Medicinal and Pharmaceutical Chemistry Commons^™

Phytochemical And In-Vitro Cytotoxic Analyses Of Flavonoid Species Isolated From Chromolaena Leivensis, Luke A. Bryant

Electronic Theses and Dissertations

As a leading cause of death worldwide, cancer and its treatments remain a primary source of interest among researchers. Modern studies are looking into bioselective cytotoxicity to create new chemotherapies that do not have the same harsh side effects as those we use today. Natural product research has a promising future for the development of such treatments. Specifically, polar flavonoids may be the key to a bioselective treatment. Such flavonoid species are native to plants, often within flower petals or within the body. A natural antioxidant, they are designed not to harm healthy cells. This study focuses on the plant …

Sirt1 And Ifi16 Cooperatively Regulate Hbv Replication Via Epigenetic Modulation And Innate Immune Activation, Zahra Zahid Piracha, Umar Saeed, Neelam Abid, Syed Shahan Gilani, Hafiz Ahmad Bilal Akhtar Chughtai, Areesha Wasti, Muhammad Waseem, Dilber Uzun Ozsahin, Andromeda M. Nauli, Surya M. Nauli

Pharmacy Faculty Articles and Research

Background

Hepatitis B virus (HBV) establishes persistent infection through the formation of a covalently closed circular DNA (cccDNA) minichromosome, which enables immune evasion and sustained viral replication. While SIRT1, IFI16, and STING are known to modulate antiviral pathways, their cooperative role in regulating HBV transcription and host immunity remains poorly defined.

Methods

We investigated the functional interplay between SIRT1, IFI16, and STING using confocal microscopy, chromatin immunoprecipitation (ChIP), gene silencing, and quantitative PCR in HBV-replicating cell models. Interactions with HBV cccDNA and effects on viral transcription and interferon-stimulated gene (ISG) expression were analyzed. Northern blotting and RT-qPCR were used to …

Investigation Of Warfarin–Human Serum Albumin Binding By Ultrafast Affinity Extraction Using Single- And Dual-Column Affinity Microcolumn Systems, Samiul Alim

Department of Chemistry: Dissertations, Theses, and Student Research

This dissertation examined the interaction of warfarin with human serum albumin (HSA) by using affinity chromatography, with particular emphasis on ultrafast affinity extraction (UAE) and affinity microcolumns. HSA affinity supports were prepared by immobilizing HSA onto diol-bonded silica via Schiff base chemistry and used to prepare affinity microcolumns for chromatographic studies under physiological-like conditions at pH 7.4 and 37.0 °C. UAE studies were performed to investigate the effects of residence time, flow rate, and column configuration on the measured apparent free fraction of warfarin and on the calculated apparent binding parameters. The results showed that the measured apparent free fraction …

Fda Approval Of Etripamil For The Treatment Of Paroxysmal Supraventricular Tachycardia, Kiley Devoll, Daniella Egbujor, Katy Grainger, Katherine Cook, Victoria Niese, Connor Dains, Brenna Hissong, Andrew Roecker

Pharmacy and Wellness Review

Paroxysmal supraventricular tachycardia (PSVT) is characterized by sudden, brief, intermittent episodes that result in a heart rate of 150 to 250 beats per minute (bpm). PSVT is difficult to diagnose, making proper treatment challenging. According to the 2015 American Heart Association (AHA)/American College of Cardiology (ACC)/Heart Rhythm Society (HRS) guidelines, current pharmacologic recommendations for PSVT include adenosine, verapamil, diltiazem, or nonpharmacologic vagal maneuvers.¹ These treatments each have a variety of adverse effects, contraindications, and dosing considerations, which highlight a need for novel therapies for the acute treatment and maintenance of PSVT.¹ The NODE-301 trial assessed the safety and …

Effects Of Normothermic Hepatic Ischemia–Reperfusion Injury On The Hepatic Disposition Of Arachidonic Acid And Its Cytochrome P450-Generated Metabolites In Rats, Vindhya Edpuganti, Reza Mehvar

Pharmacy Faculty Articles and Research

Purpose

Cytochrome P450 (P450) metabolites of arachidonic acid (AA) are potential therapeutic targets in ischemia–reperfusion (IR) injury, yet their disposition and actions in hepatic IR are unknown. Cellular AA and its P450 metabolites are primarily bound to lipid membranes, resulting in negligible free concentrations. This study investigates how hepatic IR injury impacts the disposition of free AA and its major P450 metabolites in rats.

Methods

Rats underwent 60 min of partial (70%) ischemia or sham surgery, followed by 5 min, 3 h, or 24 h of reperfusion. The effects of IR injury on free concentrations of AA and its major …

Herbularyo (Folk Healer): An Herbal Medicine Card Game, Maryjane T. Magsino, Inah Marie Q. Rivera, Armando M. Guidote, Genejane M. Adarlo

Chemistry Faculty Publications

Herbularyo, a card game teaching about herbal plants (HPs), was created and evaluated as a viable educational card game based on Tuomisto and Aksela’s criteria. A quasi-experiment was performed on 81 Grade 8 students from a private high school and 50 Grade 11 from a public high school. Independent t-test revealed that the control group (CG) and experimental group (EG) (p=0.386), and EG1 (played ≤5) and EG2 (played >5) (p=0.681) are not comparable with each other. Paired t-test showed EG performed better (p=0.001) than CG (p=0.901) whereas ANCOVA showed that playing Herbularyo improved students’ information retention (p=0.006). EG1 and EG2 …

Synthetic Explorations Towards Phenyl Benzazepine-Inspired Scaffolds And Synthesis Of Minor Cannabinoid Derivatives, Vishwashiv Kumar Emogaje

Theses and Dissertations

D1R is a compelling therapeutic target for correcting dopaminergic imbalances. However, existing ligands exhibit suboptimal pharmacokinetic properties. As such, we synthetically explored untouched structural modifications to the phenyl benzazepine scaffold. Cannabinoid-based molecules also display potential to treat neurological maladies and cancer. We synthesized Cannabichromene derivatives and uncovered enhanced anticancer activities.

Bioactive Constituents And Pharmacological Activities Of Curcuma Zedoaria: A Mini-Review, Abdulmutalib Allaq, Muneer M. Saleh Mohammed Saleh Alsayadi, Mustapha Salihu, Hasan M. Agha, Amena Hassan Hassan Gheeth, Fatimah Salim, Norrizah Jaafar Jaafar Sidik

AUIQ Complementary Biological System

Curcuma zedoaria Rosc. (white turmeric) is a rhizomatous medicinal plant in the Zingiberaceae family, widely used in traditional Asian medicine. In recent years, increasing scientific attention has focused on its diverse pharmacological properties and bioactive constituents. This mini review summarises current knowledge of the phytochemical composition and biological activities of C. zedoaria, with particular emphasis on its antimicrobial, antioxidant, anti-inflammatory, and anticancer effects. Phytochemical investigations using analytical techniques such as GC–MS and HPLC have revealed the presence of numerous bioactive compounds, including sesquiterpenes (example, germacrone, curzerenone, and curdione) and curcuminoids, which contribute to its therapeutic potential. Experimental studies demonstrate …

Iron-Based Nanoparticles As Delivery Tools, Keykavous Parang, Rajesh Vadlapatla, Ajoy Koomer, Victoria Moran, Lanie Jackson, Amir Nasrolahi Shirazi

Pharmacy Faculty Articles and Research

Iron-based nanoparticles, particularly iron oxide nanostructures (IONPs), have emerged as versatile and clinically relevant platforms for drug delivery and theranostic applications. Among these, superparamagnetic iron oxide nanoparticles (SPIONs), including magnetite (Fe₃O₄) and maghemite (γ-Fe₂O₃), are the most extensively investigated due to their biocompatibility, magnetic responsiveness, and established safety profiles. Their unique superparamagnetic behavior enables external magnetic-field-guided targeting, magnetic resonance imaging (MRI) contrast enhancement, and magnetically triggered hyperthermia, enabling simultaneous diagnosis and therapy. Surface functionalization with polymers, silica, lipids, peptides, and biomolecules further improves colloidal stability, circulation time, targeting specificity, and controlled drug …

Structural Transformation Of A Hydrogel-Forming Cell Division Protein Zapb Of Multidrug Resistant Klebsiella Pneumoniae With Small Molecules, Ayesha Khan, M. Iqbal Choudhary, Sumaira Javaid, Humaira Zafar, Innokentiy Maslennikov, Atia-Tul Wahab

Pharmacy Faculty Articles and Research

Septal ring assembly protein ZapB (EMR18431.1) is involved in Z-ring formation, and nucleoid segregation during the bacterial cell division . It promotes cell division in the initial stages of the cell cycle through direct interaction with FtsZ, thus stimulating Z-ring assembly. The ZapB inhibition can make bacterial cell susceptible to primary antibiotics, and therefore considered as an important approach for adjuvent therapy against MDR bacterial infections. Hence in the current study, ZapB protein of multidrug resistant Klebsiella pneumoniae was cloned, and expressed in E. coli system. To understand its role, and to assess the mechanism of ZapB activation, the characteristic …

Patenting The Unexpected, Sean B. Seymore

Vanderbilt Law School Faculty Publications

Unexpected discoveries have transformed human existence. They’ve revolutionized science and spawned entire new fields of research. While unexpected discoveries seem inventive and worthy of patent protection, they don’t formally align with traditional patent theory. The bedrock principle that an invention begins with the conception of an idea in the inventor’s mind and ends with implementation doesn’t apply to unexpected discoveries. This misalignment is most acute for pharmaceuticals, where the discovery of new uses for old drugs has tremendous social and economic importance. Since a drug can inherently treat multiple conditions in a patient—even those unknown to the patient, doctor, or …

2025 Novel Drug Approvals, Katherine Ghattas Pharmd, Amanda Rawa Pharmd

Transformative Medicine

The year 2025 marked another strong chapter in pharmaceutical innovation, with multiple novel therapies gaining approval from the U.S. Food and Drug Administration (FDA). These approvals reflect continued progress in addressing unmet medical needs across a wide range of disease states. This article reviews the FDA’s 2025 novel drug approvals, spotlighting a few therapeutic advancements and emerging trends. A comprehensive table of all approved agents is provided, along with a focused discussion of four particularly impactful therapies: donidalorsen (Dawnzera), taletrectinib (Ibtrozi), delgocitinib (Anzupgo), gepotidacin (Blujepa), etripamil (Cardamyst). Each of these agents represents a step forward in its respective field and …

Comparative Antiscabies Efficacy Of Sonneratia Alba Extracts: Evaluation Of Plant Parts And Concentrations In Mice, Delima Engga Maretha, Lara Mukti Taresha, Karina Yuliana, Iis Ariska, Silvia Diah Lestari

Makara Journal of Science

This study evaluated the antiscabies efficacy of 70% ethanol extracts from various parts of the mangrove Sonneratia alba (leaves, flowers, bark, and roots) as a potential alternative therapy. The primary objective was to compare the healing effects of the extracts at different concentrations on scabies lesions in mice (Mus musculus). Using a completely randomized design, 24 male Swiss Webster mice were assigned to four groups: a control (K0) group and three treatment groups to receive 10% (K1), 20% (K2), and 30% (K3) extract concentrations topically twice daily. The results demonstrated that the S. alba extracts had significant effects …

Cbx6-Ca9 Axis: An Epigenetic-Metabolic Vulnerability In Glioblastoma, Keykavous Parang

Pharmacy Faculty Articles and Research

Glioblastoma (GBM) remains one of the most therapeutically recalcitrant malignancies, with median survival rarely exceeding 15 months despite maximal therapy.¹ The hypoxic tumor microenvironment drives treatment resistance through epigenetic and metabolic adaptations.²

In this issue of Molecular Therapy Oncology, the study by Wang et al.³ demonstrates a novel regulatory axis between CBX6 (chromobox 6), a polycomb group protein, and CA9 (carbonic anhydrase 9), revealing how hypoxia-driven epigenetic reprogramming promotes tumor progression and identifying a mechanistically linked pathway for therapeutic intervention in GBM.

The study by Wang et al.3 advances our understanding of how the tumor microenvironment …

Medicines Security And Bioprospecting: A Future Agenda For Pharmaceutical Research, Geoffrey A. Cordell

The Thai Journal of Pharmaceutical Sciences

Humanity is at an extraordinary moment in history, where our interwoven future in Gaia depends on showing reverence for the modulation of our resource limits after significant losses of biodiversity and encroaching environmental change, including disappearing glaciers, rising sea levels, and changing climates. Engaging with the interconnectedness of all life on Earth and integrating sustainability and optimization of the valuable, renewable resources for future generations are essential beginning actions. Fostering economic and resource sustainability deepens the focus for contemporary research priorities toward assuring access to biological agents needed by the consumer/patient. Based on the outcomes of the COP28/29/30 and COP15/16 …

Receptor-Mediated Drug Delivery: Redefining Targeted Drug Conjugates In Oncology, Keon Niles Jafari, Charlene Chai, Shelby Kim, Kamaljit Kaur

Pharmacy Faculty Articles and Research

Targeted drug delivery (TDD), specifically through targeting ligand–drug conjugates, has reshaped oncology by enabling selective delivery of cytotoxic payloads to cancer cells while minimizing uptake by normal tissues. A key approach relies on exploiting overexpressed cell surface receptors (CSRs) to enable selective uptake of drug conjugates via receptor-mediated endocytosis. This review delineates four clinically validated CSRs (HER2, Trop-2, Nectin-4, and SSTR2) with several FDA-approved drug conjugates. Furthermore, emerging CSRs (EGFR, DLL3, and keratin 1) that may support next-generation TDD platforms for cancer treatment are also highlighted. We discuss how CSR type, density on cancer cells, and its mechanism of endocytosis, …

Selectivity Modulation Of Small Cationic Membrane-Active Cyclic Peptides With Broad-Spectrum Activity Against Bacteria And Fungi, Sandeep Lohan, Rakesh Kumar Tiwari, Innokentiy Maslennikov, Kaustav Das Gupta, Shakti Singh, Keykavous Parang

Pharmacy Faculty Articles and Research

To investigate how ring size and backbone flexibility influence antimicrobial potency and cytotoxicity, we synthesized a series of macrocyclic peptides of lead peptide p1 (c[Arg-Arg-arg-arg-dip-Trp-dip]) by incorporating Gly, 2-aminoethoxyacetic acid (EAA), or 2,4-diaminobutyric acid (Dab). Two optimized peptides, 6b and 10b, retained broad-spectrum activity against drug-resistant Gram-positive (MIC, 1.5–6.2 μg/mL) and Gram-negative bacteria (MIC, 4–25 μg/mL), as well as pathogenic fungi, while exhibiting enhanced selectivity for microbial cells. Their therapeutic indices (TI ∼407 and ∼394, respectively) were ∼2-fold higher than p1, indicating improved safety. Both peptides remained effective against Gram-negative pathogens beyond the reach of daptomycin, were rapidly bactericidal, and …

Disruption Of Proteoglycan 4 (Prg4)-Cd44 Signaling Modulates Chronic Synovitis In Conditionally Inactivated Mice, Khaled A. Elsaid, Ling Zhang, Thomas Zhao, Ava Marks, Derek Jenkins, Gregory D. Jay

Pharmacy Faculty Articles and Research

Background

Proteoglycan-4 (PRG4) is a mucinous glycoprotein secreted by synovial fibroblasts and superficial zone chondrocytes. PRG4 inhibits synovial macrophage (SM) activation via xanthine oxidase (XO) and hypoxia inducible factor alpha (HIF-1α) suppression. We aimed to evaluate the contribution of PRG4-CD44 interaction to synovial homeostasis and investigate PRG4’s signaling dysfunction in synovial tissues from patients with osteoarthritis (OA). We hypothesized that CD44 mediates synovitis due to PRG4 loss and that PRG4 signaling dysfunction is associated with high-grade synovitis in OA.

Methods

Prg4^{FrtloxP/FrtloxP} are transgenic mice wherein tamoxifen (TAM) inactivates the Frt allele and creates a knockout state (Prg4^{FrtKO/FrtKO …}

Optimization Of A Kcc2 Small Molecule Agonist And The Development Of An In-Silico Model Of Intermolecular Dynamics For The Rational Design Of Therapeutics Against Opioid Use Disorder, William H.D. Ho, Alfred Amendolara, Kenyon Mitchell, Jaden Miner, Braxton Bingham, Andrew Payne

Annual Research Symposium

Roseman University Research Symposium

Wednesday, February 18, 2026 | 3:00 – 6:00 pm (local time)

Neonatal Sepsis: Empiric Treatment And Monitoring Of Gentamicin Troughs In The Nicu, Aleese Palfreyman

Annual Research Symposium

No abstract provided.