Pharmaceutics and Drug Design Commons^™

Nudcl2 Is Required For Cytokinesis By Stabilizing Rcc2 With Hsp90 At The Midbody, Xiaoyang Xu, Yuliang Huang, Feng Yang, Xiaoxia Sun, Rijin Lin, Jiaxing Feng, Mingyang Yang, Jiaqi Shao, Xiaoqi Liu, Tianhua Zhou, Shanshan Xie, Yuehong Yang

Markey Cancer Center Faculty Publications

Cytokinesis is required for faithful division of cytoplasmic components and duplicated nuclei into two daughter cells. Midbody, a protein-dense organelle that forms at the intercellular bridge, is indispensable for success- ful cytokinesis. However, the regulatory mechanism of cytokinesis at the midbody still remains elusive. Here, we unveil a critical role for NudC-like protein 2 (NudCL2), a co-chaperone of heat shock protein 90 (Hsp90), in cytokinesis regulation by stabilizing regulator of chromosome condensation 2 (RCC2) at the midbody in mam- malian cells. NudCL2 localizes at the midbody, and its downregulation results in cytokinesis failure, multinu- cleation, and midbody disorganization. Using iTRAQ-based …

Breast Tissue As A Local Drug Reservoir For Anticancer Therapy In Breast Cancer, Saniia Shchinar

Electronic Theses and Dissertations

Breast cancer, particularly the estrogen receptor-positive (ER+) subtype, remains a formidable challenge in oncology. Traditional oral therapies for ER-positive breast cancer, such as selective estrogen receptor modulators (SERMs) like Tamoxifen (TAM) and Toremifene (TOR), often encounter issues related to limited bioavailability, metabolic complications, and significant systemic side effects. These side effects include the risk of blood clots, hot flashes, vaginal dryness, menstrual cycle disruptions, and uterus cancer, which can hinder long-term adherence to preventive therapy. The exploration of local drug delivery into breast tissue presents a promising alternative to tackle these challenges. In this study, we explored the feasibility of …

Delivery Of Gemcitabine, Stearoyl Gemcitabine And Paclitaxel Through Plga Nanoparticles And Its Effect On The Desmoplasia Of Pancreatic Cancer Spheroids, Rishabh Bahl

Electronic Theses and Dissertations

Pancreatic cancer is one of the deadliest cancers to treat. The primary cause for the drug resistance is the dense extracellular matrix (ECM) that surrounds the tumor and restricts blood supply. Gemcitabine (GEM) and paclitaxel (PTX) are drugs that are clinically used in the treatment of pancreatic cancer. GEM, however, is rapidly metabolized by cytidine deaminase (CDA) and eliminated from the body, and paclitaxel is a substrate for P- glycoprotein (P-gp) efflux receptors. Drug delivery using nanoparticles has been reported to help improve drug half-lives and bypass efflux receptors. This thesis aims to encapsulate PTX in PLGA nanoparticles (PTX-NP) and …

Tracing Antibacterial Compounds From Kaledang (Artocarpus Lanceifolius Roxb.) Stem Bark, Hamsidar Hasan, Tety Tuloli, Syamsul Bahri, La Ode Aman

Pharmaceutical Sciences and Research

Artocarpus lanceifolius Roxb. or kaledang is a species of the mulberry family, Moraceae. Several extracts from its family have been reported to have antibacterial activity. Thus, it is necessary to determine compounds that have nature as antibacterial to be raw materials for antibacterial herbal medicines. The purpose of the study was to trace compounds that have antibacterial activity from Artocarpus lanceifolius stem bark. The study method was extraction by graded maceration, fractionation with column vacuum chromatography (CVC), isolation by radial chromatography, determination of antibacterial activity by agar diffusion method using the Gram positive and Gram negative bacteria. The characterization …

Antimicrobial Activity Of Crude Fractions Of Gossypium Barbadense Leaves And Isolation Of Stigmasterol, Maryam Saddiq, Ahmed Salisu, Kamaluddeen Kabir, Yusuf Hassan

Pharmaceutical Sciences and Research

Plants have been used in traditional medicine in different parts of the world to treat several diseases. Many studies have confirmed their medicinal values, which have led to the isolation and characterization of various potential drug candidates. This study focuses on the antimicrobial activity of crude fractions of Gossypium barbadense leaves and the isolation of active compound. The pulverized plant leave was soaked in ethanol (98% v/v), and a solvent-based fractionation was carried out using n-hexane, chloroform, ethyl acetate, and ethanol. The obtained crude fractions were screened for antimicrobial activity against four (4) clinical isolates: Escherichia coli, Pseudomonas …

Antioxidant Activities Of Roja Herbal Tea: Combination Of Rosella Flower (Hibiscus Sabdariffa L.) And Ginger Rhizome (Zingiber Officinale Rosc.), Wahyu Widowati, Teresa Liliana Wargasetia, Teddy Marcus Zakaria, Michael Sebastian Gunadi, Nathanael Halim, Sherly Santiadi, Hanna Sari Widya Kusuma, Nida Firyal Fauziyah

Pharmaceutical Sciences and Research

Herbal teas and plant-based medicines have been widely used worldwide for their therapeutic and healing qualities. Rosella (Hibiscus sabdariffa L.) has various benefits in preventing digestive problems, liver disease, fever, and others. Ginger (Zingiber officinale Rosc.) or known as jahe in Indonesia is believed to benefit numerous clinical conditions linked to oxidative stress, including pancreatitis, hypertension, diabetic kidney disease, Alzheimer’s disease, and tumor development. They have been utilized in traditional medical practice to treat conditions such as fever, nausea, and headaches. In this study, we aimed to determine the antioxidant activities of rosella flower tea, ginger tea, and …

Colon Targeted Delivery Dosage Forms For Probiotics: A Review, Gede Anom Anjasmara, Pietradewi Hartrianti, Raditya Iswandana

Pharmaceutical Sciences and Research

Encapsulation was a promising method for protecting probiotics from extreme conditions during their passage through the gastrointestinal tract and delivering probiotics to specific sites in the colon for colonization. Various dosage forms have been used in recent years to encapsulate probiotics to maintain cell viability during processing, storage, and through the digestive tract to provide health benefits. However, research related to the encapsulation of probiotics as the dosage forms for colon-targeted delivery systems was still quite limited to conventional dosage forms due to the sensitivity of probiotics to extreme conditions during the process. This review focuses on various types of …

Exploring Rosella (Hibiscus Sabdariffa L.) Calyx Extracts As Natural Dye And Antioxidants In Lip Cream Product: Formulation And Evaluation, Donna Maretta Ariestanti, Abdul Mun'im, Joshita Djajadisastra, Riska Amalia Putri Hutami, Redhalfi Fadhila, Richard Johari James

Pharmaceutical Sciences and Research

Rosella, also known as Hibiscus sabdariffa L., is a plant that contains anthocyanin compounds in its calyx, which are known for their antioxidant properties. These compounds give the plant a captivating red color and can be used as natural dyes. This study aimed to exploit anthocyanins in rosella calyx as natural dyes and antioxidants in lip cream product. The formulations employed extracts from rosella calyx, a viscous extract from maceration in 96% ethanol (F1) and a commercially available powdered rosella extract (F2). Evaluation on the formulations demonstrated that both F1 and F2 effectively maintained the color integrity of the lip …

Subchronic Toxicity Study Of Sterculia Rubiginosa Zoll. Ex Miq. Leaves Extract, Rini Prastiwi, Ester Hidayati, Riska Anggraini, Cut Mauliza, Ita Anggraini, Ema Dewanti

Pharmaceutical Sciences and Research

Ki hampelas (Sterculia rubiginosa Zoll. Ex Miq.) is traditionally used as an antiasthma. It also reported has antioxidant and nephroprotective activity. This study was conducted to evaluate the subchronic toxicity of the leaf extract of ki hampelas. The extract was orally administered to male and female Sprague-Dawley rats at doses of 50, 200, and 400 mg/kg bodyweight (BW) per day for 28 days. The rats were divided into four groups, consist of consist of normal group (Na CMC 0.5%), dose 1 (50 mg/kg BW), dose 2 (200 mg/kg BW), and dose 3 (400 mg/ kg BW) of extract. The …

Study Of Anti-Hyperuricemia, Anti-Inflammatory, And Anti-Nociceptive Effects Of Hylocereus Undatus Stem Bark Extract In Animal Models, Tri Wahyuni, Sartika Harka Putri, Anton Bahtiar

Pharmaceutical Sciences and Research

Dragon fruit, known as Hylocereus undantus (HU), has traditionally been utilized in Banyuwangi, East Java, Indonesia, for addressing gout and rheumatism. Despite its empirical use, there is a lack of reported pharmacological research on this plant. This study aimed to explore the properties of HU extract in treating hyperuricemia, inflammation, and pain. Adenine-potassium oxonate-induced mice were employed to evaluate anti-hyperuricemia activity, measuring uric acid, blood urea nitrogen (BUN), and creatinine serum levels. Carrageenan-induced paw edema in rats was used to assess anti-inflammatory activity, while acetic acid-induced abdominal writhing and hot plate tests were conducted to investigate anti-nociceptive effects. The results …

The Potential Of Herbal Combinations As Adjunctive Therapy For Standard Care Of Covid-19 Patients: A Lesson Learned From Indonesia, Anna Rozaliyani, Satria Pratama, Findra Setianingrum, Fenny Yunita, C. Martin Rumende

Pharmaceutical Sciences and Research

The pandemic of novel coronavirus disease (COVID-19) has become a global disaster that occurred between the end of 2019 and 2023. It caused immeasurable damage to almost all aspects of human life. The disease has opened a lot of new perspectives on Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) origins and pathogenesis, the nature of the virus, the potential for new treatments, and new policies to overcome this pandemic. This review aims to know the potential of plants that are beneficial to combat the diseases, including immunomodulators in the management of COVID-19. Studies reporting COVID-19 with the keywords SARS-CoV-2, COVID-19, …

The Implications Of The Halogen Atom On The Physical Stability Of Amorphous Solid Dispersions, Mustafa Bookwala

Electronic Theses and Dissertations

Amorphous solid dispersions (ASD), although a promising formulation strategy for poorly water-soluble drugs, are susceptible to rapid, spontaneous recrystallization owing to their metastable nature. Non-covalent interactions (NCI) between the drug and polymer are known to help prevent ASD physical destabilization. Conventionally, hydrogen-bonding (H-bonding) is considered important for ASD formation and persistence. However, carbon-bound halogen atoms, which are frequently present on drug molecules and can form specific halogen-bonds (X-bond) with the polymer, remain relatively unexplored with respect to their ability to stabilize ASDs. It was, therefore, hypothesized that the presence of a peripheral Br on bromopropamide, and Cl on chlorpropamide will …

Functionalized Surface Of Plga Nanoparticles In Thermosensitive Gel To Enhance The Efficacy Of Antibiotics Against Antibiotic Resistant Infections In Endodontics: A Randomized Clinical Trial, Mona Arafa, Hadeel Moussa, Mohamed Medhat Kataia

Pharmacy

Enterococcus faecalis plays the key role in endodontic infections and is responsible for the formation of biofilm on dentin, which causes a resistance against periradicular lesions treatment, consequently the aim of this study is to use nanoparticles entrapping anibacterial agents coated with chitosan that in authors previous study showed a successful in vitro biofilm inhibition, additionally incorporated in thermoresponsive gel.to benefit nanoparticles` small size, and the positive charge of their surfaces that binds with the negatively charged surface of bacterial cell causing its destruction, in addition to the sustained release pattern of the drug based nanoparticles in gel. Therefore, Ciprofloxacin …

Towards A Mode Of Action For The Anti-Schistosomal Aryl Hydantoins, Thomas Schulze

Theses & Dissertations

Schistosomiasis is a significant human disease caused by the helminth parasite Schistosoma mansoni. Praziquantel remains the only clinically used treatment, yet it is rapidly metabolized and only effective against the adult stage worm infection. Ro 13-3978 (AR02) is a potent antischistosomal compound with activity against multiple S. mansoni life stages; however, it manifests anti-androgenic activity. Additionally, the mechanism of action for worm clearance remains unknown. The structure of Ro 13-3979 was used to generate optimized derivatives, including AR102, that show increased potency towards worms, reduced off-target anti-androgen effects, and extended half-life thereby increasing the feasibility for a single-dose curative treatment. …

Utilization Of Semiconductor Nanocrystals In Cancer Diagnose And Treatment, Yasir Q. Almajidi, Ahmed A. Albadri, Mazen M. Jwaid, Yaseen T. Khalaf

Maaen Journal for Medical Sciences

In contemporary times, nanotechnology has emerged as a notably sophisticated technological discipline. It possesses an interdisciplinary and multidisciplinary nature, spanning a wide array of domains including medical science, engineering, biology, physics, materials science, and chemistry. Utilization of nanotechnology offers a significant advantage by enabling precise manipulation and control of properties to effectively address specific challenges in various applications. In the fields of science and biomedicine, there has been extensive exploration into the use of functional nanomaterials, emerging as rapidly advancing and captivating areas of research. Diverse types of nanomaterials, including silicon nanowires, quantum dots, carbon nanotubes, and gold/silver nanoparticles, which …

Analyzing Functional Interactions Of Designed Peptides By Nmr Spectroscopy, Wonsuk Choi

Pharmaceutical Sciences (MS) Theses

The development of small peptide-based therapeutics can be accelerated by the knowledge of relationships between the peptide structure and its functional interactions. Here, we report the analysis of two groups of synthetic peptides designed for two applications – broad bactericidal action and inhibition of protein-protein interactions in human cells. Novel amphiphilic peptides designed for antibacterial application incorporated arginine as cationic amino acids and non-natural amino acids that have aromatic side chains with similar hydrophobic properties as tryptophan. The interaction of lead cyclic peptides and their linear analogs with a phospholipid bilayer mimicking a bacterial membrane was studied using nuclear magnetic …

The Implications Of Ferroptosis In Antibiotic Resistance, Marysol Hohl

Senior Honors Theses

Bacterial infections in the United States are becoming increasingly resistant to existing antibiotic treatments. Due to projected increases in resistance and the recent decrease in novel antibacterials, experts have determined that the United States is in the “post-antibiotic era.” The scientific community has failed to resolve resistance despite the continual discovery of new antibiotic compounds. In the past decade, a novel form of cell death called ferroptosis has been implicated in antibiotic treatment by employing the use of nanotechnology. This literature review will describe the problem of bacterial resistance and demonstrate how current research is pioneering a new age of …

Tolfenamic Acid Derivatives: A New Class Of Transcriptional Modulators With Potential Therapeutic Applications For Alzheimer’S Disease And Related Disorders, Juanetta Hill, Karim E. Shalaby, Syed W. Bihaqi, Bothaina H. Alansi, Benjamin Barlock, Keykavous Parang, Richard Thompson, Khalid Ourarhni, Nasser H. Zawia

Pharmacy Faculty Articles and Research

The field of Alzheimer’s disease (AD) has witnessed recent breakthroughs in the development of disease-modifying biologics and diagnostic markers. While immunotherapeutic interventions have provided much-awaited solutions, nucleic acid-based tools represent other avenues of intervention; however, these approaches are costly and invasive, and they have serious side effects. Previously, we have shown in AD animal models that tolfenamic acid (TA) can lower the expression of AD-related genes and their products and subsequently reduce pathological burden and improve cognition. Using TA as a scaffold and the zinc finger domain of SP1 as a pharmacophore, we developed safer and more potent brain-penetrating analogs …

Piperine Encourages Apoptosis In Human Cervical Adenocarcinoma Cells Through Ros Generation, Dna Fragmentation, Caspase-3 Activation And Cell Cycle Arrest, Asif Jafri, Juhi Rais, Sudhir Kumar, Md Arshad

Research Symposium

Background: Cancer is one of the most common destructive diseases and the second leading cause of death in humans. Among cancer, cervical cancer is the second most common malignancy among women globally. Thus, there is a continuous need to search for chemotherapeutic chemicals or naturally occurring drugs to resolve this global health problem. Piperine (1-piperoylpeperdine) is present in the fruits of black pepper (Piper nigrum Linn.) and long pepper (Piper longum Linn.). It possesses several pharmacological properties and in the present study we have evaluated its anti-cancer potential on human cervical adenocarcinoma (HeLa) cells.

Methods: The anti-proliferative effect …

Development And Evaluation Of A Nanofiber Membrane In Vitro As A Therapeutic Alternative For The Post Treatment In Breast Cancer Cell In A Murine Model, Bruno A. Valades-Aguilar, Diana Ginette Zarate-Triviño, José Raúl Rángel-López, Moises Armides Franco-Molina, Jorge Luis Menchaca-Arredondo, María Cristina Rodríguez-Padilla

Research Symposium

Worldwide female breast cancer is the most commonly diagnosed cancer, with an estimated 2.3 million new cases in 2020, reason for the need of targeted therapies that can maximize treatment success and minimize toxicity. Nanoparticles of gold (AuNps) exhibit cytotoxic properties against certain types of cancer cell lines. Nanofibers have been use in the drug delivery systems due to its degradability and high surface area. We proposed a membrane with nanometric fibers using polivinilic alcohol (PVA) and chitosan (Qts) loaded with AuNps and Doxorubicin (Doxo) with the purpose of diminish tumor regression.

PVA-Qts membrane was develop with electrospinning, the injection, …