keyword
MENU ▼
Read by QxMD icon Read
search

ADM

keyword
https://www.readbyqxmd.com/read/28218440/physiologically-based-kinetic-modeling-of-hesperidin-metabolism-and-its-use-to-predict-in-vivo-effective-doses-in-humans
#1
Rungnapa Boonpawa, Albertus Spenkelink, Ans Punt, Ivonne M C M Rietjens
SCOPE: To develop a physiologically based kinetic (PBK) model that describes the absorption, distribution, metabolism, and excretion (ADME) of hesperidin in humans, enabling the translation of in vitro concentration-response curves to in vivo dose-response curves. METHODS AND RESULTS: The PBK model for hesperidin in humans was developed based on in vitro metabolic parameters. Hesperidin was predicted to mainly occur in the systemic circulation as different monoglucuronides...
February 20, 2017: Molecular Nutrition & Food Research
https://www.readbyqxmd.com/read/28215783/synthesis-and-biological-evaluation-of-potential-inhibitors-of-the-cysteine-proteases-cruzain-and-rhodesain-designed-by-molecular-simplification
#2
Saulo Fehelberg Pinto Braga, Luan Carvalho Martins, Elany Barbosa da Silva, Policarpo Ademar Sales Júnior, Silvane Maria Fonseca Murta, Alvaro José Romanha, Wai Tuck Soh, Hans Brandstetter, Rafaela Salgado Ferreira, Renata Barbosa de Oliveira
Analogues of 8-chloro-N-(3-morpholinopropyl)-5H-pyrimido[5,4-b]indol-4-amine 1, a known cruzain inhibitor, were synthesized using a molecular simplification strategy. Five series of analogues were obtained: indole, pyrimidine, quinoline, aniline and pyrrole derivatives. The activity of the compounds was evaluated against the enzymes cruzain and rhodesain as well as against Trypanosoma cruzi amastigote and trypomastigote forms. The 4-aminoquinoline derivatives showed promising activity against both enzymes, with IC50 values ranging from 15 to 125µM...
February 9, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28215152/biological-activities-of-sesquiterpene-lactones-isolated-from-the-genus-centaurea-l-asteraceae
#3
Marina Sokovic, Ana Ciric, Jasmina Glamoclija, Helen Skaltsa
BACKGROUND: In recent years, a growing interest has developed in the field of biological activity of plant metabolites. Research in this area considering antimicrobial, antioxidant, cytotoxic, anti-inflammatory, and other properties, is currently expanding, reporting various species to possess such biological effects. Among them, Centaurea species are well known to be used in ethnomedicine. The Centaurea genus (Asteraceae) is represented by more than 500 species, mostly located in the Mediterranean region and Western Asia...
February 15, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28210552/capsular-contracture-in-implant-based-breast-reconstruction-the-effect-of-porcine-acellular-dermal-matrix
#4
Alessia M Lardi, Mark Ho-Asjoe, Klaus Junge, Jian Farhadi
BACKGROUND: Irradiation of implant-based breast reconstructions (BR) is known to increase capsular contracture (CC) rates on average by 4-fold over non-irradiated reconstructions. The use of acellular dermal matrix (ADM) has been associated with lower CC rates in non-irradiated reconstructions (0-3%). Experimental and clinical studies suggest that ADM may also reduce CC rates in irradiated breasts. The aim of this study was to evaluate CC rates in non-irradiated and irradiated one- and two-stage BRs performed with the assistance of porcine ADM (PADM)...
February 2017: Gland Surgery
https://www.readbyqxmd.com/read/28207169/design-synthesis-and-biological-evaluation-of-novel-1-2-4-trioxanes-as-potential-antimalarial-agents
#5
Amit K Gupta, Kanika Varshney, Vivek Kumar, Kumkum Srivastava, Aditya B Pant, Sunil K Puri, Anil K Saxena
A series of substituted 1,2,4-trioxanes were synthesized and evaluated for their antimalarial potential, in silico ADME properties and cytotoxicity on neuronal cell lines. Among the 15 synthesized substituted 1,2,4-trioxanes, two compounds (compound 15, IC50  = 25.71 nM; compound 21, IC50  = 19.6 nM) exhibited promising in vitro antimalarial potential comparable to those of the existing drugs chloroquine and artemisinin. Both of these compounds were found to be nontoxic up to 20 µM concentration in neuronal PC-12 cells...
February 16, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/28204936/impact-of-acellular-dermal-matrix-adm-use-under-mastectomy-flap-necrosis-on-perioperative-outcomes-of-prosthetic-breast-reconstruction
#6
So Young Kim, Sa Ik Bang
BACKGROUND: There is conflicting data on the potential necrotic complications of acellular dermal matrix (ADM) use in breast reconstruction, and most studies focus on mastectomy flap necrosis as an outcome measure associated with ADM use. The aim of this study was to examine cases with necrotic complications with and without the use of ADM and to investigate whether ADM affected perioperative outcomes in cases with necrotic complications. METHODS: Patients who experienced mastectomy flap necrosis following mastectomy with tissue expander placement between January 2009 and March 2015 were retrospectively reviewed...
February 15, 2017: Aesthetic Plastic Surgery
https://www.readbyqxmd.com/read/28203509/the-breastrial-stage-ii-adm-breast-reconstruction-outcomes-from-definitive-reconstruction-to-3-months-postoperative
#7
Shaun D Mendenhall, Layla A Anderson, Jian Ying, Kenneth M Boucher, Leigh A Neumayer, Jayant P Agarwal
BACKGROUND: The Breast Reconstruction Evaluation of Acellular Dermal Matrix as a Sling Trial is a prospective randomized trial comparing outcomes of tissue expander breast reconstruction using either AlloDerm or DermaMatrix. The trial was divided into 3 outcome stages; this study reports stage II outcomes, which are those from the time of definitive reconstruction to 3 months postoperative. METHODS: A randomized trial was conducted to compare complication rates between AlloDerm and DermaMatrix groups...
January 2017: Plastic and Reconstructive Surgery. Global Open
https://www.readbyqxmd.com/read/28198558/predictive-framework-for-estimating-exposure-of-birds-to-pharmaceuticals
#8
Thomas G Bean, Kathryn E Arnold, Julie M Lane, Ed Bergström, Jane Thomas-Oates, Barnett A Rattner, Alistair B A Boxall
Here we present and evaluate a framework for estimating concentrations of pharmaceuticals over time in wildlife feeding at wastewater treatment plants (WWTPs). The framework is composed of a series of predictive steps involving the estimation of pharmaceutical concentration in wastewater, accumulation into wildlife food items, uptake by wildlife with subsequent distribution into, and elimination from, tissues. As many pharmacokinetic parameters for wildlife are unavailable for the majority of drugs in use, a read-across approach was employed using either rodent or human data on absorption, distribution, metabolism and excretion (ADME)...
February 15, 2017: Environmental Toxicology and Chemistry
https://www.readbyqxmd.com/read/28197321/discovery-of-novel-allosteric-hcv-ns5b-inhibitors-2-lactam-containing-thiophene-carboxylates
#9
Pan Li, Warren Dorsch, David J Lauffer, Darius Bilimoria, Nathalie Chauret, John J Court, Sanjoy Kumar Das, Francois Denis, Nagraj Mani, Suganthini Nanthakumar, Olivier Nicolas, B Govinda Rao, Steven Ronkin, Subajini Selliah, Rebecca S Shawgo, Ralph Stearns, Qing Tang, Nathan D Waal, Jeremy Green
Lomibuvir (1) is a non-nucleoside, allosteric inhibitor of the hepatitis C virus NS5B polymerase with demonstrated clinical efficacy. Further development efforts within this class of inhibitor focused on improving the antiviral activity and physicochemical and pharmacokinetic properties. Recently, we reported the development of this series, leading to compound 2, a molecule with comparable potency and an improved physicochemical profile relative to 1. Further exploration of the amino amide-derived side chain led to a series of lactam derivatives, inspired by the X-ray crystal structure of related thiophene carboxylate inhibitors...
February 9, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28194226/cheminformatics-studies-to-analyze-the-therapeutic-potential-of-phytochemicals-from-rhazya-stricta
#10
Abdullah Y Obaid, Sreedhara Voleti, Roop Singh Bora, Nahid H Hajrah, Abdulkader M Shaikh Omer, Jamal S M Sabir, Kulvinder Singh Saini
Rhazya stricta is a unique medicinal plant source for many indole alkaloids, non-alkaloids, flavonoids, triterpenes and other unknown molecules with tremendous potential for therapeutic applications against many diseases. In the present article, we generated computational data on predictive properties and activity across two key therapeutic areas of cancer and obesity, and corresponding cheminformatics studies were carried out to examine druggable properties of these alkaloids. Computed physiochemical properties of the 78 indole alkaloids from R...
2017: Chemistry Central Journal
https://www.readbyqxmd.com/read/28190938/elucidation-of-the-anti-inflammatory-mechanisms-of-bupleuri-and-scutellariae-radix-using-system-pharmacological-analyses
#11
Xia Shen, Zhenyu Zhao, Hao Wang, Zihu Guo, Benxiang Hu, Gang Zhang
Objective. This study was aimed at elucidating the molecular mechanisms underlying the anti-inflammatory effect of the combined application of Bupleuri Radix and Scutellariae Radix and explored the potential therapeutic efficacy of these two drugs on inflammation-related diseases. Methods. After searching the databases, we collected the active ingredients of Bupleuri Radix and Scutellariae Radix and calculated their oral bioavailability (OB) and drug-likeness (DL) based on the absorption-distribution-metabolism-elimination (ADME) model...
2017: Mediators of Inflammation
https://www.readbyqxmd.com/read/28188450/terminal-latency-abnormality-in-amyotrophic-lateral-sclerosis-without-split-hand-syndrome
#12
Donghwi Park, Jin-Sung Park
Amyotrophic lateral sclerosis (ALS) has a peculiar involvement pattern; clinically it is known as split hand syndrome and electrophysiologically shows abnormalities in the abductor pollicis brevis (APB)/abductor digiti minimi (ADM) ratio. The aim of this study was to find a significant electrophysiological parameter in upper limb onset ALS patients with normal APB/ADM ratio when compared to cervical spondylotic amyotrophy (CSA) and healthy controls. We retrospectively reviewed the electrophysiological results of 47 upper limb onset ALS and 42 CSA cases; 20 healthy individuals were included as controls...
February 10, 2017: Neurological Sciences
https://www.readbyqxmd.com/read/28188341/evaluation-of-transcriptomic-signature-as-a-valuable-tool-to-study-drug-induced-cholestasis-in-primary-human-hepatocytes
#13
Céline Parmentier, Philippe Couttet, Armin Wolf, Thomas Zaccharias, Bruno Heyd, Philippe Bachellier, Marianne Uteng, Lysiane Richert
Primary human hepatocyte (PHH) sandwich cultures from five different donors were daily exposed to cyclosporine A (CsA), ibuprofen (IBU), chlorpromazine (CPZ), amiodarone (AMI) and paracetamol (APAP) at their respective Cmax (total) for short-term (1-3 days) and long-term treatment (14 days). Whole genome mRNA profiles (34,693 genes in total) were conducted using an Illumina microarray platform. The impact of compound treatments on gene signatures involved in liver differentiation, cholestasis and in bile acid homeostasis was evaluated...
February 10, 2017: Archives of Toxicology
https://www.readbyqxmd.com/read/28188299/novel-mechanism-of-decyanation-of-gdc-0425-by-cytochrome-p450
#14
Ryan H Takahashi, Jason S Halladay, Michael Siu, Yuan Chen, Cornelis Eca Hop, Siamak Cyrus Khojasteh, Shuguang Ma
GDC-0425 is an orally bioavailable small molecule inhibitor of checkpoint kinase 1 (Chk1) that was investigated as a novel co-therapy to potentiate chemotherapeutic drugs such as gemcitabine. In the radiolabeled ADME study in Sprague-Dawley rats, trace level but long-lived 14C-labeled plasma thiocyanate was observed. This thiocyanate originated from metabolic decyanation of GDC-0425 and rapid conversion of cyanide to thiocyanate. Excretion studies indicated decyanation was a minor metabolic pathway, but placing 14C at nitrile magnified its observation...
February 10, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28185054/identification-of-new-lead-molecules-against-ube2nl-enzyme-for-cancer-therapy
#15
Vishwanath Ramatenki, Ramakrishna Dumpati, Rajender Vadija, Santhiprada Vellanki, Sarita Rajender Potlapally, Rohini Rondla, Uma Vuruputuri
Cancer is characterized by abnormal growth of cells. Targeting ubiquitin proteins in the discovery of new anticancer therapeutics is an attractive strategy. The present study uses the structure-based drug discovery methods to identify new lead structures, which are selective to the putative ubiquitin-conjugating enzyme E2N-like (UBE2NL). The 3D structure of the UBE2NL was evaluated using homology modeling techniques. The model was validated using standard in silico methods. The hydrophobic pocket of UBE2NL that aids in binding with its natural receptor ubiquitin-conjugating enzyme E2 variant (UBE2V) was identified through protein-protein docking study...
February 9, 2017: Applied Biochemistry and Biotechnology
https://www.readbyqxmd.com/read/28177682/reversal-of-p-glycoprotein-medicated-multidrug-resistance-and-pharmacokinetics-study-in-rats-by-wyx-5
#16
Yuzhu Wang, Jian Cui, Yuxuan Dai, Yuxiang Wu, Wenlong Huang, Hai Qian, Liang Ge
Multidrug resistance (MDR) is one of the major obstacles confronted in cancer chemotherapy, which mainly due to the overexpression of P-glycoprotein (P-gp). Co-administration of anticancer drugs and P-gp inhibitors is a promising approach to overcome MDR. WYX-5, a novel P-gp inhibitor, shows a notable reversal effect with low cytotoxicity in vitro. In this paper, the reversal mechanism and safety of the MDR modulator WYX-5 were explored in vitro, and evaluated for its pharmacokinetics and effects on Adriamycin (ADM) metabolism <i>in vivo</i>...
December 22, 2016: Canadian Journal of Physiology and Pharmacology
https://www.readbyqxmd.com/read/28176881/functional-coupling-of-human-microphysiology-systems-intestine-liver-kidney-proximal-tubule-blood-brain-barrier-and-skeletal-muscle
#17
Lawrence Vernetti, Albert Gough, Nicholas Baetz, Sarah Blutt, James R Broughman, Jacquelyn A Brown, Jennifer Foulke-Abel, Nesrin Hasan, Julie In, Edward Kelly, Olga Kovbasnjuk, Jonathan Repper, Nina Senutovitch, Janet Stabb, Catherine Yeung, Nick C Zachos, Mark Donowitz, Mary Estes, Jonathan Himmelfarb, George Truskey, John P Wikswo, D Lansing Taylor
Organ interactions resulting from drug, metabolite or xenobiotic transport between organs are key components of human metabolism that impact therapeutic action and toxic side effects. Preclinical animal testing often fails to predict adverse outcomes arising from sequential, multi-organ metabolism of drugs and xenobiotics. Human microphysiological systems (MPS) can model these interactions and are predicted to dramatically improve the efficiency of the drug development process. In this study, five human MPS models were evaluated for functional coupling, defined as the determination of organ interactions via an in vivo-like sequential, organ-to-organ transfer of media...
February 8, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28176814/eunag-a-new-ligand-inducible-fluorescent-reporter-to-detect-drug-transporter-activity-in-live-cells
#18
Johannes T-H Yeh, Kwangho Nam, Joshua T-H Yeh, Norbert Perrimon
The absorption, distribution, metabolism and excretion (ADME) of metabolites and toxic organic solutes are orchestrated by the ATP-binding cassette (ABC) transporters and the organic solute carrier family (SLC) proteins. A large number of ABC and SLC transpoters exist; however, only a small number have been well characterized. To facilitate the analysis of these transporters, which is important for drug safety and physiological studies, we developed a sensitive genetically encoded bilirubin (BR)-inducible fluorescence sensor (eUnaG) to detect transporter-coupled influx/efflux of organic compounds...
February 8, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28175954/multiple-resistance-to-carcinogens-and-xenobiotics-p-glycoproteins-as-universal-detoxifiers
#19
REVIEW
Thomas Efferth, Manfred Volm
The detoxification of toxic substances is of general relevance in all biological systems. The plethora of exogenous xenobiotic compounds and endogenous toxic metabolic products explains the evolutionary pressure of all organisms to develop molecular mechanisms to detoxify and excrete harmful substances from the body. P-glycoprotein and other members of the ATP-binding cassette (ABC) transporter family extrude innumerous chemical compounds out of cells. Their specific expression in diverse biological contexts cause different phenotypes: (1) multidrug resistance (MDR) and thus failure of cancer chemotherapy, (2) avoidance of accumulation of carcinogens and prevention of carcinogenesis in healthy tissues, (3) absorption, distribution, metabolization and excretion (ADME) of pharmacological drugs in human patients, (4) protection from environmental toxins in aquatic organisms (multi-xenobiotic resistance, MXR)...
February 7, 2017: Archives of Toxicology
https://www.readbyqxmd.com/read/28168765/prediction-of-anti-alzheimer-s-activity-of-flavonoids-targeting-acetylcholinesterase-in-silico
#20
Subrata Das, Monjur A Laskar, Satyajit D Sarker, Manabendra D Choudhury, Prakash Roy Choudhury, Abhijit Mitra, Shajarahtunnur Jamil, Siti Mariam A Lathiff, Siti Awanis Abdullah, Norazah Basar, Lutfun Nahar, Anupam D Talukdar
INTRODUCTION: Prenylated and pyrano-flavonoids of the genus Artocarpus J. R. Forster & G. Forster are well known for their acetylcholinesterase (AChE) inhibitory, anti-cholinergic, anti-inflammatory, anti-microbial, anti-oxidant, anti-proliferative and tyrosinase inhibitory activities. Some of these compounds have also been shown to be effective against Alzheimer's disease. OBJECTIVE: The aim of the in silico study was to establish protocols to predict the most effective flavonoid from prenylated and pyrano-flavonoid classes for AChE inhibition linking to the potential treatment of Alzheimer's disease...
February 7, 2017: Phytochemical Analysis: PCA
keyword
keyword
51408
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"