Medicinal Chemistry and Pharmaceutics Commons^™

Dendrimer-Based Antibiotics For The Treatment Of Bacterial Biofilm In Cystic Fibrosis (Cf), Younan Ma

Theses and Dissertations

Pseudomonas aeruginosa (PA) is the predominant pathogen in chronic lung infections of cystic fibrosis (CF) patients. The most important mechanism of adaptation of PA to host defense and antibiotic treatment is the formation of biofilms within the mucus layer covering the lung bronchi. The effectiveness of antibiotics such as aminoglycosides is significantly attenuated by their limited penetration through thick mucus and embedded biofilm matrix in patients’ lung. Inhaled tobramycin (Tobra), which is the most commonly used antibiotics in the treatment of PA infections for CF patients, is usually found to be in very high concentration in patients’ lung, and yet …

Structural Characterization And In Vitro Antiproliferative Activity Of Non-Specific Lipid Transfer Protein 1 (Nsltp1) From Fennel (Foeniculum Vulgare) Seeds, Mekdes Megeressa

Pharmaceutical Sciences (PhD) Dissertations

Non-specific lipid transfer proteins (nsLTPs) are cationic proteins involved in intracellular lipid shuttling, in growth and reproduction, as well as in defense against pathogenic microbes. Even though the primary and spatial structures of some nsLTPs from different plants indicate their similar features, they exhibit distinct lipid-binding specificities signifying their various biological roles that dictate further structural study. The present study determined the complete amino acid sequence, in silico 3D structure modeling, and in vitro antiproliferative activity of nsLTP1 from fennel (Foeniculum vulgare) seeds.

Fennel is a member of the family Umbelliferae (Apiaceae) native to southern Europe and the …

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 …

Lemongrass (Cymbopogon Citratus) Ethanolic Extract Exhibited Activities That Inhibit -Glucosidase Enzymes And Postprandial Blood Glucose Elevation, Maria Dewi Puspitasari Tirtaningtyas Gunawan Puteri, Felicia Melissa Tjiptadi, Phebe Hendra, Filiana Santoso, Zalinar Udin, Nina Artanti, Florence Ignatia Florence Ignatia

Makara Journal of Science

Lemongrass is a common ingredient in Indonesian traditional herbal medicine that potently inhibits carbohydrate hydrolysis. In this study, the in vitro α-glucosidase inhibitory (AGI) activity of lemongrass was compared with its in vivo activity to retard postprandial blood glucose elevation, and the bioactive compounds responsible for these activities were observed. Both water and ethanolic extracts of lemongrass (WLG and ELG, respectively) were tested in vitro for its inhibition of the sucrose and maltose hydrolyzing activities of rat intestinal glucosidase. ELG was observed to exert higher inhibitory activities (Sucrase IC₅₀ = 8.74 mg/mL; Maltase IC₅₀ = 18.93 mg/mL) than …

Antiparasitic Peptide From The Ocean: Discovery, Synthesis And Structure-Activity Relationship Study, Kh Tanvir Ahmed

Electronic Theses and Dissertations

Millions of people die every year because of infectious diseases, and malaria is among the top five of the deadliest infectious disease. In 2018, malaria took more than four hundred thousand lives, and more than half of them are children under five years of age. Most malaria-affected parts of the world are also the home of the most underprivileged people. Seemingly, antimalarial drug discovery never achieved the attraction that it requires. Like malaria, another infectious disease that is not extensively explored by drug discovery campaigns is American trypanosomiasis or Chagas disease. More than a hundred years have passed since discovering …

Long-Acting Nanoformulated Antivirals For The Treatment And Prevention Of Hiv-1 And Hbv Infections, Dhruvkumar M. Soni Dr.

Theses & Dissertations

While antiretroviral therapy (ART) has revolutionized treatment and prevention of human immunodeficiency virus type one (HIV-1) infection, regimen adherence, viral mutations, drug toxicities, stigma and pill fatigue are limitations. These have led to the development of long acting (LA) ART. These include, but are not limited to, implantable devices, new chemical entities, prodrug modifications and nanoformulations. To these ends, this thesis focues on the transformation of nucleoside reverse transcriptase inhibitors (NRTIs) into LA parenterals, While elusive, data from our laboratories demonstrated that modifications to the PROdrug and nucleoTide technology (ProTide) enables improvements in drug apparent half-life and tissue and cell …

Acknowledgment Of Reviewers, Lily Chiu

Journal of Food and Drug Analysis

No abstract provided.

The Analytical And Biomedical Applications Of Carbon Dots And Their Future Theranostic Potential: A Review, Sukunya Ross, Ren-Siang Wu, Shih-Chun Wei, Gareth M. Ross, Huan-Tsung Chang

Journal of Food and Drug Analysis

In recent years, carbon dots (C-dots) have gained appreciable interest owing to their unique optical properties, including tunable fluorescence, stability against photobleaching and photoblinking, and strong fluorescence. Simple and low-cost hydrothermal and electrochemical approaches have been widely used in the preparation of biocompatible and high-quality C-dots. Various C-dots have been used for the quantitation of small analytes, mostly based on analyte induced fluorescence quenching. Depending on the nature of precursors, synthetic conditions (such as reaction temperature and time), and surface conjugation, multi-function C-dots can be prepared and used in diagnostics and therapeutics. Their strong fluorescence and photostability, enables use in …

Nanomaterial-Based Adsorbents And Optical Sensors For Illicit Drug Analysis, Chun-Hsien Chen, Chun-Chi Wang, Po-Yun Ko, Yen-Ling Chen

Journal of Food and Drug Analysis

The abuse of illicit drugs has been prevalent in recent years and is associated with crime and public health issues. To strengthen public security and fortify public health services with respect to the increasing severity of drug abuse, academic and government institutes have been devoted to constructing relative analytical methods for illicit drugs. To date, the development of sensors has been greatly emphasized due to their features of high sensitivity, prompt detection and flexible manipulation; thus, sensors can serve as alternatives to conventional sophisticated instruments. Recently, the use of nanomaterials has inspired the development of a series of innovative sample …

Gold Nanoparticle-Based Colorimetric And Electrochemical Sensors For The Detection Of Illegal Food Additives, Li Li, Ming Zhang, Wei Chen

Journal of Food and Drug Analysis

Lately, scandals associated with the illegal addition of poisonous chemicals to food for commercial interests have been gradually disclosed to the public. Problems related to food safety do not only harm public health but also affect the stability of economic and social development. Food safety has become a common issue in society, and strengthening the related regulations have become increasingly important. Although conventional techniques are accurate and sensitive in the detection of the vast majority of illegal food additives, they rely on time-consuming, labor-intensive procedures that depend on expensive instruments. Thus, efficient and rapid identification of poisonous, illegal additives in …

Improved Food Additive Analysis By Ever-Increasing Nanotechnology, Jing Zhang, Shui Hu, Yi Du, Ding Cao, Guirong Wang, Zhiqin Yuan

Journal of Food and Drug Analysis

Improper use of food additives may lead to potential threat to human health, making it important to develop sensitive and selective method for the detection of them. Nanomaterials with unique chemical and electrochemical properties show extensive applications in the design of food additive sensing systems. In this review, we summarize the recently adopted electrochemical and optical analysis of food additives based on nanomaterials. Detection of typical food additives (colorants and preservatives) by using different sensing mechanisms and strategies are provided. In addition, determination of illegal food additives is also briefly introduced. Finally, this review highlights the challenges and future trend …

Electrowetting-On-Dielectric (Ewod): Current Perspectives And Applications In Ensuring Food Safety, Snigdha Roy Barman, Imran Khan, Subhodeep Chatterjee, Subhajit Saha, Dukhyun Choi, Sangmin Lee, Zong-Hong Lin

Journal of Food and Drug Analysis

Digital microfluidic (DMF) platforms have contributed immensely to the development of multifunctional lab-on-chip systems for performing complete sets of biological and analytical assays. Electrowetting-on-dielectric (EWOD) technology, due to its outstanding flexibility and integrability, has emerged as a promising candidate for such lab-on-chip applications. Triggered by an electrical stimulus, EWOD devices allow precise manipulation of single droplets along the designed electrode arrays without employing external pumps and valves, thereby enhancing the miniaturization and portability of the system towards transcending important laboratory assays in resource-limited settings. In recent years, the simple fabrication process and reprogrammable architecture of EWOD chips have led to …

Nanomaterial-Based Fluorescent Biosensor For Veterinary Drug Detection In Foods, Xiaoqi Tao, Yuanyuan Peng, Juewen Liu

Journal of Food and Drug Analysis

Veterinary drugs have been widely used in the food industry. Their residues in food products need to be tightly regulated to ensure food safety. In particular, some veterinary drugs are still used illegally, although they have already been banned. Nanomaterials are playing an increasingly important role in analytical chemistry due to their unique properties. Compared to traditional organic dyes and colloidal gold nanoparticle labels, fluorescent nanomaterials appear particularly attractive for the detection of veterinary drug residues. This review summarizes recent advancements of fluorescent biosensors using nanomaterials for the detection of veterinary drug residues in foods. The useful properties of each …

Carbon Quantum Dots For The Detection Of Antibiotics And Pesticides, Han-Wei Chu, Binesh Unnikrishnan, Anisha Anand, Yang-Wei Lin, Chih-Ching Huang

Journal of Food and Drug Analysis

Carbon quantum dots (CQDs) are novel nanomaterials with interesting physical and chemical properties, which are intensely studied only in the last decade. Unique properties, such as its inherent fluorescent property, high resistance to photobleaching, high surface area, ease of synthesis, flexible choice of precursor, and surface tunability enable CQDs for promising application in biosensing. Therefore, it is highly useful in clinical, forensic, medical, food and drug analyses, disease diagnosis, and various other fields of biosensing. In addition, their fluorescence properties are tunable by the interaction with certain molecules via different mechanisms, which enables their application for sensing of those molecules, …

Noble Metal Nanomaterial-Based Aptasensors For Microbial Toxin Detection, Yue He, Cong-Ying Wen, Zhi-Jun Guo, Yu-Fen Huang

Journal of Food and Drug Analysis

Microbial toxins generated by bacteria, fungi and algae cause serious food-safety problems due to the frequent contamination of foodstuffs and their poisonous nature. Becoming acquainted with the contamination condition of foodstuffs is highly dependent on developing sensitive, specific, and accurate methods for targeting microbial toxins. Aptamers, obtained from systematic evolution of ligands by exponential enrichment (SELEX), have significant advantages for microbial toxin analysis, such as small size, reproducible chemical synthesis, and modification, as well as high binding affinity, specificity, and stability. Besides, aptamers have a predictable structure and can be tailored using biomolecular tools (e.g., ligase, endonuclease, exonuclease, …

Perspective On Recent Developments Of Nanomaterial Based Fluorescent Sensors: Applications In Safety And Quality Control Of Food And Beverages, Ailing Han, Sijia Hao, Yayu Yang, Xia Li, Xiaoyu Luo, Guozhen Fang, Jifeng Liu, Shuo Wang

Journal of Food and Drug Analysis

As the highly toxic pollutants will seriously harm human health, it is particularly important to establish the analysis and detection technology of food pollutants. Compared with the traditional detection methods, fluorescent detection technique based on nanomaterials trigger wide interesting because of reduced detection time, simple operation, high sensitivity and selectivity and economic. In this review, the application of fluorescent sensors in food pollutants detection is presented. Firstly, conventional fluorescent nanomaterials including metal-based quantum dots, carbon-based quantum dots and metal nanoclusters were summarized, with emphasis on the photoluminescence mechanism. Then, the fluorescence sensors based on these nanomaterials for food pollutants detection …

Preface, Huan-Tsung Chang, Yu-Fen Huang

Journal of Food and Drug Analysis

No abstract provided.

Dendriplex - Cyclodextrin Conjugates For Gene Delivery To Retina, Durga Deepak Puro

USF Tampa Graduate Theses and Dissertations

Gene therapy holds promise for treating a wide range of diseases including cancer and several other polygenic and monogenic disorder arising in different organs. Due to its immune privilege nature, eye is an ideal organ for gene therapy,as various visual pathologies arise from gene defect and can lead to partial or complete vision loss. The last decade, several nanoparticles have been developed and tested for their transfection efficiency in vitro and in vivo. Among them, dendrimers with small size, good physicochemical properties and endosomal escape activity have shown high transfection efficiency in various cell lines. In an attempt to further …

Examining Sodium And Potassium Channel Conductances Involved In Hyperexcitability Of Chemotherapy-Induced Peripheral Neuropathy: A Mathematical And Cell Culture-Based Study, Parul Verma, Muriel Eaton, Achim Kienle, Dietrich Flockerzi, Yang Yang, Doraiswami Ramkrishna

Purdue University Libraries Open Access Publishing Fund

Chemotherapy-induced peripheral neuropathy (CIPN) is a prevalent, painful side effect which arises due to a number of chemotherapy agents. CIPN can have a prolonged effect on quality of life. Chemotherapy treatment is often reduced or stopped altogether because of the severe pain. Currently, there are no FDA-approved treatments for CIPN partially due to its complex pathogenesis in multiple pathways involving a variety of channels, specifically, voltage-gated ion channels. One aspect of neuropathic pain in vitro is hyperexcitability in dorsal root ganglia (DRG) peripheral sensory neurons. Our study employs bifurcation theory to investigate the role of voltage-gated ion channels in inducing …

Chemical Composition Of The Volatile Fractions Of Mesembryanthemum Forskahlei Flowers And Herb, Moeen Dababneh

Al Jinan الجنان

Halophytes are succulent native plants to the northern region of the Kingdom of Saudi Arabia. They have therapeutic properties and can be potentially useful as a new source of bioactive compounds. Our study aims to investigate the chemical composition of the volatile fraction of Herb and Flowers of Mesembryanthemum forskahlei by the application of Gas Chromatography method. Our study showed that palmetic acid (420mg/ kg) and squaline (352,32mg/kg) are the main components in the herb. Furthermore, we identified that palmitic acid is the main component of the flower. Finally, Mesembryanthemum forskahlei herb has higher content of volatile compounds than the …