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Full-Text Articles in Medicinal-Pharmaceutical Chemistry

Extraction And Partial Purification Of An Antibiotic-Like Compound From The Soil Bacterium Rhodococcus Strain Kchxc3, Elizabeth Bond May 2022

Extraction And Partial Purification Of An Antibiotic-Like Compound From The Soil Bacterium Rhodococcus Strain Kchxc3, Elizabeth Bond

Undergraduate Honors Theses

Rhodococcus bacteria have many secondary metabolic pathways that may produce novel natural products. The bacterium Rhodococcus strain KCHXC3 was isolated from a soil sample collected near Kingsport, Tennessee and was found to produce an inhibitory compound active against a broad array of bacterial species, including the Gram negative pathogen Shigella sonnei. The aim of this research is to extract and purify the compound for future structure elucidation. A mixture of compounds from 3 month old agar plates inoculated with strain KCHXC3 was extracted using ethyl acetate. The crude extract was then partially purified utilizing a Sephadex LH-20 column, followed …


Preliminary Isolation And Characterization Of Root Extract Components Of Dalea Jamesii, Hyojin Ahn Jan 2020

Preliminary Isolation And Characterization Of Root Extract Components Of Dalea Jamesii, Hyojin Ahn

Undergraduate Honors Theses

The plant genus Dalea (Fabaceae) has been found to be prolific in its production of phenolic secondary metabolites including flavonoids, isoflavonoids, chalcones, pterocarpans, stilbenes, and other biosynthetically related compounds. Biological testing has revealed wide-ranging activities for these metabolites in many prior reports. Dalea jamesii has not yet been investigated for its chemical content. This study will be conducted with the hypothesis that unique phenolic secondary metabolites will be produced in the roots of D. jamesii. It will be of interest to determine if the isolated metabolites exhibit biomedically related activities. It will also be of interest to investigate whether the …


Discovery Of A Novel Inhibitory Compound Produced By The Soil Bacterium Rhodococcus Sp. Mtm3w5.2, Patrick South May 2018

Discovery Of A Novel Inhibitory Compound Produced By The Soil Bacterium Rhodococcus Sp. Mtm3w5.2, Patrick South

Undergraduate Honors Theses

Due to increases in antibiotic resistance stemming from the overuse of commercial antibiotics, the need to discover novel antibacterial compounds is becoming more urgent. A species of Rhodococcus, MTM3W5.2, has been discovered and was found to produce a metabolite with inhibitory activity against closely related species. The aim of this study is to elucidate the structure of the inhibitory metabolite by isolating and purifying it; then characterizing it using spectroscopic techniques. The compound was isolated from MTM3W5.2 RM broth cultures using n-butanol extraction, which yielded an active crude extract. The crude extract was then subjected to fractionation using a Sephedex …


Synthesis And In-Vitro Cell Viability/Cytotoxicity Studies Of Novel Pyrrolobenzodiazepine Derivatives, John M. Jarrett May 2017

Synthesis And In-Vitro Cell Viability/Cytotoxicity Studies Of Novel Pyrrolobenzodiazepine Derivatives, John M. Jarrett

Undergraduate Honors Theses

Pyrrolobenzodiazepines (PBDs) are a group of naturally occurring compounds that were discovered in the cultures of Streptomyces in the 1960s. Some natural PBDs discovered in these cultures, such as anthramycin and sibiromycin, were shown to possess a broad spectrum of anti-tumor activity. Since cancer is still a leading cause of death globally, the development of novel anti-proliferative derivatives of PBDs is essential for human welfare worldwide. Further synthesis and structure-activity relationship (SAR) studies of the parent natural products and their tetracyclic analogs will lead to the discovery of drug candidates. In this work, thirteen PBD analogues were synthesized using no …


The Role Of Type-2 Cannabinoid Receptors In Calcification Of Atherosclerotic Lesions., Kaitlyn Hinshaw May 2013

The Role Of Type-2 Cannabinoid Receptors In Calcification Of Atherosclerotic Lesions., Kaitlyn Hinshaw

Undergraduate Honors Theses

Introduction: Atherosclerosis is a chronic inflammatory disease characterized by the buildup of cholesterol, fat and other debris within arterial walls. Atherosclerotic lesions undergo a calcification process with similarities to bone remodeling. In mice, the type-2 cannabinoid receptor (CB2) is known to regulate bone remodeling processes and has also been shown to alter atherosclerotic lesion characteristics. However, the role of CB2 in lesion calcification is still unclear. CB2 modulates bone remodeling by affecting differentiation of osteogenic precursor cells; thus we hypothesize that CB2 alters lesion calcification by altering osteoblastogenesis and osteoclastogenesis of precursor cells of vascular origin. To test this hypothesis, …


Characterization Of Phytochemicals Isolated From Plants Of The Pacific Northwest And Western United States For Combating Fungal Multidrug Resistance, John David Schreiber Jan 2010

Characterization Of Phytochemicals Isolated From Plants Of The Pacific Northwest And Western United States For Combating Fungal Multidrug Resistance, John David Schreiber

Undergraduate Honors Theses

Fungal multidrug resistance is an emerging problem for those suffering from fungal infections, and for those seeking to discover or produce novel fungicidal drugs. Plants native to the Pacific Northwest as well as in the Olympic national rainforest were collected and screened for phytochemicals which exhibit direct antifungal activity toward Candida and Saccharomyces spp. as well as those that inhibit fungal ABC transporters that are, in large part, responsible for the development of multidrug resistance. Dalea formosa (Fabaceae), a plant native to the American Southwest, was also screened for phytochemicals of medicinal interest. The methanolic extract of aerial portions of …


Synthesis Towards Novel 1,3-Azaborine Heterocycles As Potential Dual-Mode Hiv-1 Protease Inhibitors, Amanda Blackmore Jan 2008

Synthesis Towards Novel 1,3-Azaborine Heterocycles As Potential Dual-Mode Hiv-1 Protease Inhibitors, Amanda Blackmore

Undergraduate Honors Theses

Drug discovery has resulted in many life-saving therapies, making a great impact on modem medicine and the human condition. Even though new therapies are available many drugs are highly susceptible to resistance development, have poor bioavailability, and some of them are toxic. HIV-I protease inhibitors presently on the market show high specificity but have low bioavailability and high toxicity. Furthermore, the available drugs have a very low affinity for mutant forms of HIV -1 protease. Recent studies have shown that boronated HIV-I protease inhibitors, which demonstrate both competitive and associative inhibition, have a higher affinity for HIV-I protease at lower …


Synthesis Of 5,6 Dihydropyran-2-Ones As Potential Inhibitors Of Hiv-1 Protease, Jesse Lee Nye Jan 2008

Synthesis Of 5,6 Dihydropyran-2-Ones As Potential Inhibitors Of Hiv-1 Protease, Jesse Lee Nye

Undergraduate Honors Theses

HIV/ AIDS has affected about 40 million people. One type of drug that is used to treat HIV/AIDS is a protease inhibitor. HIV-I protease is an enzyme responsible for the release of mature HIV viral particles in the body. HIV-I protease eventually becomes resistant to the inhibitors that are used as drugs and new inhibitors are needed. This research builds on a previous research effort, in which structures for HIV -1 protease inhibitors were designed using molecular modeling methods, including neural networks. These inhibitors were designed to possess better inhibitory properties, and possibly have increased bioavailability and less toxicity than …