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Medicinal-Pharmaceutical Chemistry Commons

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Full-Text Articles in Medicinal-Pharmaceutical Chemistry

Molecular Targeting Of Protein Arginine Deiminases To Suppress Colitis And Prevent Colon Cancer, Erin E. Witalison, Xiangli Cui, Corey P. Causey, Paul R. Thompson, Lorne J. Hofseth Nov 2015

Molecular Targeting Of Protein Arginine Deiminases To Suppress Colitis And Prevent Colon Cancer, Erin E. Witalison, Xiangli Cui, Corey P. Causey, Paul R. Thompson, Lorne J. Hofseth

Thompson Lab Publications

Ulcerative colitis (UC) is a chronic disease, in which the lining of the colon becomes inflamed and develops ulcers leading to abdominal pain, diarrhea, and rectal bleeding. The extent of these symptoms depends on disease severity. The protein arginine deiminase (PAD) family of enzymes converts peptidyl-Arginine to peptidyl-Citrulline through citrullination. PADs are dysregulated, with abnormal citrullination in many diseases, including UC and colorectal cancer (CRC). We have developed the small molecule, pan-PAD inhibitor, Chlor-amidine (Cl-amidine), with multiple goals, including treating UC and preventing CRC. Building off our recent results showing that: 1) Cl-amidine suppresses colitis in vivo in a dextran ...


Anti-Tb And Antibacterial Activities Of Natural Products Extracts, Douglas Armstrong, Nathan Krause, Drew Frey Oct 2015

Anti-Tb And Antibacterial Activities Of Natural Products Extracts, Douglas Armstrong, Nathan Krause, Drew Frey

Faculty Scholarship – Chemistry

Samples of numerous plant species were received from the southwestern part of the USA from Richard Spjut, and plant samples were collected here in Illinois. All were extracted with typical solvents, giving crude residues, some of which were subjected to counter-current or flash chromatographic methods. Some of the crude extracts and chromatographic fractions had anti-tuberculosis and/or antibacterial activity.

In a general way, bioactive natural products are dealt with very well by Liang & Fang, 2006. More specifically, the southwestern part of the United States has a large variety of indigenous plants, many of which have not been investigated for their ...


Synthesis And Flammability Testing Of Epoxy Functionalized Phosphorous-Based Flame Retardants, Vladimir Benin, Xuemei Cui, Alexander Morgan, Karl Seiwert Aug 2015

Synthesis And Flammability Testing Of Epoxy Functionalized Phosphorous-Based Flame Retardants, Vladimir Benin, Xuemei Cui, Alexander Morgan, Karl Seiwert

Chemistry Faculty Publications

Several potential new phosphorus-containing flame retardant molecules were evaluated for heat release reduction potential by incorporation of the molecules into a polyurethane, generated from methylene diphenyl diisocyanate and 1,3-propane diol. The heat release reduction potential of these substances was evaluated using the pyrolysis combustion flow calorimeter (PCFC). The polyurethanes were prepared in the presence of the potential flame retardants via solvent mixing and copolymerization methods to qualitatively evaluate their potential reactivity into the polyurethane prior to heat release testing. The functionality of the flame retardants was epoxide based that would potentially react with the diol during polyurethane synthesis. Flammability ...


The Antioxidant Activity And Their Major Antioxidant Compounds From Acanthopanax Senticosus And A. Koreanum, Young-Hyun Kim, Myoung Lae Cho, Dan-Bi Kim, Gi-Hae Shin, Jin-Ha Lee, Jong Seok Lee, Sun-Ok Park, Sang-Jong Lee, Hyun Mu Shin, Ok-Hwan Lee Jul 2015

The Antioxidant Activity And Their Major Antioxidant Compounds From Acanthopanax Senticosus And A. Koreanum, Young-Hyun Kim, Myoung Lae Cho, Dan-Bi Kim, Gi-Hae Shin, Jin-Ha Lee, Jong Seok Lee, Sun-Ok Park, Sang-Jong Lee, Hyun Mu Shin, Ok-Hwan Lee

Open Access Articles

The antioxidant activity and chlorogenic acid and caffeic acid contents were investigated from different parts of Acanthopanax senticosus and A. koreanum. Antioxidant activity was assessed by various in vitro assays such as DPPH, ABTS, FRAP, reducing power assays and ORAC, and the chlorogenic acid and caffeic acid were validated by HPLC chromatography. Among the various extracts, the fruit extracts of A. senticosus and A. koreanum exhibited strongest antioxidant activities including ABTS, FRAP, reducing power and ORAC, however, strongest DPPH radical scavenging activity was observed from the leaf extract of A. senticosus. In addition, the antioxidant activities of various extracts were ...


Structural Basis For Mutation-Induced Destabilization Of Profilin 1 In Als, Sivakumar Boopathy, Tania V. Silvas, Maeve Tischbein, Silvia Jansen, Shivender Shandilya, Jill A. Zitzewitz, John E. Landers, Bruce L. Goode, Celia A. Schiffer, Daryl A. Bosco Jun 2015

Structural Basis For Mutation-Induced Destabilization Of Profilin 1 In Als, Sivakumar Boopathy, Tania V. Silvas, Maeve Tischbein, Silvia Jansen, Shivender Shandilya, Jill A. Zitzewitz, John E. Landers, Bruce L. Goode, Celia A. Schiffer, Daryl A. Bosco

Schiffer Lab Publications

Mutations in profilin 1 (PFN1) are associated with amyotrophic lateral sclerosis (ALS); however, the pathological mechanism of PFN1 in this fatal disease is unknown. We demonstrate that ALS-linked mutations severely destabilize the native conformation of PFN1 in vitro and cause accelerated turnover of the PFN1 protein in cells. This mutation-induced destabilization can account for the high propensity of ALS-linked variants to aggregate and also provides rationale for their reported loss-of-function phenotypes in cell-based assays. The source of this destabilization is illuminated by the X-ray crystal structures of several PFN1 proteins, revealing an expanded cavity near the protein core of the ...


Chemical Biology Of Protein Arginine Modifications In Epigenetic Regulation, Jakob Fuhrmann, Kathleen W. Clancy, Paul R. Thompson Jun 2015

Chemical Biology Of Protein Arginine Modifications In Epigenetic Regulation, Jakob Fuhrmann, Kathleen W. Clancy, Paul R. Thompson

Thompson Lab Publications

Review article on histone citrullination (arginine deimination), histone arginine methylation, and noncanonical histone arginine modifications.


Heterocycles From Wine: Synthesis And Biological Evaluation Of Salidrosides, Tezcan Guney, Stephanie A. Kohles, Victoria L. Thompson, Gregory J. Phillips, George A. Kraus May 2015

Heterocycles From Wine: Synthesis And Biological Evaluation Of Salidrosides, Tezcan Guney, Stephanie A. Kohles, Victoria L. Thompson, Gregory J. Phillips, George A. Kraus

Chemistry Publications

Wine is composed of a variety of tannins, of which a sub-class includes salidrosides, which are largely uninvestigated compounds. The first syntheses of galloylated salidrosides are reported in 7 steps from commercially available starting materials through a platform approach. The antimicrobial activity of the salidrosides against Escherichia coli strains is described.


Gold Nanoparticles Stabilized With Mpeg-Grafted Poly(L-Lysine): In Vitro And In Vivo Evaluation Of A Potential Theranostic Agent, Alexei A. Bogdanov, Suresh Gupta, Nadezhda Koshkina, Stuart J. Corr, Surong Zhang, Steven A. Curley, Gang Han Jan 2015

Gold Nanoparticles Stabilized With Mpeg-Grafted Poly(L-Lysine): In Vitro And In Vivo Evaluation Of A Potential Theranostic Agent, Alexei A. Bogdanov, Suresh Gupta, Nadezhda Koshkina, Stuart J. Corr, Surong Zhang, Steven A. Curley, Gang Han

Radiology Publications

As the number of diagnostic and therapeutic applications utilizing gold nanoparticles (AuNPs) increases, so does the need for AuNPs that are stable in vivo, biocompatible, and suitable for bioconjugation. We investigated a strategy for AuNP stabilization that uses methoxypolyethylene glycol-graft-poly(l-lysine) copolymer (MPEG-gPLL) bearing free amino groups as a stabilizing molecule. MPEG-gPLL injected into water solutions of HAuCl4 with or without trisodium citrate resulted in spherical (Zav = 36 nm), monodisperse (PDI = 0.27), weakly positively charged nanoparticles (AuNP3) with electron-dense cores (diameter: 10.4 +/- 2.5 nm) and surface amino groups that were amenable to covalent modification. The AuNP3 were ...


Stability Of Lidocaine Tested By Forced Degradation And Its Interactions With Serum Albumin, Lindsay Nichols Jan 2015

Stability Of Lidocaine Tested By Forced Degradation And Its Interactions With Serum Albumin, Lindsay Nichols

STAR (STEM Teacher and Researcher) Presentations

A concern for future long-term manned space expeditions is the ability to treat illnesses with appropriate pharmaceuticals. However, pharmaceuticals degrade faster in space than on Earth presumably due to an abundance of space radiation. The stability of Lidocaine was investigated because it is a common pain reliever currently used on the International Space Station. One of the most common proteins in blood is serum albumin, which acts as a carrier to distribute drugs throughout the body. It is important to know how well the drug binds to serum albumin so that the rate of distribution of Lidocaine-bound protein in blood ...


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.