Medicinal Chemistry and Pharmaceutics Commons^™

Evaluating Daily Systemic Betaine Delivery In Alleviating Dry-Amd Pathophysiology, Dawin Khiev

USF Tampa Graduate Theses and Dissertations

MnSod (Sod2) deletion in the retinal pigment epithelium (RPE) of Sod2flox/floxVMD2-cre mice leads to oxidative stress-induced apoptosis of the RPE and photoreceptor cells that show salient features of dry-AMD. The purpose of this study was to investigate the potential antioxidant effect of betaine in protecting retinal health in Sod2flox/floxVMD2-cre mice. Betaine low dose (50mg/Kg Body Weight) and high dose (500mg/kg Body Weight, n=9) were administered intraperitoneally to 8-weeks old male and female Sod2flox/floxVMD2-cre mice daily for four months, while the control group (Sod2flox/floxVMD2-cre mice; n=9) received saline. We used spectral-domain optical coherence tomography (SD-OCT), retinal outer nuclear layer (ONL) thickness …

Quercetin Loaded Nanoparticles For The Treatment Of Dry Eye Disease, Bassma Sami Nashaat Hamed Eltanameli

USF Tampa Graduate Theses and Dissertations

Dry eye disease (DED) is a common condition that affects the eye's anterior surface due to tear deficiency or excessive evaporation. The lack of tears leads to dryness and initiation of an inflammatory response which can irritate the eye and interfere with daily activities. Current treatment depends mainly on artificial tears eye drops which offer temporary relief and require repetitive administration due to frequent blinking. Prescription medications are also available but need around three months to relieve dry eye symptoms. Quercetin is a flavonoid that has an anti-inflammatory and antioxidant effect. However, it suffers from low water solubility and low …

Artemisinin Dna Base Interaction Studies In Presence Of Fe (Ii): Lc/Tof Ms Separation Of Reaction Products, Kogila Oke, Amos Mugweru

Faculty Scholarship for the College of Science & Mathematics

Artemisinin (ART) is a sesquiterpene lactone and a popular malaria drug with potential anticancer properties. In this work, LC/TOF/MS, was used to investigate the reaction of ART with DNA bases. ART-deoxyadenosine and ART-deoxycytidine interactions, were studied in the presence of iron II ions. ART-deoxyadenosine and ART-deoxycytidine reaction mixtures gave chromatographic signatures that remained fairly unchanged at room temperature but grew after incubation at 37 °C. The change in temperature from room temperature to 37 °C was the main driver of adduct formation in these reactions. ART was found to react with Fe(II) ions as observed from several new chromatographic peaks. …

Characterization Of A Fluorescent Glucose Derivative 1-Nbdg And Its Application In The Identification Of Natural Sglt1/2 Inhibitors, Ting-Yu Kao, Hwa-Wei Wu, Shoei-Sheng Lee, Pi-Hui Liang, Jih-Hwa Guh, Lih-Ching Hsu

Journal of Food and Drug Analysis

Glucose is an important energy source for cells. Glucose transport is mediated by two types of glucose transporters: the active sodium-coupled glucose cotransporters (SGLTs), and the passive glucose transporters (GLUTs). Development of an easy way to detect glucose uptake by the cell can be valuable for research. 1-(N-(7-Nitrobenz-2-oxa-1,3-diazol-4-yl) amino)-1-deoxy-D-glucose (1-NBDG) is a newly synthesized fluorescent glucose analogue. Unlike 2-NBDG, which is a good substrate of GLUTs but not SGLTs, 1-NBDG can be transported by both GLUTs and SGLTs. Thus, 1-NBDG is useful for the screening of SGLT1 and SGLT2 inhibitors. Here we further characterized 1-NBDG and compared it …

Lucigenin-Pyrogallol Chemiluminescence For The Multiple Detection Of Pyrogallol, Cobalt Ion, And Tyrosinase, Islam M. Mostafa, Muhammad Rehan Hasan Shah Gilani, Yequan Chen, Baohua Lou, Jianping Li, Guobao Xu

Journal of Food and Drug Analysis

Developing new, cheap, sensitive and selective chemiluminescence (CL) systems with multiple detection properties is still a big challenge for biological and environmental applications. Here, we report a new CL system having multiple detection applications (environmental and biological). The developed lucigenin-pyrogallol system gave an enhancement (190 times) over the conventional lucigenin-H₂O₂ CL system. Cobalt ion and tyrosinase can inhibit lucigenin-PG CL intensity. Based on these phenomena, we have developed new CL methods for the detection of pyrogallol (LOD = 0.94 μM), lucigenin (LOD = 0.42 μM), cobalt (LOD = 68 μM), and tyrosinase (LOD = 1.8 μg/mL). Furthermore, …

Determination Of Cannabinoids In Hemp Oil Based Cosmetic Products By Lc-Tandem Ms, Yun-Hua Hsu, Ming-Chih Fang, Shou-Chieh Huang, Ya-Min Kao, Su-Hsiang Tseng, Der-Yuan Wang

Journal of Food and Drug Analysis

Cosmetic products containing hemp seed oil as permitted raw materials required the specific compound delta-9-tetrahydrocannabinol (THC) below 10 µg/g. THC was the main psychoactive constituent of cannabis. Since hemp seed oil became an increasingly popular ingredient in cosmetics over the last few years, an efficient and reliable analytical method for THC and other cannabinoids in cannabis-infused cosmetic products was in need. A liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for the determination of delta-9-tetrahydrocannabinol (THC), cannabidiol (CBD), and cannabinol (CBN) in hemp seed oil based cosmetic products was developed. Method validation was performed by fertilizing blank samples with analytes and internal …

Comprehensive Multiplexed Analysis Of Risky Drugs In Eggs Based On Magnetic Zeolitic Imidazolate Frameworks And Uhplc Q-Orbitrap Hrms, Wei Jia, Yuyang Liu, Xi Xu, Yanxi Zhang, Lin Shi

Journal of Food and Drug Analysis

A novel magnetic adsorbent solid-phase Fe₃O₄@ZIF-8 extraction method coupled with UHPLC Q-Orbitrap high resolution mass spectrometry for the sensitive and high efficiency detection of fluoroquinolones, tetracyclines, dyes and amphenicols in eggs is described. Under optimum conditions, CCβ and CCα of 0.62 to 26.97 μg.kg^–1 and 0.36 to 16.37 μg.kg^–1 was obtained, which is much better than that obtained by conventional methods. The accuracy, expressed as recovery, were achieved falling between 75% and 104%. The proposed strategy provides several advantages of simplicity and low energy consumption, thus retaining potential for the screening of …

An Extractive Nanoelectrospray Ionization-Mass Spectrometry Method For Chinese Herbal Medicine Authentication, Chia-Hsin Lee, Hui-Chi Huang, Mei-Chun Tseng, Chao-Jung Chen

Journal of Food and Drug Analysis

Herein, we describe a rapid, sensitive, and nondestructive method—extractive nanoelectrospray ionization-mass spectrometry (EnESI-MS)—for traditional Chinese medicine (TCM) authentication. The mass-spectral fingerprints of volatile compounds released from various TCMs can be rapidly acquired using EnESI-MS without sample pretreatment. EnESI-MS was applied to successfully differentiate between two commonly used medicinal herbs, Schisandra Chinensis and Schisandra sphenanthera, which are morphologically similar but exhibit different therapeutic effects. Specific volatile compounds of each herb in a ten-component Chinese herbal product, Jia Wei Xiao Yao San, were also identified, and the method was applied to discriminate between the commercial product and a substandard version.

Mesonosides A-H, Primeverose Derivatives From Mesona Procumbens Suppress Adipogenesis By Downregulating Pparγ And C/Ebpa In 3t3-L1 Cells, Hung-Tse Huang, Chia-Ching Liaw, Chun-Tang Chiou, Kung-Ta Lee, Yao-Haur Kuo

Journal of Food and Drug Analysis

Obesity is becoming a worldwide epidemic, especially in industrialized countries. We hereby report a methanolic extract of Mesona procumbens (known as Hsian-tsao in Taiwan) significantly inhibits lipid accumulation in 3T3-L1 adipocytes, and eight new primeverose derivatives, mesonosides A-H (1-8), were isolated from the methanolic extract of M. procumbens. Structural elucidation of 1-8 was established by spectroscopic methods, especially 2D NMR techniques (¹H-¹H COSY, HSQC, HMBC, and NOESY) and HRESIMS. Anti-obesity evaluation revealed that isolates 1-5, 7, and 8 showed inhibitory effects on lipid accumulation and protein levels of adipogenic transcription factor, PPARγ and C/EBPa in 3T3-L1 …

Induction Of Mitochondrial-Dependent Apoptosis By Essential Oil Of Toona Sinensis Root Through Akt, Mtor And Nf-Κb Signalling Pathways In Human Renal Cell Carcinoma Cells, Yu-Chi Chen, Chiao-Ling Hsieh, Bu-Miin Huang, Yungchia Chen

Journal of Food and Drug Analysis

Natural products have long been considered as a kind of complementary medicine. In this study, we investigate the apoptotic effect of essential oils of Toona sinensis roots (TSR) on human clear cell renal cell carcinomas (ccRCC). The sesquiterpene content of TSR essential oil was determined via GC/MS analysis. TSR decreased ccRCC cell viabilities, inducing ROS generation and reduction of the mitochondrial membrane potential. Moreover, TSR inhibited Bcl-2 and Hsp90 expression but increased PARP-1 cleavage and cytochrome c release. Akt, mTOR and NF-kB phosphorylation and HIF-a expression were all inhibited, which likely contributed to the anti-proliferative and anti-adhesive effects of TSR.

Comprehensive Detection Of 120 Additives In Food Using Nontargeted Ms Data Acquisition, Che-Lun Hsu, Mingchih Fang, Hui-Chun Tseng, Ya-Tze Lin, Su-Hsiang Tseng, Der-Yuan Wang, Deng-Fwu Hwang

Journal of Food and Drug Analysis

The compliance assessment on the labeling of food additives is a hard job, because there are nearly thousand legal food additives can be used in food, and countless illegal additives must also deal with. This study developed a nontargeted data acquisition screening method based on liquid chromatography high resolution mass spectrometry (HRMS) in which a precursor ion and two product ions of each analyte are able to be recorded. The high throughput screening method worked as foodomics that characterized and identified every food components as long as they were ionized in terms of theory. The data acquisition method called data …

Transcriptome Analysis Of Lactobacillus Rhamnosus Gg Strain Treated With Prebiotic - Bovine Lactoferrin Under A Cold Environment, Zhen-Shu Liu, Chuen-Fu Lin, Po-Wen Chen

Journal of Food and Drug Analysis

Lactoferrin (LF) is secreted by mammals and displays extensive biological effects. We previously reported that bovine LF (BLF) can boost the cold tolerance of a well-applied probiotic strain, Lactobacillus rhamnosus GG (LGG), to grow robustly under a cold environment, but the molecular mechanism is not clear. Here, RNA-seq analysis was conducted to ascertain molecular pathways underlying cold tolerance exerted by BLF. LGG was cultured in a cold environment (22°C) in the presence or absence of BLF. Transcriptome analysis indicated that BLF significantly elicited 1.2 to 3.2 fold (log2 Fold change) higher expression levels of genes related to stress, defense, cell …

Polydopamine And Silica Nanoparticles Magnetic Solid Phase Extraction Coupled With Liquid Chromatography-Tandem Mass Spectrometry To Determine Phenolic Acids And Flavonoids In Fruit Wine, Hui-Ling Lee, Chih-Yuan Kang, Yen-Jung Kuo, Shan-Ni Tseng

Journal of Food and Drug Analysis

Magnetic solid phase extraction (MSPE) have been widely applied in a variety of sample preparation techniques. Herein, Fe3O4@pDA as the sorbents for MSPE, were developed for the determination of phenolic acids and flavonoids in fruit wine samples in combination with LC-MS/MS. The Fe3O4@pDA were characterized by Fourier transform infrared spectroscopy (FT-IR), powder X-ray diffraction (PXRD), transmission electron microscopy (TEM), Superconducting Quantum Interference Device Magnetometer (SQUID) and thermogravimetric analysis (TGA) in detail. In the present study, a new, rapid, and efficient MSPE by LC-MS/MS was established for the extraction and sensitive detection of phenolic acids and flavonoids. Under the optimized condition …

Comparative Analysis Of N95 Respirators Fit Testing With Commercially Available And In House Reagent, Erum Khan, Joveria Farooqi, Humaira Shafaq, Kaleem Ullah Khushik, Syed Shamim Raza, Sara Khan, Zohra Rafiq, Bushra Ahmed, Shazia Chisti, Kehkashan Imtiaz, Hasnain Zafar, Afia Zafar

Department of Pathology and Laboratory Medicine

Background: Due to COVID-19, thousands of healthcare workers have been affected and have lost their lives in the line of duty. For the protection of healthcare workers, WHO and CDC have made standard guidelines and requirements for PPE use. N95 masks are amongst the most readily used PPE by healthcare professionals and it is highly recommended by OSHA that every make and model of N95 should go through a fit test at least once in a year.
Method: A total of 30 randomly selected healthcare professionals (who were a regular user of N95 respiratory masks) were subjected to assess in-house …

Utilizing Proteolysis-Targeting Chimeras To Target The Transcriptional Cyclin-Dependent Kinases 9 And 12, Hannah King

Theses & Dissertations

Cyclin-dependent kinases (CDKs) are a family of serine-threonine kinases involved in various cellular functions, such as regulating the cell cycle and gene transcription. CDK9, a transcriptional CDK, regulates highly expressed enhancer-associated oncogenic transcription factors, including the oncogene Myc. CDK9 is responsible for the transcription and stabilization of Myc; consequently, it was a validated target for pancreatic cancer treatment.

As such, we developed a panel of aminopyrazole based proteolysis targeting chimera where we identified PROTAC 2 as a selective degrader of CDK9 (DC₅₀ = 158 ± 6 nM). PROTAC 2 was capable of cereblon mediated proteasomal degradation of CDK9 while …

Anti-Inflammatory And Chemopreventive Activity Of Lunasin From Tofu Whey For The Management Of Gastrointestinal Diseases, Cindy Andrea Nieto Veloza

Doctoral Dissertations

Gastrointestinal diseases such as inflammatory bowel diseases (IBD) and colorectal cancer (CRC) are pathological conditions associated with chronic inflammation, characterized by intestinal damage, debilitating symptoms, and detrimental health consequences. The increased risk of CRC in IBD patients, and the adverse effects associated with current therapeutic strategies, point out the need for safer alternatives to reduce chronic inflammation in the bowel. Lunasin is a bioactive peptide naturally occurring in soybeans, with chemopreventive and anti-inflammatory properties demonstrated in several extra-intestinal diseases. However, to date, there is no evidence of the biological activity of lunasin on the gastrointestinal tract as a target site. …

Isolation And Characterization Of Ethyl Acetate Fraction From Abroma Augusta L As An Anti-Inflammatory Agent, Madyawati Latief, Indra Lasmana Tarigan, Muhaimin Muhaimin, Hilda Amanda, Nike Desvi Yulianti

Makara Journal of Science

Abroma augusta is a bush plant that lives on the edge of the river. This plant is commonly used as an anti-inflammatory drug for joints and broken bones. It contains several secondary metabolites, such as alkaloids, triterpenoids, steroids, and flavonoids, which exhibit anti-inflammatory activity. UV-visible (UV-Vis) spectrophotometry of isolate 1.3 indicated absorption at a maximum wavelength of 282 nm. The wavelength suggested that the electron transition π–π* is the absorption of UV spectra typical for triterpenoid compounds that have chromophores in the form of non-conjugated double bonds. FT-IR spectrophotometer characterization data from isolate 1.3 revealed the presence of triterpenoid compounds …

Type I Topoisomerases As Potential Targets For Therapeutics, Ahmed Seddek

FIU Electronic Theses and Dissertations

DNA topoisomerases are universal enzymes that control the topological features of DNA in all forms of life. This study aims to find potential inhibitors of some of the DNA topoisomerases in bacteria and humans that can be developed into potential therapeutics.

The first aim of this study is to find potential inhibitors of bacterial topoisomerase I that can be developed into antibiotics. There is an urgent need to develop novel antibiotics to overcome the world-wide health crisis of antimicrobial resistance. Virtual screening and biochemical assays were combined to screen thousands of compounds for potential inhibitors of bacterial topoisomerase I. NSC76027 …

Corrigendum To “Novel Uplc-Ms/Ms Method For Standardization Of Niazimicin Content In Edible Seeds And Leaves Of Moringa Oleifera Lam” [J Food Drug Anal 29 (2021) 128-143]

Journal of Food and Drug Analysis

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Corrigendum To “Determination Of Glycidyl Esters And 3-Mcpd Esters In Edible Oils By Sample Pretreatment With The Combination Of Lipase Hydrolysis And Modified Quechers For Gc-Ms Analysis” [J Food Drug Anal 29 (2021) 153-167]

Journal of Food and Drug Analysis

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