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Tumor-Targeted Delivery Of Sirna Using Fatty Acyl-Cgkrk Peptide Conjugates, Meenakshi Sharma, Naglaa Salem El-Sayed, Hung Do, Keykavous Parang, Rakesh Tiwari, Hamidreza Montazeri Aliabadi 2017 Chapman University

Tumor-Targeted Delivery Of Sirna Using Fatty Acyl-Cgkrk Peptide Conjugates, Meenakshi Sharma, Naglaa Salem El-Sayed, Hung Do, Keykavous Parang, Rakesh Tiwari, Hamidreza Montazeri Aliabadi

Pharmacy Faculty Articles and Research

Tumor-targeted carriers provide efficient delivery of chemotherapeutic agents to tumor tissue. CGKRK is one of the well-known tumor targeting peptides with significant specificity for angiogenic blood vessels and tumor cells. Here, we designed fatty acyl conjugated CGKRK peptides, based on the hypothesis that hydrophobically-modified CGKRK peptide could enhance cellular permeation and delivery of siRNA targeted to tumor cells for effective silencing of selected proteins. We synthesized six fatty acyl-peptide conjugates, using a diverse chain of saturated and unsaturated fatty acids to study the efficiency of this approach. At peptide:siRNA weight/weight ratio of 10:1 (N/P ≈ 13.6 ...


Chemical Modulation Of Cancer Cells To Enhance Tumor Immunity, Florisela Herrejon Chavez 2017 Portland State University

Chemical Modulation Of Cancer Cells To Enhance Tumor Immunity, Florisela Herrejon Chavez

PSU McNair Scholars Online Journal

Breakthroughs in immunotherapy have led to cancer therapeutics that activate the immune system by blocking inhibitory mechanisms. This class of therapeutics has resulted in longer survival rates for cancer patients, some living over 10 years after being diagnosed as terminally ill. However, only a small fraction of patients who receive immunotherapy drugs respond favorably.Recent studies suggest that certain anticancer agents (both cytotoxic chemotherapeutics and targeted drugs) stimulate immune recognition of cancers. Identification of such immunomodulatory anticancer agents would make ideal partners for current immunotherapy treatments, thus increasing the proportion of the treated patients who benefit from immunotherapy. This study ...


Synthesis And Evaluation Of Antimicrobial Activity Of [R4w4k]-Levofloxacin And [R4w4k]-Levofloxacin-Q Conjugates, Neda Riahifard, Kathy Tavakoli, Jason Yamaki, Keykavous Parang, Rakesh Tiwari 2017 Chapman University

Synthesis And Evaluation Of Antimicrobial Activity Of [R4w4k]-Levofloxacin And [R4w4k]-Levofloxacin-Q Conjugates, Neda Riahifard, Kathy Tavakoli, Jason Yamaki, Keykavous Parang, Rakesh Tiwari

Pharmacy Faculty Articles and Research

The development of a new class of antibiotics to fight bacterial resistance is a time-consuming effort associated with high-cost and commercial risks. Thus, modification, conjugation or combination of existing antibiotics to enhance their efficacy is a suitable strategy. We have previously reported that the amphiphilic cyclic peptide [R4W4] had antibacterial activity with a minimum inhibitory concentration (MIC) of 2.97 g/mL against Methicillin-resistant Staphylococcus aureus (MRSA). Herein, we hypothesized that conjugation or combination of the amphiphilic cyclic peptide [R4W4] with levofloxacin or levofloxacin-Q could improve the antibacterial activity of levofloxacin and levofloxacin-Q. Fmoc/tBu solid-phase chemistry was employed to ...


Theaflavin-3, 3'-Digallate Decreases Human Ovarian Carcinoma Ovcar-3 Cell-Induced Angiogenesis Via Akt And Notch-1 Pathways, Not Via Mapk Pathways, Ying Gao, Gary O. Rankin, Youying Tu, Yi Charlie Chen 2017 Marshall University

Theaflavin-3, 3'-Digallate Decreases Human Ovarian Carcinoma Ovcar-3 Cell-Induced Angiogenesis Via Akt And Notch-1 Pathways, Not Via Mapk Pathways, Ying Gao, Gary O. Rankin, Youying Tu, Yi Charlie Chen

Gary O. Rankin

Theaflavin-3, 3'-digallate (TF3) is a black tea polyphenol produced from polymerization and oxidization of the green tea ployphenols epicatechin gallate and (-)-epigallocatechin-3-gallate (EGCG) during fermentation of fresh tea leaves. TF3 has been reported to have anticancer properties. However, the effect of TF3 on tumor angiogenesis and the underlying mechanisms are not clear. In the present study, TF3 was verified to inhibit tumor angiogenesis. Compared with EGCG, TF3 was more potent. TF3 inhibited human ovarian carcinoma OVCAR-3 cell-induced angiogenesis in human umbilical vein endothelial cell model and in chick chorioallantoic membrane model. TF3 reduced tumor angiogenesis by downregulating HIF-1α and ...


Structure Activity Relationship Studies Of Novel Diarylpentanoid Analogs Targeting The Androgen Receptor In Prostate Cancer Cells, Haili Coffin, Marco Bisoffi 2017 Chapman University

Structure Activity Relationship Studies Of Novel Diarylpentanoid Analogs Targeting The Androgen Receptor In Prostate Cancer Cells, Haili Coffin, Marco Bisoffi

Student Research Day Abstracts and Posters

The development of prostate cancer (PCa) relies strongly on the activation of the androgen receptor (AR) signaling pathway by its natural ligand dihydrotestosterone. Furthermore, PCa progression to metastatic disease represents oncogene addiction to AR activity. Androgen ablation therapy is thus a mainstay therapy against this disease, but the development of ligand-independent AR activation and persisting AR expression eventually leads to castration resistant PCa (CRPC). Therefore, down-regulation of AR expression in PCa cells may be an effective therapeutic modality. The diarylpentanoid ca27 has previously been shown to down-regulate AR expression by an unknown mechanism of action. The present work represents a ...


Synthesis Of Non-Toxic Compounds And The Inhibition Of Oral Bacteria, Monica Patel 2017 Indiana University of Pennsylvania

Synthesis Of Non-Toxic Compounds And The Inhibition Of Oral Bacteria, Monica Patel

Theses and Dissertations (All)

In recent years, research has shown that dental care correlates with many health factors due to the amount of bacteria present in the mouth. Thus, it is important to create more efficient compounds to fight oral bacteria, specifically Streptococci mutans. This research chose cost effective compounds to inhibit the cavity causing S. mutans.

Based on a study on phenolic antibacterial compounds against oral bacteria, 4- hexylphenol had reasonable germ-kill activity and log P values. By modeling this compound with one alcohol group and a long hydrophobic carbon chain, Geraniol was chosen as a starting material.

Three compounds were synthesized and ...


Compromised External Validity: Federally Produced Cannabis Does Not Reflect Legal Markets, Daniela Vergara, L. Cinnamon Bidwell, Kent E. Hutchison, Nolan C. Kane, Reggie Gaudino, Anthony Torres, Gary Du, Travis C. Ruthenburg, Kymron deCesare, Donald P. Land 2017 University of Colorado Boulder

Compromised External Validity: Federally Produced Cannabis Does Not Reflect Legal Markets, Daniela Vergara, L. Cinnamon Bidwell, Kent E. Hutchison, Nolan C. Kane, Reggie Gaudino, Anthony Torres, Gary Du, Travis C. Ruthenburg, Kymron Decesare, Donald P. Land

University Libraries Open Access Fund Supported Publications

As the most widely used illicit drug worldwide, and as a source of numerous under-studied pharmacologically-active compounds, a precise understanding of variability in psychological and physiological effects of Cannabis varieties is essential. The National Institute on Drug Abuse (NIDA) is designated as the sole legal producer of Cannabis for use in US research studies. We sought to compare the chemical profiles of Cannabis varieties that are available to consumers in states that have statelegalized use versus what is available to researchers interested in studying the plant and its effects. Our results demonstrate that the federally-produced Cannabis has significantly less variety ...


Involuntary Competence In United States Criminal Law, Stephen J. Morse 2017 University of Pennsylvania Law School

Involuntary Competence In United States Criminal Law, Stephen J. Morse

Faculty Scholarship

This is a draft of a chapter that has been accepted for publication by Oxford University Press in the forthcoming book Fitness to Plead: International and Comparative Perspectives edited by Ronnie Mackay and Warren Brookbanks due for publication in May 2018. It addresses whether the state may forcibly medicate an unwilling defendant or prisoner to restore competence in the criminal process, including competence to stand trial, competence to plead guilty and to waive trial rights, competence to represent oneself, and competence to be sentenced. It begins with a description of the doctrinal and mental health background information and the right ...


Microtransplantation Of Rat Brain Neurolemma Into Xenopus Laevis Oocytes To Study The Effect Of Environmental Toxicants On Endogenous Voltage-Sensitive Ion Channels, Edwin Murenzi 2017 University of Massachusetts Amherst

Microtransplantation Of Rat Brain Neurolemma Into Xenopus Laevis Oocytes To Study The Effect Of Environmental Toxicants On Endogenous Voltage-Sensitive Ion Channels, Edwin Murenzi

Masters Theses

Microtransplantation of mammalian neurolemma into Xenopus laevis oocytes has been used to study ion channels in terms of their structure and function in the central nervous system. Use of microtransplanted neurolemma is advantageous in that tissue can be obtained from various sources, ion channels and receptors are present in their native configuration and they can be used to evaluate numerous channelpathies caused by environmental toxicants. Here we show that Xenopus oocytes injected with fragments of rat brain neurolemma successfully express functional native ion channels that are assembled in their own plasma membrane. Using a high throughput two electrode voltage clamp ...


Countercurrent Chromatography Fractions Of Plant Extracts With Anti-Tuberculosis Activity, Douglas Armstrong, Nathan C. Krause, Drew Frey, J. Brent Friesen, Baojie Wan, Jordan Gunn, Scott Franzblau 2016 Olivet Nazarene University

Countercurrent Chromatography Fractions Of Plant Extracts With Anti-Tuberculosis Activity, Douglas Armstrong, Nathan C. Krause, Drew Frey, J. Brent Friesen, Baojie Wan, Jordan Gunn, Scott Franzblau

Faculty Scholarship – Chemistry

Samples of numerous plant species were received from the southwestern part of the USA, from Richard Spjut, and plant samples were collected here in Illinois. All were extracted with typical solvents, giving crude residues, some of which were subjected to chromatographic methods. Some of the crude residues and some of the fractions were tested for anti-tuberculosis activity and/or antibacterial activity.

In a general way, bioactive natural products are dealt with very well by Liang & Fang. More specifically, the southwestern part of the United States has a large variety of indigenous plants many of which have not been investigated for ...


Data On The Diversion, Nonmedical Use And Adverse Outcomes Associated With Pharmaceutical Opioids, Amanuel Zimam, Teresa D. Schmidt, Alexandra Nielsen, Wayne W. Wakeland 2016 Portland State University

Data On The Diversion, Nonmedical Use And Adverse Outcomes Associated With Pharmaceutical Opioids, Amanuel Zimam, Teresa D. Schmidt, Alexandra Nielsen, Wayne W. Wakeland

Wayne W. Wakeland

Background: Recent increases in the nonmedical use of pharmaceutical opioids and the adverse outcomes associated with them have stimulated a large amount of research and data collection on this public health problem. Systematic organization of the available data sources is needed to facilitate ongoing research, analysis, and evaluation. Method: A list of keywords associated with diversion, nonmedical use, and adverse outcomes of pharmaceutical opioid use generated 94 peer-reviewed academic articles and a number of governmental and nongovernmental sources. All sources were in English, contained quantitative data, and were published between January 1995 and April 2012. A list of 20 topics ...


Dynamic Modeling Of Nonmedical Opioid Initiation: Epidemic And Access, Alexandra Nielsen, Teresa D. Schmidt, Dennis McCarty, Wayne W. Wakeland 2016 Portland State University

Dynamic Modeling Of Nonmedical Opioid Initiation: Epidemic And Access, Alexandra Nielsen, Teresa D. Schmidt, Dennis Mccarty, Wayne W. Wakeland

Wayne W. Wakeland

We report development of a systems level dynamic model of initiation and nonmedical use of pharmaceutical opioids in the US. The model calibrated to 1995-2005 National Survey of Drug Use and Health (NSDUH) data, predicts 2006-2011 data well. Preliminary findings indicate that interventions which reduce the perceived attractiveness of opioids for recreational use may be able to reduce initiation and nonmedical use most significantly, while supply restriction effected through drug take back days and prescribing changes may have more modest effects. We argue that system dynamics is an effective approach for evaluating potential interventions to this complex system where the ...


Key Data Gaps For Understanding Trends In Prescription Opioid Analgesic Abuse And Diversion Among Chronic Pain Patients And Nonmedical Users, Wayne W. Wakeland, John Fitzgerald, Aaron Gilson, J. David Haddox, Jack Homer, Lewis Lee, Louis Macovsky, Dennis McCarty, Teresa D. Schmidt, Lynn Webster 2016 Portland State University

Key Data Gaps For Understanding Trends In Prescription Opioid Analgesic Abuse And Diversion Among Chronic Pain Patients And Nonmedical Users, Wayne W. Wakeland, John Fitzgerald, Aaron Gilson, J. David Haddox, Jack Homer, Lewis Lee, Louis Macovsky, Dennis Mccarty, Teresa D. Schmidt, Lynn Webster

Wayne W. Wakeland

Population dynamics of medical and nonmedical prescription opioid usage and adverse outcomes were modeled. Critical parameter values were determined by their amount of influence on model behavior. Results suggest that closing these data gaps would help researchers to better identify ways to reduce the risk of adverse outcomes.


System Dynamics Modeling Of Medical Use, Nonmedical Use And Diversion Of Prescription Opioid Analgesics, Wayne Wakeland, Alexandra Nielsen, Teresa D. Schmidt 2016 Portland State University

System Dynamics Modeling Of Medical Use, Nonmedical Use And Diversion Of Prescription Opioid Analgesics, Wayne Wakeland, Alexandra Nielsen, Teresa D. Schmidt

Wayne W. Wakeland

The objective of the study was to develop a system dynamics model of the medical use of pharmaceutical opioids to treat pain, and the associated diversion and nonmedical use of these drugs. The model was used to test the impact of simulated interventions in this complex system. The study relied on secondary data obtained from the literature and from other public sources for the period 1995 to 2008. In addition, an expert panel provided recommendations regarding model parameters and model structure. The behavior of the resulting systems level model compared favorably with reference behavior data (R2=.95). After the base ...


Crystal Protein Cry5b As A Novel And Powerful Anthelmintic, David Koch, Zeynep Mirza, Yan Hu, Thanh-thanh Nguyen, Gary R. Ostroff, Raffi V. Aroian 2016 University of Massachusetts Medical School

Crystal Protein Cry5b As A Novel And Powerful Anthelmintic, David Koch, Zeynep Mirza, Yan Hu, Thanh-Thanh Nguyen, Gary R. Ostroff, Raffi V. Aroian

UMass Center for Clinical and Translational Science Research Retreat

Soil-transmitted helminths (STHs), most notably, hookworms, whipworms, and Ascaris, are nematodes that infect more than 1.5 billion of the poorest people and are amongst the leading causes of morbidity worldwide. Only two classes of de-worming drugs (anthelmintics) are available for treatment, and only one is commonly used in mass drug administrations. New anthelmintics are urgently needed to overcome emerging resistance and to produce higher cure rates. Crystal (Cry) proteins, in particular Cry5B, made by Bacillus thuringiensis (Bt) are promising new candidates. Cry5B has excellent anthelmintic properties against many free-living and parasitic nematodes, including in vivo efficacy against multiple STH ...


Theoretical And Experimental Analysis Of The Antioxidant And Anti-Amyloid Features Of Synthetic Resveratrol Mimics, William Horton, Anne Kokel, Fanni Török, Chris Tran, Marianna Török, Bela Török 2016 University of Massachusetts Boston

Theoretical And Experimental Analysis Of The Antioxidant And Anti-Amyloid Features Of Synthetic Resveratrol Mimics, William Horton, Anne Kokel, Fanni Török, Chris Tran, Marianna Török, Bela Török

UMass Center for Clinical and Translational Science Research Retreat

Diaryl hydrazones, possessing similar structure to the popular red wine antioxidant resveratrol, have been previously identified as multitarget compounds interfering with several processes associated with the pathogenesis of Alzheimer’s disease (AD). These compounds exhibited particularly strong inhibition of the amyloid beta (A) peptide self-assembly, including blocking the formation of fibrils and oligomers, species that are widely accepted to be neurotoxic. The molecules were also powerful free radical scavengers and thus have a potential to defend against oxidative stress.

In order to learn more about the mode of action of the compounds, theoretical and experimental studies have been carried out ...


An Analysis Of Women’S Access To Acute Opioid Detoxification Services In Maine: Identifying The Barriers To Treatment, Karen E. Conley 2016 University of Southern Maine

An Analysis Of Women’S Access To Acute Opioid Detoxification Services In Maine: Identifying The Barriers To Treatment, Karen E. Conley

Muskie School Capstones

The lack of treatment facilities and services for opioid use disorder in Maine, combined with an increased prevalence of addiction, creates a potential for health inequity between men and women that may be intensified by barriers in access to care. This capstone study utilized detoxification screening inquiry forms and data obtained from the Milestone Foundation’s acute opioid detoxification program to assess and categorize barriers to access by gender. A barriers model was developed based on existing literature and was to identify potential associations among and between the known barriers to accessing treatment. Barriers were described as internally or externally ...


Essentials Of Herb-Drug Interactions In The Elderly With Cardiovascular Disease, Sulaiman Sultan, Maria Viqar, Rabaiya Ali, A. Jamil Tajik, Arshad Jahangir 2016 Aurora Health Care

Essentials Of Herb-Drug Interactions In The Elderly With Cardiovascular Disease, Sulaiman Sultan, Maria Viqar, Rabaiya Ali, A. Jamil Tajik, Arshad Jahangir

Arshad Jahangir, MD

As the number of individuals, particularly the elderly, using herbal products with prescription drugs continues to grow, the risk for adverse interactions increases but remains poorly recognized. The true incidence and nature of adverse herb reactions or herb-drug interactions remains unknown since no postmarketing surveillance mechanism exists. Adverse events are greatly underreported, and information regarding safety mainly comes from case reports and suboptimally conducted studies in a limited number of healthy young volunteers or patients with limited comorbidities. Therefore, convincing evidence for the safety of herbal products in the elderly is lacking, and the true magnitude of problems that herb-drug ...


Inhibition Of Human Α7 Nicotinic Acetylcholine Receptors By Cyclic Monoterpene Carveol, Yusra Lozon, Ahmed Sultan, Stuart J. Lansdell, Tatiana Prytkova, Bassem Sadek, Keun-Hang Susan Yang, Frank Christopher Howarth, Neil S. Millar, Murat Oz 2016 UAE University

Inhibition Of Human Α7 Nicotinic Acetylcholine Receptors By Cyclic Monoterpene Carveol, Yusra Lozon, Ahmed Sultan, Stuart J. Lansdell, Tatiana Prytkova, Bassem Sadek, Keun-Hang Susan Yang, Frank Christopher Howarth, Neil S. Millar, Murat Oz

Biology, Chemistry, and Environmental Sciences Faculty Articles and Research

Cyclic monoterpenes are a group of phytochemicals with antinociceptive, local anesthetic, and anti-inflammatory actions. Effects of cyclic monoterpenes including vanilin, pulegone, eugenole, carvone, carvacrol, carveol, thymol, thymoquinone, menthone, and limonene were investigated on the functional properties of the cloned α7 subunit of the human nicotinic acetylcholine receptor expressed in Xenopus oocytes. Monoterpenes inhibited the α7 nicotinic acetylcholine receptor in the order carveol>thymoquinone>carvacrol>menthone>thymol>limonene>eugenole>pulegone≥carvone≥vanilin. Among the monoterpenes, carveol showed the highest potency on acetylcholine-induced responses, with IC50 of 8.3 µM. Carveol-induced inhibition was independent of the membrane potential and ...


Nitrogen And Phosphorus Availability From Various Composted Wastes For Use In Irish Agriculture And Horticulture, Alan Lee 2016 Dublin Institute of Technology

Nitrogen And Phosphorus Availability From Various Composted Wastes For Use In Irish Agriculture And Horticulture, Alan Lee

Doctoral

Current environmental EU legislation promotes recycling and recovery from organic waste products. Compost has been identified as an alternative to inorganic fertilisers and animal slurries as a nutrient source for crop plants. This study aimed to investigate nitrogen (N) and phosphorus (P) availability from various composted waste through detailed characterisations, complemented by short term lab incubations and long term plant growth experiments. Twenty-five composts were selected and classified by their groups. The composts were characterised by multiple different analytical techniques. Two incubation studies were conducted. One investigating N and P mineralisation potential of the composts and the second on the ...


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