Pharmacy and Pharmaceutical Sciences Commons^™

Diverse Glycosides From Gardenia Latifolia With Antiviral Activity And Chemosystematic Significance, Shaymaa M. Mohamed, Samir A. Ross, Mai A. M. Ahmed

Faculty and Student Publications

Several influenza pandemics have impacted our life, each with variable prevalence and severity. In a search for natural antivirals, further phytochemical investigation of Gardenia latifolia Aiton, Rubiaceae, was conducted. As a result, five structurally diverse glycosides were isolated, offering valuable chemotaxonomic data. Using the crystal violet technique, three isolates, canthoside C, (6R,7S,8S)-7α-[(β-d-glucopyranosyl) oxy] lyoniresinol, and ecdysanrosin A, were evaluated for their anti-influenza A (H1N1) activities. Based on previously reported anti-inflammatory activity of the guaiane class, we investigated the inhibitory effect of (1R,7R,8S,10R)-7,8,11-trihydroxy-guai-4-ene-3-one 8-O-β-d-glucopyranoside, a rare guaiane sesquiterpene glucoside, on inducible nitric oxide (NO) production by Griess assay. Regarding antiviral assay, …

Tlr4/Nfκb-Mediated Anti-Inflammatory And Antioxidative Effect Of Hexanic And Ethanolic Extracts Of Curcuma Longa L. In Buffalo Mammary Epithelial Cells, Insha Amin, Shahzada Mudasir Rashid, Sheikh Shubeena, Ishraq Hussain

Faculty and Student Publications

Mastitis is the commonest disease of bovines imposing a great economic setback and a drastic public health concern worldwide. Antibiotic resistance is the preliminary con of excessive antibiotics use for disease treatment. Studies validate an alarming increase in the antibiotic resistance of both humans and animals. For ages, medicinal plants have been used to treat a number of ailments in humans and animals, including mastitis. Curcuma longa, or turmeric, is the prerequisite in Indian cooking and has been used in traditional medicine for its magical properties. The rhizome of C. longa possesses significant anti-inflammatory, antibacterial, antifungal, and antioxidative properties. In …

Immunogenetic Role Of Il17a Polymorphism In The Pathogenesis Of Recurrent Miscarriage, Shafat Ali, Sabhiya Majid, Md Niamat Ali, Mujeeb Zafar Banday

Faculty and Student Publications

Interleukin-17A (IL17A) is a proinflammatory cytokine and is assumed to play an important role in fetal rejection. In order to evaluate the potential role of IL17A polymorphism in the pathogenesis of recurrent miscarriage (RM), serum IL17A levels were estimated by ELISA. Single-nucleotide polymorphism was assessed by polymerase chain reaction-restriction fragment-length polymorphism (PCR-RFLP) using gene-specific primers and the EcoNI restriction enzyme. Serum IL17A levels were nonsignificantly (p > 0.5) low in RM patients compared with the control group. IL17A gene amplification by PCR yielded the undigested product of 815 bp, and its digestion with EcoNI enzyme produced 815, 529, 286, and 270 …

Antitrypanosomal, Antitopoisomerase-I, And Cytotoxic Biological Evaluation Of Some African Plants Belonging To Crassulaceae; Chemical Profiling Of Extract Using Uhplc/Qtof-Ms/Ms, Mostafa M. Hegazy, Wael M. Afifi, Ahmed M. Metwaly, Mohamed M. Radwan

Faculty and Student Publications

In our continuous study for some African plants as a source for antitrypanosomally and cytotoxic active drugs, nine different plants belonging to the Crassulaceae family have been selected for the present study. Sedum sieboldii leaves extract showed an antitrypanosomal activity against Trypanosoma brucei with an IC50 value of 8.5 µg/mL. In addition, they have cytotoxic activities against (HCT-116), (HEPG-2) and (MCF-7), with IC50 values of 28.18 ± 0.24, 22.05 ± 0.66, and 26.47 ± 0.85 µg/mL, respectively. Furthermore, the extract displayed inhibition against Topoisomerase-1 with an IC50 value of 1.31 µg/mL. It showed the highest phenolics and flavonoids content among …

Isolation And Characterization Of Flavonoid Naringenin And Evaluation Of Cytotoxic And Biological Efficacy Of Water Lilly (Nymphaea Mexicana Zucc.), Shajrath Din, Saima Hamid, Aadil Yaseen, Ali Mohd Yatoo

Faculty and Student Publications

Despite its limited exploration, Nymphaea mexicana Zucc. can be beneficial if pharmacology, isolation, and biological evaluation are given attention. It is an aquatic species that belongs to the family Nymphaeaceae. The thrust area of the work was the extraction, isolation, and biological evaluation of different extracts of the N. mexicana Zucc. plant. The primary goal of this research was to assess the antimicrobial, antioxidant, and anticancer activities of the extracts and to isolate the target naringenin compound. Comparative FT IR analysis of different extracts of this plant revealed the presence of functional groups of plant secondary metabolites, including polyphenols, flavonoids, …

Bioassay-Guided Fractionation With Antimalarial And Antimicrobial Activities Of Paeonia Officinalis, Mamdouh Nabil Samy, Basma Khalaf Mahmoud, Nourhan Hisham Shady, Usama Ramadan Abdelmohsen

Faculty and Student Publications

Bioassay-guided fractionation technique of roots of Paeonia officinalis led to isolation and structure elucidation of seven known compounds, including four monoterpene glycosides: lactiflorin (1), paeoniflorin (4), galloyl paeoniflorin (5), and (Z)-(1S,5R)-β-pinen-10-yl β-vicianoside (7); two phenolics: benzoic acid (2) and methyl gallate (3); and one sterol glycoside: β-sitosterol 3-O-β-D-glucopyranoside (6). The different fractions and the isolated compounds were evaluated for their antimicrobial and antimalarial activities. Fraction II and III showed antifungal activity against Candida neoformans with IC50 values of 28.11 and 74.37 µg/mL, respectively, compared with the standard fluconazole (IC50 = 4.68 µg/mL), and antibacterial potential against Pseudomonas aeruginosa (IC50 = …

Cannabidiol Loaded Topical Ophthalmic Nanoemulsion Lowers Intraocular Pressure In Normotensive Dutch-Belted Rabbits, Samir Senapati, Ahmed Adel Ali Youssef, Corinne Sweeney, Chuntian Cai

Faculty and Student Publications

Cannabidiol (CBD) is the major non-psychoactive and most widely studied of the cannabinoid constituents and has great therapeutic potential in a variety of diseases. However, contradictory reports in the literature with respect to CBD’s effect on intraocular pressure (IOP) have raised concerns and halted research exploring its use in ocular therapeutics. Therefore, the current investigation aimed to further evaluate CBD’s impact on the IOP in the rabbit model. CBD nanoemulsions, containing Carbopol® 940 NF as a mucoadhesive agent (CBD-NEC), were prepared using hot-homogenization followed by probe sonication. The stability of the formulations post-moist-heat sterilization, in terms of physical and chemical …

Abcg2 Polymorphisms And Predictive Fluoroquinolone Phototoxicity In Nondomestic Felids, Alexandria E. Gochenauer, Dayna L. Dreger, Brian W. Davis, Shawna Cook

Faculty and Student Publications

Fluoroquinolones are a widely used class of chemotherapeutics within veterinary medicine, prized for their broad-spectrum bactericidal activity. These drugs present a known risk of retinal phototoxicity in domestic cats (Felis catus); therefore, using lower doses and alternative antibiotic classes is encouraged in this species. This adverse drug effect of fluoroquinolones, and enrofloxacin specifically, has been determined to be species-specific in domestic felids. Four feline-specific missense variants in ABCG2 result in four amino acid changes (E159M, S279L, H283Q, and T644I) that are unique to the domestic cat compared with multiple other nonfeline mammalian species. These changes alter the ABCG2 protein involved …

How Carbon Nanoparticles, Arbuscular Mycorrhiza, And Compost Mitigate Drought Stress In Maize Plant: A Growth And Biochemical Study, Emad A. Alsherif, Omar Almaghrabi, Ahmed M. Elazzazy, Mohamed Abdel-Mawgoud

Faculty and Student Publications

Drought negatively affects crop growth and development, so it is crucial to develop practical ways to reduce these consequences of water scarcity. The effect of the interactive potential of compost (Comp), mycorrhizal fungi (AMF), and carbon nanoparticles (CNPS) on plant growth, photosynthesis rate, primary metabolism, and secondary metabolism was studied as a novel approach to mitigating drought stress in maize plants. Drought stress significantly reduced maize growth and photosynthesis and altered metabolism. Here, the combined treatments Com-AMF or Com-AMF-CNPs mitigated drought-induced reductions in fresh and dry weights. The treatments with AMF or CNPS significantly increased photosynthesis (by 10%) in comparison …

Discovery Of A Lectin Domain That Regulates Enzyme Activity In Mouse N-Acetylglucosaminyltransferase-Iva (Mgat4a), Masamichi Nagae, Tetsuya Hirata, Hiroaki Tateno, Sushil K. Mishra

Faculty and Student Publications

N-Glycosylation is a common post-translational modification, and the number of GlcNAc branches in N-glycans impacts glycoprotein functions. N-Acetylglucosaminyltransferase-IVa (GnT-IVa, also designated as MGAT4A) forms a β1-4 GlcNAc branch on the α1-3 mannose arm in N-glycans. Downregulation or loss of GnT-IVa causes diabetic phenotypes by dysregulating glucose transporter-2 in pancreatic β-cells. Despite the physiological importance of GnT-IVa, its structure and catalytic mechanism are poorly understood. Here, we identify the lectin domain in mouse GnT-IVa’s C-terminal region. The crystal structure of the lectin domain shows structural similarity to a bacterial GlcNAc-binding lectin. Comprehensive glycan binding assay using 157 glycans and solution NMR …

Milk-Compositional Study Of Metabolites And Pathogens In The Milk Of Bovine Animals Affected With Subclinical Mastitis, Aarif Ali, Manzoor Ur Rahman Mir, Showkat Ahmad Ganie, Saima Mushtaq

Faculty and Student Publications

Bovine milk is an important food component in the human diet due to its nutrient-rich metabolites. However, bovine subclinical mastitis alters the composition and quality of milk. In present study, California mastitis testing, somatic cell count, pH, and electrical conductivity were used as confirmatory tests to detect subclinical mastitis. The primary goal was to study metabolome and identify major pathogens in cows with subclinical mastitis. In this study, 29 metabolites were detected in milk using gas chromatography–mass spectrometry. Volatile acidic compounds, such as hexanoic acid, hexadecanoic acid, lauric acid, octanoic acid, n-decanoic acid, tricosanoic acid, tetradecanoic acid, and hypogeic acid …

Validated Determination Of Nrg1 Ig-Like Domain Structure By Mass Spectrometry Coupled With Computational Modeling, Niloofar Abolhasani Khaje, Alexander Eletsky, Sarah E. Biehn, Charles K. Mobley

Faculty and Student Publications

High resolution hydroxyl radical protein footprinting (HR-HRPF) is a mass spectrometry-based method that measures the solvent exposure of multiple amino acids in a single experiment, offering constraints for experimentally informed computational modeling. HR-HRPF-based modeling has previously been used to accurately model the structure of proteins of known structure, but the technique has never been used to determine the structure of a protein of unknown structure. Here, we present the use of HR-HRPF-based modeling to determine the structure of the Ig-like domain of NRG1, a protein with no close homolog of known structure. Independent determination of the protein structure by both …

Prescribing Trends Of Proton Pump Inhibitors, Antipsychotics And Benzodiazepines Of Medicare Part D Providers, Jennifer M. Toth, Saumil Jadhav, Holly M. Holmes, Manvi Sharma

Faculty and Student Publications

Background: Proton pump inhibitors, benzodiazepines, and antipsychotics are considered potentially inappropriate medications in older adults according to the American Geriatric Society Beers Criteria, and deprescribing algorithms have been developed to guide use of these drug classes. The objective of this study was to describe the number of beneficiaries prescribed these medications, provider specialty and regional trends in prescribing, and the aggregate costs for these claims in Medicare Part D. Methods: This was a retrospective cross-sectional study using publicly available Medicare Provider Utilization and Payment Data: Part D Prescriber data for years 2013–2019. Descriptive statistics and the Cochrane-Armitage test were used …

Utility Of Fatty Acid Profile And In Vitro Immune Cell Activation For Chemical And Biological Standardization Of Arthrospira/Limnospira, Jungmoo Huh, Jin Zhang, Radka Hauerová, Joseph Lee

Faculty and Student Publications

Commercially cultivated Limnospira (species formerly classified to genus Arthrospira) is a popular food/supplement consumed by millions of people worldwide for health benefits. The objective of the current research was to advance the standardization technology for Limnospira. Quantitative methods were established to detect fatty acids as potential chemical markers and immune-enhancing activity. Analysis of 20 different batches of biomass obtained from one commercial grower demonstrated that there was a statistically significant relationship between the sum of two fatty acids (linoleic and γ-linolenic) and Toll-like receptor (TLR)2/TLR1-dependent activation (R2 = 0.48, p = 0.0007). Investigation of 12 biomass samples sourced from growers …

Comparative Pharmacokinetics And Tissue Distribution Of Primaquine Enantiomers In Mice, Pius S. Fasinu, Narayan D. Chaurasiya, N. P. Dhammika Nanayakkara, Yan‑Hong ‑H Wang

Faculty and Student Publications

Background: Primaquine (PQ) has been used for the radical cure of relapsing Plasmodium vivax malaria for more than 60 years. PQ is also recommended for prophylaxis and prevention of transmission of Plasmodium falciparum. However, clinical utility of PQ has been limited due to toxicity in individuals with genetic deficiencies in glucose 6-phosphate dehydrogenase (G6PD). PQ is currently approved for clinical use as a racemic mixture. Recent studies in animals as well as humans have established differential pharmacological and toxicological properties of the two enantiomers of PQ. This has been attributed to differential metabolism and pharmacokinetics of individual PQ enantiomers. The …

A Distinct Mechanism Of C-Type Inactivation In The Kv-Like Kcsa Mutant E71v, Ahmed Rohaim, Bram J. A. Vermeulen, Jing Li, Felix Kümmerer

Faculty and Student Publications

C-type inactivation is of great physiological importance in voltage-activated K+ channels (Kv), but its structural basis remains unresolved. Knowledge about C-type inactivation has been largely deduced from the bacterial K+ channel KcsA, whose selectivity filter constricts under inactivating conditions. However, the filter is highly sensitive to its molecular environment, which is different in Kv channels than in KcsA. In particular, a glutamic acid residue at position 71 along the pore helix in KcsA is substituted by a valine conserved in most Kv channels, suggesting that this side chain is a molecular determinant of function. Here, a combination of X-ray crystallography, …

Understanding The Dynamics Of The Structural States Of Cannabinoid Receptors And The Role Of Different Modulators, Anjela Manandhar, Mona H. Haron, Michael L. Klein, Khaled Elokely

Faculty and Student Publications

The cannabinoid receptors CB1R and CB2R are members of the G protein-coupled receptor (GPCR) family. These receptors have recently come to light as possible therapeutic targets for conditions affecting the central nervous system. However, because CB1R is known to have psychoactive side effects, its potential as a drug target is constrained. Therefore, targeting CB2R has become the primary focus of recent research. Using various molecular modeling studies, we analyzed the active, inactive, and intermediate states of both CBRs in this study. We conducted in-depth research on the binding properties of various groups of cannabinoid modulators, including agonists, antagonists, and inverse …

Evaluation Of Piperacillin/Tazobactam Utilization In Suspected Urinary Tract Infections At A Community Hospital, Adam P. Yagodinski, Jamie Gaul Pharmd, Bcps, Dana Lorber Pharmd, Bcps, Alissa Keillor Pharmd

Parkview Pharmacy Department

Poster presentation completed at ASHP Midyear Clinical Conference & Exhibition.

Objective: Evaluate and characterize the utilization of piperacillin/tazobactam in patients with a suspected urinary tract infection (UTI) at a community hospital in Fort Wayne, Indiana.

Characterization Of Vancomycin Use At A Community Hospital, Caleb Hoppe Pharmd Candidate, Jamie Gaul Pharmd, Bcps, Christina Ford Pharm, Bcpsd

Parkview Pharmacy Department

Poster presentation completed at ASHP Midyear Clinical Conference & Exhibition.

Objective: To characterize the use of vancomycin medication therapy at a non-profit community hospital (Parkview Regional Medical Center) in preparation for a potential change to AUC:MIC dosing and monitoring.

Design, Synthesis, And Evaluation Of N-Methylated H2r2w4, Talal Alrubaie

Pharmaceutical Sciences (MS) Theses

Antimicrobial peptides (AMPs) are potential candidates for developing antibiotics against multidrug-resistant bacteria. We have recently developed a potent cyclic AMP containing histidine (H), arginine (R), and tryptophan (W) residues named [H₂R₂W₄]. This peptide showed antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA) and Staphylococcus aureus (SA) with a minimum inhibitor concentration (MIC) of 3.1 μg/mL and a MIC of 6.2 μg/mL for Escherichia coli (E. coli). However, it displayed a mild cytotoxicity with cell viability of approximately 80% against normal human lung cells (MRC-5) and ~60% against normal human kidney cells (HEK-293) at the …