Medicinal and Pharmaceutical Chemistry Commons^™

Investigating Effects Of Co-Culturing With Vibrio Fischeri On Secondary Metabolite Production Of Hawaiian Bobtail Squid Symbionts, Mariam A. Zedan

Honors Scholar Theses

Microbes are a fruitful source of natural product drug discovery since many of their secondary metabolites show defensive activity and have unique structures. However, extracting and elucidating the structure of those compounds can be challenging in vitro due to particular environmental and nutritional requirements of some bacteria. Those requirements may include proximity to other organisms that the microbes have symbiotic relationships with. Under those conditions, the organism may activate silent biosynthetic gene clusters (BGCs) responsible for production of certain secondary metabolites not typically expressed otherwise. One method of BGC induction is co-culturing with other microbes since this mimics the natural …

Impact Of Blender Type On Tribocharging In Pharmaceutical Powders Using Surface Modified V-Blender, Ami Shah

Honors Scholar Theses

Powders are a vital component of the pharmaceutical industry as they provide the basis for many solid dosage forms like tablets and capsules. Although, when using powders a common challenge is electrostatic charge accumulation due to numerous particle-particle and particle-wall collisions. This accumulated charge can lead then to poor powder homogeneity and compromised powder flow properties. In this study, tribocharging of pharmaceutical powders was analyzed using various V-blenders and mixing times . The evaluated blenders include: Aluminum, Polyvinyl Chloride (PVC), and surface modified Aluminum-PVC. Using the blenders, the model drug, Ibuprofen, was processed for different time intervals such as 5, …

Characterization Of Novel Cannabinoid Receptor 2-Selective Agonists At The Biochemical And Cellular Levels: Leads For Therapeutic Agents, Ashley M. Hine

Honors Scholar Theses

Putative cannabinoid receptor 2 (CB₂)-selective agonists were identified from a library of commercially available compounds via inhibition of cAMP accumulation in high throughput screening. Binding affinity and receptor subtype selectivity were assessed using heterologous competition binding assays against the known cannabinoid orthosteric ligand CP55940. Test compounds ASX0152383 and CSC003141 preferentially bound to CB₂, with no detection of binding to CB₁ up to 1 mM. CMB038865 exhibited nearly 100-fold selectivity for CB₁ over CB₂, while CZ000026 bound non-preferentially to both receptors in the low micromolar range. To determine the extent of G protein …

Upregulation Of Antibiotic Activity Of A Streptomyces Sp. Via Co-Cultures With Challenge Pathogens, Anne A. Sung

Honors Scholar Theses

Marine natural product drug discovery has begun to play an important role in the treatment of diseases. Early drug discovery from natural products came primarily from plants, but after the discovery and development of penicillin, scientists started looking at natural products from microorganisms. Numerous natural products have been discovered from members of the order Actinomycetales, particularly in the genus Streptomyces, due to their metabolic diversity in the production of biologically active secondary metabolites. Ascidians, also known as tunicates, are marine invertebrates that contain many host-associated microbes. Adult tunicates are sessile, which makes them vulnerable to predators, and thus, they …

Investigating Propargyl-Linked Antifolates In Inhibiting Bacterial And Fungal Dihydrofolate Reductase, Joshua Andrade

Honors Scholar Theses

Antimicrobial agents have been invaluable in reducing illness and death associated with bacterial infection. However, over time, bacteria have evolved resistance to all major drug classes as a result of selective pressure. The advancement of new drug compounds is therefore vital. The Anderson-Wright Lab has focused on developing potent and selective inhibitors of dihydrofolate reductase (DHFR), an enzyme key in cell proliferation and survival, in several pathogenic species. The lab has found that a set of compounds, known as propargyl-linked antifolates, are DHFR inhibitors that are both biologically effective and have strong pharmacokinetic properties.

The efficacy of novel propargyl-linked antifolates …

Am 6545: A Novel Peripheral Cb1 Antagonist, Seth Hosmer

Honors Scholar Theses

Obesity and other related metabolic disorders are a common problem in the United States. Consequently, several drug therapies have been developed in an attempt to address this problem. Many older appetite suppressants, such as amphetamines, were dangerous and potentially addictive. For the last few years, the endocannabinoid system was investigated as a potential target for appetite suppression. Unfortunately, early cannabinoid CB1 antagonists came with an unacceptable side effect profile of their own, which is largely due to central actions of these drugs. In an attempt to reduce the side effect profile, researchers are investigating peripherally acting cannabinoid antagonists, which do …