the change of NA3Fb was not influenced by Hepatitis B virus (HBV)and cirrhosis. Furthermore, the mRNA and protein expression of N-acetylglucosaminyltransferase IVa (GnT-IVa), which was related to the synthesis of the NA3Fb, was substantially increased in HCC tissues. Knockdown of GnT-IVa leads to a decreased level of NA3Fb and decreased ability of invasion and migration in HCC cells. NA3Fb can be regarded as a specific cell surface N-glycan of HCC. The high expression of GnT-IVa is the cause of the abnormal increase of NA3Fb on the HCC cell surface, which regulates cell migration. This study demonstrated the specific N-glycans of the cell surface and the mechanisms of altered glycoform related with HCC. These findings lead to better understanding of the function of glycan and glycosyltransferase in the tumorigenesis, progression and metastasis of HCC.


Rnase L Contributes To Experimentally Induced Type 1 Diabetes Onset In Mice, Chun Zeng, Xin Yi, Danny Zipris, Hongli Liu, Lin Zhang, Qiaoyun Zheng, Krishnamurthy Malathi, Ge Jin, Aimin Zhou Dec 2014

Rnase L Contributes To Experimentally Induced Type 1 Diabetes Onset In Mice, Chun Zeng, Xin Yi, Danny Zipris, Hongli Liu, Lin Zhang, Qiaoyun Zheng, Krishnamurthy Malathi, Ge Jin, Aimin Zhou

Chemistry Faculty Publications

The cause of type 1 diabetes continues to be a focus of investigation. Studies have revealed that interferon α (IFNα) in pancreatic islets after viral infection or treatment with double-stranded RNA (dsRNA), a mimic of viral infection, is associated with the onset of type 1 diabetes. However, how IFNα contributes to the onset of type 1 diabetes is obscure. In this study, we found that 2-5A-dependent RNase L (RNase L), an IFNα-inducible enzyme that functions in the antiviral and antiproliferative activities of IFN, played an important role in dsRNA-induced onset of type 1 diabetes. Using RNase L-deficient, rat insulin promoter-B7.1 …


Distinct Conformational Behaviors Of Four Mammalian Dual-Flavin Reductases (Cytochrome P450 Reductase, Methionine Synthase Reductase, Neuronal Nitric Oxide Synthase, Endothelial Nitric Oxide Synthase) Determine Their Unique Catalytic Profiles, Mohammad Mahfuzul Haque, Mekki Bayachou, Jesus Tejero, Claire T. Kenney, Naw M. Pearl, Sang-Choul Im, Lucy Waskell, Dennis J. Stuehr Dec 2014

Distinct Conformational Behaviors Of Four Mammalian Dual-Flavin Reductases (Cytochrome P450 Reductase, Methionine Synthase Reductase, Neuronal Nitric Oxide Synthase, Endothelial Nitric Oxide Synthase) Determine Their Unique Catalytic Profiles, Mohammad Mahfuzul Haque, Mekki Bayachou, Jesus Tejero, Claire T. Kenney, Naw M. Pearl, Sang-Choul Im, Lucy Waskell, Dennis J. Stuehr

Chemistry Faculty Publications

Multidomain enzymes often rely on large conformational motions to function. However, the conformational setpoints, rates of domain motions and relationships between these parameters and catalytic activity are not well understood. To address this, we determined and compared the conformational setpoints and the rates of conformational switching between closed unreactive and open reactive states in four mammalian diflavin NADPH oxidoreductases that catalyze important biological electron transfer reactions: cytochrome P450 reductase, methionine synthase reductase and endothelial and neuronal nitric oxide synthase. We used stopped-flow spectroscopy, single turnover methods and a kinetic model that relates electron flux through each enzyme to its conformational …


Rnase L Interacts With Filamin A To Regulate Actin Dynamics And Barrier Function For Viral Entry, Krishnamurthy Malathi, Mohammad Adnan Siddiqui, Shubham Dayal, Merna Naji, Heather J, Ezelle, Chun Zeng, Aimin Zhou, Bret A. Hassel Nov 2014

Rnase L Interacts With Filamin A To Regulate Actin Dynamics And Barrier Function For Viral Entry, Krishnamurthy Malathi, Mohammad Adnan Siddiqui, Shubham Dayal, Merna Naji, Heather J, Ezelle, Chun Zeng, Aimin Zhou, Bret A. Hassel

Chemistry Faculty Publications

The actin cytoskeleton and its network of associated proteins constitute a physical barrier that viruses must circumvent to gain entry into cells for productive infection. The mechanisms by which the physical signals of infection are sensed by the host to activate an innate immune response are not well understood. The antiviral endoribonuclease RNase L is ubiquitously expressed in a latent form and activated upon binding 2-5A, a unique oligoadenylate produced during viral infections. We provide evidence that RNase L in its inactive form interacts with the actin-binding protein Filamin A to modulate the actin cytoskeleton and inhibit virus entry. Cells …


Measuring Activity Of Endothelial Nitric Oxide Synthase And Nanodisc Complex Through Nitrate Production, Christopher Verdi, Ghaith Altawallbeh, Mekki Bayachou Sep 2014

Measuring Activity Of Endothelial Nitric Oxide Synthase And Nanodisc Complex Through Nitrate Production, Christopher Verdi, Ghaith Altawallbeh, Mekki Bayachou

Undergraduate Research Posters 2014

Nitric oxide is an important bioregulator generated in various regions throughout the body by a family of isozymes referred to as Nitric Oxide Synthases (NOS). Within vascular endothelial cells, nitric oxide is generated from oxygen and arginine (amino acid) by endothelial nitric oxide synthases (eNOS). Within this environment nitric oxide plays a critical paracrine role, mainly anithrombotic and anti-atherosclerotic. This is accomplished by vessel dilation and prevention of platelet and leukocyte aggregation and adherence to the vessel wall. The activity of the eNOS enzyme has been studied within solution and is well understood. However, the impact that the lipid bilayer …


Cryoprotective Effect Of L-Carnitine On Motility, Vitality And Dna Oxidation Of Human Spermatozoa, S. Banihani, A. Agarwal, R. Sharma, Mekki Bayachou Aug 2014

Cryoprotective Effect Of L-Carnitine On Motility, Vitality And Dna Oxidation Of Human Spermatozoa, S. Banihani, A. Agarwal, R. Sharma, Mekki Bayachou

Chemistry Faculty Publications

Successful cryopreservation for human spermatozoa markedly influences the reproductive outcomes of assisted reproductive technologies. But in spite of its usefulness, cryopreservation significantly decreases sperm quality. l-carnitine has been found to improve the quality of spermatozoa in selected cases with male infertility. Here, we examined the efficacy of l-carnitine in improving sperm motility and vitality and reducing sperm DNA oxidation during cryopreservation. Semen samples from infertile patients (n = 22) were collected and analysed. Cryopreservation medium supplemented with l-carnitine was mixed with the semen at a ratio of 1 : 1 (v/v). The final l-carnitine concentration in each cryovial was 0.5 …


Metabolomics Of Apcmin/+ Mice Genetically Susceptible To Intestinal Cancer, Jean Eudes J. Dazard, Yana Sandlers, Stephanie K. Doerner, Nathan A. Berger, Henri Brunengraber Jun 2014

Metabolomics Of Apcmin/+ Mice Genetically Susceptible To Intestinal Cancer, Jean Eudes J. Dazard, Yana Sandlers, Stephanie K. Doerner, Nathan A. Berger, Henri Brunengraber

Chemistry Faculty Publications

Background: To determine how diets high in saturated fat could increase polyp formation in the mouse model of intestinal neoplasia, ApcMin/+, we conducted large-scale metabolome analysis and association study of colon and small intestine polyp formation from plasma and liver samples of ApcMin/+ vs. wild-type littermates, kept on low vs. high-fat diet. Label-free mass spectrometry was used to quantify untargeted plasma and acyl-CoA liver compounds, respectively. Differences in contrasts of interest were analyzed statistically by unsupervised and supervised modeling approaches, namely Principal Component Analysis and Linear Model of analysis of variance. Correlation between plasma metabolite concentrations and polyp numbers was …


A New Liquid Chromatography/Tandem Mass Spectrometry Method For Quantification Of Gangliosides In Human Plasma, Qianyang Huang, Xiang Zhou, Danting Liu, Baozhong Xin, Karen Cechner, Heng Wang, Aimin Zhou Jun 2014

A New Liquid Chromatography/Tandem Mass Spectrometry Method For Quantification Of Gangliosides In Human Plasma, Qianyang Huang, Xiang Zhou, Danting Liu, Baozhong Xin, Karen Cechner, Heng Wang, Aimin Zhou

Chemistry Faculty Publications

Gangliosides are a family of glycosphingolipids characterized by mono- or polysialic acid-containing oligosaccharides linked through 1,3- and 1,4-β glycosidic bonds with subtle differences in structure that are abundantly present in the central nervous systems of many living organisms. Their cellular surface expression and physiological malfunction are believed to be pathologically implicated in considerable neurological disorders, including Alzheimer and Parkinson diseases. Recently, studies have tentatively elucidated that mental retardation or physical stagnation deteriorates as the physiological profile of gangliosides becomes progressively and distinctively abnormal during the development of these typical neurodegenerative syndromes. In this work, a reverse-phase liquid chromatography/tandem mass spectrometry …


Lead Optimization Of Dual Tubulin And Hsp27 Inhibitors, Bo Zhong, Rati Lama, Daniel G. Kulman, Bibo Li Ph.D., Bin Su Ph.D. Jun 2014

Lead Optimization Of Dual Tubulin And Hsp27 Inhibitors, Bo Zhong, Rati Lama, Daniel G. Kulman, Bibo Li Ph.D., Bin Su Ph.D.

Chemistry Faculty Publications

Tubulin and heat shock protein 27 (Hsp27) are well-characterized molecular targets for anti-cancer drug development. We previously identified lead compounds that inhibited both Hsp27 and tubulin. These compounds exhibited extensive anti-cancer activities against the proliferation of various human cancer cell lines. In the current study, a systematic ligand based structural optimization led to new analogs that significantly inhibited the growth of a panel of breast cancer cell lines. Furthermore, the most potent compounds were examined with tubulin polymerization assay and Hsp27 chaperone activity assay. The compounds showed potent tubulin polymerization inhibition but no Hsp27 inhibitory effect. The structural optimization dissected …


Development And Validation Of Lc–Ms/Ms Method For Quantitative Determination Of (−)-Securinine In Mouse Plasma, Simuli L. Wabuyele, David Wald, Yan Xu Jun 2014

Development And Validation Of Lc–Ms/Ms Method For Quantitative Determination Of (−)-Securinine In Mouse Plasma, Simuli L. Wabuyele, David Wald, Yan Xu

Chemistry Faculty Publications

(−)-Securinine (SE) is a major alkaloid found in plant Securinega suffruticosa, which has a wide range of pharmacological activities including anticancer, anti-parasitic and central nervous system stimulating effects, etc. To aid the pharmacological study of SE, we developed an LC–MS/MS method for quantitative determination of SE in mouse plasma. In this method, plasma samples were first prepared with salting-out assisted liquid–liquid extraction using cold acetonitrile (−20 °C) and 2.00 M ammonium acetate. Separation of SE and the internal standard (IS) from sample matrix was achieved on a Gemini Nx C18 column using 40% acetonitrile and 60% 10.0 mM ammonium acetate …


Reclaiming The Efficacy Of Β-Lactam–Β-Lactamase Inhibitor Combinations: Avibactam Restores The Susceptibility Of Cmy-2-Producing Escherichia Coli To Ceftazidime, Krisztina M. Papp-Wallace, Marisa L. Winkler, Julian A. Gatta, Magdalena A. Taracila, Sujatha Chilakala, Yan Xu, J. Kristie Johnson, Robert A. Bonomo May 2014

Reclaiming The Efficacy Of Β-Lactam–Β-Lactamase Inhibitor Combinations: Avibactam Restores The Susceptibility Of Cmy-2-Producing Escherichia Coli To Ceftazidime, Krisztina M. Papp-Wallace, Marisa L. Winkler, Julian A. Gatta, Magdalena A. Taracila, Sujatha Chilakala, Yan Xu, J. Kristie Johnson, Robert A. Bonomo

Chemistry Faculty Publications

CMY-2 is a plasmid-encoded Ambler class C cephalosporinase that is widely disseminated in Enterobacteriaceae and is responsible for expanded-spectrum cephalosporin resistance. As a result of resistance to both ceftazidime and β-lactamase inhibitors in strains carrying blaCMY, novel β-lactam–β-lactamase inhibitor combinations are sought to combat this significant threat to β-lactam therapy. Avibactam is a bridged diazabicyclo [3.2.1]octanone non-β-lactam β-lactamase inhibitor in clinical development that reversibly inactivates serine β-lactamases. To define the spectrum of activity of ceftazidime-avibactam, we tested the susceptibilities of Escherichia coli clinical isolates that carry blaCMY-2 or blaCMY-69 and investigated the inactivation kinetics of CMY-2. Our analysis showed that …


Site-Specific Nitration Of Apolipoprotein A-I At Tyrosine 166 Is Both Abundant Within Human Atherosclerotic Plaque And Dysfunctional, Joseph A. Didonato, Kulwant Aulak, Ying Huang, Matthew A. Wagner, Gary Gerstenecker, Celalettin Topbas, Valentin Gogonea, Anthony J. Didonato, W.H. Wilson Tang, Ryan A. Mehl, Paul L. Fox, Edward F. Plow, Jonathan D. Smith, Edward A. Fisher, Stanley L. Hazen Apr 2014

Site-Specific Nitration Of Apolipoprotein A-I At Tyrosine 166 Is Both Abundant Within Human Atherosclerotic Plaque And Dysfunctional, Joseph A. Didonato, Kulwant Aulak, Ying Huang, Matthew A. Wagner, Gary Gerstenecker, Celalettin Topbas, Valentin Gogonea, Anthony J. Didonato, W.H. Wilson Tang, Ryan A. Mehl, Paul L. Fox, Edward F. Plow, Jonathan D. Smith, Edward A. Fisher, Stanley L. Hazen

Chemistry Faculty Publications

We reported previously that apolipoprotein A-I (apoA-I) is oxidatively modified in the artery wall at tyrosine 166 (Tyr166), serving as a preferred site for post-translational modification through nitration. Recent studies, however, question the extent and functional importance of apoA-I Tyr166 nitration based upon studies of HDL-like particles recovered from atherosclerotic lesions. We developed a monoclonal antibody (mAb 4G11.2) that recognizes, in both free and HDL-bound forms, apoA-I harboring a 3-nitrotyrosine at position 166 apoA-I (NO2-Tyr166-apoA-I) to investigate the presence, distribution, and function of this modified apoA-I form in atherosclerotic and normal artery wall. We also developed recombinant apoA-I with site-specific …


Lead Optimization Of Hmba To Develop Potent Hexim1 Inducers, Bo Zhong, Rati Lama, Wannarasmi Ketchart, Monica M. Montano, Bin Su Mar 2014

Lead Optimization Of Hmba To Develop Potent Hexim1 Inducers, Bo Zhong, Rati Lama, Wannarasmi Ketchart, Monica M. Montano, Bin Su

Chemistry Faculty Publications

The potency of a series of Hexamethylene bis-acetamide (HMBA) derivatives inducing Hexamethylene bis-acetamide inducible protein 1 (HEXIM1) was determined in LNCaP prostate cancer cells. Several compounds with unsymmetrical structures showed significantly improved activity. Distinct from HMBA, these analogs have increased hydrophobicity and can improve the short half-life of HMBA, which is one of the factors that have limited the application of HMBA in clinics. The unsymmetrical scaffolds of the new analogs provide the basis for further lead optimization of the compounds using combinatorial chemistry strategy.


An Abundant Dysfunctional Apolipoprotein A1 In Human Atheroma, Ying Huang, Joseph A. Didonato, Bruce S. Levison, Dave Schmitt, Lin Li, Yuping Wu, Jennifer Buffa, Timothy Kim, Gary S. Gerstenecker, Xiaodong Gu, Chandra S. Kadiyala, Zeneng Wang, Miranda K. Culley, Jennie E. Hazen, Anthony J. Didonato, Xiaoming Fu, Stela Z. Berisha, Daoquan Peng, Truc T. Nguyen, Shaohong Liang, Chia-Chi Chuang, Leslie Cho, Edward F. Plow, Paul L. Fox, Valentin Gogonea, W.H. Wilson Tang, John S. Parks, Edward A. Fisher, Jonathan D. Smith, Stanley L. Hazen Feb 2014

An Abundant Dysfunctional Apolipoprotein A1 In Human Atheroma, Ying Huang, Joseph A. Didonato, Bruce S. Levison, Dave Schmitt, Lin Li, Yuping Wu, Jennifer Buffa, Timothy Kim, Gary S. Gerstenecker, Xiaodong Gu, Chandra S. Kadiyala, Zeneng Wang, Miranda K. Culley, Jennie E. Hazen, Anthony J. Didonato, Xiaoming Fu, Stela Z. Berisha, Daoquan Peng, Truc T. Nguyen, Shaohong Liang, Chia-Chi Chuang, Leslie Cho, Edward F. Plow, Paul L. Fox, Valentin Gogonea, W.H. Wilson Tang, John S. Parks, Edward A. Fisher, Jonathan D. Smith, Stanley L. Hazen

Chemistry Faculty Publications

Recent studies have indicated that high-density lipoproteins (HDLs) and their major structural protein, apolipoprotein A1 (apoA1), recovered from human atheroma are dysfunctional and are extensively oxidized by myeloperoxidase (MPO). In vitro oxidation of either apoA1 or HDL particles by MPO impairs their cholesterol acceptor function. Here, using phage display affinity maturation, we developed a high-affinity monoclonal antibody that specifically recognizes both apoA1 and HDL that have been modified by the MPO-H2O2-Cl− system. An oxindolyl alanine (2-OH-Trp) moiety at Trp72 of apoA1 is the immunogenic epitope. Mutagenesis studies confirmed a critical role for apoA1 Trp72 in MPO-mediated inhibition of the ATP-binding …


Bsa–Boronic Acid Conjugate As Lectin Mimetics, Satya Nandana Narla, Poornima Pinnamaneni, Huan Nie, Yu Li, Xue-Long Sun Jan 2014

Bsa–Boronic Acid Conjugate As Lectin Mimetics, Satya Nandana Narla, Poornima Pinnamaneni, Huan Nie, Yu Li, Xue-Long Sun

Chemistry Faculty Publications

We report bovine serum albumin (BSA)–boronic acid (BA) conjugates as lectin mimetics and their glyco-capturing capacity. The BSA–BA conjugates were synthesized by amidation of carboxylic acid groups in BSA with aminophenyl boronic acid in the presence of EDC, and were characterized by Alizarin Red S (ARS) assay and SDS–PAGE gel. The BSA–BA conjugates were immobilized onto maleimide-functionalized silica beads and their sugar capturing capacity and specificity were confirmed by ARS displacement assay. Further, surface plasmon resonance (SPR) analysis of the glyco-capturing activity of the BSA–BA conjugates was conducted by immobilizing BSA–BA onto SPR gold chip. Overall, we demonstrated a BSA–BA-based …


The Role Of Platelets In Hyaluronan Degradation, Sami Albeiroti Jan 2014

The Role Of Platelets In Hyaluronan Degradation, Sami Albeiroti

ETD Archive

Following tissue injury, platelets rapidly interact with the exposed extracellular matrix (ECM) of blood vessel wall and the surrounding tissues. Hyaluronan (HA) is a major polysaccharide component of the ECM and plays a significant role in regulating inflammation. Human platelets can degrade HA from the surfaces of activated endothelial cells into fragments capable of inducing immune responses by monocytes. In addition, platelets contain the enzyme hyaluronidse-2 (HYAL2), one of two major hyaluronidases that digest HA in somatic tissues. The deposition of HA increases in the inflamed tissues in several inflammatory diseases, including Inflammatory Bowel Disease (IBD). This study provides evidence …