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Articles 361 - 390 of 504
Full-Text Articles in Pharmacy and Pharmaceutical Sciences
Almond Supplementation Reduces Serum Uric Acid In Coronary Artery Disease Patients: A Randomized Controlled Trial., Humaira Jamshed, Anwar Gilani, Fateh Ali Tipoo Sultan, Faridah Amin, Jamshed Arslan Arslan, Sumaira Ghani, Madiha Masroor
Almond Supplementation Reduces Serum Uric Acid In Coronary Artery Disease Patients: A Randomized Controlled Trial., Humaira Jamshed, Anwar Gilani, Fateh Ali Tipoo Sultan, Faridah Amin, Jamshed Arslan Arslan, Sumaira Ghani, Madiha Masroor
Department of Biological & Biomedical Sciences
Objective
Elevated serum uric acid (UA), a biomarker of renal insufficiency, is also an independent prognostic marker for morbidity in coronary artery disease (CAD) and poses serious health risks. This study reports the effect of almond consumption on UA in CAD patients.
Study design
A randomized controlled clinical trial was conducted with three groups: no-intervention (NI), Pakistani almonds (PA) or American almonds (AA). Patients were recruited from the Cardiology Clinics, Aga Khan University Hospital. Two follow-ups were scheduled at week-6 and week-12. 150 patients were randomly divided in three groups (50 per group). NI was not given almonds, whereas the …
Phytopharmaceuticals In Mongolia: Past, Present, And Future, Disan Gunbilig, Ulziinyam Rentsendorj
Phytopharmaceuticals In Mongolia: Past, Present, And Future, Disan Gunbilig, Ulziinyam Rentsendorj
Erforschung biologischer Ressourcen der Mongolei / Exploration into the Biological Resources of Mongolia, ISSN 0440-1298
Over the last two decades, the consumption of medicinal plants has increased in Mongolia. Once banned by the post-revolutionary government, it is now valued by the practitioners of orthodox medicine, government as well as by the society. Yet the scientific community has to give this major and crucial component of traditional Mongolian medicine the attention it deserves, scientific knowledge about biologically active principles within medicinal plants remain poorly unknown. At the same time, due to over exploitation of plants many species are becoming extinct together with invaluable traditional knowledge being lost. For these reasons, there is a certain urgency to …
The Influence Of Safety, Efficacy, And Medical Condition Severity On Natural V. Synthetic Drug Preference, Brian P. Meier, Courtney M. Lappas
The Influence Of Safety, Efficacy, And Medical Condition Severity On Natural V. Synthetic Drug Preference, Brian P. Meier, Courtney M. Lappas
Psychology Faculty Publications
Research indicates that there is a preference for natural v. synthetic products, but the influence of this preference on drug choice in the medical domain is largely unknown. We present 5 studies in which participants were asked to consider a hypothetical situation in which they had a medical issue requiring pharmacological therapy. Participants ( N = 1223) were asked to select a natural, plant-derived, or synthetic drug. In studies 1a and 1b, approximately 79% of participants selected the natural v. synthetic drug, even though the safety and efficacy of the drugs were identical. Furthermore, participants rated the natural drug as …
Cytotoxicity And Chemical Investigation Of The Aerial Parts Of Markhamia Zanzibarica (Bojer Ex Dc.) K. Schum. (Bignoniaceae), Dina M. El-Kersh, Riham S. El Dine, Dina R. Abou-Hussein, Fatma S. El-Sakhawy, Mohamed M. Elmazar
Cytotoxicity And Chemical Investigation Of The Aerial Parts Of Markhamia Zanzibarica (Bojer Ex Dc.) K. Schum. (Bignoniaceae), Dina M. El-Kersh, Riham S. El Dine, Dina R. Abou-Hussein, Fatma S. El-Sakhawy, Mohamed M. Elmazar
Pharmacy
The ethanolic extract of the aerial parts of Markhamia zanzibarica (Bignoniaceae) was tested for its cytotoxic activity against human cervical adenocarcinoma cell line (HeLa). It showed a potent effect with an IC50 of 9.68 μg/ml compared to Doxorubicin (7.28 μg/ml). The fractions obtained from the successive partitioning of the total extract, were tested against the same cell line; the results revealed that n-hexane extract was the most potent 9.23 μg/ml, followed by ethyl acetate, butanol and chloroform fractions with IC50 of 21.2, 22.4 and 49.6 μg/ml, respectively. Column chromatography led to the isolation of oleanolic acid (1), ursolic acid (2) …
Piperlongumine (Piplartine) And Analogues: Antiproliferative Microtubule-Destabilising Agents, Mary J. Meegan, Seema M. Nathwani, Brendan Twamley, Daniela M. Zisterer, Niamh O'Boyle
Piperlongumine (Piplartine) And Analogues: Antiproliferative Microtubule-Destabilising Agents, Mary J. Meegan, Seema M. Nathwani, Brendan Twamley, Daniela M. Zisterer, Niamh O'Boyle
Articles
Piperlongumine (piplartine, 1) is a small molecule alkaloid that is receiving intense interest due to its antiproliferative and anticancer activities. We investigated the effects of 1 on tubulin and microtubules. Using both an isolated tubulin assay, and a combination of sedimentation and Western blotting, we demonstrated that 1 is a tubulin-destabilising agent. This result was confirmed by immunofluorescence and confocal microscopy, which showed that microtubules in MCF-7 breast cancer cells were depolymerised when treated with 1. We synthesised a number of analogues of 1 to explore structure-activity relationships. Compound 13 had the best cytotoxic profile of this series, …
Skrining Fitokimia Dan Aktivitas Antioksidan Fraksi Etanol Alga Merah Eucheuma Spinosum, Bina Lohita Sari, Nurulia Susanti, Sutanto Sutanto
Skrining Fitokimia Dan Aktivitas Antioksidan Fraksi Etanol Alga Merah Eucheuma Spinosum, Bina Lohita Sari, Nurulia Susanti, Sutanto Sutanto
Pharmaceutical Sciences and Research
The red alga, Eucheuma spinosum from South Bangka Waters was shown to contain antioxidant activity. Natural antioxidants from algae are known to play an important role against various diseases and aging processes. The study objective was to investigate phytochemical screenings and antioxidant activity of ethanol fractions Euchema spinosum from south Bangka waters. Antioxidant activities of fresh algae (FA), dry algae (DA), and algae product (AP) were determined with DPPH (1,1-diphenyl-2-picrylhydrazyl) assay. Extraction was conducted using 70% ethanol in acidic environment for 24 hours. Then, the extract was evaporated using rotary evaporator. Dry extract was fractionated with ethanol - n - …
Enzim Papain: Aspek Green Chemistry Pada Reaksi Knoevenagel, Laurentius Haryanto, Antonius Herry Cahyana
Enzim Papain: Aspek Green Chemistry Pada Reaksi Knoevenagel, Laurentius Haryanto, Antonius Herry Cahyana
Pharmaceutical Sciences and Research
Green chemistry aspect is the chemical approach that has been studied in the past two decade. One of the principles is the development of green synthesis process that is friendly for the environment. This research showed that papain can be used as catalyst for Knoevenagel reaction with 3 kinds of substituted-benzaldehyde and malononitrile as substrates in aqueous medium. The best reaction condition with 80% yield was reached by utilizing of 25 mg papain/mmol substrate. Reaction was conducted at ambient temperature and pressure for 30 min. Products were as yellowish to yellow needle crystals and successfully characterized by melting point, UV-Vis, …
Uji Toksisitas Akut Dan Efek Antiinflamasi Ekstrak Metanol Dan Ekstrak N-Heksana Daun Pepaya (Carica Papaya L), Tahara Dilla Santi
Uji Toksisitas Akut Dan Efek Antiinflamasi Ekstrak Metanol Dan Ekstrak N-Heksana Daun Pepaya (Carica Papaya L), Tahara Dilla Santi
Pharmaceutical Sciences and Research
The acute toxicity test and antiinflammatory effect of methanolic and n-hexane extracts Carica papaya L leaf have been studied. The results of phytochemical screening show that papaya leaf contains alkaloid, steroid, and flavonoid compound. Flavonoid and alkaloid extracted from methanolic extract of papaya leaf and steroid extracted from n-hexane extract of papaya leaf. The acute toxicity test of methanolic and n-hexane extracts Carica papaya L leaf have been studied on rat with giving a single dose of samples. The aim of this work was to investigate the behavioral responses (pharmacological profile), the development of body weight and mortality for 14 …
Daun Jambu Biji (Psidium Guajava L.) Sebagai Antikanker Payudara, Dwitiyanti Dwitiyanti
Daun Jambu Biji (Psidium Guajava L.) Sebagai Antikanker Payudara, Dwitiyanti Dwitiyanti
Pharmaceutical Sciences and Research
Guava leaves are used as a cytotoxic. Previous research has demonstrated that guava leaves contained 61.71% of quersetin and has potential as an cytotoxic. The aim of this study was to determine the cytotoxic activity of 70% ethanol extract of guava leaves against cancer cells T47D. The method used direct counting (viable cell count) to obtained LC50 value. This study used a test solution with six concentrations that were 130.62; 67.98; 35.98; 18.43; 9.56 and 5 µg/ml. The LC50 value from the 70% ethanol extract of guava leaves was 27.54 µg/ml. The results suggested the extract of guava leaves has …
Milking The Information: Resources On Herbal Lactation Aids, Erica Rosalle
Milking The Information: Resources On Herbal Lactation Aids, Erica Rosalle
PCOM Scholarly Works
This article provides information for the layperson on herbs commonly used as galactagogues (lactation aids), their effectiveness, and risks according to existing scientific literature. In addition, resources for further research on herbal lactation aids are listed.
The Effects Of Rhein And Thymoquinone On Obesity And Diabetes In Diet-Induced Obese Mice., Emily Martell
The Effects Of Rhein And Thymoquinone On Obesity And Diabetes In Diet-Induced Obese Mice., Emily Martell
Senior Honors Projects
Natural product extracts and chemicals isolated from natural products (e.g. plants, berries, seeds) have been commonly used in various types of traditional medicines. In addition, some drugs on the market today have been derived from natural product sources. The purpose of our study was to evaluate two natural products, Rhein and Thymoquinone, for as potential anti-diabetic and anti–obesity agents. According to the Center for Disease Control (CDC), the number of people in the US diagnosed with diabetes has increase from 11.9 million people in the year 2000 to 20.8 million people in the year 2011. Rhein is a natural compound …
Anti-Neoplastic Effects Of Extracts From Gnaphalium Gracile On Colon, Pancreatic, And Prostate Cancer Cells, Joshua R. Canter
Anti-Neoplastic Effects Of Extracts From Gnaphalium Gracile On Colon, Pancreatic, And Prostate Cancer Cells, Joshua R. Canter
Undergraduate Honors Theses
Over 4,000 flavonoids have been identified, and among these, many of them are known to possess cardioprotective, anti-inflammatory, antimicrobial, and antitumor effects. However, most of these properties have yet to be fully understood. In this study, extracts from Gnaphalium gracile, thought to possess a mixture of flavonoids, have been tested for cytotoxic activity on pancreatic (MiaPaca, Panc28), colon (HCT-116, Caco-2), and prostate (PC3, LNCaP), cancer cell lines. Polar extracts from the leaves of G. gracile have the most cytotoxic effect on these cancer cell lines, particularly the prostate cancer cell lines PC3 and LNCaP. Evidence suggests the extracts have …
Penetapan Kadar Fenolik Dan Flavonoid Total Ekstrak Metanol Buah Dan Daun Patikala (Etlingera Elatior (Jack) R.M.Sm), Aktsar Roskiana Ahmad, Juwita Juwita, Siti Afrianty Daniya Ratulangi
Penetapan Kadar Fenolik Dan Flavonoid Total Ekstrak Metanol Buah Dan Daun Patikala (Etlingera Elatior (Jack) R.M.Sm), Aktsar Roskiana Ahmad, Juwita Juwita, Siti Afrianty Daniya Ratulangi
Pharmaceutical Sciences and Research
Fruit and leaves of patikala (Etlingera elatior (Jack) R.M.Sm), is a traditional medicinal plants used by people to treat various diseases. The purpose of this study was to determine the total phenolic and flavonoid compounds of E. elatior fruits and leaves extracts. We extracted dried fruits and leaves samples by maceration method using methanol. Qualitative analysis of chemical compounds with certain eluent was done using Thin Layer Chromatography (TLC) to determine the group of active compounds in the extract. The amount of phenolic compounds in the sample was determined by the colorimetric method at a maximum wavelength of 744.8 nm …
Aktivitas Antioksidan Ekstrak, Fraksi Dan Golongan Senyawakimia Daun Premna Oblongata Miq, Katrin Katrin, Atika Bendra
Aktivitas Antioksidan Ekstrak, Fraksi Dan Golongan Senyawakimia Daun Premna Oblongata Miq, Katrin Katrin, Atika Bendra
Pharmaceutical Sciences and Research
Indonesia has many kinds of plants which can be used as natural antioxidant sources. This study was focused on antioxidant activity of Cincau Perdu leaves extract (Premna oblongata Miq.) using 1-Diphenyl-2-picrylhydrazyl (DPPH) methods. P. oblongata leaves was extracted using n-hexane, ethylacetate and methanol. It was found that methanol extract has the highest activity with IC50 value 20.01 μg/mL. The extract with highest antioxidant activity were fractionated with accelerated column chromatography and were earned 6 combination fractions. The antioxidant activity of each combination fractions were tested by DPPH methods. Fraction-5 showed the highest activity as antioxidant with IC50 23.51 μg/mL. The …
Sintesis Ramah Lingkungan Senyawa Imina Turunan Vanilin Dan 2-Hidroksi Asetofenon Serta Uji Aktivitas Biologi Dan Antioksidan, Herry Cahyana, Putri Pratiwi
Sintesis Ramah Lingkungan Senyawa Imina Turunan Vanilin Dan 2-Hidroksi Asetofenon Serta Uji Aktivitas Biologi Dan Antioksidan, Herry Cahyana, Putri Pratiwi
Pharmaceutical Sciences and Research
Eco-friendly synthesis of imine derivative compound from 2-hydroxy acetophenone and vanillin had been conducted by using a method of stirring (with stirrer) in a water solvent. The whole experiment began with the synthesis of imine compounds, followed by purification and characterization of the synthesis products and finally analysis on their biological and antioxidant activities. The experiments showed that imine compounds could be synthesized by a chemical reaction of 4-amino antipirin aqueous solution with 2-hydroxy acetophenone and vanillin at magnetic stirrer speed of 250 and 450 rpm, respectively, which produced product A, (E)-4-(1-(2-hydroxyphenyl) ethylideneamino)-1,5-dimethyl-2-phenyl-1H-pyrazol-3(2H) -one and product B, (E)-4-(4-hydroxy-3-(vinyloxy) benzylideneamino)-1,5-dimethyl-2-phenyl-1H-pyrazol-3(2H)-one. Yield …
Evaluasi Kadar Kurkumin Dalam Jamu Tradisional Kunir Asam Yang Dijual Di Pasar Kota Gede Bulan Februari 2015, Fitrilya Mustikahati Yusuf, Nurkhasanah Nurkhasanah
Evaluasi Kadar Kurkumin Dalam Jamu Tradisional Kunir Asam Yang Dijual Di Pasar Kota Gede Bulan Februari 2015, Fitrilya Mustikahati Yusuf, Nurkhasanah Nurkhasanah
Pharmaceutical Sciences and Research
Javanese women often consume kunir asam to relieve dysmenorrhea symptom. It is a traditional herbal medicine which is conventionally prepared from curcuma domestica. One of the active compound of curcuma domestica is curcumin. The purpose of this research is to determine the amount of curcumin available in kunir asam selling in daily market of Kota Gede. Curcumin level in daily batches consistency was also evaluated. Curcumin analysis was conducted by qualitative and quantitative tests by TLC densitometry method. A total of 50.0 ml kunir asam was extracted with 25.0 ml of chloroform, and then the mixture was dried by evaporation. …
Toksisitas Ekstrak Etanol Mangifera Foetida L. Sebagai Pengkelat Besi Ditinjau Dari Ld50 Dan Komponen Sel Darah, Tri Wahyuni, Santi Purna Sari, Ari Estuningtyas, Hj Freisleben
Toksisitas Ekstrak Etanol Mangifera Foetida L. Sebagai Pengkelat Besi Ditinjau Dari Ld50 Dan Komponen Sel Darah, Tri Wahyuni, Santi Purna Sari, Ari Estuningtyas, Hj Freisleben
Pharmaceutical Sciences and Research
Ethanolic extract of bacang mango leaves (Mangifera foetida L.) decreased iron concentration in blood Sprague dawley rats that had been induced iron overload. The aim of this experiment was to determine acute toxicity (LD50) value of ethanolic extract of M.foetida by weil method and its effect to blood component. This study was conducted by employing a complete random design using 25 male and 25 female mice of DDY strain which devided into 5 groups. The first group until fourth group were administered ethanolic extract of M.foetida with dose variation which suspension in aquadest orally. The fifth group was control that …
Pengaruh Kandungan Komponen Minor Dari Minyak Kelapa Sawit (Elaeis Guineensis Jacq.) Terhadap Aktivitas Antioksidan Pada Proses Pemurnian Karotenoid, Ahmad Gazali Sofwan Sinaga, Donald Siahaan
Pengaruh Kandungan Komponen Minor Dari Minyak Kelapa Sawit (Elaeis Guineensis Jacq.) Terhadap Aktivitas Antioksidan Pada Proses Pemurnian Karotenoid, Ahmad Gazali Sofwan Sinaga, Donald Siahaan
Pharmaceutical Sciences and Research
Palm oil contains carotenoid and vitamin E which possess antioxidant properties. A long exposure of heat and chemical substances during the purification process may lower antioxidant activity. This research was conducted to compare antioxidant activity of carotenoid and vitamin E obtained from each stage of three continuous purification process (transesterification, solvolytic micellization, and saponification). Total carotenoid concentration was analyzed by UV-visible spectrophotometer at λ 446 nm and total vitamin E concentration was analyzed by high-performance liquid chromatography, while ester and triglyceride concentration were analyzed by gas chromatography. Antioxidant activity was measured by DPPH assay with incubation time in 60 minutes. …
Sintesis Dan Karakterisasi Hidrogel Superabsorben Kitosan Poli(N-Vinilkaprolaktam) (Pnvcl) Dengan Metode Full Ipn (Interpenetrating Polymer Network), Nadhrah Wivanius, Emil Budianto
Sintesis Dan Karakterisasi Hidrogel Superabsorben Kitosan Poli(N-Vinilkaprolaktam) (Pnvcl) Dengan Metode Full Ipn (Interpenetrating Polymer Network), Nadhrah Wivanius, Emil Budianto
Pharmaceutical Sciences and Research
Polymer material used for hydrogel should have capability to swell and to keep water molecules in its structure without solubilised in water. Natural polymers has functional groups which can perform as active sites in modification to produce polymer with better characteristic. Chitosan is a natural polymer which has good swelling ability but lack of structural strength. Synthesis of chitosan hydrogel by interpenetrating polymer network (IPN) will increase its strength through crosslinking. In this research, the first step of modification was the synthesis of chitosan polymer network crosslinked by acetaldehyde. The next step was the synthesis of PNVCL polymer network crosslinked …
Losio Antioksidan Buah Naga Merah (Hylocereus Polyrhizusbritton And Rose), Amanda Angelina Sinaga, Sri Luliana, Andhi Fahrurroji
Losio Antioksidan Buah Naga Merah (Hylocereus Polyrhizusbritton And Rose), Amanda Angelina Sinaga, Sri Luliana, Andhi Fahrurroji
Pharmaceutical Sciences and Research
Hylocereus polyrhizus Britton and Rose (Red dragon fruit) has been shown to have antioxidant activity which contains vitamin C, polyphenol, and flavonoid. This research was aimed to investigate antioxidant activity from H. polyrhizus in form of lotion. Lotion were made with 5 concentration from H. polyrhizus methanol extract were 0.04, 0.08, 0.16, 0.32 and 0.64%. Lotion antioxidant activity was measured using DPPH method. The result showed that H. polyrhizus methanol extract had antioxidant activity with inhibition concentration were 19.99±0.33; 25.01±0.08; 39.14±0.04; 66.69±0.12 and 83.37±0.05. The result showed significant differences on antioxidant activity. The physical stability observation of five formula with …
Pembentukan 8-Ohdg Dari Zat Toksik Pemicu Radikal Bebas, Intan Cahaya Dani, Budiawan Budiawan
Pembentukan 8-Ohdg Dari Zat Toksik Pemicu Radikal Bebas, Intan Cahaya Dani, Budiawan Budiawan
Pharmaceutical Sciences and Research
This study was conducted to observe the profile of DNA Adduct (8-OHdG) formation as DNA damage indicators, by using calf thymus DNA incubated with toxic and carcinogenic compounds. The compounds which could trigger free radicals in this research were PAH(Benzo[a]Pyrene), TiO2, and CuCl2. Calf thymus DNA was incubated with Benzo[a]Pyrene and CuCl2 compounds under pH and temperature variations. The incubation of calf thymus DNA with TiO2-UV radiation (254 nm) was used to induce the formation of reactive oxygen species (ROS) in the process of oxidative DNA damage. From this research, all of compounds have potency to trigger the formation of …
Evaluasi Aktivitas Antioksidan Senyawa 4-[(E)-2-(4-Okso-3-Fenilkuinazolin-2-Il)Etenil]-Benzensulfonamida Dan Analognya, Catur Jatmika, Baitha Palanggatan Maggadani, Hayun Hayun
Evaluasi Aktivitas Antioksidan Senyawa 4-[(E)-2-(4-Okso-3-Fenilkuinazolin-2-Il)Etenil]-Benzensulfonamida Dan Analognya, Catur Jatmika, Baitha Palanggatan Maggadani, Hayun Hayun
Pharmaceutical Sciences and Research
Quinazolinone derivative compounds exhibit a broad spectrum of biological activity, including antioxidant. Quinazolinone derivative compound 4-[(E)-2-(4-oxo-3-phenyl quinazolin-2-yl)ethenyl]-benzensulfonamida and its analogs (2a-f) have been synthesized and demonstrated its activity as a selective inhibitor of cyclooxygenase-2. The aim of this research was to evaluate the antioxidant activity of compound 4-[(E) -2-(4-oxo-3-fenilkuinazolin-2-yl)ethenyl]-benzensulfonamida and its analogs with DPPH radical scavenging method, ferric reducing activity potential (FRAP), and phosphomolybdenum method. The experiment revealed that the % inhibition and antioxidant capacity of compound 2c, 2e and 2f were higher compared to compound 2a, 2b and 2d. The DPPH radical scavenging analysis found that the % inhibition …
Curcumin Induces Apoptosis Of Upper Aerodigestive Tract Cancer Cells By Targeting Multiple Pathways, Arm R. Amin, A. Haque, M. A. Rahman, Z. G. Chen, F. R. Khuri, D. M. Shin
Curcumin Induces Apoptosis Of Upper Aerodigestive Tract Cancer Cells By Targeting Multiple Pathways, Arm R. Amin, A. Haque, M. A. Rahman, Z. G. Chen, F. R. Khuri, D. M. Shin
Pharmaceutical Science and Research
Curcumin, a natural compound isolated from the Indian spice "Haldi" or "curry powder", has been used for centuries as a traditional remedy for many ailments. Recently, the potential use of curcumin in cancer prevention and therapy urges studies to uncover the molecular mechanisms associated with its anti-tumor effects. In the current manuscript, we investigated the mechanism of curcumin-induced apoptosis in upper aerodigestive tract cancer cell lines and showed that curcumin-induced apoptosis is mediated by the modulation of multiple pathways such as induction of p73, and inhibition of p-AKT and Bcl-2. Treatment of cells with curcumin induced both p53 and the …
Fda Approves 18 New Molecular Entities/Biologics, Rodney Richmond
Fda Approves 18 New Molecular Entities/Biologics, Rodney Richmond
Faculty Research and Publications
No abstract provided.
Target-Directed Biosynthetic Evolution: Redirecting Plant Evolution To Genomically Optimize A Plant’S Pharmacological Profile, Dustin Paul Brown
Target-Directed Biosynthetic Evolution: Redirecting Plant Evolution To Genomically Optimize A Plant’S Pharmacological Profile, Dustin Paul Brown
Theses and Dissertations--Neuroscience
The dissertation describes a novel method for plant drug discovery based on mutation and selection of plant cells. Despite the industry focus on chemical synthesis, plants remain a source of potent and complex bioactive metabolites. Many of these have evolved as defensive compounds targeted on key proteins in the CNS of herbivorous insects, for example the insect dopamine transporter (DAT). Because of homology with the human DAT protein some of these metabolites have high abuse potential, but others may be valuable in treating drug dependence. This dissertation redirects the evolution of a native Lobelia species toward metabolites with greater activity …
Design, Synthesis, And Pharmacological Evaluation Of Three Series Of Lobelane Analogs As Inhibitors Of The Vesicular Monoamine Transporter (Vmat2), John P. Culver
Theses and Dissertations--Pharmacy
Methamphetamine (METH) abuse is a serious problem in the United States and worldwide. The reward experienced by METH users is due to the increase in extracellular dopamine (DA) concentrations caused by an interaction between METH and the DA transporter (DAT) as well as the Vesicular Monoamine Transporter-2 (VMAT2). The reward felt by users of METH leads to further use of the drug and subsequent abuse. The current project examined the ability of three novel series of lobelane analogs to interact with a binding site on the Vesicular Monoamine Transporter-2 (VMAT2) in an attempt to inhibit the effects of METH. Lobelane …
Chemoenzymatic Studies To Enhance The Chemical Space Of Natural Products, Jhong-Min Chen
Chemoenzymatic Studies To Enhance The Chemical Space Of Natural Products, Jhong-Min Chen
Theses and Dissertations--Pharmacy
Natural products provide some of the most potent anticancer agents and offer a template for new drug design or improvement with the advantage of an enormous chemical space. The overall goal of this thesis research is to enhance the chemical space of two natural products in order to generate novel drugs with better in vivo bioactivities than the original natural products.
Polycarcin V (PV) is a gilvocarcin-type antitumor agent with similar structure and comparable bioactivity with the principle compound of this group, gilvocarcin V (GV). Modest modifications of the polyketide-derived tetracyclic core of GV had been accomplished, but the most …
Antibiotics Targeting Tuberculosis: Biosynthesis Of A-102395 And Discovery Of Novel Actinomycins, Wenlong Cai
Antibiotics Targeting Tuberculosis: Biosynthesis Of A-102395 And Discovery Of Novel Actinomycins, Wenlong Cai
Theses and Dissertations--Pharmacy
The increase in antibiotic resistance of many bacterial strains including multidrug-resistant tuberculosis (MDR-TB) due to over- and misuse of antibiotics is a serious medical and economical problem. Therefore discovery and development of new antibiotics are urgently needed. Two projects were undertaken to address the need for new anti-tuberculosis antibiotics.
1. Discovery of new chemical entities. A-102395, a new nucleoside inhibitor of bacterial MraY (translocase I, EC 2.7.8.13) that is essential for bacterial survival, was isolated from the culture broth of Amycolatopsis sp. SANK 60206 in 2007. Although A-102395 is a potent inhibitor of translocase I with IC50 of 11 nM, …
Elucidating The Mechanism Of Lipl: A Non-Heme Fe(Ii), Α -Ketoglutarate: Uridine-5’-Monophosphate Dioxygenase, Anwesha Goswami
Elucidating The Mechanism Of Lipl: A Non-Heme Fe(Ii), Α -Ketoglutarate: Uridine-5’-Monophosphate Dioxygenase, Anwesha Goswami
Theses and Dissertations--Pharmacy
Several nucleoside natural product antibiotics from Streptomyces sp. and actinomycetes have recently been shown to target bacterial peptidoglycan cell wall biosynthesis by inhibiting the bacterial translocase I (MraY). The biosynthetic gene clusters for A-90289, liposidomycins and caprazamycins revealed a protein with sequence similarity to proteins annotated as α-KG:taurine dioxygenases (TauD). This enzyme (LipL) is a mononuclear, non-heme, Fe(II) dependent α-keto glutarate (α-KG) :uridine monophosphate (UMP) dioxygenase responsible for the net dephosphorylation and two electron oxidation of UMP to uridine-5’-aldehyde. The postulated reaction coordinates involving the activation of the C-5’ center in UMP and the corresponding formation of uridine-5’-aldehyde are modeled …
Feasibility Of Integrating Tripterygium Wilfordii Into Modern Cancer Therapy For Increased Efficacy And Minimal Toxicity, Ngoc T. Vo
Undergraduate Research Posters
Cancer is the second leading cause of death in the U.S. and millions of novel cancer cases are being diagnosed each year. While chemotherapy and ionizing radiation are effective treatments against these malignant tumors, the adverse effects that accompany such treatments are devastating. In order to find alternative treatment methods with less side effects, we turn to Eastern herbal medicine. Recent scientific research has found that Tripterygium wilfordii, an herbal medicine traditionally used to treat inflammation in China, contains compounds (triptolide and celastrol) that prevent the growth of solid tumors, induce apoptosis, and prevent metastasis of developed tumors. Investigations …