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https://www.readbyqxmd.com/read/29656318/a-novel-tetrasubstituted-imidazole-as-a-prototype-for-the-development-of-anti-inflammatory-drugs
#1
Marcus Vinicius P S Nascimento, Antonio C M Munhoz, Lais C Theindl, Eduarda Talita B Mohr, Najla Saleh, Eduardo B Parisotto, Thaís A Rossa, Ariane Zamoner, Tania B Creczynski-Pasa, Fabíola B Filippin-Monteiro, Marcus M Sá, Eduardo Monguilhott Dalmarco
Although inflammation is a biological phenomenon that exists to protect the host against infections and/or related problems, its unceasing activation results in the aggravation of several medical conditions. Imidazoles, whether natural or synthetic, are molecules related to a broad spectrum of biological effects, including anti-inflammatory properties. In this study, we screened eight novel small molecules of the imidazole class synthesized by our research group for their in vitro anti-inflammatory activity...
April 14, 2018: Inflammation
https://www.readbyqxmd.com/read/29656237/vascularized-microfluidic-organ-chips-for-drug-screening-disease-models-and-tissue-engineering
#2
REVIEW
Tatsuya Osaki, Vivek Sivathanu, Roger D Kamm
Vascularization of micro-tissues in vitro has enabled formation of tissues larger than those limited by diffusion with appropriate nutrient/gas exchange as well as waste elimination. Furthermore, angiocrine signaling from the vasculature may be essential in mimicking organ-level functions in these micro-tissues. In drug screening applications, the presence of an appropriate blood-organ barrier in the form of a vasculature and its supporting cells (pericytes, appropriate stromal cells) may be essential to reproducing organ-scale drug delivery pharmacokinetics...
April 12, 2018: Current Opinion in Biotechnology
https://www.readbyqxmd.com/read/29656007/mir-195-potentiates-the-efficacy-of-microtubule-targeting-agents-in-non-small-cell-lung-cancer
#3
Xiaojie Yu, Yiqiang Zhang, Xiuye Ma, Alexander Pertsemlidis
Microtubule-targeting agents (MTAs) are widely used for the treatment of non-small cell lung cancer (NSCLC). The response rate is only ∼25%, mainly attributable to drug resistance. To identify determinants of resistance in NSCLC, we performed a high-throughput screen using a library of miRNA mimics. Here we report that miR-195 synergizes with MTAs to inhibit the growth of NSCLC cells in vitro, that increased expression of miR-195 sensitizes NSCLC cells to MTAs and that repression of miR-195 confers resistance to MTAs...
April 13, 2018: Cancer Letters
https://www.readbyqxmd.com/read/29655691/functionalized-liposomes-and-phytosomes-loading-annona-muricata-l-aqueous-extract-potential-nanoshuttles-for-brain-delivery-of-phenolic-compounds
#4
Simona Mancini, Luca Nardo, Maria Gregori, Inês Ribeiro, Francesco Mantegazza, Cristina Delerue-Matos, Massimo Masserini, Clara Grosso
BACKGROUND: Multi-target drugs have gained significant recognition for the treatment of multifactorial diseases such as depression. Under a screening study of multi-potent medicinal plants with claimed antidepressant-like activity, the phenolic-rich Annona muricata aqueous extract (AE) emerged as a moderate monoamine oxidase A (hMAO-A) inhibitor and a strong hydrogen peroxide (H2 O2 ) scavenger. PURPOSE: In order to protect this extract from gastrointestinal biotransformation and to improve its permeability across the blood-brain barrier (BBB), four phospholipid nanoformulations of liposomes and phytosomes functionalized with a peptide ligand promoting BBB crossing were produced...
March 15, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/29655499/genetic-testing-in-clinical-settings
#5
Nora Franceschini, Amber Frick, Jeffrey B Kopp
Genetic testing is used for screening, diagnosis, and prognosis of diseases consistent with a genetic cause and to guide drug therapy to improve drug efficacy and avoid adverse effects (pharmacogenomics). This In Practice review aims to inform about DNA-related genetic test availability, interpretation, and recommended clinical actions based on results using evidence from clinical guidelines, when available. We discuss challenges that limit the widespread use of genetic information in the clinical care setting, including a small number of actionable genetic variants with strong evidence of clinical validity and utility, and the need for improving the health literacy of health care providers and the public, including for direct-to-consumer tests...
April 11, 2018: American Journal of Kidney Diseases: the Official Journal of the National Kidney Foundation
https://www.readbyqxmd.com/read/29653365/bene%C3%AF-cial-health-effects-of-lupenone-triterpene-a-review
#6
REVIEW
Feng Xu, Xulong Huang, Hongmei Wu, Xiangpei Wang
There are a large number of new structure compounds with good pharmacological activity in the natural plants, can be applied to the treatment of human diseases. Finding active ingredients from the plants is one of the important ways to develop new drugs. Triterpenes are widespread in plants, and lupenone belongs to lupane type triterpenoids. Lupenone is very common natural ingredient distributed in multi-family plants including Asteraceae, Balanophoraceae, Cactaceae, Iridaceae, Musaceae, Urticaceae, Leguminosae, Bombacaceae, etc...
April 10, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29653287/detecting-the-functional-complexities-between-high-density-lipoprotein-mimetics
#7
Yoshitaka J Sei, Jungho Ahn, Taeyoung Kim, Eunjung Shin, Angel J Santiago-Lopez, Seung Soon Jang, Noo Li Jeon, Young C Jang, YongTae Kim
High-density lipoprotein (HDL) is a key regulator of lipid homeostasis through its native roles like reverse cholesterol transport. The reconstitution of this natural nanoparticle (NP) has become a nexus between nanomedicine and multi-disease therapies, for which a major portion of HDL functionality is attributed to its primary scaffolding protein, apolipoprotein A1 (apoA1). ApoA1-mimetic peptides were formulated as cost-effective alternatives to apoA1-based therapies; reverse-4F (r4F) is one such peptide used as part of a nanoparticle platform...
April 6, 2018: Biomaterials
https://www.readbyqxmd.com/read/29653190/evaluation-of-whole-genome-sequencing-and-software-tools-for-drug-susceptibility-testing-of-mycobacterium-tuberculosis
#8
Janko van Beek, Marjo Haanperä, Pieter W Smit, Silja Mentula, Hanna Soini
OBJECTIVES: Culture-based assays are currently the gold standard for drug susceptibility testing (DST) for Mycobacterium tuberculosis. They provide good sensitivity and specificity, but are time-consuming. The objective of this study was to evaluate whether whole genome sequencing (WGS), combined with software tools for data analysis, can replace routine culture based assays for drug susceptibility testing of M. tuberculosis. METHODS: M. tuberculosis cultures sent to the Finnish mycobacterial reference laboratory in 2014 (n=211) were phenotypically tested by Mycobacteria Growth Indicator Tube (MGIT) for first line drug susceptibilities...
April 10, 2018: Clinical Microbiology and Infection
https://www.readbyqxmd.com/read/29653073/a-zebrafish-heart-failure-model-for-assessing-therapeutic-agents
#9
Xiao-Yu Zhu, Si-Qi Wu, Sheng-Ya Guo, Hua Yang, Bo Xia, Ping Li, Chun-Qi Li
Heart failure is a leading cause of death and the development of effective and safe therapeutic agents for heart failure has been proven challenging. In this study, taking advantage of larval zebrafish, we developed a zebrafish heart failure model for drug screening and efficacy assessment. Zebrafish at 2 dpf (days postfertilization) were treated with verapamil at a concentration of 200 μM for 30 min, which were determined as optimum conditions for model development. Tested drugs were administered into zebrafish either by direct soaking or circulation microinjection...
March 20, 2018: Zebrafish
https://www.readbyqxmd.com/read/29652911/pharmacogenetic-landscape-of-metabolic-syndrome-components-drug-response-in-tunisia-and-comparison-with-worldwide-populations
#10
Haifa Jmel, Lilia Romdhane, Yosra Ben Halima, Meriem Hechmi, Chokri Naouali, Hamza Dallali, Yosr Hamdi, Jingxuan Shan, Abdelmajid Abid, Henda Jamoussi, Sameh Trabelsi, Lotfi Chouchane, Donata Luiselli, Sonia Abdelhak, Rym Kefi
Genetic variation is an important determinant affecting either drug response or susceptibility to adverse drug reactions. Several studies have highlighted the importance of ethnicity in influencing drug response variability that should be considered during drug development. Our objective is to characterize the genetic variability of some pharmacogenes involved in the response to drugs used for the treatment of Metabolic Syndrome (MetS) in Tunisia and to compare our results to the worldwide populations. A set of 135 Tunisians was genotyped using the Affymetrix Chip 6...
2018: PloS One
https://www.readbyqxmd.com/read/29652682/kratom-an-emerging-drug-of-abuse-a-case-report-of-overdose-and-management-of-withdrawal
#11
Jack Diep, David Tian Chin, Somdatta Gupta, Faraz Syed, Ming Xiong, Jianguo Cheng
Kratom is an herb indigenous to Southeast Asia with psychoactive opioid compounds, often used as a treatment for chronic pain or opiate withdrawal symptoms. It is legally and readily available via Internet sales and has been identified as an emerging drug of abuse in the United States. Kratom use has been associated with psychosis, seizures, and even death. At lower doses, kratom acts as a stimulant, while at higher doses, it produces analgesia and euphoria. Here, we describe the successful management of kratom overdose and withdrawal in a young man with negative toxicology screens...
April 15, 2018: A&A practice
https://www.readbyqxmd.com/read/29652519/drug-induced-stevens-johnson-syndrome-and-toxic-epidermal-necrolysis-call-for-optimum-patient-stratification-and-theranostics-via-pharmacogenomics
#12
Chonlaphat Sukasem, Theodora Katsila, Therdpong Tempark, George P Patrinos, Wasun Chantratita
The Global Genomic Medicine Collaborative, a multinational coalition of genomic and policy experts working to implement genomics in clinical care, considers pharmacogenomics to be among the first areas in genomic medicine that can provide guidance in routine clinical practice, by linking genetic variation and drug response. Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN) are severe life-threatening reactions to medications with a high incidence worldwide. Genomic screening prior to drug administration is a key opportunity and potential paradigm for using genomic medicine to reduce morbidity and mortality and ultimately eliminate one of the most devastating adverse drug reactions...
April 13, 2018: Annual Review of Genomics and Human Genetics
https://www.readbyqxmd.com/read/29652493/reprogramming-probiotic-lactobacillus-reuteri-as-a-biosensor-for-staphylococcus-aureus-derived-aip-i-detection
#13
David Lubkowicz, Chun Loong Ho, In Young Hwang, Wen Shan Yew, Yung Seng Lee, Matthew Wook Chang
Gram-positive Staphylococcus aureus infection that results in pneumonia, urinary tract infection, and in severe cases, sepsis, has recently been classified as a serious threat to public health. Rapid and cost-effective detection of these infections are costly and time-consuming. Here, we present probiotic lactic acid bacteria engineered to detect autoinducer peptide-I (AIP-I), a quorum sensing molecule produced by Staphylococcus sp. during pathogenesis. We achieved this by adapting the well-characterized agr quorum sensing ( agrQS) from Staphylococcus aureus into Lactobacillus reuteri...
April 13, 2018: ACS Synthetic Biology
https://www.readbyqxmd.com/read/29652194/molecular-docking-revealed-the-binding-of-nucleotide-side-inhibitors-to-zika-viral-polymerase-solved-structures
#14
A A Elfiky, A M Ismail
A new Zika virus (ZIKV) outbreak started in 2015. According to the World Health Organization, 84 countries confirmed ZIKV infection. RNA-dependent RNA polymerase (RdRp) was an appealing target for drug designers during the last two decades. Through molecular docking, we screened 16 nucleotide/side inhibitors against ZIKV RdRp. While the mode of interaction with ZIKV is different from that in the hepatitis C virus (HCV), nucleotide/side inhibitors in this study (mostly anti-HCV) showed promising binding affinities (-6...
May 2018: SAR and QSAR in Environmental Research
https://www.readbyqxmd.com/read/29652143/reviewing-hit-discovery-literature-for-difficult-targets-glutathione-transferase-omega-1-as-an-example
#15
Yiyue Xie, Jayme L Dahlin, Aaron J Oakley, Marco G Casarotto, Philip G Board, Jonathan B Baell
Early-stage drug discovery reporting on relatively new or difficult targets is often associated with insufficient hit triage. Literature reviews of such targets seldom delve into the detail required to critically analyze the associated screening hits reported. Here we take the enzyme GSTO1-1 as an example of a relatively difficult target and review the associated literature involving small-molecule inhibitors. As part of this process we deliberately play closer-than-usual attention to assay interference and hit quality aspects...
April 13, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29651943/benzoin-schiff-bases-design-synthesis-and-biological-evaluation-as-potential-antitumor-agents
#16
Dima A Sabbah, Fatima Al-Tarawneh, Wamidh H Talib, Kamal Sweidan, Sanaa K Bardaweel, Eveen Al-Shalabi, Haizhen A Zhong, Ghassan Abu Sheikha, Reema Abu Khalaf, Mohammad S Mubarak
BACKGROUND: Phosphoinositide 3-kinase α (PI3Kα) is an attractive target for anticancer drug design. OBJECTIVES: Target compounds were designed to probe the significance of alcohol and imine moieties tailored on a benzoin scaffold to better understand the structure activity relation (SAR) and improve their biological activity as anticancer compounds. METHODS: Chemical synthesis of the targeted compounds, biological evaluation tests against human colon adenocarcinoma (HCT-116), breast adenocarcinoma (MCF-7), and breast carcinoma (T47D) cell lines, as well as Glide docking studies were employed in this investigation...
April 12, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29651937/an-emerging-role-of-endometrial-inflammasome-in-reproduction-new-therapeutic-approaches
#17
Fiorella Di Nicuolo, Monia Specchia, Lorenza Trentavizi, Giovanni Scambia, Nicoletta Di Simone
One of the common complications of pregnancy is spontaneous pregnancy loss which occurs in an estimated 5- 15% of pregnancies. Of all women 1%-5% suffer from recurrent pregnancy loss (RPL). Despite the fact that RPL has been associated to various anatomic, hormonal, immune, hematologic, and genetic defects, in 30% of the patients, screening tests included in the RPL workup may have negative results. Recently, we demonstrated a significant increased activation of endometrial NALP-3 inflammasome, and a caspase-1 dependent secretion of IL-18 and IL-1β in the endometrial tissues obtained from RPL women compared with a fertile women group...
April 12, 2018: Protein and Peptide Letters
https://www.readbyqxmd.com/read/29651932/alternative-host-models-for-testing-anti-protozoal-or-antifungal-compounds-and-fungal-infection
#18
Ana Claudia Torrecilhas, Patricia Xander, Karen Spadari Ferreira, Wagner Luiz Batista
The neglected tropical diseases (NTDs) are caused by several parasites, fungi, bacteria and viruses and affect more than one billion people in the world. The control and prevention against NTDs need implementation of alternative methods for testing new compounds against these diseases. For the implementation of alternative methods, it is necessary to apply the principles of replacement, reduction and refinement (the 3Rs) for the use of laboratory animals. Accordingly, the present review addressed a variety of alternative models to study the infections caused by protozoa and fungi...
April 12, 2018: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/29651850/exploring-the-potential-of-a-global-emerging-contaminant-early-warning-network-through-the-use-of-retrospective-suspect-screening-with-high-resolution-mass-spectrometry
#19
Nikiforos A Alygizakis, Saer Samanipour, Juliane Hollender, María Ibáñez, Sarit Kaserzon, Varvara Kokkali, Jan A van Leerdam, Jochen F Mueller, Martijn Pijnappels, Malcolm J Reid, Emma L Schymanski, Jaroslav Slobodnik, Nikolaos S Thomaidis, Kevin V Thomas
A key challenge in the environmental and exposure sciences is to establish experimental evidence of the role of chemical exposure in human and environmental systems. High resolution and accurate tandem mass spectrometry (HRMS) is increasingly being used for the analysis of environmental samples. One lauded benefit of HRMS is the possibility to retrospectively process data for (previously omitted) compounds that has led to the archiving of HRMS data. Archived HRMS data affords the possibility of exploiting historical data to rapidly and effectively establish the temporal and spatial occurrence of newly identified contaminants through retrospective suspect screening...
April 13, 2018: Environmental Science & Technology
https://www.readbyqxmd.com/read/29651790/novel-insights-for-inhibiting-mutant-heterodimer-idh1-wt-r132h-in-cancer-an-in-silico-approach
#20
Ezequiel Iván Juritz, Juan Pablo Bascur, Daniel Eduardo Almonacid, Fernando Danilo González-Nilo
BACKGROUND: Isocitrate dehydrogenase 1 (IDH1) is a dimeric enzyme responsible for supplying the cell's nicotinamide adenine dinucleotide phosphate (NADPH) reserves via dehydrogenation of isocitrate (ICT) and reduction of NADP+. Mutations in position R132 trigger cancer by enabling IDH1 to produce D-2-hydroxyglutarate (2-HG) and reduce inhibition by ICT. Mutant IDH1 can be found as a homodimer or a heterodimer. OBJECTIVE: We propose a novel strategy to inhibit IDH1 R132 variants as a means not to decrease the concentration of 2-HG but to provoke a cytotoxic effect, as the cell malignancy at this point no longer depends on 2-HG...
April 12, 2018: Molecular Diagnosis & Therapy
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