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Secondary Metabolites Isolated From Perovskia Atriplicifolia And Their In Vitro Binding Affinity For Human Opioid And Cannabinoid Receptors, Ashli Fitzpatrick
Secondary Metabolites Isolated From Perovskia Atriplicifolia And Their In Vitro Binding Affinity For Human Opioid And Cannabinoid Receptors, Ashli Fitzpatrick
Honors Theses
Plants and their natural products have been utilized for thousands of years in the treatment of many human diseases. Because of their structural diversity, natural products are ideal lead compounds for drug development. In this thesis, the natural products of the plant Perovskia atriplicifolia were investigated, specifically their in vitro binding affinity to receptors in opioid and cannabinoid classes. Extracts that demonstrated good selective opioid and cannabinoid receptor binding were subjected to bioassay-guided fractionation. Four active compounds were identified from the crude extract in Perovskia atriplicifolia: 1) 5-hydroxy-3',4',6,7-tetramethoxy flavone, 2) 5,7-dihydroxy-3',4',6,-trimethoxy flavone, 3) 5-hydroxy-4',6,7-trimethoxy flavone, and 4) 5,7-dihydroxy-4',6,-dimethoxy flavone. Each …
Targeting G-Quadruplexes Within The Adam-15 Promoter: A Novel Therapeutic Approach For Breast Cancer, Rachel L. Jenkins
Targeting G-Quadruplexes Within The Adam-15 Promoter: A Novel Therapeutic Approach For Breast Cancer, Rachel L. Jenkins
Honors Theses
ADAM-15 is a protein that is up-regulated in many diseases, particularly breast cancer; its over-expression is correlated with more aggressive and invasive phenotypes. The critical core promoter region of ADAM-15 is capable of forming a secondary DNA structure known as a G-quadruplex. The stabilization of this G-quadruplex has the potential to decrease the transcription of the over-expressed ADAM-15 protein. Six hundred forty compounds were screened for their ability to cause a shift in the melting temperature of an ADAM-15 oligonucleotide using FRET melt. Two compounds, NSC 146771 and NSC 260594, produced a significant shift in the melting temperature; further experimentation, …
Exploration Of Cannabinoid And Opioid Agents From Plants Used In Traditional Medicine, John Fitzpatrick
Exploration Of Cannabinoid And Opioid Agents From Plants Used In Traditional Medicine, John Fitzpatrick
Honors Theses
Ten plants, with known medicinal uses, were gathered to study for their possible production of secondary metabolites that act as opioid and cannabinoid agents. All plants were subjected to in vitro bioassays testing for their affinity for the opioid and cannabinoid receptors. Banisteriopsis caapi extracts displayed the greatest affinity for both opioid and cannabinoid receptors. B. caapi extracts underwent column fractionation yielding fractions that were subjected to further in vitro studies. We discovered that the ethanolic extract of this plant (foliage) binds to all three opioid receptors (µ, κ and δ) and cannabinoid receptors (CB1 and CB2) with values ranging …
Design And Synthesis Of Sigma-1 Probe For Positron Emission Tomography (Pet) Imaging, May Ly
Design And Synthesis Of Sigma-1 Probe For Positron Emission Tomography (Pet) Imaging, May Ly
Honors Theses
Sigma-1 receptor radioligands have the potential to detect and monitor various neurological diseases. Because sigma-1 receptors are believed to be associated with numerous psychiatric conditions and neurodegenerative diseases, radioligands for sigma-1 receptors have the potential to serve as novel diagnostic tools and may be useful in assessing treatment effectiveness. A benzothiazolone 18F-labeled sigma-1 receptor ligand, CM304, has demonstrated promise as a specific positron emission tomography radiotracer for visualizing sigma-1 receptors in living subjects. Based on CM304, backup molecules were created to improve the overall drug profile, including half- life and bioavailability.