Book ChapterDOI
Validation of in-vitro bioassay methods: Application in herbal drug research.
TLDR
Seven sequencing steps that can be taken for performing a valid bioassay include: literature survey, sample stability evaluation, Biosystem performance testing, Sample performance evaluation, determination of 50% effective concentration or cytotoxic concentrations, selective index evaluation, and determination of accurate relative potency of sample.Abstract:
This present review described the validation method of in-vitro bioassay for its application in herbal drug research. Seven sequencing steps that can be taken for performing a valid bioassay include: literature survey, sample stability evaluation, Biosystem performance testing, Sample performance evaluation, determination of 50% effective concentration or cytotoxic concentrations, selective index evaluation, and determination of accurate relative potency of sample. Detailed methods and acceptance criteria for each step are described herein. Method calculations of the relative potency of sample using European Pharmacopeia 10.0, 5.3 (2020) were recommended instead of using United States Pharmacopeia 42 (2019). For having reliable data and conclusions, all methods (chemical and bioassay) need to be first validated before any data collection. Absence of any validation method may results in incorrect conclusions and bias.read more
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Journal ArticleDOI
Design and synthesis of thiazolidine-2,4-diones hybrids with 1,2-dihydroquinolones and 2-oxindoles as potential VEGFR-2 inhibitors: in-vitro anticancer evaluation and in-silico studies
Mohammed S Taghour,Hazem Elkady,Wagdy M. Eldehna,Nehal M. El-Deeb,Ahmed M. A. Kenawy,Eslam B. Elkaeed,Aisha A. Alsfouk,Mohamed S Alesawy,Ahmed M. Metwaly,Ibrahim H. Eissa +9 more
TL;DR: Molecular dynamic simulations authenticated the high affinity, accurate binding, and perfect dynamics of compound 12a against VEGFR-2.
Journal ArticleDOI
Robust antiviral activity of commonly prescribed antidepressants against emerging coronaviruses: in vitro and in silico drug repurposing studies
Omnia Kutkat,Yassmin Moatasim,Ahmed A. Al-Karmalawy,Hamada S. Abulkhair,Mokhtar R. Gomaa,Ahmed Nageh El-Taweel,Noura M. Abo Shama,Mohamed S. Gaballah,Dina B. Mahmoud,Ghazi Kayali,Mohamed A. Ali,Ahmed Kandeil,Ahmed Mostafa +12 more
TL;DR: In this paper , the efficacy of eight commonly prescribed FDA-approved antidepressants on the inhibition of both SARS-CoV-2 and MERS-coV was assessed, and the in vitro anti-SARS CoV2 and anti-MERS CoV activities were evaluated.
Journal ArticleDOI
New quinoline and isatin derivatives as apoptotic VEGFR-2 inhibitors: design, synthesis, anti-proliferative activity, docking, ADMET, toxicity, and MD simulation studies
Eslam B. Elkaeed,Mohammed S Taghour,Hazem A. Mahdy,Wagdy M. Eldehna,Nehal M. El-Deeb,Ahmed M. A. Kenawy,Bshra A Alsfouk,Mohammed A. Dahab,Ahmed M. Metwaly,Ibrahim H. Eissa,Mohamed El-Zahabi +10 more
TL;DR: New quinoline and isatin derivatives having the main characteristics of VEGFR-2 inhibitors was synthesised and showed the highest value of safety and selectivity and induced apoptosis in Caco-2 through the expressive down-regulation of the apoptotic genes.
Journal ArticleDOI
In-Silico Screening of Novel Synthesized Thienopyrimidines Targeting Fms Related Receptor Tyrosine Kinase-3 and Their In-Vitro Biological Evaluation
TL;DR: The present investigation describes the design strategy and synthesis of novel thienopyrimidine compounds in addition to their anticancer activity targeting tyrosine kinase FLT3 enzyme and results showed that the 2-morpholinoacetamido derivative 10a exhibited highestFLT3 inhibitory activity among the tested compounds.
Journal ArticleDOI
Cynometra cauliflora essential oils loaded-chitosan nanoparticles: Evaluations of their antioxidant, antimicrobial and cytotoxic activities.
Benedict Samling,Zaini Assim,Woei Yenn Tong,Chean Ring Leong,Syarifah Ab Rashid,Nik Nur Syazni Nik Mohamed Kamal,Musthahimah Muhamad,Wen-Nee Tan +7 more
TL;DR: In this article , C. cauliflora essential oils (CCEOs) were nanoencapped in chitosan nanoparticles (CSNPs) using an emulsion-ionic gelation technique.
References
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Journal ArticleDOI
A Simple Statistical Parameter for Use in Evaluation and Validation of High Throughput Screening Assays.
TL;DR: A screening window coefficient, called "Z- factor," is defined, which is reflective of both the assay signal dynamic range and the data variation associated with the signal measurements, and therefore is suitable for assay quality assessment.
Book
Performance standards for antimicrobial susceptibility testing
Melvin P. Weinstein,Clinical +1 more
TL;DR: The tabular information presented here represents the most current information for drug selection, interpretation, and QC using the procedures standardized in the most recent editions of M02, M07, and M11, and users should replace outdated editions with the current editions of CLSI documents.
Journal ArticleDOI
Gene-wide analysis detects two new susceptibility genes for Alzheimer's disease.
Valentina Escott-Price,Céline Bellenguez,Li-San Wang,Seung Hoan Choi,Denise Harold,Lesley Jones,Peter Holmans,Amy Gerrish,Alexey Vedernikov,Alexander Richards,Anita L. DeStefano,Jean-Charles Lambert,Carla A. Ibrahim-Verbaas,Adam C. Naj,Rebecca Sims,Gyungah Jun,Joshua C. Bis,Gary W. Beecham,Benjamin Grenier-Boley,Giancarlo Russo,Tricia A. Thornton-Wells,Nicola Denning,Albert V. Smith,Vincent Chouraki,Charlene Thomas,M. Arfan Ikram,Diana Zelenika,Badri N. Vardarajan,Badri N. Vardarajan,Yoichiro Kamatani,Chiao-Feng Lin,Helena Schmidt,Brian W. Kunkle,Melanie L. Dunstan,Maria Vronskaya,Andrew D. Johnson,Agustín Ruiz,Marie-Thérèse Bihoreau,Christiane Reitz,Florence Pasquier,Paul Hollingworth,Olivier Hanon,Annette L. Fitzpatrick,Joseph D. Buxbaum,Dominique Campion,Paul K. Crane,Clinton T. Baldwin,Tim Becker,Vilmundur Gudnason,Carlos Cruchaga,David Craig,Najaf Amin,Claudine Berr,Oscar L. Lopez,Philip L. De Jager,Philip L. De Jager,Vincent Deramecourt,Janet A. Johnston,Denis A. Evans,Simon Lovestone,Luc Letenneur,Isabel Hernández,David C. Rubinsztein,Gudny Eiriksdottir,Kristel Sleegers,Alison Goate,Nathalie Fievet,Matthew J. Huentelman,Michael Gill,Kristelle Brown,M. Ilyas Kamboh,Lina Keller,Pascale Barberger-Gateau,Bernadette McGuinness,Eric B. Larson,Eric B. Larson,Amanda J. Myers,Carole Dufouil,Stephen Todd,David Wallon,Seth Love,Ekaterina Rogaeva,John Gallacher,Peter St George-Hyslop,Jordi Clarimón,Alberto Lleó,Antony James Bayer,Debby W. Tsuang,Lei Yu,Magda Tsolaki,Paola Bossù,Gianfranco Spalletta,Petra Proitsi,John Collinge,Sandro Sorbi,Florentino Sanchez Garcia,Nick C. Fox,John Hardy,Maria Candida Deniz Naranjo,Paolo Bosco,Robert Clarke,Carol Brayne,Daniela Galimberti,Elio Scarpini,Ubaldo Bonuccelli,Michelangelo Mancuso,Gabriele Siciliano,Susanne Moebus,Patrizia Mecocci,Maria Del Zompo,Wolfgang Maier,Harald Hampel,Alberto Pilotto,Ana Frank-García,Francesco Panza,Vincenzo Solfrizzi,Paolo Caffarra,Benedetta Nacmias,William Perry,Manuel Mayhaus,Lars Lannfelt,Hakon Hakonarson,Sabrina Pichler,Minerva M. Carrasquillo,Martin Ingelsson,Duane Beekly,Victoria Alvarez,Fanggeng Zou,Otto Valladares,Steven G. Younkin,Eliecer Coto,Kara L. Hamilton-Nelson,Wei Gu,Cristina Razquin,Pau Pastor,Ignacio Mateo,Michael John Owen,Kelley Faber,Palmi V. Jonsson,Onofre Combarros,Michael Conlon O'Donovan,Laura B. Cantwell,Hilkka Soininen,Deborah Blacker,Simon Mead,Thomas H. Mosley,David A. Bennett,Tamara B. Harris,Laura Fratiglioni,Laura Fratiglioni,Clive Holmes,Renée F.A.G. de Bruijn,Peter Passmore,Thomas J. Montine,Karolien Bettens,Jerome I. Rotter,Alexis Brice,Kevin Morgan,Tatiana Foroud,Walter A. Kukull,Didier Hannequin,John Powell,Mike A. Nalls,Karen Ritchie,Kathryn L. Lunetta,John S. K. Kauwe,Eric Boerwinkle,Matthias Riemenschneider,Mercè Boada,Mikko Hiltunen,Eden R. Martin,Reinhold Schmidt,Dan Rujescu,Jean-François Dartigues,Richard Mayeux,Christophe Tzourio,Albert Hofman,Markus M. Nöthen,Caroline Graff,Bruce M. Psaty,Bruce M. Psaty,Jonathan L. Haines,Jonathan L. Haines,Mark Lathrop,Margaret A. Pericak-Vance,Lenore J. Launer,Christine Van Broeckhoven,Lindsay A. Farrer,Cornelia M. van Duijn,Alfredo Ramirez,Sudha Seshadri,Sudha Seshadri,Gerard D. Schellenberg,Philippe Amouyel,Julie Williams +194 more
TL;DR: The additional genes identified in this study, have an array of functions previously implicated in Alzheimer's disease, including aspects of energy metabolism, protein degradation and the immune system and add further weight to these pathways as potential therapeutic targets in Alzheimers disease.
Journal ArticleDOI
Anti-infective potential of natural products: how to develop a stronger in vitro 'proof-of-concept'.
TL;DR: This review provides a number of recommendations that will help to define a more sound 'proof-of-concept' for antibacterial, antifungal, antiviral and antiparasitic potential in natural products.
Reference BookDOI
Bioassay Techniques for Drug Development
TL;DR: The goal of an activity-directed isolation process is to isolate bioactive compounds which may provide structural leads of therapeutic importance as mentioned in this paper, whereas the traditional process of drug development is long and expensive, simple and rapid bioassays can serve as the starting point for drug discovery.