keyword
MENU ▼
Read by QxMD icon Read
search

Mode of action

keyword
https://www.readbyqxmd.com/read/28637198/multi-target-activity-of-hemidesmus-indicus-decoction-against-innovative-hiv-1-drug-targets-and-characterization-of-lupeol-mode-of-action
#1
Francesca Esposito, Manuela Mandrone, Claudia Del Vecchio, Ilaria Carli, Simona Distinto, Angela Corona, Mariacaterina Lianza, Dario Piano, Massimo Tacchini, Elias Maccioni, Filippo Cottiglia, Elisa Saccon, Ferruccio Poli, Cristina Parolin, Enzo Tramontano
Despite the availability of several anti-retrovirals there is still an urgent need for developing novel therapeutic strategies and finding new drugs against underexplored HIV-1 targets. Among them, there are the HIV-1 Reverse Transcriptase (RT)-associated Ribonuclease H (RNase H) function and the cellular α-glucosidase, involved in the control mechanisms of N-linked glycoproteins formation in the endoplasmic reticulum. It is known that many natural compounds, such as pentacyclic triterpenes, are a promising class of HIV-1 inhibitors...
June 20, 2017: Pathogens and Disease
https://www.readbyqxmd.com/read/28637123/inhibition-of-swarming-motility-of-pseudomonas-aeruginosa-by-methanol-extracts-of-alpinia-officinarum-hance-and-cinnamomum-tamala-t-nees-and-eberm
#2
Divya Lakshmanan, Jishudas Nanda, K Jeevaratnam
Bacterial drug resistance is a challenge in clinical settings, especially in countries like India. Hence, discovery of novel alternative therapeutics has become a necessity in the fight against drug resistance. Compounds that inhibit bacterial virulence properties form new therapeutic alternatives. Pseudomonas aeruginosa is an opportunistic, nosocomial pathogen that infects immune-compromised patients. Swarming motility is an important virulence property of Pseudomonas which aids it in reaching host cells under nutrient limiting conditions...
June 15, 2017: Natural Product Research
https://www.readbyqxmd.com/read/28636348/the-development-of-an-aryloxazole-class-of-hepatitis-c-virus-inhibitors-targeting-the-entry-stage-of-the-viral-replication-cycle
#3
Shanshan He, Kelin Li, Billy Lin, Zonyi Hu, Jingbo Xiao, Xin Hu, Amy Q Wang, Xin Xu, Marc Ferrer, Noel Southall, Wei Zheng, Jeffrey Aubé, Frank J Schoenen, Juan J Marugan, T Jake Liang, Kevin J Frankowski
Reliance on hepatitis C virus (HCV) replicon systems and protein-based screening assays has led to treatments that target HCV viral replication proteins. The model does not encompass other viral replication cycle steps, such as entry, processing, assembly and secretion, or viral host factors. We previously applied a phenotypic high-throughput screening platform based on an infectious HCV system and discovered an aryloxazole-based anti-HCV hit. Structure-activity relationship studies revealed several compounds exhibiting EC50 values below 100 nM...
June 21, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28636319/green-catanionic-gemini-surfactant-lichenysin-mixture-improved-surface-antimicrobial-and-physiological-properties
#4
Albert Ruiz, Aurora Pinazo, Lourdes Pérez, Angeles Manresa, Ana M M Marqués
Catanionic surfactant mixtures form a wide variety of organized assemblies and aggregates with improved physicochemical and biological properties. The green catanionic mixture C3(CA)2:lichenysin (molar ratio 8:2) showed antimicrobial synergies against Yersinia enterocolitica, Bacillus subtilis, Escherichia coli O157:H7 and Candida albicans. Flow cytometry and viability studies indicated that this catanionic mixture increases the probability of Y. enterocolitica (38.2%) and B. subtilis (17.1%) cells entering a viable but nonculturable state...
June 21, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28636236/assessment-of-silibinin-as-a-potential-antifungal-agent-and-investigation-of-its-mechanism-of-action
#5
Dae Gyu Yun, Dong Gun Lee
Silibinin, which is derived from Silybum marianum (milk thistle), has used as a traditional remedy for liver or biliary disorders and known to have superior antioxidant activity. In addition, silibinin was recently reported to have antifungal effect related to fungal apoptosis against Candida albicans and the interest in the therapeutic effect is increasing. In this study, we found another mode of antifungal action of silibinin and its antibiofilm activity on C. albicans. To investigate influence on fungal plasma membrane, propidium iodide and bis-(1, 3-dibutylbarbituric acid) trimethineoxonol [DiBAC4 (3)] assay were primarily carried out...
June 21, 2017: IUBMB Life
https://www.readbyqxmd.com/read/28636110/cumulative-toxicity-of-neonicotinoid-insecticide-mixtures-to-chironomus-dilutus-under-acute-exposure-scenarios
#6
Erin M Maloney, Christy A Morrissey, John V Headley, Kerry M Peru, Karsten Liber
Extensive agricultural use of neonicotinoid insecticide products has resulted in the presence of neonicotinoid mixtures in surface waters worldwide. Although many aquatic insect species are known to be sensitive to neonicotinoids, the impact of neonicotinoid mixtures is poorly understood. In the present study, the cumulative toxicity of binary and ternary mixtures of select neonicotinoids (imidacloprid, clothianidin, and thiamethoxam) was characterized under acute (96-h) exposure scenarios using the larval midge Chironomus dilutus as a representative aquatic insect species...
June 21, 2017: Environmental Toxicology and Chemistry
https://www.readbyqxmd.com/read/28635645/cembrene-diterpenoids-with-ether-linkages-from-sarcophyton-ehrenbergi-an-anti-proliferation-and-molecular-docking-assessment
#7
Mohamed-Elamir F Hegazy, Abdelsamed I Elshamy, Tarik A Mohamed, Ahmed R Hamed, Mahmoud A A Ibrahim, Shinji Ohta, Paul W Paré
Three new cembrene diterpenoids, sarcoehrenbergilid A-C (1-3), along with four known diterpenoids, sarcophine (4), (+)-7α,8β-dihydroxydeepoxysarcophine (5), sinulolide A (6), and sinulolide B (7), and one steroid, sardisterol (8), were isolated and characterized from a solvent extract of the Red Sea soft coral Sarcophyton ehrenbergi. Chemical structures were elucidated by NMR and MS analyses with absolute stereochemistry determined by X-ray analysis. Since these isolated cembrene diterpenes contained 10 or more carbons in a large flexible ring, conformer stabilities were examined based on density functional theory calculations...
June 21, 2017: Marine Drugs
https://www.readbyqxmd.com/read/28635081/understanding-and-improving-photo-control-of-ion-channels-in-nociceptors-with-azobenzene-photoswitches
#8
Alexandre Mourot, Christian Herold, Michael A Kienzler, Richard H Kramer
BACKGROUND AND PURPOSE: We previously developed a photoisomerizable local anaesthetic, named QAQ, to gain rapid, optical control over pain signaling without involving genetic modification. In darkness or in green light, trans-QAQ blocks voltage-gated K(+) and Na(+) channels and silences action potentials in pain-sensing neurons. Upon photoisomerization to cis with near UV light, QAQ blockade is rapidly relieved and neuronal activity is restored. However, the molecular mechanism of cis and trans QAQ blockade is not known...
June 20, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28634804/biocontrol-of-the-wheat-pathogen-zymoseptoria-tritici-using-cyclic-lipopeptides-from-bacillus-subtilis
#9
Samara Mejri, Ali Siah, François Coutte, Maryline Magnin-Robert, Béatrice Randoux, Benoit Tisserant, François Krier, Philippe Jacques, Philippe Reignault, Patrice Halama
Innovation toward ecofriendly plant protection products compatible with sustainable agriculture and healthy food is today strongly encouraged. Here, we assessed the biocontrol activity of three cyclic lipopeptides from Bacillus subtilis (mycosubtilin, M; surfactin, S; fengycin, F) and two mixtures (M + S and M + S + F) on wheat against Zymoseptoria tritici, the main pathogen on this crop. Foliar application of these biomolecules at a 100-mg L(-1) concentration on the wheat cultivars Dinosor and Alixan, 2 days before fungal inoculation, provided significant reductions of disease severity...
June 21, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/28634478/transcriptional-and-antagonistic-responses-of-biocontrol-strain-lysobacter-enzymogenes-oh11-to-the-plant-pathogenic-oomycete-pythium-aphanidermatum
#10
Yangyang Zhao, Guoliang Qian, Yuan Chen, Liangcheng Du, Fengquan Liu
Lysobacter enzymogenes is a ubiquitous, beneficial, plant-associated bacterium emerging as a novel biological control agent. It has the potential to become a new source of antimicrobial secondary metabolites such as the Heat-Stable Antifungal Factor (HSAF), which is a broad-spectrum antimycotic with a novel mode of action. However, very little information about how L. enzymogenes detects and responds to fungi or oomycetes has been reported. An in vitro confrontation bioassay between the pathogenic oomycete Pythium aphanidermatum and the biocontrol bacterial strain L...
2017: Frontiers in Microbiology
https://www.readbyqxmd.com/read/28634477/metabolomic-analysis-and-mode-of-action-of-metabolites-of-tea-tree-oil-involved-in-the-suppression-of-botrytis-cinerea
#11
Jiayu Xu, Xingfeng Shao, Yonghua Li, Yingying Wei, Feng Xu, Hongfei Wang
Tea tree oil (TTO), a volatile essential oil, has been widely used as an antimicrobial agent. However, the mechanism underlying TTO antifungal activity is not fully understood. In this study, a comprehensive metabolomics survey was undertaken to identify changes in metabolite production in Botrytis cinerea cells treated with TTO. Significant differences in 91 metabolites were observed, including 8 upregulated and 83 downregulated metabolites in TTO-treated cells. The results indicate that TTO inhibits primary metabolic pathways through the suppression of the tricarboxylic acid (TCA) cycle and fatty acid metabolism...
2017: Frontiers in Microbiology
https://www.readbyqxmd.com/read/28633390/investigating-microrna-mediated-regulation-of-the-nascent-nuclear-transcripts-in-plants-a-bioinformatics-workflow
#12
Dongliang Yu, Zhonghai Tang, Chaogang Shao, Xiaoxia Ma, Taihe Xiang, Zhihong Fan, Huizhong Wang, Yijun Meng
Most of the microRNAs (miRNAs) play their regulatory roles through posttranscriptional target decay or translational inhibition. For both plants and animals, these regulatory events were previously considered to take place in cytoplasm, as mature miRNAs were observed to be exported to the cytoplasm for Argonaute (AGO) loading and subsequent target binding. Recently, this notion was challenged by increasing pieces of evidence in the animal cells that uncovered the nuclear importation and action of the AGO-associated miRNAs...
June 14, 2017: Briefings in Bioinformatics
https://www.readbyqxmd.com/read/28632782/microbial-inhibitors-of-the-fungus-pseudogymnoascus-destructans-the-causal-agent-of-white-nose-syndrome-in-bats
#13
Emma W Micalizzi, Jonathan N Mack, George P White, Tyler J Avis, Myron L Smith
Pseudogymnoascus destructans, the fungus that causes white-nose syndrome in hibernating bats, has spread across eastern North America over the past decade and decimated bat populations. The saprotrophic growth of P. destructans may help to perpetuate the white-nose syndrome epidemic, and recent model predictions suggest that sufficiently reducing the environmental growth of P. destructans could help mitigate or prevent white-nose syndrome-associated bat colony collapse. In this study, we screened 301 microbes from diverse environmental samples for their ability to inhibit the growth of P...
2017: PloS One
https://www.readbyqxmd.com/read/28632039/thiocyanate-a-review-and-evaluation-of-the-kinetics-and-the-modes-of-action-for-thyroid-hormone-perturbations
#14
Marie-Emilie Willemin, Annie Lumen
Exposure of the population to thiocyanate is predominantly through the diet and cigarette smoke. Thiocyanate is a potential thyroid disruptor due to its capacity to inhibit the uptake of iodide by the thyroid. Thiocyanate also interacts with the enzymatic reactions associated with iodide organification and thyroid hormone synthesis. Quantification of the dose-response relationships of thiocyanate and alteration in thyroid hormone levels is important for evaluating the risk of exposure to thiocyanate in humans...
March 6, 2017: Critical Reviews in Toxicology
https://www.readbyqxmd.com/read/28629724/in-vitro-antiviral-effects-of-peganum-harmala-seed-extract-and-its-total-alkaloids-against-influenza-virus
#15
Mohammad-Taghi Moradi, Ali Karimi, Mahmoud Rafieian-Kopaei, Fatemeh Fotouhi
This research was aimed to evaluate the in vitro antiviral effect and the mechanism of the effect of Peganum. harmala seeds extract against influenza A virus infection using Madin-Darby canine kidney (MDCK) cells. In this research, ethyl alcohol extract of P. harmala seeds and its total alkaloids was prepared. The potential antiviral activity of the extract and its total alkaloids against influenza A/Puerto Rico/8/34 (H1N1; PR8) virus was assessed. The mode of action of the extract to inhibit influenza replication was investigated using virucidal activity, hemagglutination inhibition assay, time of addition assays, RNA replication, western blot analysis and RNA polymerase blocking assay...
June 16, 2017: Microbial Pathogenesis
https://www.readbyqxmd.com/read/28629516/context-dependent-skeletal-effects-of-erythropoietin
#16
Sahar Hiram-Bab, Drorit Neumann, Yankel Gabet
Erythropoietin (Epo) is the main hormone that regulates the production of red blood cells (hematopoiesis), by stimulating their progenitors. Beyond this vital function, several emerging roles have been noted for Epo in other tissues, including neurons, heart, and retina. The skeletal system is also affected by Epo; however, its actions on bone are, as yet, controversial. Here, we review the seemingly contradicting evidence regarding Epo effects on bone remodeling. We also discuss the evidence pointing to a direct vs indirect effect of Epo on the osteoblastic and osteoclastic cell lineages...
2017: Vitamins and Hormones
https://www.readbyqxmd.com/read/28629201/systemic-induction-of-the-defensin-and-phytoalexin-pisatin-pathways-in-pea-pisum-sativum-against-aphanomyces-euteiches-by-acetylated-and-nonacetylated-oligogalacturonides
#17
Sameh Selim, Jean Sanssené, Stéphanie Rossard, Josiane Courtois
Oligogalacturonides (OGs) are known for their powerful ability to stimulate the plant immune system but little is known about their mode of action in pea (Pisum sativum). In the present study, we investigated the elicitor activity of two fractions of OGs, with polymerization degrees (DPs) of 2-25, in pea against Aphanomyces euteiches. One fraction was nonacetylated (OGs - Ac) whereas the second one was 30% acetylated (OGs + Ac). OGs were applied by injecting the upper two rachises of the plants at three- and/or four-weeks-old...
June 19, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28628823/drug-development-against-tuberculosis-impact-of-alkaloids
#18
REVIEW
Shardendu K Mishra, Garima Tripathi, Navneet Kishore, Rakesh K Singh, Archana Singh, Vinod K Tiwari
Despite of the advances made in the treatment and management, tuberculosis (TB) still remains one of main public health problem. The contrary effects of first and second-line anti-tuberculosis drugs have generated extended research interest in natural products in the hope of devising new antitubercular leads. Interestingly, plethoras of natural products have been discovered to exhibit activity towards various resistant strains of M. tuberculosis. Extensive applications of alkaloids in the field of therapeutics is well-established and nowday's researches being pursued to develop new potent drugs from natural sources for tuberculosis...
June 3, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28628229/troxerutin-with-copper-generates-oxidative-stress-in-cancer-cells-its-possible-chemotherapeutic-mechanism-against-hepatocellular-carcinoma
#19
A Subastri, A Suyavaran, Preedia Babu E, Nithyananthan S, R Bharathidasan, C Thirunavukkarasu
Troxerutin (TXER) a rutin derivative is known for its anticancer effect against hepatocellular carcinoma (HCC). As part of large study, recently we have shown TXER interact with genetic material and its anti-mutagenic property. In the present study we have explored its possible mode of action in HCC. Since TXER alone did not show significant anticancer effect on Huh-7 cells, in vitro biochemical assays were performed for determining anticancer efficacy of TXER + metal complex using transition metals such as Cu, Zn & Fe...
June 19, 2017: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/28627678/bevacizumab-counteracts-vegf-dependent-resistance-to-erlotinib-in-an-egfr-mutated-nsclc-xenograft-model
#20
Chinami Masuda, Mieko Yanagisawa, Keigo Yorozu, Mitsue Kurasawa, Koh Furugaki, Nobuyuki Ishikura, Toshiki Iwai, Masamichi Sugimoto, Kaname Yamamoto
Erlotinib, an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI), shows superior efficacy in patients with non-small cell lung cancer (NSCLC) harboring activating EGFR mutations (EGFR Mut+). However, almost all tumors eventually develop resistance to erlotinib. Recently, the Phase II JO25567 study reported significant prolongation of progression-free survival (PFS) by erlotinib plus bevacizumab combination compared with erlotinib in EGFR Mut+ NSCLC. Herein, we established a preclinical model which became refractory to erlotinib after long-term administration and elucidated the mode of action of this combination...
June 8, 2017: International Journal of Oncology
keyword
keyword
83136
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"