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https://www.readbyqxmd.com/read/30515635/synthesis-sar-and-in-vitro-therapeutic-potentials-of-thiazolidine-2-4-diones
#1
Sucheta, Sumit Tahlan, Prabhakar Kumar Verma
BACKGROUND: Thiazolidinedione is a pentacyclic moiety having five membered unsaturated ring system composed with carbon, oxygen, nitrogen and sulfur molecules at 1 and 3 position of the thiazole ring and widely found throughout nature in various form. They favourably alter concentration of the hormones secreted by adipocytes, particularly adiponectin. They also increase total body fat and have mixed effects on circulating lipids. Thiazolidinedione nucleus is present in numerous biological moieties and has different pharmacological activities likes, e...
December 4, 2018: Chemistry Central Journal
https://www.readbyqxmd.com/read/30514402/preclinical-pharmacokinetic-evaluation-to-facilitate-repurposing-of-tyrosine-kinase-inhibitors-nilotinib-and-imatinib-as-antiviral-agents
#2
Hari Krishna Ananthula, Scott Parker, Erin Touchette, R Mark Buller, Gopi Patel, Daniel Kalman, Johanna S Salzer, Nadia Gallardo-Romero, Victoria Olson, Inger K Damon, Tessa Moir-Savitz, Larry Sallans, Milton H Werner, Catherine M Sherwin, Pankaj B Desai
BACKGROUND: Several tyrosine kinase inhibitors (TKIs) developed as anti-cancer drugs, also have anti-viral activity due to their ability to disrupt productive replication and dissemination in infected cells. Consequently, such drugs are attractive candidates for "repurposing" as anti-viral agents. However, clinical evaluation of therapeutics against infectious agents associated with high mortality, but low or infrequent incidence, is often unfeasible. The United States Food and Drug Administration formulated the "Animal Rule" to facilitate use of validated animal models for conducting anti-viral efficacy studies...
December 4, 2018: BMC Pharmacology & Toxicology
https://www.readbyqxmd.com/read/30513856/improving-encapsulation-of-hydrophilic-chloroquine-diphosphate-into-biodegradable-nanoparticles-a-promising-approach-against-herpes-virus-simplex-1-infection
#3
Tábata Loíse Cunha Lima, Renata de Carvalho Feitosa, Emanuell Dos Santos-Silva, Alaine Maria Dos Santos-Silva, Emerson Michell da Silva Siqueira, Paula Renata Lima Machado, Alianda Maira Cornélio, Eryvaldo Sócrates Tabosa do Egito, Matheus de Freitas Fernandes-Pedrosa, Kleber Juvenal Silva Farias, Arnóbio Antônio da Silva-Júnior
Chloroquine diphosphate (CQ) is a hydrophilic drug with low entrapment efficiency in hydrophobic nanoparticles (NP). Herpes simplex virus type 1 (HSV-1) is an enveloped double-stranded DNA virus worldwide known as a common human pathogen. This study aims to develop chloroquine-loaded poly(lactic acid) (PLA) nanoparticles (CQ-NP) to improve the chloroquine anti- HSV-1 efficacy. CQ-NP were successfully prepared using a modified emulsification-solvent evaporation method. Physicochemical properties of the NP were monitored using dynamic light scattering, atomic force microscopy, drug loading efficiency, and drug release studies...
December 3, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/30513570/implications-of-hiv-1-nef-for-shock-and-kill-strategies-to-eliminate-latent-viral-reservoirs
#4
REVIEW
Xiaomei T Kuang, Mark A Brockman
Finding a cure for HIV is challenging because the virus is able to integrate itself into the host cell genome and establish a silent state, called latency, allowing it to evade antiviral drugs and the immune system. Various "shock and kill" strategies are being explored in attempts to eliminate latent HIV reservoirs. The goal of these approaches is to reactivate latent viruses ("shock"), thereby exposing them to clearance by viral cytopathic effects or immune-mediated responses ("kill")...
November 30, 2018: Viruses
https://www.readbyqxmd.com/read/30511358/quercetin-and-3-o-methylquercetin-in-vitro-skin-layers-permeation-retention-from-hydrogels-why-only-a-methoxy-group-difference-determines-different-behaviors
#5
Liege C Schwingel, Sara E Bianchi, Giovanni K Zorzi, Paulo Gonçalves, Helder F Teixeira, Valquiria L Bassani
OBJECTIVES: The present study was designed to verify if quercetin (QCT), a flavonoid with antioxidant and antiviral activity, and 3-O-methylquercetin (3OMQ), a quercetin C3-methoxylated derivative, present differences in their behavior against complexation with β-cyclodextrin (β-CD) and the corresponding permeation/retention trhough porcine ear skin, when incorporated into hydroxypropyl methylcellulose (HPMC) or chitosan (CS) hydrogels. METHODS: The influence of β-CD on the skin permeation/retention of QCT and 3OMQ from hydrogels is comparatively evaluated for both flavonoids using porcine ear skin in Franz cells model...
December 3, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/30508602/evaluation-of-imidazole-and-its-derivative-against-newcastle-disease-virus-infection-in-chicken-a-drug-repurposing-approach
#6
Moushumee Das, Sangeeta Baro, Sachin Kumar
Despite recent progress in vaccination options, Newcastle disease virus (NDV) stands a severe global epidemic and economic burden. It is difficult to control NDV with vaccination alone due to its evolving genetic variability; therefore, an effective therapeutic must target to resist its replication and further evolution. Drug repurposing is a practical and economical method to develop therapeutics against pathogenic organisms. Applying the knowledge of the broadly used antimicrobial activity of imidazole and its derivatives, we performed repurposing-based design of therapeutics to induce protection against NDV...
November 30, 2018: Virus Research
https://www.readbyqxmd.com/read/30505886/detection-and-differentiation-of-multiple-viral-rnas-using-branched-dna-fish-coupled-to-confocal-microscopy-and-flow-cytometry
#7
Nicholas van Buuren, Karla Kirkegaard
Due to the exceptionally high mutation rates of RNA-dependent RNA polymerases, infectious RNA viruses generate extensive sequence diversity, leading to some of the lowest barriers to the development of antiviral drug resistance in the microbial world. We have previously discovered that higher barriers to the development of drug resistance can be achieved through dominant suppression of drug-resistant viruses by their drug-susceptible parents. We have explored the existence of dominant drug targets in poliovirus, dengue virus and hepatitis C virus (HCV)...
October 20, 2018: Bio-protocol
https://www.readbyqxmd.com/read/30505191/identification-of-bioactive-phytochemical-from-two-punica-species-using-gc-ms-and-estimation-of-antioxidant-activity-of-seed-extracts
#8
Asma A Al-Huqail, Gehan A Elgaaly, Mohamed M Ibrahim
Punica species are medicinally important plants belonging to the family Lythraceae. The pomegranate is widely reported to exhibit antiviral, antioxidant, anticancer, anti-proliferative activities. In the present study the ethanolic extract of the peel seeds of two species of Punica ( Punica granatum and Punica protopunica ) were subjected to GC-MS analysis. Twenty-one and 14 compounds were identified in P. granatum and P. protopunica peel seeds, respectively. The main chemical constituents in P. granatum- peel seeds were propanoic acid, benzenedicarboxylic acid, methoxypropionic acid and methyl amine...
November 2018: Saudi Journal of Biological Sciences
https://www.readbyqxmd.com/read/30502490/future-management-of-viral-diseases-role-of-new-technologies-and-new-approaches-in-microbial-interactions
#9
REVIEW
Fabrizio Maggi, Mauro Pistello, Guido Antonelli
BACKGROUND: New technologies allow rapid detection and counting of viral genomes in clinical specimens, definition of susceptibility to specific antivirals, pinpointing molecular sequences correlated to virulence traits, and identifying viral and host factors driving resolution or chronicity of infections. As a result, during the past three decades, the diagnostic virology laboratory has become pivotal for patient care and integral component of the multifarious armamentarium for patient management...
November 28, 2018: Clinical Microbiology and Infection
https://www.readbyqxmd.com/read/30501598/identification-of-novel-small-molecule-inhibitors-against-the-ns3-4a-protease-of-hepatitis-c-virus-genotype-4a
#10
Sara M El-Sayed, Mohamed A M Ali, Bahaa El-Dien M El-Gendy, Samar S Dandash, Yvette Issac, Reda Saad, Mohamed M Azab, Mohamed R Mohamed
Background Hepatitis C virus (HCV) infection poses a considerable threat to the public health. The current standard of care treatment with pegylated interferon-alpha in combination with ribavirin (PEG-IFN-α+RBV) is associated with significant side effects, poorly tolerated, and provides limited efficacy. The development of direct-acting antiviral agents (DAAs) targeting key viral enzymes essential for viral replication represents a significant milestone in the treatment of chronic HCV infection. Given its critical role in the viral polyprotein processing and the evasion of the host innate immunity, the NS3/4A protease has emerged as a promising drug target for the development of anti-HCV therapies...
December 3, 2018: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/30496872/repurposing-approach-identifies-new-treatment-options-for-invasive-fungal-disease
#11
Isis Regina Grenier Capoci, Daniella Renata Faria, Karina Mayumi Sakita, Franciele Abigail Vilugron Rodrigues-Vendramini, Patricia de Souza Bonfim-Mendonça, Tania Cristina Alexandrino Becker, Érika Seki Kioshima, Terezinha Inez Estivalet Svidzinski, Bernard Maigret
Drug repositioning is the process of discovery, validation and marketing of previously approved drugs for new indications. Our aim was drug repositioning, using ligand-based and structure-based computational methods, of compounds that are similar to two hit compounds previously selected by our group that show promising antifungal activity. Through the ligand-based method, 100 compounds from each of three databases (MDDR, DrugBank and TargetMol) were selected by the Tanimoto coefficient, as similar to LMM5 or LMM11...
November 19, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/30488694/chromatographic-data-segmentation-method-a-hybrid-analytical-approach-for-investigation-of-antiviral-substances-in-medicinal-plant-extracts
#12
Tomas Drevinskas, Audrius Maruska, Laimutis Telksnys, Stellan Hjerten, Manatas Stankevičius, Raimundas Lelešius, Rūta Mickienė, Agneta Karpovaite, Algirdas Salomskas, Nicola Tiso, Ona Ragazinskiene
The methodology described in this paper will significantly reduce the time required for understanding the relations between chromatographic data and bio-activity assays. The methodology is a hybrid of hypothesis based and data-driven scientific approaches. In this work, a novel chromatographic data segmentation method is proposed, which demonstrates the capability of finding what volatile substances are responsible for antiviral and cytotoxic effects in the medicinal plant extracts. Up to now the full potential of the separation methods has not been exploited in the life sciences...
November 29, 2018: Analytical Chemistry
https://www.readbyqxmd.com/read/30487288/sirtuin-2-mediated-deacetylation-of-cyclin-dependent-kinase-9-promotes-stat1-signaling-in-type-i-interferon-responses
#13
Ewa M Kosciuczuk, Swarna Mehrotra, Diana Saleiro, Barbara Kroczynska, Beata Majchrzak-Kita, Pawel Lisowski, Caroline Driehaus, Anna Rogalska, Acara Turner, Thomas Lienhoop, David Gius, Eleanor N Fish, Athanassios Vassilopoulos, Leonidas C Platanias
Type I interferons (IFNs) induce expression of multiple genes that control innate immune responses to invoke both antiviral and antineoplastic activities. Transcription of these interferon-stimulated genes (ISGs) occurs upon activation of the canonical Janus kinase (JAK)-signal transducer and activator of transcription (STAT) signaling pathways. Phosphorylation and acetylation are both events crucial to tightly regulate expression of ISGs. Here, using mouse embryonic fibroblasts and an array of biochemical methods including immunoblotting and kinase assays, we show that sirtuin 2 (SIRT2), a member of the NAD-dependent protein deacetylase family, is involved in type I IFN signaling...
November 28, 2018: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/30483751/-%C3%A2-pinoresinol%C3%A2-o%C3%A2-%C3%AE-%C3%A2-d%C3%A2-glucopyranoside-from-eucommia-ulmoides-oliver-and-its-anti%C3%A2-inflammatory-and-antiviral-effects-against-influenza-a-h1n1-virus-infection
#14
Jing Li, Xiaoli Liang, Beixian Zhou, Xiaowei Chen, Peifang Xie, Haiming Jiang, Zhihong Jiang, Zifeng Yang, Xiping Pan
Eucommia ulmoides Oliver (Du-Zhong) is an ancient Chinese herbal remedy used for the treatment of various diseases. To date, the effects of its constituent lignans on influenza viruses remain to be elucidated. In the present study, a lignan glycoside was isolated and purified from Eucommia ulmoides Oliver. Its structures were identified via extensive spectroscopic analysis, and its antiviral and anti‑inflammatory activities, specifically against influenza viruses, were determined via a cytopathic effect (CPE) assay, plaque‑reduction assays, a progeny virus yield reduction assay, reverse transcription‑quantitative polymerase chain reaction analysis and a Luminex assay...
November 26, 2018: Molecular Medicine Reports
https://www.readbyqxmd.com/read/30481858/-establish-a-predictive-modeling-under-antiviral-therapy-for-hepatitis-b-e-antigen-seroconversion-in-chronic-hepatitis-b
#15
G W Liu, K C Tang, Q Li, W Lu
Objective: To explore the predictive factors by demonstrating a predictive modeling under antiviral therapy for hepatitis B e antigen seroconversion in HBeAg-positive chronic hepatitis B patients. Methods: 198 cases with HBeAg-positive chronic hepatitis B were enrolled. Fatty liver, family history of hepatitis B, age, sex, drinking history, HBsAg, HBeAg, HBV-DNA levels, total bilirubin (TBil), CD4/CD8, albumin (ALB), alanine amino transferase (ALT) levels were used as a predictor variables of HBeAg seroconversion...
September 20, 2018: Zhonghua Gan Zang Bing za Zhi, Zhonghua Ganzangbing Zazhi, Chinese Journal of Hepatology
https://www.readbyqxmd.com/read/30478256/structures-of-coxsackievirus-a10-unveil-the-molecular-mechanisms-of-receptor-binding-and-viral-uncoating
#16
Ling Zhu, Yao Sun, Jinyan Fan, Bin Zhu, Lei Cao, Qiang Gao, Yanjun Zhang, Hongrong Liu, Zihe Rao, Xiangxi Wang
Coxsackievirus A10 (CVA10), a human type-A Enterovirus (HEV-A), can cause diseases ranging from hand-foot-and-mouth disease to polio-myelitis-like disease. CVA10, together with some other HEV-As, utilizing the molecule KREMEN1 as an entry receptor, constitutes a KREMEN1-dependent subgroup within HEV-As. Currently, there is no vaccine or antiviral therapy available for treating diseases caused by CVA10. The atomic-resolution structure of the CVA10 virion, which is within the KREMEN1-dependent subgroup, shows significant conformational differences in the putative receptor binding sites and serotype-specific epitopes, when compared to the SCARB2-dependent subgroup of HEV-A, such as EV71, highlighting specific differences between the sub-groups...
November 26, 2018: Nature Communications
https://www.readbyqxmd.com/read/30477957/the-evaluation-of-an-immunoperoxidase-assay-applicable-in-antiviral-drug-screening
#17
Liqian Zhu, Liai Huang, Aiping Wang, Qingmei Li, Junqing Guo, Li Wang, Gaiping Zhang
Bovine viral diarrhea virus (BVDV) fall into cytopathic (CP) and noncytopathic (NCP) biotypes, based on their ability to kill cultured cells. NCP-BVDV can not be titrated by conventional means as used for CP-BVDV, which has impeded the identification of antiviral drugs targeting NCP-BVDV virus strains. In this study, the application of an immunoperoxidase assay in the screening of antiviral drugs was tested using two known BVDV inhibitors, ribavirin and ammonium chloride (NH4Cl). Phospholipase C inhibitor U73122 was identified to affect BVDV infection by using this immunoperoxidase assay...
November 23, 2018: Biologicals: Journal of the International Association of Biological Standardization
https://www.readbyqxmd.com/read/30472042/long-term-histological-change-in-chronic-hepatitis-c-patients-who-had-received-peginterferon-plus-ribavirin-therapy-with-sustained-virological-response
#18
Chia-Ying Chu, Chun-Han Cheng, Huan-Lin Chen, I-Tsung Lin, Chia-Hsien Wu, Yuan-Kai Lee, Ming-Jong Bair
BACKGROUND: The improvement in liver histology is an important aim in the management of hepatitis C virus (HCV) infection. Previous studies suggest that antiviral treatment could reduce the progression of hepatic fibrosis, especially in patients with sustained virological response (SVR). However, most studies were limited by short-term evaluations and the liver stiffness was assessed by non-invasive methods. In our study, we performed a paired liver biopsy study aimed at analyzing the long-term histological changes in patients with SVR...
November 21, 2018: Journal of the Formosan Medical Association, Taiwan Yi Zhi
https://www.readbyqxmd.com/read/30471396/effect-of-different-non-conventional-extraction-methods-on-the-antibacterial-and-antiviral-activity-of-fucoidans-extracted-from-nizamuddinia-zanardinii
#19
Mehdi Alboofetileh, Masoud Rezaei, Mehdi Tabarsa, Massimo Rittà, Manuela Donalisio, Francesco Mariatti, SangGuan You, David Lembo, Giancarlo Cravotto
In the current study, fucoidans from brown alga Nizamuddinia zanardinii were isolated with conventional and non-conventional extraction procedures to evaluate the effects of recently introduced technologies on biochemical characteristics and saccharide composition of the extracts, along with their antibacterial, antiviral and cytotoxic properties. The results demonstrated that subcritical water extraction showed the highest fucoidans yield (13.15%), while the lowest yield was obtained using viscozyme extraction method (4...
November 21, 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/30471070/new-techniques-to-study-intracellular-receptors-in-living-cells-insights-into-rig-i-like-receptor-signaling
#20
M J Corby, Valerica Raicu, David N Frick
This review discusses new developments in Förster resonance energy transfer (FRET) microscopy and its application to cellular receptors. The method is based on the kinetic theory of FRET, which can be used to predict FRET not only in dimers, but also higher order oligomers of donor and acceptor fluorophores. Models based on such FRET predictions can be fit to observed FRET efficiency histograms (also called FRET spectrograms) and used to estimate intracellular binding constants, free energy values, and stoichiometries...
November 24, 2018: Advances in Experimental Medicine and Biology
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