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Full-Text Articles in Pharmacy and Pharmaceutical Sciences

Analysis Of Docosanol Using Gc/Ms: Method Development, Validation, And Application To Ex Vivo Human Skin Permeation Studies, Vijay Kumar Shankar, Mei Wang, Srinivas Ajjarapu, Praveen Kolimi Apr 2022

Analysis Of Docosanol Using Gc/Ms: Method Development, Validation, And Application To Ex Vivo Human Skin Permeation Studies, Vijay Kumar Shankar, Mei Wang, Srinivas Ajjarapu, Praveen Kolimi

Faculty and Student Publications

Docosanol is the only US Food and Drug Administration (FDA) approved over-the-counter topical product for treating recurrent oral-facial herpes simplex labialis. Validated analytical methods for docosanol are required to demonstrate the bioequivalence of docosanol topical products. A gas chromatography/selected ion monitoring mode mass spectrometry (GC/SIM-MS) method was developed and validated for docosanol determination in biological samples. Docosanol and isopropyl palmitate (internal standard) were separated on a high-polarity GC capillary column with (88% cyanopropy)aryl-polysiloxane employed as the stationary phase. The ions of m/z 83 and 256 were selected to monitor docosanol and isopropyl palmitate, respectively; the total run time was 20 …


Protocol: A Scoping Review Of Graduate Student Education, Curriculum Impact, And Interest In Interdisciplinary Research Training, David D. Allen Iii Mar 2022

Protocol: A Scoping Review Of Graduate Student Education, Curriculum Impact, And Interest In Interdisciplinary Research Training, David D. Allen Iii

Faculty and Student Publications

Title: PROTOCOL: A Scoping Review of Graduate Student Education, Curriculum Impact, and Interest in Interdisciplinary Research Training

Background: Alongside traditional graduate education practices, implementing curriculum focused on providing interdisciplinary research training to graduate students may help support their academic development. This additional educational focus can bolster graduate student understanding of methodological practices, develop alternative routes of thinking or approaching a problem/ issue/ topic, may assist in developing student professional socialization skills, and may positively impact student internal motivations, beliefs, and perceptions.

Methods: Our scoping review protocol was developed a priori utilizing the Joanna Briggs Institute guidance, by …


Predictors Of Job Satisfaction Among Pharmacists: A Regional Workforce Survey, Rotana M. Radwan, John P. Bentley, Julie A. Patterson, Dave L. Dixon Mar 2022

Predictors Of Job Satisfaction Among Pharmacists: A Regional Workforce Survey, Rotana M. Radwan, John P. Bentley, Julie A. Patterson, Dave L. Dixon

Faculty and Student Publications

Background: Job satisfaction affects organizational outcomes including performance and retention. The pharmacy job satisfaction literature points to several predictors of job satisfaction, but educational debt and various work settings have not been previously examined. Objectives: To identify predictors of Virginia pharmacists' job satisfaction. Methods: This cross-sectional study used data from the 2018 Virginia Pharmacist Workforce Survey. Of 15,424 registered pharmacists, 13,962 (90.5%) completed the survey. Pharmacists who reported being employed and working in Virginia in the previous year (2017) were included in the analysis (n = 6042). Data were summarized using descriptive statistics. Multiple logistic regression identified predictors of job …


In Silico Tools For Analysis Of Single-Nucleotide Polymorphisms In The Bovine Transferrin Gene, Aarif Ali, Muneeb U. Rehman, Syed Mudasir Ahmad, Tabish Mehraj Mar 2022

In Silico Tools For Analysis Of Single-Nucleotide Polymorphisms In The Bovine Transferrin Gene, Aarif Ali, Muneeb U. Rehman, Syed Mudasir Ahmad, Tabish Mehraj

Faculty and Student Publications

Dairy cattle with a high milk yield are susceptible to many infectious diseases, such as mastitis. Subclinical mastitis (SCM) is the most prevalent form of mastitis that predominantly affects animal health, and causes adverse effects on the quality and quantity of milk. In dairy animals, subclinical mastitis often remains undetected, as no gross changes in udder characteristics are visible. In the present study, 135 Holstein Friesian dairy animals were selected and screened as healthy (n = 25) and mastitic (n = 110) based on diagnostic tests such as the California mastitis test, pH, electrical conductivity, and somatic cell count. In …


Real-World, Multicentre Evaluation Of The Incidence And Risk Factors For Non-Susceptible Stenotrophomonas Maltophilia Isolates, Bruce M. Jones, Jamie L. Wagner, Daniel B. Chastain, P. Brandon Bookstaver Mar 2022

Real-World, Multicentre Evaluation Of The Incidence And Risk Factors For Non-Susceptible Stenotrophomonas Maltophilia Isolates, Bruce M. Jones, Jamie L. Wagner, Daniel B. Chastain, P. Brandon Bookstaver

Faculty and Student Publications

Background: Stenotrophomonas maltophilia is a cause of infection most commonly in the opportunistic host. Trimethoprim-sulfamethoxazole and levofloxacin are considered first-line treatment agents. With reports of increasing resistance to these first-line agents, it is important to determine risk factors associated with a non-susceptible isolate. Methods: This was a real-world, multicentre, retrospective case-control study from five centres in the southeast United States evaluating S. maltophilia. The primary outcome was risk factors associated with non-susceptibility of S. maltophilia isolates to ≥1 antimicrobial agents. Secondary outcomes include incidence of S. maltophilia non-susceptibility, all-cause mortality, and 30-day readmission rates. Results: There were 325 patients included …


Chemical Composition Analysis, Cytotoxic, Antimicrobial And Antioxidant Activities Of Physalis Angulata L.: A Comparative Study Of Leaves And Fruit, Jayachithra Ramakrishna Pillai, Adil Farooq Wali, Godfred Antony Menezes, Muneeb U. Rehman Mar 2022

Chemical Composition Analysis, Cytotoxic, Antimicrobial And Antioxidant Activities Of Physalis Angulata L.: A Comparative Study Of Leaves And Fruit, Jayachithra Ramakrishna Pillai, Adil Farooq Wali, Godfred Antony Menezes, Muneeb U. Rehman

Faculty and Student Publications

Physalis angulata L. belongs to the family Solanaceae and is distributed throughout the tropical and subtropical regions. Physalis angulata leaf and fruit extracts were assessed for in vitro anticancer, antioxidant activity, and total phenolic and flavonoid content. The GC-MS technique investigated the chemical composition and structure of bioactive chemicals reported in extracts. The anticancer activity results revealed a decrease in the percentage of anticancer cells’ viability in a concentration-and time-dependent way. We also noticed morphological alterations in the cells, which we believe are related to Physalis angulata extracts. Under light microscopy, we observed that as the concentration of ethanolic extract …


Safety And Pharmacokinetics Of Intranasally Administered Heparin, Hannah M. Harris, Katherine L. Boyet, Hao Liu, Rohini Dwivedi Mar 2022

Safety And Pharmacokinetics Of Intranasally Administered Heparin, Hannah M. Harris, Katherine L. Boyet, Hao Liu, Rohini Dwivedi

Faculty and Student Publications

Purpose: Intranasally administered unfractionated heparin (UFH) and other sulfated polysaccharides are potential prophylactics for COVID-19. The purpose of this research was to measure the safety and pharmacokinetics of clearance of intranasally administered UFH solution from the nasal cavity. Methods: Double-blinded daily intranasal dosing in C57Bl6 mice with four doses (60 ng to 60 μg) of UFH was carried out for fourteen consecutive days, with both blood coagulation measurements and subject adverse event monitoring. The pharmacokinetics of fluorescent-labeled UFH clearance from the nasal cavity were measured in mice by in vivo imaging. Intranasal UFH at 2000 U/day solution with nasal spray …


Which Pharmacists Are Performing Antimicrobial Stewardship: A National Survey And A Call For Collaborative Efforts, Brandon Dionne, Jamie L. Wagner, Daniel B. Chastain, Meagen Rosenthal Feb 2022

Which Pharmacists Are Performing Antimicrobial Stewardship: A National Survey And A Call For Collaborative Efforts, Brandon Dionne, Jamie L. Wagner, Daniel B. Chastain, Meagen Rosenthal

Faculty and Student Publications

Abstract Objectives: To determine how pharmacists with formal antimicrobial stewardship program (ASP) responsibilities prioritize their time and pharmacists without formal antimicrobial stewardship program responsibilities contribute to ASP activities. Design: A nationwide survey. Respondents: Members of the American College of Clinical Pharmacy who subscribe to the following practice and research network e-mail listservs: infectious diseases, adult medicine, cardiology, critical care, hematology-oncology, immunology and transplantation, and pediatrics. Methods: A survey was distributed via listservs. Respondents were asked about their personal and institutional demographics and ASP activities. Results: In total, 245 pharmacists responded: 135 pharmacists with formal antimicrobial stewardship program responsibilities; 110 pharmacists …


The Influence Of Social Determinants Of Health On The Provision Of Postpartum Contraceptives In Medicaid, Irene Nsiah, Nidhi Vij Mali, Marie Barnard, Swarnali Goswami Feb 2022

The Influence Of Social Determinants Of Health On The Provision Of Postpartum Contraceptives In Medicaid, Irene Nsiah, Nidhi Vij Mali, Marie Barnard, Swarnali Goswami

Faculty and Student Publications

Disparities continue to exist in the timely provision of postpartum contraception. This study aimed to identify prevalence and factors associated with postpartum contraception provision among women enrolled in Medicaid. A retrospective cohort study was conducted using the 2014 National Medicaid data, linked to county‐level social vulnerability index (SVI) data. Women aged 15–44 with a live birth in 2014 were included. Multivariable logistic regression was used to predict 3‐day provision of long‐acting reversible contraception (LARC) and 60‐day provision of most effective or moderately effective contraceptives (MMEC). Overall, 3‐day LARC provision was 0.2% while 60‐day MMEC was 36.3%. Significantly lower odds of …


Phytochemical Screening, In Vitro And In Silico Studies Of Volatile Compounds From Petroselinum Crispum (Mill) Leaves Grown In Saudi Arabia, Ahmed I. Foudah, Mohammad H. Alqarni, Aftab Alam, Mohammad Ayman Salkini Feb 2022

Phytochemical Screening, In Vitro And In Silico Studies Of Volatile Compounds From Petroselinum Crispum (Mill) Leaves Grown In Saudi Arabia, Ahmed I. Foudah, Mohammad H. Alqarni, Aftab Alam, Mohammad Ayman Salkini

Faculty and Student Publications

The herbal plant Petroselinum crispum (P. crispum) (Mill) is commonly available around the world. In this study, the leaves of the herbal plant P. crispum were collected from the central region of Al-Kharj, Saudi Arabia, to explore their in vitro pharmacological activity. Essential oil from the leaves of P. crispum was isolated using the hydrodistillation method. The composition of P. crispum essential oil (PCEO) was determined using Gas chromatography-mass spectrometry (GC-MS). A total of 67 components were identified, representing approximately 96.02% of the total volatile composi-tion. Myristicin was identified as the principal constituent (41.45%). The in vitro biological activity was …


A Multitarget Approach To Evaluate The Efficacy Of Aquilaria Sinensis Flower Extract Against Metabolic Syndrome, Hee Sung Chae, Olivia Dale, Tahir Maqbool Mir, Bharathi Avula Feb 2022

A Multitarget Approach To Evaluate The Efficacy Of Aquilaria Sinensis Flower Extract Against Metabolic Syndrome, Hee Sung Chae, Olivia Dale, Tahir Maqbool Mir, Bharathi Avula

Faculty and Student Publications

Aquilaria sinensis (Lour.) Spreng is known for its resinous secretion (agarwood), often secreted in defense against injuries. We investigated the effects of A. sinensis flower extract (AF) on peroxisome proliferator-activated receptors alpha and gamma (PPARα and PPARγ), liver X receptor (LXR), glucose uptake, and lipid accumulation (adipogenesis). Activation of PPARα, PPARγ and LXR was determined in hepatic (HepG2) cells by reporter gene assays. Glucose uptake was determined in differentiated muscle (C2C12) cells using 2-NBDG (2-deoxy-2-[(7-nitro-2,1,3-benzoxadiazol-4-yl)amino]-D-glucose). Adipogenesis was determined in adipocytes (3T3-L1 cells) by Oil red O staining. At a concentration of 50 µg/mL, AF caused 12.2-fold activation of PPARα and …


Lip Reconstruction By Double Layer And Double Flap New Combination Technique: A Case Series, Antonio Cortese, Salvatore Catalano, Antonio Alberto Maria Giunta, Antonio Borri Feb 2022

Lip Reconstruction By Double Layer And Double Flap New Combination Technique: A Case Series, Antonio Cortese, Salvatore Catalano, Antonio Alberto Maria Giunta, Antonio Borri

Faculty and Student Publications

In the past, lip reconstruction after ablative surgery has been performed by primary closure and more recently by free flap transfer technique. Cheek’s skin flap has been used to reconstruct the lower lip cutaneous portion. This study presents a reconstructive method for the vermillion and the lip’s cutaneous portion using the Goldstein-Robotti techniques (for the vermillion) and the buccinator flap to reconstruct the cutaneous lip portion and the perioral muscles. This procedure allows a complete reconstruction with a double layer technique for defects of more than one-third of both lips, together or alone, including modiolus, showing satisfactory functionality and aesthetics. …


Do Formulation And Dose Of Long-Term Opioid Therapy Contribute To Risk Of Adverse Events Among Older Adults?, Monika Salkar, Sujith Ramachandran, John P. Bentley, Ike Eriator Feb 2022

Do Formulation And Dose Of Long-Term Opioid Therapy Contribute To Risk Of Adverse Events Among Older Adults?, Monika Salkar, Sujith Ramachandran, John P. Bentley, Ike Eriator

Faculty and Student Publications

Background: Chronic non-cancer pain (CNCP) is highly prevalent in older adults and long-term opioid therapy (LTOT) has been used to manage chronic pain. However, the safety of LTOT among older adults with CNCP is not well-established and there is a need to identify therapy-related risk factors of opioid-related adverse events among older adults. Objective: To evaluate the relationship between opioid dose and formulation and the risk of opioid-related adverse events among Medicare-eligible older adults on LTOT. Design: Nested case-control study. Participants: Older Medicare beneficiaries (N=35,189) who received > 3 opioid prescriptions with a total days-supply of >45 days within a 90-day …


Designing A Clinical Study With Dietary Supplements: It's All In The Details, Z. Elizabeth Floyd, David M. Ribnicky, Ilya Raskin, Daniel S. Hsia Jan 2022

Designing A Clinical Study With Dietary Supplements: It's All In The Details, Z. Elizabeth Floyd, David M. Ribnicky, Ilya Raskin, Daniel S. Hsia

Faculty and Student Publications

A successful randomized clinical trial of the effect of dietary supplements on a chosen endpoint begins with developing supporting data in preclinical studies while paying attention to easily overlooked details when planning the related clinical trial. In this perspective, we draw on our experience studying the effect of an ethanolic extract from Artemisia dracunculus L. (termed PMI-5011) on glucose homeostasis as a potential therapeutic option in providing resilience to metabolic syndrome (MetS). Decisions on experimental design related to issues ranging from choice of mouse model to dosing levels and route of administration in the preclinical studies will be discussed in …


Phytochemical Investigation Of Egyptian Riverhemp: A Potential Source Of Antileukemic Metabolites, Shimaa M. Abdelgawad, Mona H. Hetta, Mohamed A. Ibrahim, Premalatha Balachandran Jan 2022

Phytochemical Investigation Of Egyptian Riverhemp: A Potential Source Of Antileukemic Metabolites, Shimaa M. Abdelgawad, Mona H. Hetta, Mohamed A. Ibrahim, Premalatha Balachandran

Faculty and Student Publications

As part of our research group's continuous efforts to find alternative treatments for cancer, the aqueous ethanol extract of Sesbania sesban L. Merr. (SS, Egyptian riverhemp) demonstrated an antileukemic activity against K562 cell line. Bioguided fractionation of SS leaves hydroethanolic extract resulted in the isolation of one new compound (33) named as hederatriol 3-O-β-D-glucuronic acid methyl ester as well as 34 known compounds. Seven compounds ((34), (22), (20), (24), (21), (19), and (35)) showed high antiproliferative effects (IC50 = 22.3, 30.8, 31.3, 33.7, 36.6, 37.5, and 41.5 μM, respectively), while four compounds ((32), (5), (29), and (1)) showed milder activities …


Cryptococcosis In A Patient With Multiple Myeloma Receiving Pomalidomide: A Case Report And Literature Review, Daniel B. Chastain, Sahand Golpayegany, Andrés F. Henao-Martínez, Brittany T. Jackson Jan 2022

Cryptococcosis In A Patient With Multiple Myeloma Receiving Pomalidomide: A Case Report And Literature Review, Daniel B. Chastain, Sahand Golpayegany, Andrés F. Henao-Martínez, Brittany T. Jackson

Faculty and Student Publications

While overall survival with multiple myeloma (MM) has improved, patients suffer from overwhelming tumor burden, MM-associated comorbidities, and frequent relapses requiring administration of salvage therapies. As a result, this vicious cycle is often characterized by cumulative immunodeficiency stemming from a combination of disease- and treatment-related factors leading to neutropenia, T-cell deficiency, and hypogammaglobulinemia. Infectious etiologies differ based on the duration of MM and treatment-related factors, such as number of previous treatments and cumulative dose of corticosteroids. Herein, we present the case of a patient who was receiving pomalidomide without concomitant corticosteroids for MM and was later found to have cryptococcosis, …


Age-Related Neuroendocrine, Cognitive, And Behavioral Co-Morbidities Are Promoted By Hiv-1 Tat Expression In Male Mice, Alaa N. Qrareya, Fakhri Mahdi, Marc J. Kaufman, Nicole M. Ashpole Jan 2022

Age-Related Neuroendocrine, Cognitive, And Behavioral Co-Morbidities Are Promoted By Hiv-1 Tat Expression In Male Mice, Alaa N. Qrareya, Fakhri Mahdi, Marc J. Kaufman, Nicole M. Ashpole

Faculty and Student Publications

In the U.S. about half of the HIV-infected individuals are aged 50 and older. In men living with HIV, secondary hypogonadism is common and occurs earlier than in seronegative men, and its prevalence increases with age. While the mechanisms(s) are unknown, the HIV-1 trans-activator of transcription (Tat) protein disrupts neuroendocrine function in mice partly by dysregulating mitochondria and neurosteroidogenesis. We hypothesized that conditional Tat expression in middle-aged male transgenic mice [Tat(+)] would promote age-related comorbidities compared to age-matched controls [Tat(−)]. We expected Tat to alter steroid hormone milieu consistent with behavioral deficits. Middle-aged Tat(+) mice had lower circulating testosterone and …


Synthesis Of 3,4,5-Trisubstituted Isoxazoles In Water Via A [3 + 2]-Cycloaddition Of Nitrile Oxides And 1,3-Diketones, Β-Ketoesters, Or Β-Ketoamides, Md Imran Hossain, Md Imdadul H. Khan, Seong Jong Kim, Hoang V. Le Jan 2022

Synthesis Of 3,4,5-Trisubstituted Isoxazoles In Water Via A [3 + 2]-Cycloaddition Of Nitrile Oxides And 1,3-Diketones, Β-Ketoesters, Or Β-Ketoamides, Md Imran Hossain, Md Imdadul H. Khan, Seong Jong Kim, Hoang V. Le

Faculty and Student Publications

Herein we report a method for the synthesis of 3,4,5-trisubstituted isoxazoles in water under mild basic conditions at room temperature via a [3 + 2]-cycloaddition of nitrile oxides and 1,3-diketones, β-ketoesters, or β-ketoamides. We optimized the reaction conditions to control the selectivity of the production of isoxazoles and circumvent other competing reactions, such as O-imidoylation or hetero [3 + 2]-cycloaddition. The reaction happens fast in water and completes within 1-2 hours, which provides an environmentally friendly access to 3,4,5-trisubstituted isoxazoles, an important class of structures found in numerous bioactive natural products and pharmaceuticals. Additionally, we optimized the reaction conditions to …


Identification Of An Orally Bioavailable, Brain-Penetrant Compound With Selectivity For The Cannabinoid Type 2 Receptor, Meirambek Ospanov, Suresh P. Sulochana, Jason J. Paris, John M. Rimoldi Jan 2022

Identification Of An Orally Bioavailable, Brain-Penetrant Compound With Selectivity For The Cannabinoid Type 2 Receptor, Meirambek Ospanov, Suresh P. Sulochana, Jason J. Paris, John M. Rimoldi

Faculty and Student Publications

Modulation of the endocannabinoid system (ECS) is of great interest for its therapeutic relevance in several pathophysiological processes. The CB2 subtype is largely localized to immune effectors, including microglia within the central nervous system, where it promotes anti-inflammation. Recently, a rational drug design toward precise modulation of the CB2 active site revealed the novelty of Pyrrolo[2,1-c][1,4]benzodiazepines tricyclic chemotype with a high conformational similarity in comparison to the existing leads. These compounds are structurally unique, confirming their chemo-type novelty. In our continuing search for new chemotypes as selective CB2 regulatory molecules, following SAR approaches, a total of 17 selected (S,E)-11-[2-(arylmethylene)hydrazono]-PBD analogs …


1,2,3-Triazole Derivatives As Highly Selective Cannabinoid Receptor Type 2 (Cb2) Agonists, Amer H. Tarawneh, Pankaj Pandey, Lo'ay A. Al-Momani, Anastassiya V. Gadetskaya Jan 2022

1,2,3-Triazole Derivatives As Highly Selective Cannabinoid Receptor Type 2 (Cb2) Agonists, Amer H. Tarawneh, Pankaj Pandey, Lo'ay A. Al-Momani, Anastassiya V. Gadetskaya

Faculty and Student Publications

The cannabinoid receptor 2 (CB2 receptor) has attracted considerable interest, mainly due to its potential as a target for therapeutics for treating various diseases that have a neuroinflammatory or neurodegenerative component while avoiding the adverse psychotropic effects that accompany CB1 receptor-based therapies. With the appreciation that CB2-selective ligands show marked functional selectivity, there is a renewed opportunity to explore this promising area of research from both a mechanistic as well as a therapeutic perspective. In this research, we are interested in the discovery of new chemotypes as highly selective CB2 modulators, which may serve as good starting points for further …


Dual Drug Loaded Lipid Nanocarrier Formulations For Topical Ocular Applications, Ahmed Adel Ali Youssef, Narendar Dudhipala, Soumyajit Majumdar Jan 2022

Dual Drug Loaded Lipid Nanocarrier Formulations For Topical Ocular Applications, Ahmed Adel Ali Youssef, Narendar Dudhipala, Soumyajit Majumdar

Faculty and Student Publications

Introduction: Untreated ocular infections can damage the unique fine structures of the eye with possible visual impairments and blindness. Ciprofloxacin (CIP) ophthalmic solution is prescribed as first-line therapy in ocular bacterial infections. Natamycin (NT) ophthalmic suspension is one of the progenitors in ocular antifungal therapy. Nanostructured lipid carriers (NLCs) have been widely examined for ocular penetration enhancement and distribution to deeper ocular tissues. The objective of the current study was to prepare NLCs loaded with a combination of CIP and NT (CIP-NT-NLCs) and embed them in an in-situ gelling system (CIP-NT-NLCs-IG). This novel formulation will target the co-delivery of CIP …


Preparation, Evaluation, And Pharmacokinetics In Beagle Dogs Of A Taste-Masked Flunixin Meglumine Orally Disintegrating Tablet Prepared Using Hot-Melt Extrusion Technology And D-Optimal Mixture Design, Yangfeng Xu, Guoqing Yan, Xuemei Wen, Liqin Wu Jan 2022

Preparation, Evaluation, And Pharmacokinetics In Beagle Dogs Of A Taste-Masked Flunixin Meglumine Orally Disintegrating Tablet Prepared Using Hot-Melt Extrusion Technology And D-Optimal Mixture Design, Yangfeng Xu, Guoqing Yan, Xuemei Wen, Liqin Wu

Faculty and Student Publications

Flunixin meglumine (FM) is a nonsteroidal anti-inflammatory drug limited by irritation of the respiratory tract and mucosa in veterinary tissue. This study aimed to develop a taste-masked FM solid dispersion (SD) by hot-melt extrusion (HME) and formulate an orally disintegrating tablet (ODT) with selected excipients by direct compression. Eudragit® E PO was chosen as the matrix, and HME parameters were optimized: extrusion temperature, 135℃; screw speed, 100 rpm; and drug loading, 20%. Characterization techniques proved that FM was rendered amorphous in the HME extrudate. In vitro dissolution studies showed that FM SD released significantly slower than the corresponding physical mixture …


Discovery Of New 1h-Pyrazolo[3,4-D]Pyrimidine Derivatives As Anticancer Agents Targeting EgfrWt And EgfrT790m, Ahmed A. Gaber, Mohamed Sobhy, Abdallah Turky, Hanan Gaber Abdulwahab Jan 2022

Discovery Of New 1h-Pyrazolo[3,4-D]Pyrimidine Derivatives As Anticancer Agents Targeting EgfrWt And EgfrT790m, Ahmed A. Gaber, Mohamed Sobhy, Abdallah Turky, Hanan Gaber Abdulwahab

Faculty and Student Publications

New 1H-pyrazolo[3,4-d]pyrimidine derivatives were designed and synthesised to act as epidermal growth factor receptor inhibitors (EGFRIs). The synthesised derivatives were assessed for their in vitro anti-proliferative activities against A549 and HCT-116 cancer cells. Compounds 8, 10, 12a, and 12b showed potent anti-proliferative activities. Compound 12b was the most promising member with IC50 values of 8.21 and 19.56 µM against A549 and HCT-116, respectively. Compounds 8, 10, 12a, and 12b were evaluated for their kinase inhibitory activities against wild EGFR (EGFRWT). Compound 12b was the most potent member showing an IC50 value of 0.016 µM. In addition, compound 12b showed noticeable …


Guide To Common Shallow Sponges Of St. Thomas, Usvi, Deborah Gochfeld, M. Cristina Diaz Jan 2022

Guide To Common Shallow Sponges Of St. Thomas, Usvi, Deborah Gochfeld, M. Cristina Diaz

Faculty and Student Publications

No abstract provided.


Early Multicenter Experience With Imipenem-Cilastatin-Relebactam For Multidrug-Resistant Gram-Negative Infections, Nicholas Rebold, Taylor Morrisette, Abdalhamid M. Lagnf, Sara Alosaimy Dec 2021

Early Multicenter Experience With Imipenem-Cilastatin-Relebactam For Multidrug-Resistant Gram-Negative Infections, Nicholas Rebold, Taylor Morrisette, Abdalhamid M. Lagnf, Sara Alosaimy

Faculty and Student Publications

A multicenter case series of 21 patients were treated with imipenem-cilastatin-relebactam. There were mixed infection sources, with pulmonary infections (11/21,52%) composing the majority. The primary pathogen was Pseudomonas aeruginosa (16/21, 76%), and 15/16 (94%) isolates were multidrug-resistant. Thirty-day survival occurred in 14/21 (67%) patients. Two patients experienced adverse effects.


Cryo-Em Reveals The Architecture Of Placental Malaria Var2csa And Provides Molecular Insight Into Chondroitin Sulfate Binding, Kaituo Wang, Robert Dagil, Thomas Lavstsen, Sandeep K. Misra Dec 2021

Cryo-Em Reveals The Architecture Of Placental Malaria Var2csa And Provides Molecular Insight Into Chondroitin Sulfate Binding, Kaituo Wang, Robert Dagil, Thomas Lavstsen, Sandeep K. Misra

Faculty and Student Publications

Placental malaria can have severe consequences for both mother and child and effective vaccines are lacking. Parasite-infected red blood cells sequester in the placenta through interaction between parasite-expressed protein VAR2CSA and the glycosaminoglycan chondroitin sulfate A (CS) abundantly present in the intervillous space. Here, we report cryo-EM structures of the VAR2CSA ectodomain at up to 3.1 Å resolution revealing an overall V-shaped architecture and a complex domain organization. Notably, the surface displays a single significantly electropositive patch, compatible with binding of negatively charged CS. Using molecular docking and molecular dynamics simulations as well as comparative hydroxyl radical protein foot-printing of …


Identification Of A Solo Acylhomoserine Lactone Synthase From The Myxobacterium Archangium Gephyra, Hanan Albataineh, Maya Duke, Sandeep K. Misra, Joshua S. Sharp Dec 2021

Identification Of A Solo Acylhomoserine Lactone Synthase From The Myxobacterium Archangium Gephyra, Hanan Albataineh, Maya Duke, Sandeep K. Misra, Joshua S. Sharp

Faculty and Student Publications

Considered a key taxon in soil and marine microbial communities, myxobacteria exist as coordinated swarms that utilize a combination of lytic enzymes and specialized metabolites to facilitate predation of microbes. This capacity to produce specialized metabolites and the associated abundance of biosynthetic pathways contained within their genomes have motivated continued drug discovery efforts from myxobacteria. Of all myxobacterial biosynthetic gene clusters deposited in the antiSMASH database, only one putative acylhomoserine lactone (AHL) synthase, agpI, was observed, in genome data from Archangium gephyra. Without an AHL receptor also apparent in the genome of A. gephyra, we sought to determine if AgpI …


Characterization And In Vitro And In Vivo Evaluation Of Tacrolimus-Loaded Poly(Ε-Caprolactone) Nanocapsules For The Management Of Atopic Dermatitis, Guilherme Dos Anjos Camargo, Leandro Ferreira, Diego José Schebelski, Amanda Martinez Lyra Dec 2021

Characterization And In Vitro And In Vivo Evaluation Of Tacrolimus-Loaded Poly(Ε-Caprolactone) Nanocapsules For The Management Of Atopic Dermatitis, Guilherme Dos Anjos Camargo, Leandro Ferreira, Diego José Schebelski, Amanda Martinez Lyra

Faculty and Student Publications

Background: Tacrolimus (TAC) is a drug of natural origin used in conventional topical dosage forms to control atopic dermatitis. However, direct application of the drug often causes adverse side effects in some patients. Hence, drug nanoencapsulation could be used as an improved novel therapy to mitigate the adverse effects and enhance bioavailability of the drug. Methods: Physicochemical properties, in vitro drug release experiments, and in vivo anti-inflammatory activity studies were performed. Results: TAC-loaded nanocapsules were successfully prepared by the interfacial deposition of preformed polymer using poly(ε-caprolactone) (PCL). The nanoparticu-late systems presented a spherical shape with a smooth and regular surface, …


Extracts From Pulsatilla Patens Target Cancer-Related Signaling Pathways In Hela Cells, Grażyna Łaska, Magdalena Maciejewska-Turska, Elwira Sieniawska, Łukasz Świątek Dec 2021

Extracts From Pulsatilla Patens Target Cancer-Related Signaling Pathways In Hela Cells, Grażyna Łaska, Magdalena Maciejewska-Turska, Elwira Sieniawska, Łukasz Świątek

Faculty and Student Publications

The purpose of this study was to determine if a methanolic extract of the Pulsatilla patens (L.) Mill. can inhibit the progression of cancer through the modulation of cancer-related metabolic signaling pathways. We analyzed a panel of 13 inducible luciferase reporter gene vectors which expression is driven by enhancer elements that bind to specific transcription factors for the evaluation of the activity of cancer signaling pathways. The root extract of P. patens exhibited strong inhibition of several signaling pathways in HeLa cells, a cervical cancer cell line, and was found to be the most potent in inhibiting the activation of …


Functional Genomics Study Of Pseudomonas Putida To Determine Traits Associated With Avoidance Of A Myxobacterial Predator, Shukria Akbar, D. Cole Stevens Dec 2021

Functional Genomics Study Of Pseudomonas Putida To Determine Traits Associated With Avoidance Of A Myxobacterial Predator, Shukria Akbar, D. Cole Stevens

Faculty and Student Publications

Predation contributes to the structure and diversity of microbial communities. Predatory myxobacteria are ubiquitous to a variety of microbial habitats and capably consume a broad diversity of microbial prey. Predator–prey experiments utilizing myxobacteria have provided details into predatory mechanisms and features that facilitate consumption of prey. However, prey resistance to myxobacterial predation remains underexplored, and prey resistances have been observed exclusively from predator–prey experiments that included the model myxobacterium Myxococcus xanthus. Utilizing a predator–prey pairing that instead included the myxobacterium, Cystobacter ferrugineus, with Pseudomonas putida as prey, we observed surviving phenotypes capable of eluding predation. Comparative transcriptomics between P. putida …