Pharmacology Commons^™

Tofacitinib, Inderbir S. Padda, Rajat Bhatt, Mayur S. Parmar

HPD Articles

No abstract provided.

Anticancer Effect Of Indanone-Based Thiazolyl Hydrazone Derivative On P53 Mutant Colon Cancer Cell Lines: In Vitro And In Vivo Study, Silpa Narayanan

Theses and Dissertations

Colorectal cancer is the third leading cause of cancer related deaths in the United States. Currently, irinotecan, a topoisomerase I inhibitor, is an important anticancer drug approved for patients with advanced or recurrent colorectal cancer. Considering the low response rate and the events of high toxicity caused by irinotecan, we evaluated a series of thirteen thiazolyl hydrazone derivatives of 1-indanone for their potential antineoplastic activity and four compounds showed promising anticancer activity against most of the tested colon cancer cell lines with IC50 values ranging from 0.41 ± 0.19 to 6.85 ± 1.44 μM. It is noteworthy that the compound, …

Effect Of Inhibition Of Glycogen Catabolism In Hepatocellular Carcinoma Cells, Shrikant Barot

Theses and Dissertations

Metabolic reprogramming is one of the important features of cancers, and there has been growing interest in targeting metabolic proteins to treat cancer. Glycogen is a polymer of glucose and serves as its storage unit in cells. Glycogen can provide energy to cells during the situations of high energy demand. A number of tumors are known to contain high levels of glycogen than their normal tissue counterparts. The liver plays an essential role in maintaining glucose homeostasis in the body via storing it into glycogen. The significance of glycogen metabolism in patients suffering from hepatocellular carcinoma (HCC) has not been …

Boost The Dsicovery Of Mrp7/Abcc10 Substrates And Inhibitors: Establishment Of New In Vitro And In Silico Models, Jingquan Wang

Theses and Dissertations

ATP-binding cassette (ABC) transporters are responsible for the efflux of structurally distinct endo- and xenobiotics energized by ATP hydrolysis. MRP7/ABCC10 belongs to the 10th member of subfamily C and responsible for mediating MDR against a series of chemotherapeutic drugs such as taxanes, epothilones, Vinca alkaloids, anthracyclines and epipodophyllotoxins. Establishment of new in silico and in vitro models for MRP7 substrates/inhibitors prediction Considering the limited knowledge of MRP7, we established a homology model based on bovine MRP1 cryo-EM models. The final model was used for protein global motion analysis and docking analysis. Before docking, potential drug binding pockets were identified and …

Design, Synthesis And Pharmacological Evaluation Of Quinazolinamine Derivatives As Bcrp And P-Gp Inhibitors With Improved Metabolic Stability, Chao-Yun Cai

Theses and Dissertations

A series of twenty-two quinazolinamine derivatives showing potent inhibitory activities on BCRP and P-gp was synthesized. The reversal study showed that when combined with the potent dual BCRP and P-gp inhibitors 7-8, 29-31, and 34, the IC50 value of mitoxantrone was decreased from 6.50 µM to the range of 0.24 - 0.35 µM for BCRP, and IC50 value of colchicine was decreased from 7.34 μM to the range of 0.12 - 0.29 µM for P-gp. Cyclopropyl quinazolinamine 29 (VKCY-1), which was a dual BCRP and P-gp inhibitor, and azide quinazolinamine 40 (VKCY-2), which was a BCRP inhibitor, were selected for …

Pharmaceuticals In The Environment: Health Implications And Environmental Toxicity, Jessica Phillips

Wayne State University Dissertations

Approximately 2.9 billion prescriptions are written annually in the United States, with a multitude of biochemical actions, with 63151 tons used by food producing animals worldwide and an additional 55-77 million prescriptions written for companion animals. With increasing prescription and unknown toxicologic effects of many of these chemicals, zebrafish (danio rerio), an NIH approved human model, were used to model potentially health effects. Significant abnormalities were seen with extended duration metformin exposure from 4 hours post fertilization up to 5 days post fertilization, although short term metformin exposure for 24 hours at 4-5 days post fertilization did not lead to …

Amphiphilic Cell-Penetrating Peptides Containing Natural And Unnatural Amino Acids As Drug Delivery Tools And Antimicrobial Agents, David Salehi

Pharmaceutical Sciences (MS) Theses

Cell-penetrating peptides containing arginine as positively charged residues and tryptophan or diphenylalanine as hydrophobic residues were synthesized. The synthesis was accomplished through the Fmoc solid-phase peptide synthesis in the presence of HBTU and DIPEA. The side-chain protected linear peptides were cleaved from the resin and cyclized in the presence of DIC and HOAt in the solution phase overnight. MALDI-TOF mass spectrometry was used to characterize the peptides.

The cytotoxicity of the synthesized peptides was determined in CCRF-CEM (human, lymphoblast peripheral blood), and HEK-293 (human, embryonic epithelial kidney healthy) cells using the MTS assay. A concentration of 10 µM was found …

Investigating Lifespan And Legacy Health Effects Of Developmental Exposure To Environmental Toxicants, Danielle Meyer

Wayne State University Dissertations

The environmental presence of toxicants such as persistent organic pollutants, heavy metals, and contaminants of emerging concern is estimated to contribute to over 2 million deaths worldwide and health care costs ranging from ~3-9% of total global expenditures yearly. Many of the above toxicants are classified as endocrine-disrupting chemicals capable of interfering with endogenous hormonal function at environmentally relevant levels. Exposures during sensitive developmental windows can lead to reproductive, neurodevelopmental, and metabolic dysfunction that can last across the lifespan and/or be passed down to future generations. Such long-term effects remain to be well-understood; therefore, we modeled the effects of various …

Science-Based Regulation Of Pharmacological Substances In Competition Horses, Jacob Machin

Theses and Dissertations--Toxicology and Cancer Biology

Current testing methodologies within equine forensic toxicology focus on arbitrary thresholds and zero-tolerance policy. Modern analytical chemistry’s limits of detection are low enough that oftentimes femtogram-per-milliliter amounts of a substance can readily be identified in both blood and urine of a horse. For most pharmacologically relevant compounds, these concentrations have no relevance to pharmacological effect. It is therefore crucial that testing methodologies to determine appropriate thresholds and cut-offs be developed that are driven by biological activity rather than arbitrary limits of detection. This dissertation looks to address this by suggesting a system of calculated Effective Plasma Concentrations by which a …

Investigation Of Sodium Laurylglucosides Hydroxypropyl Sulfonate Through Response Surface Methodology – Effects Of Amphoteric Surfactant And Electrolyte, Phantira Uongpitakpan, Jutarat Kitsongsermthon

The Thai Journal of Pharmaceutical Sciences

The goal of this research was to investigate the effect of electrolyte and an amphoteric surfactant on the viscosity, foamability, and foam stability of sodium laurylglucosides hydroxypropyl sulfonate (SLHS), a new anionic surfactant. Different concentrations of cocamidopropyl betaine (CAPB, 0–6% w/w) and sodium chloride (NaCl, 0–3% w/w) were added into 10% w/w SLHS solution. Each formulation was evaluated for its viscosity using a viscometer, whereas the foamability and foam stability were measured using the cylinder shaking method and analyzed by response surface methodology. The result demonstrated that an increased viscosity of the mixture resulted with an increased NaCl concentration over …

Prospective Process Validation For The Manufacture Of Ketoprofen Fast Dissolving Tablets, Mariam Omari, P. Rashmi, G.S. Shantha Kumar, Pratiksha Patil, Arijit Das

The Thai Journal of Pharmaceutical Sciences

As validation is an integral part of current good manufacturing practice, nowadays, it is practiced in all pharmaceutical industries to assure that the manufacturing process is in control and products of high quality are obtained. Building of quality needs attention in the manufacturing process, from the raw materials to finalized product. The current research work is to perform prospective process validation for the manufacture of ketoprofen fast dissolving tablets (FDT) of 50 mg dose. Various trials and challenge studies were done to finalize critical process parameters. Three consecutive batches of ketoprofen FDT with the same batch size, procedure, equipment, and …

Pegloticase, Inderbir S. Padda, Rajat Bhatt, Mayur S. Parmar

HPD Articles

No abstract provided.

Apremilast, Inderbir S. Padda, Rajat Bhatt, Mayur S. Parmar

HPD Articles

No abstract provided.

Lenvatinib, Inderbir S. Padda, Mayur S. Parmar

HPD Articles

No abstract provided.

Covid (Sars-Cov-2) Vaccine, Inderbir S. Padda, Mayur S. Parmar

HPD Articles

No abstract provided.

Aducanumab, Inderbir S. Padda, Mayur S. Parmar

HPD Articles

No abstract provided.

Obeticholic Acid, Kristina Krupa, Vera Hapshy, Hiep Nguyen, Mayur S. Parmar

HPD Articles

No abstract provided.

Neuroprotective Effects Of Farnesol On Motor And Cognitive Impairment Against 3- Nitropropionic Acid-Induced Huntington’S Disease, S. Deepa, Emdormi Rymbai, T. K. Praveen, J. Saravanan

The Thai Journal of Pharmaceutical Sciences

Objective: The purpose of this study is to evaluate the role of farnesol as a potential neuroprotective agent against 3-nitropropionic acid (3-NP) acid-induced Huntington’s disease (HD) by in vitro, in vivo, and in silico models. 3-NP acid-induced Huntington’s disease in male Wistar rats was used to evaluate the neuroprotective potential of farnesol. Materials and Methods: 3-NP (10 mg/kg/day) was used for the induction of disease, followed by treatment with 50 mg/kg and 100 mg/kg of farnesol for 7 days. The effect of farnesol on motor symptoms was evaluated using actophotometer and rotarod apparatus and effect of farnesol on learning and …

Morphological Changes In Dorsal Root Ganglia Macrophages Associated With Neuropathic Pain Mechanisms Suggest A Novel Target For Chronic Pain Therapy, Emily Kussick

CMC Senior Theses

The present study examined morphological changes in the dorsal root ganglia (DRG) following an innate immune stimulus. The importance of the DRG has increasingly become recognized in pain processing as more than just the home of primary afferent cell bodies. All sensory information passes through the DRG via the primary afferents, and on to the spinal cord. The primary afferents synapse with second-order neurons in the spinal cord that ascend towards the brain, where they transmit the pain signal to the limbic forebrain and/or the somatosensory cortex for processing. The DRG is an interesting niche to study at as it …

Human Regulatory T Cells Control Inflammation From Effector T Cells In Prediabetes, Rui Liu

Theses and Dissertations--Pharmacy

Type 2 diabetes (T2D) is a chronic low-grade inflammatory disease. A T cell cytokine profile (Th17) from PBMCs can distinguish obese T2D from obese non-diabetes subjects. Individual T cell subsets interact with each other and the diverse subsets jointly determine overall inflammation. Cellular metabolism drives cytokine production of CD4⁺ T cells, and therefore contributes to inflammation in T2D. However, specific changes in metabolism and function of CD4⁺ T cells during the progression from lean healthy to obese and diabetic stages in people have not been clarified.

We hypothesize that human regulatory T cells (Treg) impact metabolism of effector …