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Characterization Of G-Protein Coupled Receptors In Pain, Depression And Anxiety, Neil Lax 2018 Duquesne University

Characterization Of G-Protein Coupled Receptors In Pain, Depression And Anxiety, Neil Lax

Electronic Theses and Dissertations

Chronic pain and major depressive disorder are widespread conditions in the world. Interestingly, these conditions often occur comorbidly, with each individual disease amplifying the symptoms of the other. A significant amount of preclinical research in pain and depression focuses on G-protein coupled receptors (GPCRs), implying that GPCRs may be useful in treating this comorbidity. Our efforts have sought to characterize several poorly understood GPCRs, including the serotonin receptor subtypes 2C and 7 (5-HT2CR and 5-HT7R) and metabotropic glutamate receptor 5 (mGluR5), along with more well-known GPCRs such as the mu opioid receptor (MOR), and the role that they play in ...


Actinomycin Heterocyle Thesis 122018 For Submission.Pdf, Matt McErlean 2018 University of Kentucky

Actinomycin Heterocyle Thesis 122018 For Submission.Pdf, Matt Mcerlean

Matt McErlean

Actinomycins are a class of compounds consisting of phenoxazinone-like core attached to two peptidolactone rings, denoted as α and β. A unique component of a few families—actinomycins G, Y, and Z—is a chlorinated β-ring threonine residue. Families G and Y also contained an actinomycin that possess a β-ring heterocycle (actinomycins G5 and Y5, respectively); prior to this work, no β-ring heterocycle-containing actinomycins were reported for the Z family. Unlike other actinomycin derivatives, Y5’s cytotoxicity was abolished while still maintaining some antibacterial potency.
We constructed a model compound to probe the physical properties of the actinomycin core to ...


Determination Of Pyrrolizidine Alkaloids In Dietary Sources Using A Spectrophotometric Method, Oana C. Șeremet, Octavian T. Olaru, Mihaela Ilie, Claudia M. Guțu, Mihai G. Nițulescu, Camelia Diaconu, Catalina Motofei, Denisa Margină, Simona Negreș, Cristina E. Zbârcea, Emil Ștefănescu 2018 Carol Davila University of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacology and Clinical Pharmacy, Bucharest, Romania

Determination Of Pyrrolizidine Alkaloids In Dietary Sources Using A Spectrophotometric Method, Oana C. Șeremet, Octavian T. Olaru, Mihaela Ilie, Claudia M. Guțu, Mihai G. Nițulescu, Camelia Diaconu, Catalina Motofei, Denisa Margină, Simona Negreș, Cristina E. Zbârcea, Emil Ștefănescu

Journal of Mind and Medical Sciences

Pyrrolizidine alkaloids (PAs) are a class of toxic compounds found in the composition of more than 6000 plants. People can be exposed to PAs by consuming phytotherapeutic products, food from crops contaminated with seeds of some species with high content of PAs, and/ or contaminated animal products like bee products. For this reason we developed and validated a method for quantitative determination of PAs, from the most frequently contaminated food sources, honey and flour. Colorimetric Ehrlich reagent method was used with standard addition (1mg/kg senecionine). The extraction solvent was methanol 50% acidified with citric acid to pH 2-3, as ...


A V-To-F Substitution In Sk2 Channels Causes Ca2+ Hypersensitivity And Improves Locomotion In A C. Elegans Als Model, Young-Woo Nam, Sabia N. Baskoylu, Dimitris Gazgalis, Razan Orfali, Meng Cui, Anne C. Hart, Miao Zhang 2018 Chapman University

A V-To-F Substitution In Sk2 Channels Causes Ca2+ Hypersensitivity And Improves Locomotion In A C. Elegans Als Model, Young-Woo Nam, Sabia N. Baskoylu, Dimitris Gazgalis, Razan Orfali, Meng Cui, Anne C. Hart, Miao Zhang

Pharmacy Faculty Articles and Research

Small-conductance Ca2+-activated K+ (SK) channels mediate medium afterhyperpolarization in the neurons and play a key role in the regulation of neuronal excitability. SK channels are potential drug targets for ataxia and Amyotrophic Lateral Sclerosis (ALS). SK channels are activated exclusively by the Ca2+-bound calmodulin. Previously, we identified an intrinsically disordered fragment that is essential for the mechanical coupling between Ca2+/calmodulin binding and channel opening. Here, we report that substitution of a valine to phenylalanine (V407F) in the intrinsically disordered fragment caused a ~6 fold increase in the Ca2+ sensitivity of SK2-a channels. This substitution resulted in a ...


Extraction And Purification Of (E)-Resveratrol From The Bark Of Maine's Native Spruces, Panduka S. Piyaratne 2018 University of Maine

Extraction And Purification Of (E)-Resveratrol From The Bark Of Maine's Native Spruces, Panduka S. Piyaratne

Electronic Theses and Dissertations

Resveratrol is a plant secondary metabolite which protects plants from pathogenic invasions and acts as a remedial agent against injury, stress, and tissue damage by UV radiation. With its characteristic stilbene structure, resveratrol adopts (E) and (Z) isomeric forms. However, the (E) isomer is the most biologically active and abundant form of resveratrol in nature.

(E)- Resveratrol confers a variety of benefits to human health and well-being. Besides its antioxidant activity, the role of (E)-resveratrol as an anti-inflammatory, anti-aging, cardioprotection, and anticancer agent has been a widely explored research interest. Many plant species including mulberry, peanut, and grape are ...


Comparing The Side Effects Of Prescription Opioids And Medicinal Marijuana In The Treatment Of Chronic Pain, Callie Glenn, Ryan Bopp 2018 Carroll College - Helena

Comparing The Side Effects Of Prescription Opioids And Medicinal Marijuana In The Treatment Of Chronic Pain, Callie Glenn, Ryan Bopp

Carroll College Student Undergraduate Research Festival

Opioids are medications that interact with receptors in the central nervous system to provide pain relief, and have been a standard foundation for treatment of chronic pain since their discovery. But advancements in medical technology have led to the discovery of several alternatives to narcotics, one being medical marijuana. Cannabis has become increasingly pertinent in the medical field due to the medicinal and recreational legalization of the substance in several states. The purpose of this Evidence Based Practice Brief is to determine how the side effects of medical marijuana compared to those of opioid treatment affect quality of life for ...


Nutraceuticals: An Alternative Treatment For Influenza Virus, Siale Teaupa 2018 Brigham Young University

Nutraceuticals: An Alternative Treatment For Influenza Virus, Siale Teaupa

FHSS Mentored Research Conference

Influenza virus is a contagious respiratory pathogen that infects hundreds of thousands of people a year, making it a serious global health concern. The virus has a rapid mutation rate and has developed resistance to current antiviral agents, making it a difficult target for effective treatment. There is an increasing need to identify new treatments for Influenza. Recently, we have tested nutraceuticals as an effective alternative for blocking Influenza. We have tested Jamaican Sorrel, Black Currant Berries, and Manuka Honey paired with Bee Pollen for antiviral activity. We have demonstrated that these nutraceuticals block the 2009 Pandemic California Influenza strain ...


Discovery Of Natural Product Analogs Against Ethanol-Induced Cytotoxicity In Hippocampal Slice Cultures, Meredith A. Saunders-Mattingly 2018 University of Kentucky

Discovery Of Natural Product Analogs Against Ethanol-Induced Cytotoxicity In Hippocampal Slice Cultures, Meredith A. Saunders-Mattingly

Theses and Dissertations--Psychology

An estimated 13.9% of Americans currently meet criteria for an alcohol (ethanol; EtOH) use disorder (AUD). While there are 4 medications approved by the Food and Drug Administration (FDA) to treat AUD, these treatments have demonstrated poor clinical efficacy. Our ongoing research program encompasses a multi-tiered screening of a natural product library and validation process to provide novel information about the mechanisms underlying EtOH-induced changes in neurobiology and to identify novel chemical scaffolds to be exploited in the development of pharmacological treatments for AUD in a rodent organotypic hippocampal slice culture model. Initial screens of several natural product compounds ...


Synthesis Of 2,4,6-Substituted Pyrrolo[2,3-D]Pyrimidines As Potential Anticancer Agents, Si Yang 2017 Duquesne University

Synthesis Of 2,4,6-Substituted Pyrrolo[2,3-D]Pyrimidines As Potential Anticancer Agents, Si Yang

Electronic Theses and Dissertations

This thesis mainly focuses on the introduction of the background and work have been done in the areas of antifolates development, such as folate function, its three uptake mechanisms inside human cells, antifolates’ role in chemotherapy, et. al. In addition, the Structure-Activity-Relationship design rationale for the series of antifolates will also be discussed. Nevertheless, the details of synthesizing these pyrrolo[2,3-d]pyrimidines as potential antifolates have been described, including chemistry reviews on the pyrrolo[2,3-d]pyrimidine scaffold, and the challenges encountered and the solutions how to solve or improve in order to achieve better yield.


Progress Toward The Development Of A "Catch/Release" Strategy For Isolating Salvinorin A, From Plant Materails Including Microwave Promotion, Douglas Armstrong, Logan Smith 2017 Olivet Nazarene University

Progress Toward The Development Of A "Catch/Release" Strategy For Isolating Salvinorin A, From Plant Materails Including Microwave Promotion, Douglas Armstrong, Logan Smith

Faculty Scholarship – Chemistry

We are investigating using the Diels-Alder and retro-Diels-Alder reactions as a potential “catch/release” strategy for isolating Salvinorin A from plant samples (Salvia divinorum), hopefully to improve the current method, which is very long and laborious. Salvinorin A has analgesic activity by activating the kappa opioid receptor, not the mu receptor, and thus it has potential for being developed into a non-addicting analgesic.


Applied Drug Development And Combinatorial Strategies For Antimicrobial Treatment, Steven K. Lai Hing 2017 Texas A & M University - College Station

Applied Drug Development And Combinatorial Strategies For Antimicrobial Treatment, Steven K. Lai Hing

Andrews Research Conference

Streptococcus mutans JH1140 is a strain of bacteria which produces a lantibiotic product, named mutacin 1140. Mutacin 1140 has been shown to be effective at inhibiting Gram-positive bacterial infections caused by Staphylococcus aureus and Streptococcus pneumoniae. Mutacin 1140 is a ribosomally synthesized peptide antibiotic that undergoes extensive posttranslational modifications (PTM). We have found that Mutacin 1140 and an aminoglycoside, Kanamycin, when combined together, act synergistically against Staphylococcus aureus. This was determined by performing serial kill curve dilution overlays on solid media, followed up with kill curve by microdilution plate, and most recently confirmed with kill curve CFU count plates on ...


The Effect Of Luteolin On Human Glioblastoma, David M. Anson, Samson Amos, Robert L. Paris, Denise S. Simpson 2017 Cedarville University

The Effect Of Luteolin On Human Glioblastoma, David M. Anson, Samson Amos, Robert L. Paris, Denise S. Simpson

Denise (Simpson) Jean-Louis, Ph.D.

Glioblastoma multiforme (GBM) is widely recognized as the most common and lethal of the malignant gliomas. Few effective therapeutic treatments are available as five-year survival rates of diagnosed individuals are less than five percent. Luteolin, a common flavonoid found in a variety of fruits and vegetables, has demonstrated significant promise in combating cancers of the breast, colon, liver, lung, and bone. In this study, we investigated the effects of luteolin on glioblastoma multiforme cell lines U-251, U-87, and U-1242. Cell viability was assessed using cell count with trypan blue exclusion and MTT assays. Results revealed that luteolin reduces GBM cell ...


Discovery Of Natural Product-Based Antimycobacterial Agents Effective Against Non-Replicating Bacilli, Shajila Siricilla 2017 University of Tennessee Health Science Center

Discovery Of Natural Product-Based Antimycobacterial Agents Effective Against Non-Replicating Bacilli, Shajila Siricilla

Theses and Dissertations (ETD)

New antimycobacterial molecules that kill non-replicating Mycobacterium tuberculosis (Mtb) were identified by screening libraries of synthetic natural products. De novo screening of a 400-membered library of aurachin RE analogs resulted in discovery of UT-317 ((R)-20). UT-317 is a selective vitamin K2 biosynthesis (MenA) inhibitor that killed replicating and non-replicating Mtb at 2.31 μg/mL (MIC) and 0.85 μg/mL, respectively. A 50-membered library of capuramycin analogs was evaluated in their enzymatic inhibitory activities against translocase I (MraY/MurX) and prenyl-phosphate-GlcNAc-1-phosphate transferase (WecA). UT-01320 (45) is identified as a selective WecA inhibitor that kills both replicating and non-replicating ...


The Pharmacognosy And Therapeutic Efficacy Of Turmeric (Curcuma Longa): A Systematic Review, Maghan Ballantyne 2017 University of Rhode Island

The Pharmacognosy And Therapeutic Efficacy Of Turmeric (Curcuma Longa): A Systematic Review, Maghan Ballantyne

Senior Honors Projects

Turmeric is a well-known natural product, native to Southeast Asia, commonly

used for a variety of cultural traditions and health benefits. Generally referred

to as curcumin, it is a member of the Zingiberaceae, or ginger family, utilized

for its roots and known for its vibrant yellow hue. Culturally, it is primarily

incorporated into cooking and as an integral part of religious rituals and

ceremonies. Chemically, turmeric is classified as a phenolic compound, made

up of many curcuminoids, each with varying levels of activity. Therapeutically,

its health benefits include anti-inflammatory, anti-hyperlipidemia, anti-oxidant

and anti-pruritic properties. The pharmacognosy of curcumin modulates

inflammatory ...


The Effects Of Apigenin On Cell Proliferation And Apoptosis In Glioblastoma Multiforme, Trevor Stump, Brittany Santee, Lauren Williams, Chelsae Heinze, Rachel Kunze, Samson Amos, Denise S. Simpson 2017 Cedarville University

The Effects Of Apigenin On Cell Proliferation And Apoptosis In Glioblastoma Multiforme, Trevor Stump, Brittany Santee, Lauren Williams, Chelsae Heinze, Rachel Kunze, Samson Amos, Denise S. Simpson

Denise (Simpson) Jean-Louis, Ph.D.

Glioblastoma multiforme (GBM) is a WHO grade IV brain tumor. These tumors are highly proliferative, infiltrative, necrotic, angiogenic, and resistant to apoptosis. One major characteristic of GBM is the overexpression of epidermal growth factor receptor (EGFR), which leads to cell growth and proliferation when activated. GBM is very difficult to treat due to its location, heterogeneity, and invasiveness; an effective treatment is therefore needed. The use of flavonoids, which are natural compounds found in many fruits and vegetables, has been studied in the treatment of many different tumor types. Apigenin is a specific flavonoid that has previously been shown to ...


Crispr: The Last Piece Of The Genetic Puzzle, Brad Broyles 2017 Butler University

Crispr: The Last Piece Of The Genetic Puzzle, Brad Broyles

BU Well

CRISPR/Cas9 is an emerging gene editing tool. This technology, which evolved naturally as a defense mechanism for bacteria and other prokaryotes, has been repurposed to edit genes in a wide array of cells, including human cells. This paper outlines the discovery, mechanism, and potential applications of CRISPR/Cas9.


Adverse Reactions Of Biological Therapies In Patients With Psoriasis, Maria I. Sârbu, Mircea Tampa, Mădălina I. Mitran, Cristina I. Mitran, Alexandra M. Limbău, Simona R. Georgescu 2017 Carol Davila University, Department of Dermatology

Adverse Reactions Of Biological Therapies In Patients With Psoriasis, Maria I. Sârbu, Mircea Tampa, Mădălina I. Mitran, Cristina I. Mitran, Alexandra M. Limbău, Simona R. Georgescu

Journal of Mind and Medical Sciences

Psoriasis is a chronic, immune-mediated disorder characterized by well demarcated, erythematous plaques covered by thick, silvery-white scales, most often located on the knees, elbows, sacral area and scalp. It has a significant impact on the patient's quality of life.

Biological therapies revolutionized the treatment of psoriasis vulgaris but there has been concern regarding the use of those agents due to severe adverse reactions reported in patients receiving TNF-α inhibitors for various inflammatory diseases.

The aim of this paper is to review the most important adverse reactions reported in patients receiving biological treatments. The most common and severe side effects ...


Pharmacological Basis For The Medicinal Use Of Polyherbal Formulation And Its Ingredients In Cardiovascular Disorders Using Rodents, A Malik, Malik Hassan Mehmood, H Channa, MS Akhtar, AH Gilani 2017 Aga Khan University

Pharmacological Basis For The Medicinal Use Of Polyherbal Formulation And Its Ingredients In Cardiovascular Disorders Using Rodents, A Malik, Malik Hassan Mehmood, H Channa, Ms Akhtar, Ah Gilani

Department of Biological & Biomedical Sciences

A compound herbal formulation (POL4) has been used in the indigenous system of medicine to treat cardiometabolic disorders like diabetes and associated hypertension. POL4 and most of its constituents have not been studied widely for its therapeutic use in hypertension. This study is aimed to determine the efficacy and possible insight into mechanism(s) for the medicinal use of POL4 and its ingredients in hypertension.


Ethical Imperatives Of Timely Access To Orphan Drugs: Is Possible To Reconcile Economic Incentives And Patients’ Health Needs?, Rosa Rodriguez-Monguio, T. Spargo, Enrique Seoane-Vazquez 2017 University of Massachusetts Amherst

Ethical Imperatives Of Timely Access To Orphan Drugs: Is Possible To Reconcile Economic Incentives And Patients’ Health Needs?, Rosa Rodriguez-Monguio, T. Spargo, Enrique Seoane-Vazquez

Pharmacy Faculty Articles and Research

Background

More than 6,800 rare diseases and conditions have been identified in the US, which affect 25–30 million Americans. In 1983, the US Congress enacted the Orphan Drug Act (ODA) to encourage the development and marketing of drugs to treat rare diseases and conditions. This study analyzed all orphan designations and FDA approvals since 1983 through 2015, discussed the effectiveness of incentives for the development of treatments for rare diseases, and reflected on the ethical imperatives for timely access to orphan drugs.

Methods

Study data were derived from the Food and Drug Administration (FDA) Orange Book and the ...


The International Scientific Association For Probiotics And Prebiotics (Isapp) Consensus Statement On The Definition And Scope Of Prebiotics, Glenn R. Gibson, Robert W. Hutkins, Mary Ellen Sanders, Susan L. Prescott, Raylene A. Reimer, Seppo J. Salminen, Karen Scott, Catherine Stanton, Kelly S. Swanson, Patrice D. Cani, Kristin Verbeke, Gregor Reid 2017 University of Reading

The International Scientific Association For Probiotics And Prebiotics (Isapp) Consensus Statement On The Definition And Scope Of Prebiotics, Glenn R. Gibson, Robert W. Hutkins, Mary Ellen Sanders, Susan L. Prescott, Raylene A. Reimer, Seppo J. Salminen, Karen Scott, Catherine Stanton, Kelly S. Swanson, Patrice D. Cani, Kristin Verbeke, Gregor Reid

Faculty Publications in Food Science and Technology

In December 2016, a panel of experts in microbiology, nutrition and clinical research was convened by the International Scientific Association for Probiotics and Prebiotics to review the definition and scope of prebiotics. Consistent with the original embodiment of prebiotics, but aware of the latest scientific and clinical developments, the panel updated the definition of a prebiotic: a substrate that is selectively utilized by host microorganisms conferring a health benefit. This definition expands the concept of prebiotics to possibly include non-carbohydrate substances, applications to body sites other than the gastrointestinal tract, and diverse categories other than food. The requirement for selective ...


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