Medicinal and Pharmaceutical Chemistry Commons^™

Design, Synthesis, And Characterization Of Multi-Targeting Pyrrolopyrimidine Antifolates As Potential Single Agent Chemotherapeutic Entities, Tejashree Magdum

Electronic Theses and Dissertations

In cancer chemotherapy, the currently marketed antifolates have two major disadvantages: dose-limiting toxicities to normal tissues and susceptibility to drug resistance. These are due to their major transport by the ubiquitously expressed transporter and mutagenesis in enzymes present in cancer cells. This thesis describes an introduction, background, and research progress in antimetabolites-antifolates designed to multi-target (a) one-carbon metabolism and de novo nucleotide synthesis pathway and (b) target overexpressed transporter in cancer cells for selective tumor-targeting.

Cancer cells transport folate through three transporters: ubiquitously expressed reduced folate carrier (RFC), limitedly expressed proton-coupled folate transporter (PCFT), and folate receptors (FRs). The research …

Fda Approves Neffy®- First Nasal Spray For Anaphylaxis, Abigail Carter, Penlope Mazivanhanga, Haylee Whyde, Rileigh Rahrig, Ashley Jacob, Anna Spalvieri, Joshua Honaker, Samantha Mccord, Andrew Roecker

Pharmacy and Wellness Review

Between 1.6 and 5.1% of the United States population have experienced anaphylaxis, a severe allergic reaction.1 Anaphylaxis occurs when someone is exposed to an allergen, most commonly foods, medications, and insect venom. Epinephrine is the first-line agent for anaphylaxis treatment, and it is critical to administer this medication immediately after the onset of anaphylactic symptoms to prevent worsening that could lead to death. Epinephrine, more commonly known as EpiPen® or Auvi-Q®, has historically only been available as an intramuscular (IM) injection. Many people are afraid, anxious, or uneducated on how to properly give someone an IM injection, causing anaphylaxis treatment …

Proteoglycan 4 (Lubricin) And Regulation Of Xanthine Oxidase In Synovial Macrophage As A Mechanism Of Controlling Synovitis, Khaled A. Elsaid, Ling X. Zhang, Thomas Zhao, Ava Marks, Derek Jenkins, Tannin A. Schmidt, Gregory D. Jay

Pharmacy Faculty Articles and Research

Background

Synovial macrophages (SMs) are important effectors of joint health and disease. A novel Cx3CR1 + TREM2 + SM population expressing the tight junction protein claudin-5, was recently discovered in synovial lining. Ablation of these SMs was associated with onset of arthritis. Proteoglycan 4 (PRG4) is a mucinous glycoprotein that fulfills lubricating and homeostatic roles in the joint. The aim of this work is to study the role of PRG4 in modulating synovitis in the context of SM homeostasis and assess the contribution of xanthine oxidase (XO)-hypoxia inducible factor alpha (HIF-1a) axis to this regulation.

Methods

We used Prg4FrtloxP/FrtloxP …

Comparing Multivalent Cross-Linked Sodium Alginate/ Montmorillonite Beads Containing Curcumin Or Cayenne Pepper As Drug Carriers And Their Antimicrobial Resistance, Shionainn Traynor, Shubham Sharma

SURE Journal: Science Undergraduate Research Experience Journal

The aim of the following work was to investigate and compare curcumin and cayenne pepper in microbeads composed of sodium alginate (SA) crosslinked with montmorillonite (MMT) to act as drug carriers and their antimicrobial resistance. The microbeads were prepared through ion-exchange in multivalent solutions of CaCl₂, MgCl₂ and AlCl₃. The microbeads were characterized by Scanning Electron Microscopy (SEM), Energy Dispersive X-ray analysis (EDX) and the time required for intercalation of curcumin and cayenne pepper with MMT. Simulated intestinal fluid (pH 7.3) and gastric fluid (pH 1.2) at 37°C were used for comparison in swelling studies. …

A Conjugate Of An Egfr-Binding Peptide And Doxorubicin Shows Selective Toxicity To Triple-Negative Breast Cancer Cells, Phi-Phung Than, Shih-Jing Yao, Emad Althagafi, Kamaljit Kaur

Pharmacy Faculty Articles and Research

Selective targeting of cancer cells via overexpressed cell-surface receptors is a promising strategy to enhance chemotherapy efficacy and minimize off-target side effects. In this study, we designed peptide 31 (YHWYGYTPERVI) to target the overexpressed epidermal growth factor receptor (EGFR) in triple-negative breast cancer (TNBC) cells. Peptide 31 is internalized by TNBC cells through EGFR-mediated endocytosis and shares sequence and structural similarities with human EGF (hEGF), a natural EGFR ligand. Unlike hEGF, peptide 31 does not induce cell migration in TNBC cells. A novel conjugate of peptide 31 with doxorubicin (Dox) retains selectivity for TNBC cells and exhibits significant toxicity comparable …

Design, Synthesis, And Nmr-Guided Characterization Of A Targeted Covalent Inhibitor-Like Molecule Against Ivyp1 From P. Aeruginosa, Samuel Taylor Moore

Master's Theses

Multi-drug resistance poses a serious threat to future generations and historical antibiotic pipelines; consequently, the medical and economic burdens associated with treating multidrug-resistant bacteria are substantiated. In this context, P. aeruginosa (PA) emerges as one of the most significant healthcare challenges, being a leading cause of resistance-associated mortality worldwide. Despite modern efforts to combat these poor outcomes, drug-resistant cases continue to rise, and the need for novel antibiotic treatment is apparent. To this end, we investigated relevant resistance mechanisms and past antibiotic targets within PA, and in doing so, we identified relationships between peptidoglycan biology and a periplasmic protein, Inhibitor …

Voltammetric Analysis Of Pholcodine On Graphene-Modified Gnps/Pts With Green Assessment, Ekram Hany Mohamed, Nahla Abdel Shafy, Hadeer Elkhouly, Nehal Khoudary, Hany Darwish, Aswak Alanzi, Ibrahim Naguib

Pharmacy

Pholcodine, an anti-tussive medication widely used as an over-the-counter, OTC drug, has recently faced restrictions in several countries. This paper presents a sensitive electrochemical approach for pholcodine detection. The electrochemical method involved fabricating a graphene nanoplatelets electrode, incorporating polythiophene nanospheres polymer to promote electron transfer and increase the activated surface area. Characterization of the fabricated electrode was performed using transmission electron microscopy, ATR-Fourier-transform infrared spectroscopy, X-ray crystallography, X-ray photoelectron spectroscopy, and electrochemical impedance spectroscopy. The electrochemical behavior of pholcodine with the fabricated electrode was investigated using cyclic voltammetry, chronoamperometry, square wave voltammetry (SWV), and differential pulse voltammetry (DPV). The developed …

Synthesis Of Photocleavable Molecules For Neurological Applications, Nishal Madujith Egodawaththa Arachchilage Don

Theses and Dissertations

In recent biomedical research, the precise control of molecular dynamics through light activation has emerged as a powerful tool, particularly in the field of neurobiology. This approach involves the use of photocleavable cages or photoprotective groups (PPGs) that are chemically tethered to biologically active molecules such as neurotransmitters or calcium chelators. These cages remain inert until exposed to specific wavelengths of light, typically in the visible range, triggering the release of the active compound with high spatiotemporal precision.

For neurotransmitter systems, such as glutamate (Glu), which plays a critical role in synaptic transmission and memory formation, researchers have developed novel …

Unravelling The Erythropoietin Heterodimeric Complex: In Silico Analysis Of Complex Assembly And Binding Interface, Atiya Habib, Urooj Qureshi, Mohammad Nur-E-Alam, Aftab Ahmed, Zaheer Ul-Haq

Pharmacy Faculty Articles and Research

Erythropoietin (Epo), a glycosylated protein categorized as a member of the cytokine family, is responsible for the modulation of erythrogenesis. Besides this, the nonhaematopoietic effects of Epo are associated with tissue-protective activity via an antiapoptotic pathway. This function of Epo is linked with its heterodimeric form, i.e. EpoR/βcR belonging to the cytokine family as well. Both receptors are dissected into three domains: extracellular (also known as ligand-binding domain), transmembrane and cytoplasmic domain. The transmembrane and cytoplasmic domains are assumed to play a paramount role in dimerization and tissue protection. However, the tertiary structure of cytoplasmic domains of both …

Effects Of Sex And Estrous Cycle On Extended-Access Oxycodone Self-Administration And Cue-Induced Drug Seeking Behavior, Bhumiben P Patel, Jessica A Loweth

Rowan-Virtua School of Osteopathic Medicine Departmental Research

INTRODUCTION: Increasing evidence indicates that sex is a factor that impacts the abuse liability and relapse vulnerability of prescription opioids like oxycodone. However, while women are more likely than men to be prescribed and to use these drugs, the impact of sex and ovarian hormones on prescription opioid use and relapse vulnerability remains unclear. Accurately assessing these measures is complicated by the fact that chronic opioid exposure can lower ovarian hormone levels and cause cycle irregularities.

METHODS: Adult male and female Sprague-Dawley rats self-administered oxycodone (0.1 mg/kg/infusion) under extended-access conditions (6 h/day, 10 days) followed by forced abstinence. Separate groups …

Synthesis And Evaluation Of Cyclic Peptide-Dasatinib Conjugates As Anti-Melanoma Agents, Shaban Darwish, Dorna Davani-Davari, Shirley Tong, Rakesh Kumar Tiwari, Sun Yang, Keykavous Parang

Pharmacy Faculty Articles and Research

Herein, we synthesized two amphiphilic cyclic peptides, incorporating tryptophan and arginine residues, linked to dasatinib via a Cathepsin B-sensitive tetrapeptide (Gly-Phe-Leu-Gly). To mitigate steric hindrance and optimize drug release, we integrated two different linkers, succinate and glutarate, between the drug and peptide. The synthesis involved solid-phase techniques for the assembly of the peptide, followed by the coupling of the peptide on-resin with the linker, mild cleavage, and solution-phase cyclization. Conjugation of the peptide-attached linker with dasatinib was conducted in the presence of N-methylmorpholine and 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide (EDC), generating the novel prodrugs. The synthesized compounds were characterized by high-resolution mass …

Identification Of New Leads Against Ubiquitin Specific Protease-7 (Usp7): A Step Towards The Potential Treatment Of Cancers, Sumaira Javaid, Seema Zadi, Muhammad Awais, Atai-Tul Wahab, Humaira Zafar, Innokentiy Maslennikov, M. Iqbal Choudhary

Pharmacy Faculty Articles and Research

Ubiquitin-specific protease-7 (USP7) is an important drug target as it regulates multiple proteins and genes (such as MDM2 and p53) with roles in cancer progression. Its inhibition can hinder the function of oncogenes, increase tumor suppression, and enhance immune response. The current study was designed to express USP7 in a prokaryotic system, followed by screening of small molecules against it using biophysical methods, primarily STD-NMR technique. Among them, 12 compounds showed interaction with USP7 as inferred from NMR-based screening. These compounds further caused destabilization of USP7 by reducing its melting temperature (T_m) up to 6 °C in …

The Role Of Peptides In Combatting Hiv Infection: Applications And Insights, Naiera M. Helmy, Keykavous Parang

Pharmacy Faculty Articles and Research

Peptide-based inhibitors represent a promising approach for the treatment of HIV-1, offering a range of potential advantages, including specificity, low toxicity, and the ability to target various stages of the viral lifecycle. This review outlines the current state of research on peptide-based anti-HIV therapies, highlighting key advancements and identifying future research directions. Over the past few years, there has been significant progress in developing synthetic peptide-based drugs that target various stages of the viral life cycle, including entry and replication. These approaches aim to create effective anti-HIV therapies. Additionally, peptides have proven valuable in the development of anti-HIV vaccines. In …

Subterranean Medicinal Bottles Are Treasures That Reveal The Growth Of Lincoln's Early Drug Stores, Mark Griep, June Weber, Erik Schulz, Effie Athanassopoulos

Department of Anthropology: Faculty Publications

Archeologists unearthed medicine bottles embossed with the names of nine early Lincoln (Nebraska) drug stores, giving insight into the rapid growth of pharmacies and health care from the 1880s up to the Pure Food and Drug Act of 1906.

The Impact Of Pdcd4, A Translation Inhibitor, On Drug Resistance, Qing Wang, Hsin-Sheng Yang

Markey Cancer Center Faculty Publications

Programmed cell death 4 (Pdcd4) is a tumor suppressor, which has been demonstrated to efficiently suppress tumorigenesis. Biochemically, Pdcd4 binds with translation initiation factor 4A and represses protein translation. Beyond its role in tumor suppression, growing evidence suggests that Pdcd4 enhances the chemosensitivity of several anticancer drugs. To date, numerous translational targets of Pdcd4 have been identified. These targets govern important signal transduction pathways, and their attenuation may improve chemosensitivity or overcome drug resistance. This review will discuss the signal transduction pathways regulated by Pdcd4 and the potential mechanisms through which Pdcd4 enhances chemosensitivity or counteracts drug resistance.

Authentication Of Shallots From Brebes Using Gas Chromatography Fingerprinting Technique Combined With Chemometrics, Yana Setyani Pradina, Adelia Puteri, Gina Fauzia Rachma, Nazwa Balqis, Gerli Puspita Anggraini, Hendri Wasito

Makara Journal of Science

Shallots from Brebes, also called Bima Brebes, have a more pungent aroma compared to other varieties. Its high demand results in increased prices in the market, leading to frequent cases of fraud wherein Bima Brebes shallots are replaced with other types of shallots. This study aimed to develop an analytical method using gas chromatography–flame ionization detector (GC-FID) fingerprinting combined with chemometrics to authenticate Bima Brebes shallots. Essential oils were extracted through ultrasonic hydrodistillation, followed by organoleptic, refractive index, GC-FID fingerprinting and chemometric analysis. The yield value of the five studied shallot varieties ranged from 0.02% to 0.08% w/w. Meanwhile, the …

Cellular Uptake And Computational Analysis Of [131i]-Xanthine And [131i]-Hypoxanthine In Human Prostate Cancer Cell Line (Lncap), Hendris Wongso, Isa Mahendra, Yanuar Setiadi, Badra Sanditya Rattyananda, Asep Rizaludin, Ni Made Yuktikamura Galih Pranisuari, Crhisterra Ellen Kusumaningrum

Makara Journal of Science

Potent radiolabelled compounds eligible for therapy of prostate cancer need to be developed. Hence, we developed two candidate therapeutic agents bearing the iodine-131 (¹³¹I) radionuclide, namely, [¹³¹I]-xanthine (3,7-dihydropurine-2,6-dione) and [¹³¹I]-hypoxanthine (1,9-dihydro-6H-purin-6-one). The radiolabelled compounds were subjected to a cellular uptake study, which was accomplished by incubating [¹³¹I]-xanthine and [¹³¹I]-hypoxanthine with the human prostate cancer cell line (LNCaP) for 5, 15, 30, 60, and 90 min. Results showed that the accumulation of both [¹³¹I]-xanthine and [¹³¹I]-hypoxanthine in prostate cancer cells was significantly higher than the …

An Unusual Case Of Metronidazole-Induced Encephalopathy In A Patient With Hereditary Hemorrhagic Telangiectasia, Tina H. Dao, Kinza Khan, Christopher D. Jackson

Journal of Community Hospital Internal Medicine Perspectives

Metronidazole-induced encephalopathy (MIE) is a rare toxic encephalopathy. We describe a reversible MIE case in a patient with hereditary hemorrhagic telangiectasia (HHT), treated with metronidazole for brain abscess, who developed dizziness, weakness, dysarthria, and severe dysmetria. His Magnetic Resonance Imaging (MRI) brain revealed bilateral, symmetric lesions in bilateral symmetrical regions of increased intensity in the medullary olives, cerebellar dentate nuclei, and the dorsal pons, all characteristic of MIE. Upon metronidazole discontinuation, the patient experienced significant symptom improvement, with subsequent MRI showing resolution of the lesions

Incorporating Solvation Thermodynamic Mapping In Computer-Aided Drug Design, Yeonji Ji

Dissertations, Theses, and Capstone Projects

Advancements in computational techniques have revolutionized structure-based drug design, substantially improving the efficiency and effectiveness of the drug discovery process by reducing time, costs, and labor requirements. These advancements include various methods, such as investigating small molecule ligands binding to proteins, exploring alternative protein conformations, and solvation mapping on the protein surfaces. Among these methods, understanding the correlation between protein-ligand binding and the role of solvation is important.

A fundamental concept in protein-ligand binding is shape and electrostatic complementarity, which is complicated by the inherent flexibility of proteins. In the absence of small molecule ligands, proteins are complementary to surface …

Challenges And Future Perspective Of Gastroretentive Mucoadhesive Dosage Forms, Rayhan Akbar, Heri Setiawan, Baitha Palanggatan Maggadani, Raditya Iswandana, Kurnia Sari Setio Putri

Pharmaceutical Sciences and Research

Gastroretentive Mucoadhesive Dosage Form (GMDF) is one type of Gastroretentive Drug Delivery System (GRDDS) technology designed to exploit the adhesiveness of dosage forms in the gastric mucosa. This aims to increase drug residence time, enhance drug solubility and absorption, and ultimately improve drug bioavailability and therapeutic effect. Various studies have explored the use of different polymers to develop GMDF systems and dosage forms. However, despite extensive research in this field, there are still limited GMDF products approved by the US FDA and INA FDA. Therefore, this review addresses the challenges in developing GMDF, its current state, and potential future opportunities. …

Recent Updates On Dried Blood Spot And Volumetric Absorptive Microsampling As Microsampling Technique For Antiepileptic Drug Determination: A Systematic Review, Asmiladita Pridilla, Yahdiana Harahap, Denni Joko Purwanto, Baitha Palanggatan Maggadani

Pharmaceutical Sciences and Research

Implementation of Therapeutic Drug Monitoring (TDM) can be useful for patients with uncontrolled seizures. This review article aims to collect and compare the recent development of bioanalytical methods for antiepileptic drugs using microsampling techniques, namely DBS (Dried Blood Spot) and VAMS (Volumetric Absorptive Microsampling). Studies were searched through databases, namely Science Direct, Pubmed, and the Google Scholar search engine using pre-determined keywords. Studies published between 2019 and 2024 and used micro-sampling techniques for antiepileptic drug analysis were included. Non-English studies, non-related studies, duplication, and full text unavailable were excluded. Primary sources were used to build a conclusion regarding the purpose …

Identifying The Roles Of Mir-17 In Ciliogenesis And Cell Cycle, Ashwaq Alanazi, Ayan K. Barui, Ashraf M. Mohieldin, Ankan Gupta, Ramani Ramachandran, Surya M. Nauli

Pharmacy Faculty Articles and Research

Emerging evidence suggests a significant contribution of primary cilia to cell division and proliferation. MicroRNAs, especially miR-17, contribute to cell cycle regulation and proliferation. Recent investigations have highlighted the dysregulated expression of miR-17 in various malignancies, underlining its potential role in cancer. However, the correlation between primary cilia and miR-17 has yet to be fully elucidated. The present study examines the presence of miR-17 in primary cilia. The miR-17 expression is studied in selected ciliary protein knockdown cells. Using in situ hybridization (ISH), we identified the subcellular localization of miR-17 in both cilium and cell body. We confirmed the importance …

The Potential Renoprotective Effects Of Ticagrelor In Rhabdomyolysis-Induced Acute Kidney Injury In Rat, Zahraa Talib Hussein, Ayad Ali Hussein

Maaen Journal for Medical Sciences

Background: Rhabdomyolysis is a potentially lethal range of symptoms results from muscle cell destruction. It is recognized by the escape of cell contents such as myoglobin, creatine kinase, and electrolyte into the bloodstream then undergo glomeruli filtering. Therefore, among the most dangerous complication of rhabdomyolysis is acute renal injury. The complex and interrelated processes underlying rhabdomyolysis that ends with acute kidney injury include obstruction and damage of tubules, inflammation, and intrarenal vasoconstriction (activation of the sympathetic, renin-angiotensin).Glycerol is frequently used to inflict this kind of harm when used as a single dose injection that given intramuscularly to an animal …

Design, Synthesis, And Evaluation Of Oleyl-Wrh Peptides For Sirna Delivery, Mrigank Shekhar Rai, Muhammad Imran Sajid, Jonathan Moreno, Keykavous Parang, Rakesh Kumar Tiwari

Pharmacy Faculty Articles and Research

Delivering nucleic acid therapeutics across cell membranes is a significant challenge. Cell-penetrating peptides (CPPs) containing arginine (R), tryptophan (W), and histidine (H) show promise for siRNA delivery. To improve siRNA delivery and silence a model STAT3 gene, we hypothesized that oleyl acylation to CPPs, specifically (WRH)n, would enhance STAT3 silencing efficiency in breast and ovarian cancer cells. Using Fmoc/tBu solid-phase peptide chemistry, we synthesized, purified, and characterized the oleyl-conjugated (WRH)n (n = 1–4) peptides. The peptide/siRNA complexes were non-cytotoxic at N/P 40 (~20 μM) against MDA-MB-231, MCF-7, SK-OV-3, and HEK-293 cells after 72 h incubation. All peptide/siRNA complexes showed serum …

Preventive Effects Of Quercetin On The Leaky Gut By Suppression Of Il-1beta-Induced Transcription Factors Involved In An Inflammatory Pathway In Colonic Epithelial Cells, Wannaporn Chayalak, Sumpun Thammacharoen, Chatsri Deachapunya, Sutthasinee Poonyachoti

The Thai Journal of Veterinary Medicine

Flavonol quercetin (Q), found in vegetables and fruits, demonstrates the most potent anti-inflammatory effect. The preventive effect and cellular mechanisms of Q (Q1, Q10, and Q100 µM) on IL-1β induced leaky gut via the signaling molecules of inflammatory pathway, NF-κB p65-iκB/or p38/ERK1/2/MLCK/phospho(p)-MLC were investigated in Caco-2 cells. The cytotoxic effect of Q was initially determined by MTT assay. Transepithelial electrical resistance (TER) and apical-to-basolateral fluorescein isothiocyanate-labeled dextran (FD-4) flux were used to determine paracellular permeability. The protein expression of signaling molecules was examined by Western blot analysis, and their target MLCK mRNA expression was determined using real-time PCR. All Q …

One More Negative Regulator Of Ac6: S-Nitrosylation, Isabella Cattani-Cavalieri, Rennolds S. Ostrom

Pharmacy Faculty Articles and Research

"In this issue of the Journal, Maghsoudi and colleagues (pp. 82–96) report a series of studies that delineate the biochemical and pharmacological mechanism of this resistance (4). The study focuses on adenylyl cyclase (AC), an enzyme crucial for pulmonary vasodilation through its action of synthesizing cAMP. There are nine isoforms of AC (AC1–AC9) that are all stimulated by Gs but otherwise are distinct in their regulatory qualities, subcellular localization, and expression profiles throughout the body (5). AC6 plays a significant role in fetal and neonatal lung, especially in pulmonary artery smooth muscle cells, where …

Review Of Mpges-1 Inhibitors Based On The Benzoxazole And Its Isostere Scaffold For The Treatment Of Inflammatory Diseases, Abdullah M. Alwagdani

Longitudinal Scholar's Project

The vital role of the prostanoid pathway in inflammation, pain, cancer, Alzheimer’s and many other diseases has attracted the drug discovery community to discover targets for therapeutic development. Although existing non-steroidal anti-inflammatory drugs (NSAIDs) inhibiting cyclooxygenases (COX) are widely used, the side effects of these NSAIDs limit the ling time medication. Microsomal prostaglandin E synthase-1 (mPGES-1) is an attractive target that is overexpressed during inflammations, and it could be a safe alternative to NSAIDs for treating inflammatory diseases.Since the discovery of mPGES-1 in 1997, many inhibitors have been developed since 2001. Only a few compounds were able to make it …

Potent And Selective Small Molecule Mcl-1 Inhibitor Demonstrates Anti-Myeloma Activity And Overcomes Chemotherapy Resistance, Omar Sami Faleh Al-Odat

Theses and Dissertations

Despite a record number of clinical studies investigating various anti-myeloma treatments, the 5-year survival rate for multiple myeloma (MM) patients in the US is only 55%, and nearly all patients relapse. Poor patient outcomes demonstrate that myeloma cells are "born to survive” which means they can adapt and evolve following treatment. Thus, new therapeutic approaches to combat survival mechanisms and target treatment resistance are required. Importantly, Mcl-1, anti-apoptotic protein, is required for the development of MM and treatment resistance. This study looks at the possibility of KS18, a selective Mcl-1 inhibitor, to treat MM and overcome resistance. Our investigation demonstrates …

Mechanistic Study Of Antimicrobial Effectiveness Of Cyclic Amphipathic Peptide [R4W4] Against Methicillin-Resistant Staphylococcus Aureus Clinical Isolates, Ajayi David Akinwale, Keykavous Parang, Rakesh Kumar Tiwari, Jason Yamaki

Pharmacy Faculty Articles and Research

Antimicrobial peptides (AMPs) are being explored as a potential strategy to combat antibiotic resistance due to their ability to reduce susceptibility to antibiotics. This study explored whether the [R₄W₄] peptide mode of action is bacteriostatic or bactericidal using modified two-fold serial dilution and evaluating the synergism between gentamicin and [R₄W₄] against Escherichia coli (E. coli) and methicillin-resistant Staphylococcus aureus (MRSA) by a checkered board assay. [R₄W₄] exhibited bactericidal activity against bacterial isolates (MBC/MIC ≤ 4), with a synergistic effect with gentamicin against E. coli (FICI = 0.3) but …

Mechanistic Insight Into The Mode Of Inhibition Of Dietary Flavonoids; Targeting Macrophage Migration Inhibitory Factor, Ali Raza Siddiqui, Mamona Mushtaq, Madiha Sardar, Lubna Atta, Mohammad Nur-E-Alam, Aftab Ahmad, Zaheer Ul-Haq

Pharmacy Faculty Articles and Research

Introduction: The Macrophage Migration Inhibitory Factor (MIF), a key pro-inflammatory mediator, is responsible for modulating immune responses. An array of inflammatory and autoimmune diseases has been linked to the dysregulated activity of MIF. The significance in physiological as well as pathophysiological phenomena underscores the potential of MIF as an attractive target with pharmacological relevance. Extensive research in past has uncovered a number of inhibitors, while the ISO-1, or (S, R)-3-(4-hydroxyphenyl)-4,5-dihydro-5-isoxazole acetic acid methyl ester being recognized as a benchmark standard so far. Recent work by Yang and coworkers identified five promising dietary flavonoids, with superior activity compared to the standard …