Other Pharmacy and Pharmaceutical Sciences Commons^™

Cytokine-Targeted Therapeutics For Kshv-Associated Disease, Nedaa Alomari, Jennifer Totonchy

Pharmacy Faculty Articles and Research

Kaposi’s sarcoma-associated herpesvirus (KSHV) also known as human herpesvirus 8 (HHV-8), is linked to several human malignancies including Kaposi sarcoma (KS), primary effusion lymphoma (PEL), multicentric Castleman’s disease (MCD) and recently KSHV inflammatory cytokine syndrome (KICS). As with other diseases that have a significant inflammatory component, current therapy for KSHV-associated disease is associated with significant off-target effects. However, recent advances in our understanding of the pathogenesis of KSHV have produced new insight into the use of cytokines as potential therapeutic targets. Better understanding of the role of cytokines during KSHV infection and tumorigenesis may lead to new preventive or therapeutic …

Parent Responses To Pediatric Pain: The Differential Effects Of Ethnicity On Opioid Consumption, Candice D. Donaldson, Brooke N. Jenkins, Michelle A. Fortier, Michael T. Phan, Daniel M. Tomaszewski, Sun Yang, Zeev N. Kain

Psychology Faculty Articles and Research

Objective

Within the context of the United States opioid epidemic, some parents often fear the use of opioids to help manage their children's postoperative pain. As a possible consequence, parents often do not dispense optimal analgesic medications to their children after surgery, putting their children at risk of suffering from postsurgical pain. The objective of this research was to assess ethnicity as a predictor of both pain and opioid consumption, and to examine how Hispanic/Latinx and Non-Hispanic White parents alter their child's opioid consumption in response to significant postsurgical pain.

Methods

Participants were 254 children undergoing outpatient tonsillectomy and/or adenoidectomy …

Evaluation Of Sodium Valproate Low Dose Efficacy In Radicular Pain Management And It’S Relation With Pharmacokinetics Parameters, Mona Ghasemian, Mohammad Bagher Owlia, Mohammad Hossein Mosaddegh, Masoud Nakhaie Nejad, Seyed Mojtaba Sohrevardi

BioMedicine

Background: Radiculopathy due to lumbar or cervical disc disease is the most common chronic neuropathic pain in adults. The aim of present study was evaluation of low dose of sodium valproate on radicular pain and determining VPA pharmacokinetics.

Materials and Methods: In this double blind randomized placebo control clinical study, 80 patients with established lumbar or cervical radicular pain, have been randomly allocated into two study groups: 40 have received sodium valproate 200 mg/day and Celecoxib 100 mg/day and acetaminophen 500 mg PRN as rescue medication, and second group has received placebo, Celecoxib and acetaminophen. Quantitative assessment of pain was …

Artificial Intelligence–Powered Smartphone App To Facilitate Medication Adherence: Protocol For A Human Factors Design Study, Don Roosan, Jay Chok, Mazharul Karim, Anandi V. Law, Andrius Baskys, Angela Hwang, Moom Roosan

Pharmacy Faculty Articles and Research

Background: Medication Guides consisting of crucial interactions and side effects are extensive and complex. Due to the exhaustive information, patients do not retain the necessary medication information, which can result in hospitalizations and medication nonadherence. A gap exists in understanding patients’ cognition of managing complex medication information. However, advancements in technology and artificial intelligence (AI) allow us to understand patient cognitive processes to design an app to better provide important medication information to patients.

Objective: Our objective is to improve the design of an innovative AI- and human factor–based interface that supports patients’ medication information comprehension that could potentially …

Acute And Chronic Dosing Of A High-Affinity Rat/Mouse Chimeric Transferrin Receptor Antibody In Mice, Demi M. Castellanos, Jiahong Sun, Joshua Yang, Weijun Ou, Alexander C. Zambon, William M. Pardridge, Rachita K. Sumbria

Pharmacy Faculty Articles and Research

Non-invasive brain delivery of neurotherapeutics is challenging due to the blood-brain barrier. The revived interest in transferrin receptor antibodies (TfRMAbs) as brain drug-delivery vectors has revealed the effect of dosing regimen, valency, and affinity on brain uptake, TfR expression, and Fc-effector function side effects. These studies have primarily used monovalent TfRMAbs with a human constant region following acute intravenous dosing in mice. The effects of a high-affinity bivalent TfRMAb with a murine constant region, without a fusion partner, following extravascular dosing in mice are, however, not well characterized. Here we elucidate the plasma pharmacokinetics and safety of a high-affinity bivalent …

Click-Free Synthesis Of A Multivalent Tricyclic Peptide As A Molecular Transporter, Sumit Kumar, Dindyal Mandal, Shaima Ahmed El-Mowafi, Saghar Mozaffari, Rakesh Kumar Tiwari, Keykavous Parang

Pharmacy Faculty Articles and Research

The cellular delivery of cell-impermeable and water-insoluble molecules remains an ongoing challenge to overcome. Previously, we reported amphipathic cyclic peptides c[WR]₄ and c[WR]₅ consisting of alternate arginine and tryptophan residues as nuclear-targeting molecular transporters. These peptides contain an optimal balance of positive charge and hydrophobicity, which is required for interactions with the phospholipid bilayer to facilitate their application as a drug delivery system. To further optimize them, we synthesized and evaluated a multivalent tricyclic peptide as an efficient molecular transporter. The monomeric cyclic peptide building blocks were synthesized using Fmoc/tBu solid-phase chemistry and cyclization in the …

Effect Of High Glucose On Ocular Surface Epithelial Cell Barrier And Tight Junction Proteins, Saleh M. Alfuraih, Ashley Barbarino, Christopher Ross, Kiumars Shamloo, Vishal Jhanji, Miao Zhang, Ajay Sharma

Pharmacy Faculty Articles and Research

PURPOSE. Patients with diabetes mellitus are reported to have ocular surface defects, impaired ocular surface barrier function, and a higher incidence of corneal and conjunctival infections. Tight junctions are critical for ocular surface barrier function. The present study was designed to investigate the effect of high glucose exposure on human corneal and conjunctival epithelial cell barrier function and tight junction proteins.

METHODS. Human corneal and conjunctival epithelial cells were exposed to 15 mM and 30 mM glucose for 24 and 72 hours. The barrier function was measured using transepithelial electrical resistance (TEER). The cell migration was quantified using scratch assay. …

Epigenetic Diet To Modulate Immune Response Against Sars-Cov-2, Andika Andika, Risa Ahdyani, Linda Erlina, Azminah Azminah, Arry Yanuar

Pharmaceutical Sciences and Research

The COVID-19 pandemic has spread to various parts of the world and caused many deaths. The victims are infected by SARS-CoV-2, a new type of coronavirus that has appeared since December 2019 and caused respiratory symptoms, fever, coughing, and shortness of breath. In addition to social distancing, wearing masks and washing hands, diet is important as a defense of the body against SARS-CoV-2. In this review, researchers conducted epigenetic diet studies that could potentially inhibit SARS-CoV-2, and can be consumed and used on a daily basis.

Antioxidant And Elastase Inhibitor Potential Of Petals And Receptacle Of Rose Flower (Rosa Damascena), Evi Mawarni, Chrismis Novalinda Ginting, Linda Chiuman, Ermi Girsang, Rr. Anisa Siwianti Handayani, Wahyu Widowati

Pharmaceutical Sciences and Research

Free radicals can cause damage to cells or tissues, autoimmune diseases, degenerative diseases, or cancer. Therefore, the body needs important substances, namely antioxidants that can help protect the body by reducing negative effect from free radicals. Rose flower (Rosa damascena) has anthocyanin pigment which belongs to flavonoid group which has a function as antioxidant or free radical scavenger. This study aims to determine antioxidant and anti-elastase potentials of rose petals and receptacles. The method used in this study was a qualitative phytochemical test to determine the compounds contained in the Rose Petal Extract (RPE) and Rose Receptacle Extract (RRE), ABTS …

Potential Risk Factors For Mortality Due To Cardiovascular Disease Among Hemodialysed Patients In Indonesia, Diana Laila Ramatillah, Syed Azhar Syed Sulaiman, Kashif Ullah Khan

Pharmaceutical Sciences and Research

Severe vascular calcifications, alterations in cardiovascular structure and function, immune dysfunction, and anemia are adverse effects of parathyroid hormone (PTH), which may contribute to increase risk factors of cardiovascular morbidity and mortality among renal failure patients. To evaluate the potential risk factors for mortality due to cardiovascular disease among hemodialysed patients in Indonesia, this cohort study was conducted. This study included 178 patients on hemodialysis who had been followed up two times a week for nine months (prospective cohort) and 185 patients who died in the last five years (retrospective cohort). Universal sampling technique were used to select the study …

A Study On The Formulation Of Plant Matrix Tablets From Coarse Botanical Materials Using Cinnamon Bark And Areca Nut As The Model Botanical Materials, Natalia Veronica, Xiu Hui Ang, Shing Ming Ooi, Celine Valeria Liew, Paul Wan Sia Heng

Pharmaceutical Sciences and Research

Background: There is much interest in formulating botanical materials into tablets due to the compactness and ease of administration. However, tableting of coarse milled botanical materials poses a challenge due to poor tableting properties. Objective: To evaluate the feasibility of wet granulation to produce tablets from coarse milled botanical materials and to assess the effect of formulation on properties of the tablets. Materials and Methods: Cinnamon bark and areca nut were milled to obtain 1–2 mm particle size, which was subsequently used in wet granulation using maltodextrin solution as a granulating liquid. Two diluents were tried; microcrystalline …

Antagonistic Drug-Herb Interactions Between Clinacanthus Nutans And Cyclophosphamide On Wrl 68 Cell Line, Nurliana Abd Mutalib, Normala Abd Latip

Pharmaceutical Sciences and Research

Clinacanthus nutans (Acanthaceae), locally known as Sabah snake grass, is popularly taken as prevention as well as treatment for cancer in Malaysia, despite lack of concrete clinical evidence. However, it is crucial to evaluate potential antagonistic, additive, or synergistic interactions that may result from the co-treatment of this plant in chemotherapy. In this study, we demonstrate the drug-herb interaction using combination treatment of C. nutans extracts and cyclophosphamide on the WRL 68 cell line. Materials and Methods: Aqueous and 70% ethanol extract of C. nutans leaves were prepared using decoction and maceration methods. MTT assay was used to test …

Long-Lasting, Patient-Controlled, Procedure-Free Contraception: A Review Of Annovera With A Pharmacist Perspective, Jennifer J. Virro, Kathleen Besinque, Christiane E. Carney, Danielle Gross, Brian Bernick, Sebastian Mirkin

Pharmacy Faculty Articles and Research

Annovera (segesterone acetate and ethinyl estradiol vaginal system) is a US Food and Drug Administration FDA-approved long-lasting, reversible contraceptive that is fully administered by the user and does not require a procedure for insertion or removal. The vaginal system is in the shape of a ring and contains low doses of a novel progestin, egesterone acetate, and ethinyl estradiol. It is made of silicone and is fully pliable and flexible. The vaginal system is reusable for 13 cycles, using a 21 days in/7 days out regimen, providing women with the ability to control their fertility. Particularly now during the COVID-19 …

Pharmacogenomics Cascade Testing (Phact): A Novel Approach For Preemptive Pharmacogenomics Testing To Optimize Medication Therapy, Don Roosan, Angela Hwang, Moom Roosan

Pharmacy Faculty Articles and Research

The implementation of pharmacogenomics (PGx) has come a long way since the dawn of utilizing pharmacogenomic data in clinical patient care. However, the potential benefits of sharing PGx results have yet to be explored. In this paper, we explore the willingness of patients to share PGx results, as well as the inclusion of family medication history in identifying potential family members for pharmacogenomics cascade testing (PhaCT). The genetic similarities in families allow for identifying potential gene variants prior to official preemptive testing. Once a candidate patient is determined, PhaCT can be initiated. PhaCT recognizes that further cascade testing throughout a …

Cyclic Peptide-Gadolinium Nanoparticles For Enhanced Intracellular Delivery, Amir Nasrolahi Shirazi, Shang Eun Park, Shirin Rad, Luiza Baloyan, Dindyal Mandal, Muhammad Imran Sajid, Ryley Hall, Sandeep Lohan, Khalid Zoghebi, Keykavous Parang, Rakesh Tiwari

Pharmacy Faculty Articles and Research

A cyclic peptide containing one cysteine and five alternating tryptophan and arginine amino acids [(WR)₅C] was synthesized using Fmoc/tBu solid-phase methodology. The ability of the synthesized cyclic peptide to produce gadolinium nanoparticles through an in situ one-pot mixing of an aqueous solution of GdCl₃ with [(WR)₅C] peptide solution was evaluated. Transmission electron microscopy showed the formed peptide-Gd nanoparticles in star-shape morphology with a size of ~250 nm. Flow cytometry investigation showed that the cellular uptake of a cell-impermeable fluorescence-labeled phosphopeptide (F′-GpYEEI, where F′ = fluorescein) was approximately six times higher in the presence of [(WR) …

Development Of An Lc-Esi-Ms/Ms Method For Determination Of A Novel Pyrrolomycin (Mp-1) And Application To Pre-Clinical Adme Studies, Wafaa N. Aldhafiri

Theses & Dissertations

A rapid, selective, and sensitive liquid chromatography coupled with tandem mass spectrometry (LC-MS/MS) method was developed and validated for quantitation of a novel Pyrrolomycin (MP-1) in mouse plasma. MP-1 was extracted from plasma utilizing a structural analog (PL-3) as the internal standard (IS). Analyte separation was achieved using a Waters Acquity UPLC®BEH C18 column (1.7 µm, 100 x 2.1 mm) protected with Acquity UPLC C18 guard column. Mobile phase consisted of 0.1% acetic acid in water (10%) and methanol (90%) at a total flow rate of 0.25 mL/min. The mass spectrometer was operated at unit resolution in the multiple reaction …

Understanding Covid-19: From Origin To Potential Therapeutics, Muhammad Moazzam, Muhammad Imran Sajid, Hamza Shahid, Jahanzaib Butt, Irfan Bashir, Muhammad Jamshaid, Amir Nasrolahi Shirazi, Rakesh Kumar Tiwari

Pharmacy Faculty Articles and Research

Currently, a global pandemic era of public health concerns is going on with the Coronavirus Disease 2019 (COVID-19), which is caused by severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2). The first case of COVID-19 was reported from Wuhan’s Huanan seafood market in China late December 2019. Bats, pangolins, and snakes have been nominated as salient carriers of the virus. Thanks to its high pathogenicity, it can cause severe respiratory infections. Fever, dry cough, sore throat, pneumonia, septic shock, and ground-glass opacities are the foremost clinical manifestations of COVID-19. Immunocompromised patients are at high risk for COVID-19 infection and may lead to …

Cyclic Peptide [R4w4] In Improving The Ability Of First-Line Antibiotics To Inhibit Mycobacterium Tuberculosis Inside In Vitro Human Granulomas, Joshua Hernandez, David Ashley, Ruoqiong Cao, Rachel Abrahem, Timothy Nguyen, Kimberly To, Aram Yegiazaryan, Ajayi Akinwale David, Rakesh Kumar Tiwari, Vishwanath Venketaraman

Pharmacy Faculty Articles and Research

Tuberculosis (TB) is currently one of the leading causes of global mortality. Medical non-compliance due to the length of the treatment and antibiotic side effects has led to the emergence of multidrug-resistant (MDR) strains of Mycobacterium tuberculosis (M. tb) that are difficult to treat. A current therapeutic strategy attempting to circumvent this issue aims to enhance drug delivery to reduce the duration of the antibiotic regimen or dosage of first-line antibiotics. One such agent that may help is cyclic peptide [R₄W₄], as it has been shown to have antibacterial properties (in combination with tetracycline) …

Heat Shock Protein 90 (Hsp90)-Inhibitor-Luminespib-Loaded-Protein-Based Nanoformulation For Cancer Therapy, Ankit K. Rochani, Sivakumar Balasubramanian, Aswathy Ravindran Girija, Toru Maekawa, Gagan Kaushal, Phd, D Sakthi Kumar

College of Pharmacy Faculty Papers

Drugs targeting heat shock protein 90 (Hsp90) have been extensively explored for their anticancer potential in advanced clinical trials. Nanoformulations have been an important drug delivery platform for the anticancer molecules like Hsp90 inhibitors. It has been reported that bovine serum albumin (BSA) nanoparticles (NPs) serve as carriers for anticancer drugs, which have been extensively explored for their therapeutic efficacy against cancers. Luminespib (also known as NVP-AUY922) is a new generation Hsp90 inhibitor that was introduced recently. It is one of the most studied Hsp90 inhibitors for a variety of cancers in Phase I and II clinical trials and is …

The Potential Roles Of Jamu For Covid-19: A Learn From The Traditional Chinese Medicine, Dwi Hartanti, Binar Asrining Dhiani, Shintia Lintang Charisma, Retno Wahyuningrum

Pharmaceutical Sciences and Research

As the pandemic of the coronavirus disease 2019 (COVID-19) continues while there is no drug and vaccine available, every effort to discover one should be considered. This review aimed to discuss the potential use of jamu, the Indonesian traditional herbal medicine, to deal with COVID-19 by following those of more-established traditional Chinese medicine (TCM). The online literature search using the PubMed database, as well as the circulars from the Indonesian Ministry of Health, were carried out to collect data up to June 07, 2020. The use of TCM for the treatment and prevention of COVID-19 has been officiated in the …

Sars-Cov-2: Virology And Drug Repurposing Approaches, Ratika Rahmasari, Heri Setiawan, Rezi Riadhi Syahdi, Ayun Arifianti, Marina Ika Irianti, Rani Sauriasari, Juliann Nzembi Makau, Muhareva Raekiansyah

Pharmaceutical Sciences and Research

An emerging coronavirus, SARS-CoV-2, is the causative agent for the ongoing pandemic of coronavirus disease 2019 (COVID-19), which has caused a worldwide social and economic disruption. Currently, no antiviral drugs with proven clinical efficacy, or vaccines for its prevention. Therefore, to combat the pandemic of this novel coronavirus, new effective treatments are urgently needed. In the process of traditional drug development, developing new drugs from scratch is a time- consuming process, requires high-investment, and is a high-risk process, which is impractical to face the immediate global challenge of the SARS-CoV-2 pandemic. Drug repurposing strategy is one of the effective ways …

Dermaseptin-Based Antiviral Peptides To Prevent Covid-19 Through In Silico Molecular Docking Studies Against Sars-Cov-2 Spike Protein, Taufik Muhammad Fakih

Pharmaceutical Sciences and Research

A pandemic coronavirus disease of 2019 (COVID-19) caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has now been declared a global pandemic by the World Health Organization. The search for new drugs, especially by utilizing antiviral peptides is a very potential area. Through this study, protein-peptide docking and protein-protein docking simulations were conducted using in silico methods to identify, evaluate, and explore the molecular affinity and interaction of dermaseptin peptide molecules produced by frogs of the genus Phyllomedusa against the SARS-CoV-2 spike protein macromolecule, and its effect on attachment to the surface of the ACE-2 (Angiotensin Converting Enzyme-2) receptor. …

Chloroquine: An Old To Be Repurposed Drug For Covid-19 Infection (Risk And Benefit), Oki Nugraha Putra, Ana Khusnul Faizah, Nani Wijayanti Dyah Nurrahman, Hardiyono Hardiyono

Pharmaceutical Sciences and Research

Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) causes Coronavirus Disease 2019 (COVID-19) with a high rate of mortality. Chloroquine and hydroxychloroquine have been used for antimalarial and autoimmune diseases for many years. Due to low toxicity and well tolerability as well as immunomodulatory properties, these drugs are proposed to treat viral infection. Some studies, both in vitro and in a clinical setting, have been evaluated for their ability to treat SARS- CoV-2 as promising therapies. Although The National Agency of Drugs and Food Control of The Republic of Indonesia issued emergency authorization for chloroquine and hydroxychloroquine to be used against …

Cytokine Storm In Covid-19: An Overview, Mechanism, Treatment Strategies, And Stem Cell Therapy Perspective, Nuriza Ulul Azmi, Meidi Utami Puteri, Donny Lukmanto

Pharmaceutical Sciences and Research

Coronavirus disease 2019 (COVID-19) is the disease caused by the highly transmittable novel coronavirus (SARS-CoV-2) infections. The disease was found at the end of December 2019, in Wuhan, China, and quickly spread worldwide with a higher mortality rate compared to the previous coronavirus disease. Cytokine plays an important role in the inflammatory response against coronavirus infection. However, in severely ill patients with COVID-19, an excessive amount of cytokine serum level (cytokine storm) has been associated with the aggravation of coronavirus disease leading to acute respiratory distress syndrome (ARDS). Thus, the management of the cytokine storm could be the key to …

A Mini Review : Clinically Significant Potential Drug-Drug Interactions In Covid-19 And Comorbid Therapy, Ana Khusnul Faizah, Nani Wijayanti Dyah Nurrahman, Oki Nugraha Putra

Pharmaceutical Sciences and Research

Coronavirus disease 2019 (COVID-19) is a disease caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) and can be aggravated by comorbid diseases. In administering COVID-19 therapy, we need to consider potential drug-drug interactions (pDDIs) with comorbid drugs. Most patients with comorbid diseases get polypharmacy, therefore the risk of pDDIs increases. Potential drug-drug interactions can cause unwanted effects such as toxicity to death. There is no on-label therapy for COVID-19 but FDA has Emergency Use Authorization (EUA) for hydroxychloroquine, chloroquine, azithromycin, remdesivir, ritonavir, and lopinavir. Some COVID-19 treatment potential drug-drug interactions have a level of severity C and D, so …

Remdesivir: Mechanism And Effectiveness For Coronavirus Disease 2019 (Covid-19), Vina Neldi, Suharjono Suharjono

Pharmaceutical Sciences and Research

Currently, coronavirus disease 2019 (COVID-19) is a very serious health problem. The World Health Organization (WHO) has characterized this disease as a pandemic. Recommendations related to vaccines and drugs are not available yet because they are still in the clinical trial phase, and one of the superior drugs is remdesivir which has an antiviral activity. Several clinical trials of this drug are being carried out with the aim of evaluating its safety and efficacy in COVID-19 patients. There are two clinical trials with completed recruitment status, which are NCT04257656 and NCT04280705. NCT04257656 showed that remdesivir had faster time for clinical …

Prediction Of Asiatic Acid Derivatives Affinity Against Sars-Cov-2 Main Protease Using Molecular Docking, Ida Musfiroh, Alia Resti Azura, Driyanti Rahayu

Pharmaceutical Sciences and Research

COVID-19 is a pandemic that currently occurs in almost all parts of the world, caused by a new coronavirus species that can infect humans, namely SARS-CoV-2. To date, there is no effective drug to treat COVID-19. There are studies proving that the secondary metabolites of pentacyclic triterpenes have antiviral activity, one of which is asiatic acid. The aims of this study are to obtain the affinity and interactions of asiatic acid derivative structures in inhibiting the main protease of SARS-CoV-2. The research method was molecular docking of asiatic acid and its derivatives against the main protease of SARS-CoV-2 (6LU7) consisting …

Design And Evaluation Of Peptide Lipid-Associated Nucleic Acids (Planas) For Sirna And Crispr/Cas9 Delivery And Protein Silencing, Ryley Hall

Pharmaceutical Sciences (MS) Theses

Breast cancer affects 1 in 8 women in the United States. The American Cancer Society has estimated that in 2020 about 276,480 new cases of invasive breast cancer will be diagnosed in women. Cancer research has taken a turn in the last several decades to focus on new approaches to combat the disease. This project focuses on two approaches, siRNA and CRISPR/Cas9 that can have potential applications in cancer research.

The first approach is a specific type of RNA interference (RNAi) that has been pursued due to its therapeutic potential in cancer research. In short, siRNA delivery is a method …

Prospects For Rnai Therapy Of Covid-19, Hasan Uludağ, Kylie Parent, Hamidreza Montazeri Aliabadi, Azita Haddadi

Pharmacy Faculty Articles and Research

COVID-19 caused by the SARS-CoV-2 virus is a fast emerging disease with deadly consequences. The pulmonary system and lungs in particular are most prone to damage caused by the SARS-CoV-2 infection, which leaves a destructive footprint in the lung tissue, making it incapable of conducting its respiratory functions and resulting in severe acute respiratory disease and loss of life. There were no drug treatments or vaccines approved for SARS-CoV-2 at the onset of pandemic, necessitating an urgent need to develop effective therapeutics. To this end, the innate RNA interference (RNAi) mechanism can be employed to develop front line therapies against …

Uplc-Ms/Ms Analysis Of Cyp1a-Mediated Ethoxyresorufin-O-Deethylation Activity In The Rat Kidney Microsomes, Devaraj Venkatapura Chandrashekar, Reza Mehvar

Pharmacy Faculty Articles and Research

Ethoxyresorufin (ER)-O-deethylation (EROD) activity has been widely used to assess cytochrome P450 1A (CYP1A) activity. The kinetics of CYP1A activity have been well characterized in the liver microsomes. However, studies in kidney microsomes are limited due to the much lower EROD activity in this organ. Here, we developed and validated a sensitive UPLC-MS/MS assay for the characterization of the EROD activity in the rat kidney microsomes. In a 50 µL reaction mixture, rat kidney microsomes (0.25 mg/mL) were incubated with ER (0.1–5 µM) and NADPH (1 mM) for 10 min. Acidic solvents, such as trichloroacetic acid or formic …