Chemicals and Drugs Commons^™

Nifuroxazide And 4-Hydroxybenzhydrazone Derivatives As New Antiparasitic (Trypanosoma Cruzi And Leishmania Mexicana) And Anti-Mycobacterium Tuberculosis Agents, Timoteo Delgado-Maldonado, Diana V. Navarrete-Carriola, Lenci K. Vazquez-Jimenez, Alma D. Paz-Gonzalez, Baojie Wan, Scott Franzblau, Othman Mueen Mohammed, Lorena Rodríguez-Páez, Charmina Aguirre-Alvarado, Debasish Bandyopadhyay

School of Integrative Biological & Chemical Sciences Faculty Publications

Background/Objectives: Nifuroxazide (Nfz) is a drug that has been used as a scaffold for designing antimicrobial and antiparasitic agents. This study aimed to synthesize and evaluate in vitro of Nfz and twenty-five 4-hydroxybenzhydrazone derivatives as potential anti-Trypanosoma cruzi, anti-Leishmania mexicana, and anti-Mycobacterium tuberculosis agents.

Methods: The compounds were synthesized by condensing 4-hydroxybenzhydrazide with appropriate aldehydes in acidic conditions and structurally confirmed by spectroscopic techniques. All compounds were evaluated in vitro against T. cruzi strains (NINOA and A1), L. mexicana (M379 and FCQEPS strains), and M. tuberculosis (H37Rv strain), followed by enzymatic assays against T. cruzi …

Statin Effects On The Lipidome: Predicting Statin Usage And Implications For Cardiovascular Risk Prediction, Changyu Yi, Kevin Huynh, Yvette Schooneveldt, Gavriel Olshansky, Amy Liang, Tingting Wang, Habtamu B. Beyene, Aleksandar Dakic, Joanne E. Curran, John Blangero

School of Medicine Publications

Statin therapy is a highly successful and cost-effective strategy for the prevention and treatment of cardiovascular diseases (CVD). Adjusting for statin usage is crucial when exploring the association of the lipidome with CVD to avoid erroneous conclusions. However, practical challenges arise in real-world scenarios due to the frequent absence of statin usage information. To address this limitation, we demonstrate that statin usage can be accurately predicted using lipidomic data. Using three large population datasets and a longitudinal clinical study, we show that lipidomic-based statin prediction models exhibit high prediction accuracy in external validation. Furthermore, we introduce a re-weighted model, designed …

Unveiling The Potential Of Urolithin A In Cancer Therapy: Mechanistic Insights To Future Perspectives Of Nanomedicine, Vinita Karumuru, Anupam Dhasmana, Narsimha Mamidi, Subhash Chauhan, Murali Yallapu

School of Medicine Publications

Cancer remains a leading global health challenge, with high mortality rates persisting despite significant advancements in therapeutic interventions. Major obstacles, including systemic toxicity, therapy resistance, metastasis, and relapses, emphasize the urgent need for safer, more effective, and readily accessible treatment strategies. Among emerging alternatives, natural bioactive compounds have gained considerable attention because of their diverse therapeutic potential and lower toxicity profiles. Urolithin A (UA), a metabolite derived from ellagic acid through gut microbiota metabolism, has emerged as a compelling anticancer agent. UA has multiple mechanisms of action, including the regulation of autophagy, enhancement of mitochondrial function, and inhibition of tumor …

Small-Molecule Mitotic Inhibitors As Anticancer Agents: Discovery, Classification, Mechanisms Of Action, And Clinical Trials, Yazmin Salinas, Subhash Chauhan, Debasish Bandyopadhyay

School of Medicine Publications

Despite decades of research, cancer continues to be a disease of great concern to millions of people around the world. It has been responsible for a total of 609,820 deaths in the U.S. alone in 2023. Over the years, many drugs have been developed to remove or reduce the disease’s impact, all with varying mechanisms of action and side effects. One class of these drugs is small-molecule mitotic inhibitors. These drugs inhibit cancer cell mitosis or self-replication, impeding cell proliferation and eventually leading to cell death. In this paper, small-molecule mitotic inhibitors are discussed and classified through their discovery, underlying …

Efficacy Of Glucagon-Like Peptide-1 Receptor Agonists For Prevention Of Stroke Among Patients With And Without Diabetes: A Meta-Analysis With The Select And Flow Trails, Asmita Gera, Fakhar Latif, Vamsikalayan Borra, Sidra Naz, Vivek Mittal, Fathima Shehnaz Ayoobkhan, Tushar Kumar, Zarghoona Wajid, Novonil Deb, Tanisha Prasad

School of Medicine Publications

Background

Glucagon-like peptide-1 receptor agonists (GLP-1 RAs) have shown a reduction in major adverse cardiovascular events (MACE) among patients with type 2 diabetes mellitus (T2DM). However, its efficacy on cerebrovascular events is yet to be well established among diabetic and non diabetic patients.

Objective

We sought to evaluate the efficacy of GLP-1 RAs on stroke risk among its different types in patients with and without Diabetes.

Methods

We performed a systematic literature search on PubMed, EMBASE, and ClinicalTrials.gov for relevant randomized controlled trials (RCTs) from inspection until 15th July 2024, without any language restrictions. Odds ratios (OR) and 95 % …

Relevance Of Cellular Homeostasis-Related Gene Expression Signatures In Distinct Molecular Subtypes Of Breast Cancer, Sharda P. Singh, Chathurika S. Dhanasekara, Michael W. Melkus, Chhanda Bose, Sonia Y. Khan, Flavia Sardela De Miranda, Maria F. Mahecha, Prrishti J. Gukhool, Sahil S. Tonk, Se-Ran Jun

School of Medicine Publications

Background: Breast cancer is a complex and heterogeneous disease characterized by distinct molecular subtypes with varying prognoses and treatment responses. Multiple factors influence breast cancer outcomes including tumor biology, patient characteristics, and treatment modalities. Demographic factors such as age, race/ethnicity, menopausal status, and body mass index have been correlated with variations in incidence, mortality, and survival rates. Over the past decade, comprehensive genomic profiling has been widely used to identify molecular biomarkers and signatures to develop novel therapeutic strategies for patients. For instance, the FLEX registry (NCT03053193) enrolled stage I-III breast cancer patients across 90 institutions in the …

Small Molecule B-Raf Inhibitors As Anti-Cancer Therapeutics: Advances In Discovery, Development, And Mechanistic Insights, Yamile Abuchard Anaya, Ricardo Pequeno Bracho, Subhash Chauhan, Manish K. Tripathi, Debasish Bandyopadhyay

School of Medicine Publications

B-RAF is a serine/threonine kinase that plays a crucial role in the MAPK signaling pathway, regulating cell proliferation and survival. Mutations in B-RAF, particularly V600E, are associated with several malignancies, including melanoma, colorectal cancer, and non-small cell lung cancer, making it a key therapeutic target. The development of B-RAF inhibitors, such as Vemurafenib, Dabrafenib, and second-generation inhibitors like Encorafenib, has led to significant advancements in targeted cancer therapy. However, acquired resistance, driven by MAPK pathway reactivation, RAF dimerization, and alternative signaling pathways, remains a major challenge. This review explores the molecular mechanisms of B-RAF inhibitors, their therapeutic efficacy, and resistance …

Exploring Cucurbitacin D'S Protective Mechanism Against Benzo[A]Pyrene-Induced Liver Injury Through Nrf2 Activation, Shabnam Malik, Mohammed Sikander, Anyssa Rodriguiez, Daniel Zubieta, Debanhi Esparaza, Fathi T. Halaweish, Sheema Khan, Murali M. Yallapu, Meena Jaggi, Subhash C. Chauhan

Research Symposium

Background: Numerous studies have established a strong association between hepatocellular carcinoma (HCC) and various co-morbidity factors, including smoking. Tobacco smoke is a significant source of benzo[a]pyrene, a highly carcinogenic compound known to cause liver damage. Cucurbitacin, a triterpene with diverse biological activities, exhibits antioxidant, antiinflammatory, and anticancer effects. However, its hepatoprotective properties have not been thoroughly investigated. In this study, we aimed to evaluate the hepatoprotective effects of cucurbitacin D, a novel analog of cucurbitacin, against liver injury induced by benzo[a]pyrene in human HepG2 cells.

Method: To investigate the hepatoprotective effect of cucurbitacin D against benzo[a]pyreneinduced liver damage, proliferation, clonogenicity, …

Evaluating The Potential Of Herbal Extracts As Treatment In Immune Thrombocytopenia: A Review Of Evidence And Limitations, Russell Wiggins, Jihoo Woo, John Cauba, Shizue Mito

Research Symposium

Immune thrombocytopenia, formerly idiopathic thrombocytopenia purpura (ITP), is an autoimmune disease characterized by the depletion of platelets below 100,000/µl when other causes of thrombocytopenia have been ruled out. It is associated with several infectious pathologies, disease states, and as a known side effect and complication of several drugs and chemotherapies. Standard treatment calls for glucocorticoid mediated immunosuppression, intravenous immunoglobin transfusion, platelet stimulation, platelet transfusion, and splenectomy in instances of chronic and severe disease. While standard treatments are often effective, some cases prove resistant, and more commonly, some patients are unable to tolerate standard treatment protocols or opt out of surgical …

Improving Niclosamide's Effectiveness In Cancer Therapy: Advances In Drug Modification And Delivery, Russell Wiggins, Jihoo Woo, Shizue Mito

Research Symposium

The property of niclosamide to inhibit multiple cancer-related pathways has made it a promising candidate for the treatment of various cancers. However, poor bioavailability and solubility have significantly restricted its clinical application. This literature review explores various strategies that enhance the bioavailability and efficacy of Niclosamide through the development of Niclosamide derivatives and the utilization of drug delivery systems. We also briefly discuss Niclosamide’s suspected mechanisms of action in several cancer related pathways. Derivatives such as Niclosamide Ethanolamine (NEN) and Niclosamide Piperazine (NPP) have demonstrated improved pharmacokinetic properties, including increased solubility and bioavailability, without compromising anticancer activity. Importantly, these formulations …

The Role Of The Female Reproductive Cycle In Social Communication And Relevance To Mental Health, Julissa Amaro Castillo, Fernando Dominguez, Ariana Hinojosa, Giselle Padilla, Mario Gil

Research Symposium

The female reproductive cycle is characterized by fluctuating hormones, including estrogens and progesterone, that are involved in reproductive health; however, they have also been linked to disorders like Premenstrual syndrome (PMS), Premenstrual Dysphoric Disorder (PMDD), mood swings, depression and others. The goal of this study is to use the Syrian hamster (Mesocricetus auratus) as an animal model to examine the influence of the reproductive cycle and hormones on behavior. Scent-marking activity known as flank marking is exhibited by territorial or sociable animals. In essence, animals mark their territory or convey information such as reproductive status by rubbing their flanks or …

Effects Of Arginine-Vasopressin In The Brain On Cardiovascular Function In A Psychosocial Stress Animal Model, Esmeralda Lopez-Garcia, Ariana V. Hinojosa, Esperanza I. Alaniz, Fernando Dominguez, Giselle Padilla, Mario Gil

Research Symposium

Background: Psychosocial stress impacts cardiovascular health, increasing the risk of events like myocardial infarction (MI), stress cardiomyopathy, and neuropsychiatric disorders, including Major Depressive Disorder (MDD) and Anxiety. However, our understanding of the biological mechanisms that connect psychosocial stress with negative cardiovascular and psychological outcomes remains incomplete. Arginine-vasopressin (AVP) is linked to both mental and physical health by regulating social behavior, blood pressure, and anxiety-related behaviors. This study investigates the potential cardioprotective effects of the neuropeptide AVP, in an effort to generate evidence that it may strengthen heart function and lessen the severity of adverse cardiovascular events caused by stress, brain …

Synthesis Of Medicinally Privileged Spiro-Β-Lactams, Debasish Bandyopadhyay, Reinaldo Mendes, Subhash C. Chauhan

Research Symposium

Background: Four-membered cyclic amide, commonly known as β-lactam, has been playing a crucial role in drug discovery research since its discovery by Alexander Fleming in 1928 from Penicillium notatum. The β-lactam antibiotics are broadly effective against several bacterial infections through acylating the transpeptidase involved in cross-linking peptides to form peptidoglycan or periplasmic murein, which is a fundamental constituent of the bacterial cell wall for both the gram-positive (ten or more layers) and gram-negative (one or two layers) bacteria. Although for more than eight decades, β-lactams have been recognized as antibiotics, later, other medicinal activities of β-lactam derivatives have been …

Exploring The Effects Of Serotonin And Ssris On The Neurological, Behavioral, And Cardiovascular Systems Under Induced Stress –Using The Animal Model Of The Syrian Hamster, Ariana V. Hinojosa, Esperanza I. Alaniz, Esmeralda Lopez-Garcia, Giselle Padilla, Fernando Dominquez, Mario Gil

Research Symposium

Background: Serotonin is a neurotransmitter that has been found to have a wide range of effects on not just the neuropsychological processes but has also been found to exert effects outside the central nervous system (CNS); regulating numerous biological processes, such as metabolism, gastrointestinal system, reproductive function, and even the cardiovascular system. However, there is still a limited understanding of how serotonin affects all these systems due to its complexity and ability to regulate homeostasis. This project aims to create a stronger foundation of knowledge about serotonin and its influence on the interaction between the CNS, behavior, and cardiac function …

Long-Term Safety And Comparative Efficacy Of Il-17 Inhibitors In Treating Ankylosing Spondylitis, Alyssa L. Sepulveda, Yolanda V. Gutierrez, Ronald A. Shaju

Research Symposium

Background:
Ankylosing Spondylitis (AS) is a chronic inflammatory disease affecting the axial skeleton, characterized by spinal stiffness, sacroiliitis, and potential vertebral fusion. While nonsteroidal anti-inflammatory drugs (NSAIDs) and tumor necrosis factor (TNF) inhibitors are first-line treatments, IL-17 inhibitors, such as secukinumab and ixekizumab, are used in patients with inadequate response or contraindications to TNF inhibitors. These targeted therapies address IL-17’s role in driving inflammation and structural damage in AS.

Methods:
A systematic review was conducted using PubMed, Science Direct, and Cochrane to identify studies published between 2000 and 2025. Keywords included “Ankylosing spondylitis” and “IL-17 inhibitors” and “efficacy.” Inclusion criteria …

Role Of Urolithin A In Cancer Therapy, Aanya S. Chauhan, Vinita Karumuru, Mahi P. Yallapu, Anupam Dhasmana

Research Symposium

Background: Cancer is a big health problem around the world, causing many deaths even though there have been improvements in treatments. Some of the main challenges in treating cancer include side effects, resistance to treatments, cancer spreading to other parts of the body (metastasis), and the disease coming back (recurrence). Scientists are looking for safer and better ways to treat cancer. One promising option is using natural substances that come from plants, which are less toxic and have a lot of potential for fighting diseases. One of these substances is Urolithin A (UA), a compound made in the body when …

Single-Chain Variable Fragments: Targeting Snake Venom Phospholipase A2 And Serine Protease, Ying Jia, Ariane Garcia, Elizabeth Reyes

School of Integrative Biological & Chemical Sciences Faculty Publications

Snakebite is a critical global public health issue, causing substantial mortality and morbidity, particularly in tropical and subtropical regions. The development of innovative antivenoms targeting snake venom toxins is therefore of paramount importance. In this study, we adopted an epitope-directed approach to design three degenerate 15-mer peptides based on amino acid sequence alignments of snake venom phospholipase A2s (PLA2s) and snake venom serine proteases (SVSPs) from snake (Crotalus atrox). By leveraging their immunogenic and inhibitory profiles, these peptides were specifically designed to target the Asp49 and Lys49 variants of PLA2 and SVSP toxins. Groups of five mice were immunized with …

Molecular Screening And Dynamics Simulation Reveal Potential Phytocompounds In Swertia Chirayita Targeting The Uspa1 Protein Of Moraxella Catarrhalis For Copd Therapy, Md. Moin Uddin, Md. Shydhur Rahman Chowdhury, Md. Arju Hossain, Asif Ahsan, Md. Tanvir Hossain, Abdul Barik, Md. Arif Hossen, Md. Faisal Amin, Rafsan Abir, Mohammad Shah Alam

School of Integrative Biological & Chemical Sciences Faculty Publications

Chronic obstructive pulmonary disease (COPD) is a global health burden, with Moraxella catarrhalis significantly contributing to acute exacerbations and increased healthcare challenges. This study aimed to identify potential drug candidates in Swertia chirayita, a traditional Himalayan medicinal plant, demonstrating efficacy against the ubiquitous surface protein A1 (UspA1) of M. catarrhalis through an in-silico computational approach. The three-dimensional structures of 46 phytocompounds of S. chirayita were retrieved from the IMPPAT 2.0 database. The structures underwent thorough analysis and screening, emphasizing key factors such as binding energy, molecular docking performance, drug-likeness, and toxicity prediction to assess their therapeutic potential. Considering the …

Lipid Discovery Enabled By Sequence Statistics And Machine Learning, Priya M. Christensen, Jonathan Martin, Aparna Uppuluri, Luke R. Joyce, Yahan Wei, Ziqiang Guan, Faruck Morcos, Kelli L. Palmer

School of Podiatric Medicine Publications

Bacterial membranes are complex and dynamic, arising from an array of evolutionary pressures. One enzyme that alters membrane compositions through covalent lipid modification is MprF. We recently identified that Streptococcus agalactiae MprF synthesizes lysyl-phosphatidylglycerol (Lys-PG) from anionic PG, and a novel cationic lipid, lysyl-glucosyldiacylglycerol (Lys-Glc-DAG), from neutral glycolipid Glc-DAG. This unexpected result prompted us to investigate whether Lys-Glc-DAG occurs in other MprF-containing bacteria, and whether other novel MprF products exist. Here, we studied protein sequence features determining MprF substrate specificity. First, pairwise analyses identified several streptococcal MprFs synthesizing LysGlc-DAG. Second, a restricted Boltzmann machine-guided approach led us to discover an …

Impact Of Pegylated Liposomes On Cytotoxicity Of Tamoxifen And Piperine On Mcf-7 Human Breast Carcinoma Cells, Klaudi K. Vaiphei, A Prabakaran, Singh Snigdha, Satyajit Laxman Murkute, Purusottam Mohapatra, Rakesh Kumar Sahoo, Sanya Batheja, Umesh Gupta, Anu Puri, Upal Roy

Health & Biomedical Sciences Faculty Publications

Tamoxifen (TMF) is an anticancer agent used for managing estrogen receptor-positive breast cancer. It has limited therapeutic efficacy against breast cancer, which could be enhanced by the coadministration of herbal drugs like piperine (PIP). However, the hydrophobic nature of TMF and PIP restricts their therapeutic application. Therefore, the present study focuses on the impact of the anticancer activity of TMF in combination with PIP and after entrapping them into liposomes (TMF-PIP-LPs and TMF-PIP-PEG-LPs). The liposomes were prepared using the thin film hydration method. In addition, the morphology of the prepared liposomes was found spherical after SEM and TEM analyses. Further, …

Lipid-Based Niclosamide Delivery: Comparative Efficacy, Bioavailability, And Potential As A Cancer Drug, Jihoo Woo, Russel Wiggins, Shizue Mito

School of Medicine Publications

Niclosamide, an FDA-approved anti-parasitic drug, has demonstrated significant potential as a repurposed anti-cancer agent due to its ability to interfere with multiple oncogenic pathways. However, its clinical application has been hindered by poor solubility and bioavailability. Lipid-based nanocarrier systems such as liposomes, solid lipid nanoparticles (SLNs), nanostructured lipid carriers (NLCs), and lipid nanoemulsions (LNE), along with lipid prodrugs, have successfully been employed by researchers to overcome these limitations and improve niclosamide’s pharmacokinetic profile. Lipids are the core organic compounds which serve as the foundation of these advanced drug delivery methods and in turn play a critical role in enhancing niclosamide’s …

Optimizing Niclosamide For Cancer Therapy: Improving Bioavailability Via Structural Modification And Nanotechnology, Russell Wiggins, Jihoo Woo, Shizue Mito

School of Medicine Publications

Niclosamide, a drug originally used to treat parasitic infections, has shown potential as a possible cancer treatment, but poor absorptive and solubility properties are believed to limit its effectiveness. Researchers are exploring modified structures of the drug along with advanced delivery methods, particularly nanotechnology, to improve niclosamide’s absorption profile and improve its specificity in regard to targeting cancerous cells. These efforts intend to produce more effective tumor-targeting compounds, which can be employed as pharmacological cancer treatment options when appropriate. If successful, these efforts will provide new tools for scientists and doctors, offering a novel approach regarding the treatment of a …

Targeted Therapy In Breast Cancer: Advantages And Advancements Of Antibody-Drug Conjugates, A Type Of Chemo-Biologic Hybrid Drugs, Attrayo Mukherjee, Debasish Bandyopadhyay

School of Integrative Biological & Chemical Sciences Faculty Publications

Cancer is a significant health challenge globally, with millions of people affected every year, resulting in high morbidity and mortality. Although other treatment options are available with limitations, chemotherapy, either standalone or combined with other therapeutic procedures, is the most commonly used practice of treating cancer. In chemotherapy, cancer cells/malignant tumors are targeted; however, due to less target specificity, along with malignant cells, normal cells are also affected, which leads to various off-target effects (side effects) that impact the patient quality of life. Out of all the different types of cancers, breast cancer is the most common type of cancer …

Mannosylated Pamam G2 Dendrimers Mediated Rate Programmed Delivery Of Efavirenz Target Hiv Viral Latency At Reservoirs, Rohini Kharwad, Mohsin Kazi, Nilesh Mahajan, Payal Badole, Sachin More, Asaad Kayali, Md Noushad Javed, Mohammed Kaleem

Mechanical Engineering Faculty Publications

In this current research, we conceptualized a novel nanotechnology-enabled synthesis approach of targeting HIV-harboring tissues via second-generation (G2) polyamidoamine (PAMAM) mannosylated (MPG2) dendrimers for programmed delivery of anti-HIV drugs efavirenz (EFV) and ritonavir (RTV). Briefly, here mannose served purpose of ligand in this EFV and RTV-loaded PAMAM G2 dendrimers, synthesized by divergent techniques, denoted as MPG2ER. The developed nanocarriers were characterized by different analytical tools FTIR, NMR, zeta potential, particle size, and surface morphology. The results of confocal microscopy showed substantial alterations in the morphology of H9 cells, favored by relatively higher drug uptake through the MPG2ER. Interestingly, the drug …

Quinoxaline 1,4-Di-N-Oxide Derivatives As New Antinocardial Agents, Isidro Palos, Alonzo Gonzalez-Gonzalez, Alma D. Paz-Gonzalez, José C. Espinoza-Hicks, Debasish Bandyopadhyay, Norma Paniagua-Castro, Marlene S. Galeana-Salazar, Jorge Ismael Castañeda-Sánchez, Julieta Luna-Herrera, Gildardo Rivera-Sanchez

School of Integrative Biological & Chemical Sciences Faculty Publications

Mycetoma is currently considered as a neglected tropical disease. The incidence of mycetoma is unknown but most of the worldwide cases are present in the “mycetoma belt” including countries like Mexico, India, Senegal, and others. The treatment of mycetoma depends on the etiological agent responsible for the case. Treatment success reaches 60 to 90%; however, common treatment has been reported to be ineffective in some cases, due in part to resistance to the prescribed antibiotics. Therefore, it is necessary to develop new therapeutic options. In the past two decades, quinoxaline derivatives have shown relevance as antibacterial agents. Therefore, in this …

Breathe Easy: The Potential Of Vitamins As Adjunct Therapy In Asthma Management, Elena Dike, Alex Zuo

Research Colloquium

Asthma, a prevalent respiratory disease, imposes a heavy burden on patients and healthcare systems. This research poster reviews recent findings on the potential of Vitamins A, C and E as adjunct therapies in asthma management. Comprehensive searches in PubMed, the NIH and Google Scholar identify multiple relevant publications and articles. Key results indicate that Vitamin A reduces Th2/Th17 levels and ROS, protecting the airway epithelium; Vitamin C decreases inflammatory cells and increases cGMP levels, reducing airway hyper-reactivity; and Vitamin E reduces eosinophils, basophils and neutrophils while also reducing ROS. These findings suggest that increasing intake of these vitamins, under medical …

Targeting Ribosome Biogenesis Is A Novel Approach For The Management Of Pancreatic Cancer, Mudassier Ahmad, Haider Ahsan, Carlos Perez, Muhammad Bangash, Andrew Massey, Emmanuel Anning, Manish Tripathi, Dae Kim, Subhash C. Chauhan, Bilal Bin Hafeez

Research Colloquium

Pancreatic ductal adenocarcinoma is the third leading cause of cancer-related deaths in the United States with limited therapeutic options available. Gemcitabine, a deoxycytidine nucleoside analog is currently considered the most effective therapy for PanCa. However, it shows only a marginal survival benefit of six months. Aberrant ribosome biogenesis occurs in most tumor types. We observed that PanCa cells are addicted to ribosome biogenesis, which supports their highly aggressive metastatic phenotypes. Thus, strategically targeting ribosome biogenesis process could be one of the ideal strategies for the prevention and treatment of PanCa. In this study, we elucidated the molecular mechanisms of POLR1A …

A Pseudo-Surfactant Chemical Permeation Enhancer To Treat Otitis Media Via Sustained Transtympanic Delivery Of Antibiotics, Sophie S. Liu, Joanna M. White, Zhongmou Chao, Ruye Li, Shuxian Wen, Ally Garza, Wenjing Tang, Xiaojing Ma, Pengyu Chen, Susan Daniel

Health & Biomedical Sciences Faculty Publications

Chemical permeation enhancers (CPEs) represent a prevalent and safe strategy to enable non-invasive drug delivery across skin-like biological barriers such as the tympanic membrane (TM). While most existing CPEs interact strongly with the lipid bilayers in the stratum corneum to create defects as diffusion paths, their interactions with the delivery system, such as polymers forming a hydrogel, could compromise gelation, formulation stability, and drug diffusion. To overcome that challenge, we explore the differing interactions present with sodium dodecyl sulfate (SDS), an ionic surfactant and a common CPE, and methyl laurate (ML), a non-ionic counterpart with a similar length alkyl chain. …

Nebulization Based Inhalation Nanomedicine For Lung Cancer Treatments, Rahul Tiwari, Meghana Kolli, Neeraj Chauhan, Eswara Naga Hanuma, Vivek Kashyap, Subhash Chauhan, Murali Yallapu

Research Symposium

Background: Lung cancer is reported to have a high incidence rate and first leading cause of cancer-related morbidity and mortality across the world including in the United States. Noninvasive nebulized inhalation is a promising delivery strategy for lung, which can enhance the targeting efficiency and detention time interval of nanoparticles in the lung tissue, thus elevating the therapeutic index of therapeutic agent(s) at lower dosages. The aim of this study is to develop inhalable nanoparticles (INPs) for effective delivery of therapeutic agents in lung cancer cell lines and ex vivo models.

Methods: The inhalation nanoparticles (INPs) were prepared by solvent …

Mechanistic Investigation Of C—C Bond Activation Of Phosphaalkynes With Pt(0) Complexes, Roberto M. Escobar, Abdurrahman C. Ateşin, Christian Müller, William D. Jones, Tülay Ateşin

Research Symposium

Carbon–carbon (C–C) bond activation has gained increased attention as a direct method for the synthesis of pharmaceuticals. Due to the thermodynamic stability and kinetic inaccessibility of the C–C bonds, however, activation of C–C bonds by homogeneous transition-metal catalysts under mild homogeneous conditions is still a challenge. Most of the systems in which the activation occurs either have aromatization or relief of ring strain as the primary driving force. The activation of unstrained C–C bonds of phosphaalkynes does not have this advantage. This study employs Density Functional Theory (DFT) calculations to elucidate Pt(0)-mediated C–CP bond activation mechanisms in phosphaalkynes. Investigating the …