Natural Products Chemistry and Pharmacognosy Commons^™

Flavonoids With Novel Nicotinic Activity As Potential Pharmacotherapies To Treat Ethanol-Induced Neurotoxicity, Joseph A. Lutz

Theses and Dissertations--Pharmacy

Ethanol causes neurotoxicity via several mechanisms at different points in the cycle of dependence, including neuroinflammation and oxidative stress during ethanol exposure as well as excitotoxicity during ethanol withdrawal. The primary therapeutic implication is that ethanol-induced neurotoxicity requires multifunctional pharmacotherapies which reduce all mechanisms. Using an innovative pharmacological high throughput screening method on a large plant extract library we discovered flavonoids with alpha7 nicotinic acetylcholine receptor (nAChR) activity. In addition to their well-known anti-inflammatory and antioxidant properties, this novel activity means they can potentially reduce excitotoxicity and therefore makes them ideal for inhibition of ethanol-induced neurotoxicity. Rhamnetin, the candidate compound, …

Meta-Analysis Of Herbal Cannabis Therapy For Chronic Pain, Michael J. Seneca

UNF Graduate Theses and Dissertations

Since the first so-called “medical marijuana” legislation was passed in California in 1996, a total of twenty states and the District of Columbia have passed laws permitting limited use of cannabis. Despite the changes in state laws, cannabis remains illegal for any purpose under federal law. Changes in state laws have coincided with a renewed interest in the substance for the treatment of a variety of conditions. There has been a significant increase in published data over the past twenty years examining the efficacy of cannabis as an appetite stimulant, antiemetic agent, and analgesic adjuvant. The purpose of this meta-analysis …

Attenuation Of Parenteral Nutritionassociated Liver Disease By Omega-3 Long-Chain Polyunsaturated Fatty Acids, Emma Monique Tillman

Theses and Dissertations (ETD)

No abstract provided.

Development Of Tools To Assess The Effects Of Lunasin On Normal Development And Tumor Progression In Drosophila Melanogaster, Gillian E. Jones

Masters Theses & Specialist Projects

Soy contains many bioactive molecules known to elicit anti-cancer effects. One such peptide, Lunasin, has been shown to selectively act on newly transformed cells while having no cytotoxic effect on non-tumorigenic or established cancer cell lines. In this study we attempt to understand the developmental effects of Lunasin overexpression in vivo and create reagents that will help us understand Lunasin’s anti tumorigenic effects in an intact organism. cDNA encoding lunasin and EGFP-lunasin were cloned into pUAST and microinjected into Drosophila embryos. Tissue-specific overexpression of EGFP-Lun in the resulting transgenic lines was accomplished by crossing transgenics to various GAL4 driver lines. …

Isolation And Structural Elucidation Of Phytochemicals Present In Red Maple Flowers, Holly Tran

Senior Honors Projects

Natural medicines and the use of botanical extracts in the prevention and treatment of ailments is globally gaining interest (Mazzio and Soliman, 2009). Detrimental side effects may be reduced using natural therapies (Desai et al., 2008). Worldwide, there are about 120 different maple species. Of those, thirteen are native to eastern North America (Maple Field Guide, 2002). Maple syrup is a natural sweetener derived from collected and concentrated maple tree sap. It takes about 40 liters of sap to make one liter of syrup. Maple plant parts have been used by Native Americans for medicinal purposes. The University of Rhode …

Isolation And Partial Characterization Of Bioactive Fucoxanthin From Himanthalia Elongata Brown Seaweed: A Tlc-Based Approach, Gaurav Rajauria, Nissreen Abu-Ghannam

Articles

Seaweeds are important sources of carotenoids, and numerous studies have shown the beneficial effects of these pigments on human health. In the present study, Himanthalia elongata brown seaweed was extracted with a mixture of low polarity solvents, and the crude extract was separated using analytical thin-layer chromatography (TLC).The separated compounds were tested for their potential antioxidant capacity and antimicrobial activity against Listeria monocytogenes bacteria using TLC bioautography approach. For bio-autography, the coloured band on TLC chromatogram was visualized after spraying with DPPH and triphenyltetrazolium chloride reagents which screen antioxidant and antimicrobial compounds, respectively, and only one active compound was screened …

Effect Of Coconut Oil On Ulcerative Colitis In The Mouse Model, Pranav Chandra Alok

Masters Theses & Specialist Projects

Ulcerative colitis (UC) is a chronic disease of the colon or large intestine that causes inflammation and ulceration of the inner lining of the colon and rectum. In patients with ulcerative colitis, the body’s immune system overreacts and the body mistakes food, bacteria or other internal materials in the colon for an invading substance. The immune system attacks the material, thus irritating the colon. Limited knowledge of inflammatory conditions coupled with a narrow range of therapeutic options necessitates investigating the role of natural products. This study describes the effect of natural coconut oil on chemically-induced acute and chronic disease in …

Chemically Diverse Microtubule Stabilizing Agents Initiate Distinct Mitotic Defects And Dysregulated Expression Of Key Mitotic Kinases., Cristina C. Rohena, Jiangnan Peng, Tyler A. Johnson, Phillip Crews, Susan L. Mooberry

Natural Sciences and Mathematics | Faculty Scholarship

Microtubule stabilizers are some of the most successful drugs used in the treatment of adult solid tumors and yet the molecular events responsible for their antimitotic actions are not well defined. The mitotic events initiated by three structurally and biologically diverse microtubule stabilizers; taccalonolide AJ, laulimalide/fijianolide B and paclitaxel were studied. These microtubule stabilizers cause the formation of aberrant, but structurally distinct mitotic spindles leading to the hypothesis that they differentially affect mitotic signaling. Each microtubule stabilizer initiated different patterns of expression of key mitotic signaling proteins. Taccalonolide AJ causes centrosome separation and disjunction failure to a much greater extent …

In Vitro Anticancer Screening Of 24 Locally Used Nigerian Medicinal Plants, Saudat Adamson Fadeyi, Olugbeminiyi O. Fadeyi, Adedeji A. Adejumo, Cosmas Okoro, Elbert L. Myles

Chemistry Faculty Research

Background

Plants that are used as traditional medicine represent a relevant pool for selecting plant candidates that may have anticancer properties. In this study, the ethnomedicinal approach was used to select several medicinal plants native to Nigeria, on the basis of their local or traditional uses. The collected plants were then evaluated for cytoxicity.

Methods

The antitumor activity of methanolic extracts obtained from 24 of the selected plants, were evaluated in vitro on five human cancer cell lines.

Results

Results obtained from the plants screened indicate that 18 plant extracts of folk medicine exhibited promising cytotoxic activity against human carcinoma …

Gambogic Acid Is A Tissue-Specific Proteasome Inhibitor In Vitro And In Vivo, Xiaofen Li, Shouting Liu, Hongbiao Huang, Ningning Liu, Chong Zhao, Siyan Liao, Changshan Yang, Yurong Liu, Canguo Zhao, Shujue Li, Xiaoyu Lu, Chunjiao Liu, Lixia Guan, Kai Zhao, Xiaoqing Shi, Wenbin Song, Ping Zhou, Xiaoxian Dong, Haiping Guo, Guanmei Wen, Change Zhang, Lili Jiang, Ningfang Ma, Bing Li, Shunqing Wang, Huo Tan, Xuejun Wang, Q. Ping Dou, Jinbao Lin

Oncology Faculty Publications

Gambogic acid (GA) is a natural compound derived from Chinese herbs that has been approved by the Chinese Food and Drug Administration for clinical trials in cancer patients; however, its molecular targets have not been thoroughly studied. Here, we report that GA inhibits tumor proteasome activity, with potency comparable to bortezomib but much less toxicity. First, GA acts as a prodrug and only gains proteasome-inhibitory function after being metabolized by intracellular CYP2E1. Second, GA-induced proteasome inhibition is a prerequisite for its cytotoxicity and anticancer effect without off-targets. Finally, because expression of the CYP2E1 gene is very high in tumor tissues …

Lipophilic Stinging Nettle Extracts Possess Potent Anti-Inflammatory Activity, Are Not Cytotoxic And May Be Superior To Traditional Tinctures For Treating Inflammatory Disorders., Tyler A. Johnson, Johann Sohn, Wayne D Inman, Leonard F. Bjeldanes, Keith Rayburn

Natural Sciences and Mathematics | Faculty Scholarship

Extracts of four plant portions (roots, stems, leaves and flowers) of Urtica dioica (the stinging nettle) were prepared using accelerated solvent extraction (ASE) involving water, hexanes, methanol and dichloromethane. The extracts were evaluated for their anti-inflammatory and cytotoxic activities in an NF-κB luciferase and MTT assay using macrophage immune (RAW264.7) cells. A standardized commercial ethanol extract of nettle leaves was also evaluated. The methanolic extract of the flowering portions displayed significant anti-inflammatory activity on par with a standard compound celastrol (1) but were moderately cytotoxic. Alternatively, the polar extracts (water, methanol, ethanol) of the roots, stems and leaves displayed moderate …

Investigating Key Post-Pks Enzymes From Gilvocarcin Biosynthetic Pathway, Nidhi Tibrewal

Theses and Dissertations--Pharmacy

Gilvocarcin V (GV) belongs to the angucycline class of antibiotics that possesses remarkable anticancer and antibacterial activities with low toxicity. Gilvocarcin exhibits its light induced anticancer activity by mediating crosslinking between DNA and histone H3. When photo-activated by near-UV light, the C8 vinyl group forms a [2+2] cycloadduct with thymine residues of double stranded DNA. _D-fucofuranose is considered essential for histone H3 interactions. However, the poor water solubility has rendered it difficult to develop gilvocarcin as a drug. We aim to design novel gilvocarcin analogues with improved pharmaceutical properties through chemo-enzymatic synthesis and mutasynthesis. Previous studies have characterized many …

Preparasi, Karakterisasi Dan Evaluasi Pelepasan Obat Dari Beads Kalsium Alginat Deksametason Dengan Metode Gelasi Ionik, Christye Aulia, Joshita Djajadisastra

Majalah Ilmu Kefarmasian

Inflammatory Bowel Disease (IBD) is a disease of inflammation in the colon. Targeted delivery systems for the treatment of IBD is designed to increase the drug concentration in the local tissue. Dexamethasone is a drug having anti-inflammatory and antifibrosis effects which is used to repair scar tissue arising from postoperative IBD. This research purpose to create calciumalginate beads dexamethasone to be released only in the colon. Beads were made by using sodium-alginate and Ca2+ as crosslinker by ionic gelation method, with ratio between sodium alginate-dexamethasone (3:1). A concentration of solution sodium alginate 3 % b/v with variation concentration of crosslinker …

New Applications Of Mass Spectrometry For Drug And Lipid Analysis, Elizabeth Lauren Emerson

Graduate Theses and Dissertations

Mass spectrometry is an important tool used in many different disciplines and settings that include forensics, drug discovery, environmental analysis, and proteomics. Gas chromatography - mass spectrometry (GC-MS) and matrix assisted laser desorption/ionization time-of-flight mass spectrometry (MALDI - TOF MS) are two of the most important instruments used for analysis of compounds. Chapters 1 and 2 of this discussion use GC-MS for the investigation of synthetic cannabinoids in `K2' incense products and the detection of metabolites in urine samples from individuals suspected of consuming these mixtures. Analytical standards were synthesized and used for identification and confirmation of structures. Detection of …

North American Bioactive Plants For Human Health And Performance, Maria Pontes Ferreira, Fidji Gendron, Katrina C. Mcclure, Kelly Kindscher

Nutrition and Food Science Faculty Research Publications

Native and naturalized bioactive plants of the Canadian and American temperate biome are examined for their health and performance enhancement properties. Some of these plants are now being used as natural health products, and many have a long history as traditional foods and/or medicines with indigenous groups. This paper reviews the medicinal/cultural uses and bioactive properties of selected plant families: the Holly family (Aquifoliaceae) as stimulants, the Celery family (Apiaceae) as normoglycemic aids and analgesics, the Ginseng family (Araliaceae) as energy- boosting aids, the Sunflower family (Compositae) as anti-inflammatory aids, and the Legume family (Fabaceae) and Nightshade family (Solanaceae) as …

Anabolic And Androgenic Effects Of Certain Atriplex Species Grown In Egypt, Dina M. El-Kersh, Fatma S. El-Sakhawy, Dina R. Abou-Hussein, Amany A. Sleem

Pharmacy

20-Hydroxyecdysone (20-HE) was detected by TLC in the ethyl acetate fraction of two Atriplex species grown in Egypt: A. lindleyi subsp. inflata and A. leucoclada. EIA quantification of 20-HE proved its presence in a concentration of 9.15 and 7.3 μg/g dried aerial parts in each of the two species, respectively. Significant anabolic and androgenic activities were demonstrated for 20-HE comparing to testosterone; the study also revealed that the total alcohol extract and the ethyl acetate fraction of A. lindleyi subsp. inflata exhibited greater activities than their analogues in A. leucoclada. Column chromatographic fractionation of the ethyl acetate fraction of the …

Development And Validation Of A Simple Method For The Detection Of Fascaplysin In Plasma, Kenneth H. Swartz, Frederick A. Valeriote, Joseph Media, Tyler A. Johnson, Karen Tenney, Phillip Crews, Jiajiu Shaw

Natural Sciences and Mathematics | Faculty Scholarship

Fascaplysin is a cytotoxic natural product isolated from a variety of Indo-Pacific marine organisms, primarily Fascaplysinopsis sponges and Didemnum tunicates. Positive xenograft studies involving this alkaloid structural class have indicated that fascaplysin may serve as an important lead compound for preclinical development. This study was undertaken as a prelude to a full pharmacokinetics and therapeutic assessment of fascaplysin. We describe here a simple plasma preparation and a rapid HPLC method for the detection of fascaplysin in mice. The method was validated by parameters including good linear correlation, a limit of quantification of 107.1 μg/ mL, and a good precision with …

Activation Of Amp-Activated Protein Kinase By 3,39-Diindolylmethane (Dim) Is Associated With Human Prostate Cancer Cell Death In Vitro And In Vivo, Di Chen, Sanjeev Banerjee, Qiuzhi C. Cui, Dejuan Kong, Fazlul H. Sarkar, Q. Ping Dou

Oncology Faculty Publications

There is a large body of scientific evidence suggesting that 3,39-Diindolylmethane (DIM), a compound derived from the digestion of indole-3-carbinol, which is abundant in cruciferous vegetables, harbors anti-tumor activity in vitro and in vivo. Accumulating evidence suggests that AMP-activated protein kinase (AMPK) plays an essential role in cellular energy homeostasis and tumor development and that targeting AMPK may be a promising therapeutic option for cancer treatment in the clinic. We previously reported that a formulated DIM (BR-DIM; hereafter referred as B-DIM) with higher bioavailability was able to induce apoptosis and inhibit cell growth, angiogenesis, and invasion of prostate cancer cells. …

Uji Penghambatan Aktivitas Alfa-Glukosidase Ekstrak Dan Fraksi Daun Antidesma Montanum Blume, Nofiantini Nofiantini, Berna Elya, Azizahwati Azizahwati

Majalah Ilmu Kefarmasian

alpha-Glucosidase inhibitor has known to be a therapeutic agent for diabetes mellitus (DM) treatment, especially type 2 DM. Based on previous studies. There are various plants that have the effect of inhibiting the activity of a-glucosidase, one of which is garu leaves (Antidesma montanum Blume). This research aimed to get the fraction which had the highest Il-glucosidase inhibiting activity from ethanol extract of garu leaves and identify the chemical compounds from the most active fraction. Simplisia powder was extracted by maseration using 80% ethanol then fractionated using n-hexane, ethyl acetate, and methanol. Inhibitory activity test was performed by measuring absorbance …

Analisis Zat Warna Merah Sintetik Pada Selai Stroberi Yang Dijual Di Pasar Tradisional Kota Depok, Putri Ayuningtyas, Rani Sauriasari, Maryati Kurniadi

Majalah Ilmu Kefarmasian

Jam is a semi-solid food products made of fruit cooked with sugar that used as aflavoring on bakery including strawberry jam. Strawberry jam is added to food additives such as food dyes. The purpose of this study is to know about ponceau 4R, allura red, rodamin B, and amaran in the sample of strawberry jam in the traditional market at Depok City and to determine the levels of synthetic red dyes that are permitted on the sample strawberry jam. The method applied was dye isolation with wool and followed by analysis using a color reaction, then followed by paper chromatography …