Natural Products Chemistry and Pharmacognosy Commons^™

The Value Of Universally Available Raw Nmr Data For Transparency, Reproducibility, And Integrity In Natural Product Research., James B. Mcalpine, Shao-Nong Chen, Andrei Kutateladze, John B. Macmillan, Giovanni Appendino, Andersson Barison, Mehdi A. Beniddir, Maique W. Biavatti, Stefan Bluml, Asmaa Boufridi, Mark S. Butler, Robert J. Capon, Young H. Choi, David Coppage, Phillip Crews, Michael T. Crimmins, Marie Csete, Pradeep Dewapriya, Joseph M. Egan, Mary J. Garson, Grégory Genta-Jouve, William H Gerwick, Harald Gross, Mary Kay Harper, Precilia Hermanto, James M. Hook, Luke Hunter, Damien Jeannerat, Nai-Yun Ji, Tyler A. Johnson, David G. I. Kingston, Hiroyuki Koshino, Hsiau-Wei Lee, Guy Lewin, Jie Li, Roger G Linington, Miaomiao Liu, Kerry L Mcphail, Tadeusz F Molinski, Bradley S Moore, Joo-Won Nam, Ram P Neupane, Matthias Niemitz, Jean-Marc Nuzillard, Nicholas H Oberlies, Fernanda M M Ocampos, Guohui Pan, Ronald J Quinn, D Sai Reddy, Jean-Hugues Renault, José Rivera-Chávez, Wolfgang Robien, Carla M Saunders, Thomas J Schmidt, Christoph Seger, Ben Shen, Christoph Steinbeck, Hermann Stuppner, Sonja Sturm, Orazio Taglialatela-Scafati, Dean J Tantillo, Robert Verpoorte, Bin-Gui Wang, Craig M Williams, Philip G Williams, Julien Wist, Jian-Min Yue, Chen Zhang, Zhengren Xu, Charlotte Simmler, David C Lankin, Jonathan Bisson, Guido F Pauli

Natural Sciences and Mathematics | Faculty Scholarship

With contributions from the global natural product (NP) research community, and continuing the Raw Data Initiative, this review collects a comprehensive demonstration of the immense scientific value of disseminating raw nuclear magnetic resonance (NMR) data, independently of, and in parallel with, classical publishing outlets. A comprehensive compilation of historic to present-day cases as well as contemporary and future applications show that addressing the urgent need for a repository of publicly accessible raw NMR data has the potential to transform natural products (NPs) and associated fields of chemical and biomedical research. The call for advancing open sharing mechanisms for raw data …

Actinomycin Familial Diversity Driven By Phenoxazinone-Core Reactivity, Matthew Richard Mcerlean

Theses and Dissertations--Pharmacy

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 …

Development Of Mithramycin Analogues With Improved Efficacy And Reduced Toxicity For Treatment Of Ets-Dependent Tumors In Ewing Sarcoma And Prostate Cancer, Joseph Michael Eckenrode

Theses and Dissertations--Pharmacy

Introduction: Genetic rearrangements in Ewing sarcoma, prostate, and leukemia cells result in activation of oncogenic ETS transcription factor fusions. Mithramycin (MTM) has been identified as an inhibitor of EWS-FLI1 transcription factor, a gene fusion product responsible for oncogenesis in Ewing sarcoma. Despite preclinical success, a phase I/II clinical trial testing MTM therapy in refractory Ewing sarcoma was terminated. Liver and blood toxicities resulted in dose de-escalation and sub-therapeutic exposures. However, the promise of selectively targeting oncogenic ETS transcription factors like EWS-FLI1 prompted us to undertake the discovery of more selective, less toxic analogues of MTM. MTM is a potent inhibitor …

Anti-Inflammatory, Anti-Nociceptive And Antipyretic Activity Of Young And Old Leaves Of Vernonia Amygdalina, Du-Bois Asante, Isaac Tabiri Henneh, Desmond Omane Acheampong, Foster Kyei, Christian Kweku Adokoh, Eric Gyamerah Ofori, Nelson Kwabla Domey, Emmanuel Adakudugu, Lokeswari Prathyusha Tangella, Elvis Ofori Ameyaw

Research outputs 2014 to 2021

Background

Both young and old leaves of Vernonia amygdalina (VA) are traditionally used to treat inflammation, pain and fever. However, the efficacy of young and old leaves for treating these ailments have not been compared till date.

Aim

To ascertain the effect of young and old leaves of VA in managing inflammation, pain and fever.

Methods

Both quantitative and qualitative phytochemical screening of ethanol extracts of young (EthYL) and old (EthOL) leaves of VA were performed. The anti-inflammatory activity of orally administered EthYL and EthOL (50–200 mg/kg) and Diclofenac (10 mg/kg) were evaluated in carrageenan-induced inflammation model in rats. Antipyretic …

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

Matt McErlean

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 this …

Evaluasi Kesesuaian Dosis Pada Pasien Pediatri Bronkitis Akut Di Rumah Sakit Tentara Kartika Husada Kubu Raya, Variandini Aldhila Kharis, Rise Desnita, Hariyanto Ih

Pharmaceutical Sciences and Research

Selection and usage of rational drugs determine the success of expected therapeutic effect, especially for pediatrics. Acute bronchitis in pediatrics is one of the highest incidents of Acute Respiratory Infection (ARI) in Army Hospital Kartika Husada Kubu Raya. This study aimed to evaluate rationality of drug doses conformity in outpatient pediatric acute bronchitis in Army Hospital Kartika Husada Kubu Raya on 2015. This research was a descriptive observational research with cross-sectional design. The sample was taken with purposive sampling amounted to 36 prescriptions. Then the evaluation of drug doses conformity was counted according to the literature. The results showed that …

Evaluasi Kesesuaian Penulisan Resep Pada Kasus Ispa Non Pneumonia Di Poli Mtbs Puskesmas Kecamatan Cengkareng, Jakarta, Rani Sauriasari, Annisa Azka Hikmawati Aulia, Adisa Swastika

Pharmaceutical Sciences and Research

Acute respiratory infections (ARI) is one of the major health problems in Indonesia. There are three classifications of cases of ARI, consist of pneumonia, severe pneumonia and non pneumonia. This study aimed to find an overview of the use of antibiotics and the evaluation of suitability prescriptions performed in cases of non pneumonia Acute Respiratory Infections (ARI) in IMCI Polyclinic, Cengkareng District Community Health Centre (Puskesmas Cengkareng), West Jakarta. Evaluation for the prescription suitability was useful to find the percentage of the suitability of prescribing on the existing management. This activity was done using retrospective method with data of 100 …

L-Citrulline As Alternative Pharmacological Substance In Protecting Against Cardiovascular Disease, Andrea Laurentius, Gregorius Bhaskara Wikanendra, Tzeto Han Cong, Wawaimuli Arozal

Pharmaceutical Sciences and Research

Cardiovascular disease (CVD) has taken up to average 30% of death diagnoses in the world. Prevalent attempts of physicians to treat this disease came down to focus on using drugs with their specific mechanism of action. Since the method only cures the symptoms and need to be pharmacologically monitored, physicians and scientists have been struggling to find other treatment strategies. This problem led us to search for another substance dealing with CVD via preventive therapy, which does not require such close monitoring by physicians in its use. The answer relies on using L-citrulline as potential therapeutics in treating and preventing …

Pemodelan Molekul Turunan P-Metoksi Sinnamoil Hidrazida Sebagai Inhibitor Checkpoint Kinase 1 Dan Inhibitor Aromatase Secara In Silico, Galih Satrio Putra, Melanny Ika Sulistyowatya, Juni Ekowati, Tutuk Budiati

Pharmaceutical Sciences and Research

The development of anticancer drugs from ethyl p-methoxycinnamate (EPMC) derivatives has been done to compounds high activity in inducing cancer cells apoptosis and minimal side effects. p-Methoxycinnamoyl hydrazide derivates, modified from EPMC structure, were docked into the ligand-binding pocket of Check point kinase 1 enzymes (2YWP) and the aromatase enzyme (3S7S) using software Molegro Virtual Docker (MVD) Ver.5.5. We compared the Rerank score of native ligand with p-Methoxycinnamoyl hydrazide derivates. Rerank scores of compounds 4b and 4c (-99.98 Kcal/mol and -99.80 Kcal/mol) were lower than the native ligand A42 in inhibiting the enzyme checkpoint kinase 1. Rerank values of p-Methoxycinnamoyl …

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 novel interaction between …

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. …

Potency Of (Poly) Acrylic/Carboxymethyl Starch-Chitosan Biohydrogel For Curcumin Oral Delivery Matrix, Eka Ruriani, Djumali Mangunwidjaja, Nur Richana, Titi Candra Sunarti

Pharmaceutical Sciences and Research

Biohydrogel has gathered great interest in the pharmaceuticals field. This natural polymers were biodegradable, non-toxic, biocompatible, and its specific ability to response environment change can be considered for the controlled released matric of bioactive compound. In this study, the biohydrogel was synthesized by graft-copolymerization of acrylic acid onto carboxymethyl starch (CMS) and chitosan. The objective of this research was to determine the effect of CMS-chitosan ratio on the biohydrogel characteristic. The acrylic acid was grafted on to the backbone (3:1) using cerric ammonium nitrate as the inisiator.A standarded curcumin was applied to test the binding potency of matrix. A higher …

Aktivitas Mukolitik Kombinasi Ekstrak Etanol Daun Kemangi Dan Ekstrak Etanol Daun Sirih Merah, Neng Fisheri Kurniati, Deden Winda Suwandi, Safira Yuniati

Pharmaceutical Sciences and Research

A cough is a protective physiological mechanism that is useful for removing and clearing the respiratory tract from sputum and foreign particles that can cause infection. Treatments for cough disorders using medicinal plants were conducted because medicinal plants were widely known to have less side effects than synthetic drugs. Basil leaves (Ocimum sanctum L.) and red betel leaves (Piper crocatum Ruiz and Pav) have been used traditionally to treat a cough. The purpose of this study was to determine the mucolytic activity, and the effective concentration of the combination of basil and red betel leaves ethanol extract. The mucolytic activity …

Evaluation Of Propolis And Milk Administration On Caffein-Induced Mus Musculus Fetus Skeletal, Dwisari Dillasamola, Almahdy A, Novita Purnama Sari, Biomechy Oktomalio Putri, Noverial Noverial, Skunda Diliarosta

Pharmaceutical Sciences and Research

Caffeine consumption by pregnant women at doses above 300 mg/day was suggested to cause skeletal damage. Propolis with high flavonoids concentration could increase the number of osteoblasts. This research aims to evaluate the effect of propolis and milk administration on fetal skeletal of caffeine-induced female mice (Mus musculus). Mice were divided into six groups: negative group, positive group of caffeine (a dose of 75 mg/kg BW), positive group of propolis (a dose of 1400 mg/kg BW), positive group of milk (200 ml), group D1 (caffeine 75 mg/kg BW and propolis 1400 mg/kg BW) and group D2 (caffeine 75 mg/kg BW …

Evaluasi Rasionalitas Penggunaan Obat Antihipertensi Di Puskesmas Siantan Hilir Kota Pontianak Tahun 2015, Eka Kartika Untari, Alvani Renata Agilina, Ressi Susanti

Pharmaceutical Sciences and Research

Hypertension is widely known as cardiovascular disease. In addition to resulting heart failure, hypertension can result in kidney failure and cerebrovascular disease. This study was aimed to determine the percentage of treatment rationality of hypertensive patient treatment outpatient in Puskesmas Siantan Hilir Pontianak 2015 which includes the appropriate indication, appropriate drug, appropriate patient, and appropriate dose based on the guideline JNC 7. This study was cross-sectional study using medical records of outpatient hypertension patients in 2015. The total of sample analyzed in this research were 92 medical records of hypertension patients from 118 medical records. The percentage of using the …

Optimasi Aktivitas Bakteriosin Yang Dihasilkan Oleh Bakteri Lactobacillus Plantarum Dari Minuman Ce Hun Tiau, Rafika Sari, Pratiwi Apridamayanti, Melly Octaviani

Pharmaceutical Sciences and Research

Bacteriocin is a protein compound with a small molecular weight that has an antibacterial activity. Bacteriocin has been widely applied as a natural food preservative, as it effectively prevents the growth of pathogenic bacteria in foods and beverages. The aim of this research was to know the activity of bacteriocin produced by lactic acid bacteria Lactobacillus plantarum from Ce hun tiau beverages against Escherichia coli and Staphylococcus aureuswith different pH and temperature treatments. In this study, Lactobacillus plantarum bacteria isolated from Ce hun tiau beverages were characterized by Gram staining test. Bacteriocin was extracted from Lactobacillus plantarum bacteria which had …

Peran Tenaga Kefarmasian Dalam Penanggulangan Bencana Role Of Pharmacist In Disaster Management, Meutia Faradilla

Pharmaceutical Sciences and Research

Indonesia is a country that has high potency to be affected by disaster, either by natural or man-made disaster. After the 2004 tsunami, Indonesian government has improved its disaster prevention policy and program. In disaster management study, health management in disaster setting is aimed to assure the implementation of health service toward victims accordingly. As integrated part of the healthcare team in disaster management, pharmacists have to understand the importance of pharmaceutical care in pre-disaster, disaster, and post-disaster phase. This article aims to provide an overview on pharmacists’ role in disaster management from preparing and distributing medicine and medical devices …

Sensitivity Of Escherichia Coli Bacteria Towards Antibiotics In Patient With Diabetic Foot Ulcer, Rafika Sari, Pratiwi Apridamayanti, Indira Diah Puspita

Pharmaceutical Sciences and Research

Chronic complication of diabetes mellitus is diabetic foot ulcers. Diabetic foot ulcer can be defined as an open wound in the feet which will become infected as the result of high blood sugar levels that develops and become place of bacteria. One of the bacteria in diabetic foot ulcer is Escherichia coli. Imprecise use of antibiotics in the treatment of diabetic foot ulcers can cause antibiotic resistance to bacteria. This study aims to determine antibiotic sensitivity of Escherichia coli bacteria in diabetic foot ulcer Wagner grade III and IV. Samples of diabetic foot ulcer swab’s with Wagner grade III and …