keyword
MENU ▼
Read by QxMD icon Read
search

ADM

keyword
https://www.readbyqxmd.com/read/29224415/preclinical-evaluation-of-saroglitazar-magnesium-a-dual-ppar-%C3%AE-%C3%AE-agonist-for-treatment-of-dyslipidemia-and-metabolic-disorders
#1
Harilal Patel, Poonam Giri, Prakash Patel, Sanjay Singh, Laxmikant Gupta, Urvesh Patel, Nirav Modi, Kalpesh Shah, Mukul R Jain, Nuggehally R Srinivas, Pankaj Patel
Saroglitazar, a novel peroxisome proliferator-activated receptor agonist (PPAR), regulates lipid and glucose metabolism. The objective of this report is to provide a preclinical evaluation (in vitro/in vivo) of ADME properties of saroglitazar. In vitro studies included determination of permeability, metabolic stability, plasma protein binding, CYP reaction phenotyping and CYP inhibitory liability. In vivo studies included oral bioavailability and pharmacokinetic assessment in mouse, rat and dog. The excretion of saroglitazar was determined in rats...
December 9, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/29218953/-exploiture-and-application-of-an-internet-based-computation-platform-for-integrative-pharmacology-of-traditional-chinese-medicine
#2
Hai-Yu Xu, Zhen-Ming Liu, Yan Fu, Yan-Qiong Zhang, Jian-Jun Yu, Fei-Fei Guo, Shi-Huan Tang, Chuan-Yu Lv, Jin Su, Ru-Yi Cui, Hong-Jun Yang
Recently, integrative pharmacology(IP) has become a pivotal paradigm for the modernization of traditional Chinese medicines(TCM) and combinatorial drugs discovery, which is an interdisciplinary science for establishing the in vitro and in vivo correlation between absorption, distribution, metabolism, and excretion/pharmacokinetic(ADME/PK) profiles of TCM and the molecular networks of disease by the integration of the knowledge of multi-disciplinary and multi-stages. In the present study, an internet-based Computation Platform for IP of TCM(TCM-IP, www...
September 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/29218926/-determination-of-eight-steroidal-saponins-in-15-kinds-of-genus-paris
#3
Yuan-Yuan Huang, Da-Hui Liu, Hua-Sheng Peng, Qing-Xiu Hao, Mei-Lan Chen, A-Zhong Zhang, Min Chen, Li-Ping Kang, Lu-Qi Huang
The study was established an HPLC method for simultaneous determination of 8 steroidal saponins (polyphyllins Ⅶ, H, Ⅵ, Ⅱ, Ⅰ, and Ⅴ, dioscin, and gracillin) in Paridis Rhizoma, and made an evaluation by determining steroidal saponins in 15 kinds of genus Paris. The analysis was performed on a Waters Acquity H-ClassTM UPLC ultrafine liquid chromatography system coupled with a PDA detector. The chromatographic separation was achieved through a CAPCELL PAK ADME (4.6 mm× 250 mm, 5 μm) column and the optimal mobile phase consisted of acetonitrile and water...
September 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/29211475/optimization-of-orally-bioavailable-enhancer-of-zeste-homolog-2-ezh2-inhibitors-using-ligand-and-property-based-design-strategies-identification-of-development-candidate-r-5-8-dichloro-7-methoxy-oxetan-3-yl-methyl-2-4-methoxy-6-methyl-2-oxo-1-2-dihydropyridin
#4
Pei-Pei Kung, Patrick Bingham, Alexei Brooun, Michael R Collins, Ya-Li Deng, Dac M Dinh, Connie Fan, Ketan S Gajiwala, Rita Grantner, Hovhannes J Gukasyan, Wenyue Hu, Buwen Huang, Robert S Kania, Susan E Kephart, Cody T Krivacic, Robert A Kumpf, Penney Khamphavong, Manfred Kraus, Wei Liu, Karen A Maegley, Lisa Nguyen, Shijian Ren, Daniel Tyler Richter, Robert A Rollins, Neal W Sach, Shikhar Sharma, John Sherrill, Jillian E Spangler, Albert E Stewart, Scott C Sutton, Sean Uryu, Dominique Verhelle, Hui Wang, Shuiwang Wang, Martin Wythes, Shuibo Xin, Shinji Yamazaki, Huichun Zhu, Jinjiang Zhu, Luke Zehnder, Martin P Edwards
A new series of lactam-derived EZH2 inhibitors was designed via a ligand- and physicochemical property-based strategy to address metabolic stability and thermodynamic solubility issues associated with previous lead compound 1. The new inhibitors incorporated an sp3 hybridized carbon atom at the 7-position of the lactam moiety present in lead compound 1 as a replacement for a dimethylisoxazole group. This transformation enabled optimization of the physicochemical properties and potency compared to compound 1...
December 6, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29206206/anneal-hardening-behavior-of-cr-fe-c-alloy-deposits-prepared-in-a-cr3-based-bath-with-fe2-ions
#5
Ching An Huang, Jhih You Chen, Hai Wang, Po Liang Lai
Cr-Fe-C alloy deposits were successfully prepared on high-carbon tool steel in a Cr3+-based electroplating bath containing Fe2+ ions and suitable complex agents. A Cr-based alloy deposit was obtained with an electroplating current density higher than 25 Adm-2, and a Fe-based alloy deposit was obtained using a current density of 20 Adm-2. Following electroplating, these alloy deposited specimens were annealed via rapid thermal annealing (RTA) at 500 °C for different periods up to 30 s. The experimental results show that Cr- and Fe-based alloy deposits could be significantly hardened after RTA at 500 °C for a few seconds...
December 5, 2017: Materials
https://www.readbyqxmd.com/read/29200281/discovery-and-optimization-of-thiazolidinyl-and-pyrrolidinyl-derivatives-as-inhaled-pde4-inhibitors-for-respiratory-diseases
#6
Laura Carzaniga, Gabriele Amari, Andrea Rizzi, Carmelida Capaldi, Renato De Fanti, Eleonora Ghidini, Gino Villetti, Chiara Carnini, Nadia Moretto, Fabrizio Facchinetti, Paola Caruso, Gessica Marchini, Loredana Battipaglia, Riccardo Patacchini, Valentina Cenacchi, Roberta Volta, Francesco Amadei, Alice Pappani, Silvia Capacchi, Valentina Bagnacani, Maurizio Delcanale, Paola Puccini, Silvia Catinella, Maurizio Civelli, Elisabetta Armani
Phosphodiesterase 4 (PDE4) is a key cAMP-metabolising enzyme involved in the pathogenesis of inflammatory disease and its pharmacological inhibition has been shown to exert therapeutic efficacy in chronic obstructive pulmonary disease (COPD). Herein we describe a drug discovery program aiming at the identification of novel classes of potent PDE4 inhibitors suitable for pulmonary administration. Starting from a previous series of benzoic acid esters, we explored the chemical space in the solvent-exposed region of the enzyme catalytic binding pocket...
December 4, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29196176/assessing-value-in-breast-reconstruction-a-systematic-review-of-cost-effectiveness-studies
#7
Clifford C Sheckter, Evan Matros, Arash Momeni
INTRODUCTION: Breast reconstruction is one of the most common procedures performed by plastic surgeons and is achieved through various choices in both technology and method. Cost-effectiveness analyses are increasingly important in assessing differences in value between treatment options, which is relevant in a world of confined resources. A thorough evaluation of the cost-effectiveness literature can assist surgeons and health systems evaluate high-value care models. METHODS: A systematic review of PubMed, Web of Science, and the Cost-Effectiveness Analysis Registry was conducted...
October 9, 2017: Journal of Plastic, Reconstructive & Aesthetic Surgery: JPRAS
https://www.readbyqxmd.com/read/29194347/in-vivo-and-in-vitro-activities-and-adme-tox-profile-of-a-quinolizidine-modified-4-aminoquinoline-a-potent-anti-p-falciparum-and-anti-p-vivax-blood-stage-antimalarial
#8
Nicoletta Basilico, Silvia Parapini, Anna Sparatore, Sergio Romeo, Paola Misiano, Livia Vivas, Vanessa Yardley, Simon L Croft, Annette Habluetzel, Leonardo Lucantoni, Laurent Renia, Bruce Russell, Rossarin Suwanarusk, Francois Nosten, Giulio Dondio, Chiara Bigogno, Daniela Jabes, Donatella Taramelli
Natural products are a prolific source for the identification of new biologically active compounds. In the present work, we studied the in vitro and in vivo antimalarial efficacy and ADME-Tox profile of a molecular hybrid (AM1) between 4-aminoquinoline and a quinolizidine moiety derived from lupinine (Lupinus luteus). The aim was to find a compound endowed with the target product profile-1 (TCP-1: molecules that clear asexual blood-stage parasitaemia), proposed by the Medicine for Malaria Venture to accomplish the goal of malaria elimination/eradication...
December 1, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29191453/apigenin-sensitizes-hepatocellular-carcinoma-cells-to-doxorubic-through-regulating-mir-520b-atg7-axis
#9
Ai-Mei Gao, Xiao-Yu Zhang, Juan-Ni Hu, Zun-Ping Ke
Chemo-resistance is a serious obstacle for successful treatment of cancer. Apigenin, a dietary flavonoid, has been reported as an anticancer drug in various malignant cancers. This study aimed to investigate the potential chemo-sensitization effect of apigenin in doxorubicin-resistant hepatocellular carcinoma cell line BEL-7402/ADM. We observed that apigenin significantly enhanced doxorubicin sensitivity, induced miR-520b expression and inhibited ATG7-dependent autophagy in BEL-7402/ADM cells. In addition, we also showed that miR-520b mimics increased doxorubicin sensitivity and inhibited ATG7-dependent autophagy...
November 27, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/29190510/predicted-activity-of-ugt2b7-abcb1-oprm1-and-comt-using-full-gene-haplotypes-and-their-association-with-the-cyp2d6-inferred-metabolizer-phenotype
#10
Frank R Wendt, Antti Sajantila, Bruce Budowle
The pharmacogene, CYP2D6, is commonly used to infer metabolizer phenotype of many marketed drugs and endogenous toxins in ante- and post-mortem patients but only represents the efficiency of phase 1 metabolism. Downstream metabolic enzymes encoded by UGT2B7, ABCB1, OPRM1, and COMT also have been implicated in variable individual response to drugs due to their activity at different stages of the tramadol ADME (absorption, distribution, metabolism, and excretion) process. While commonly studied as single genes using targeted genotyping approaches, a more comprehensive tramadol metabolism profile has not been evaluated...
November 26, 2017: Forensic Science International. Genetics
https://www.readbyqxmd.com/read/29184072/adrenomedullin-protects-leydig-cells-against-lipopolysaccharide-induced-oxidative-stress-and-inflammatory-reaction-via-mapk-nf-%C3%AE%C2%BAb-signalling-pathways
#11
Wei Hu, Lei Shi, Ming-Yong Li, Pang-Hu Zhou, Bo Qiu, Ke Yin, Hui-Hui Zhang, Yong Gao, Ran Kang, Song-Lin Qin, Jin-Zhuo Ning, Wei Wang, Li-Jun Zhang
This study aimed to explore the possible benefits of adrenomedullin (ADM) in preventing oxidative stress and inflammation by using an in vitro primary culture model of rat Leydig cells exposed to lipopolysaccharide (LPS). Cell proliferation was detected through CCK-8 and BrdU incorporation assays. ROS were determined with a DCFDA kit, and cytokine concentrations were measured with ELISA assay kits. Protein production was examined by immunohistochemical staining and Western blot, and gene expression was observed through RT-qPCR...
November 28, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29175309/altered-neuro-inflammatory-gene-expression-in-hippocampus-in-major-depressive-disorder
#12
Gouri J Mahajan, Eric J Vallender, Michael R Garrett, Lavanya Challagundla, James C Overholser, George Jurjus, Lesa Dieter, Maryam Syed, Damian G Romero, Hamed Benghuzzi, Craig A Stockmeier
Major Depressive Disorder (MDD) is a common psychiatric disorder for which available medications are often not effective. The high prevalence of MDD and modest response to existing therapies compels efforts to better understand and treat the disorder. Decreased hippocampal volume with increasing duration of depression suggests altered gene expression or even a decrease in neurogenesis. Tissue punches from the dentate gyrus were collected postmortem from 23 subjects with MDD and 23 psychiatrically-normal control subjects...
November 22, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/29173116/3-nitro-1-2-4-triazol-5-one-2014
#13
(no author information available yet)
3-Nitro-1,2,4-triazol-5-one (NTO) is a potential replacement for energetics in military munitions. It is a component of IMX-101, a munition designed to prevent unintentional detonation. This report summarizes the dermal, oral, and inhalation animal toxicity data, including the results of genotoxicity and limited reproductive and developmental studies. NTO has an acute LD50 in rats and mice of >5000 mg/kg, is a potential eye and skin irritant, but does not induce skin sensitization. Acute inhalation toxicity studies in rats were negative, but testicular hypoplasia was observed in a 14-day oral study in rats administered NTO at >500 mg/kg/day...
January 1, 2017: Toxicology and Industrial Health
https://www.readbyqxmd.com/read/29173093/molecular-network-selected-pharmacogenomics-in-a-case-of-bipolar-spectrum-disorder
#14
Stefano Fortinguerra, Alessandro Buriani, Vincenzo Sorrenti, Michele Lenzi, Pietro Giusti
Personal genomic analysis was used for molecular diagnosis and pharmacogenomics in a 53-year-old female suffering from alternating depressive and dysphoric episodes. A total of 52 genes and 108 SNPs were analyzed in the whole genome. Results from the pharmacogenomic analysis were consistent with the pharmacological history and indicate mutations associated with low monoaminergic tone, but also a hyperactive 5HT2A receptor, a feature that associates to a high probability of developing a bipolar condition, especially under 5-hydroxytryptamine potentiating pharmacology...
November 27, 2017: Pharmacogenomics
https://www.readbyqxmd.com/read/29171346/computational-and-in-vitro-insights-on-snake-venom-phospholipase-a2-inhibitor-of-phytocompound-ikshusterol3-o-glucoside-of-clematis-gouriana-roxb-ex-dc
#15
Sathishkumar Chinnasamy, Subbiah Nagarajan, Thirunavukkarasu Sivaraman, Karthikeyan Muthusamy
Ikshusterol3-O-glucoside was isolated from Clematis gouriana Roxb. ex DC root. A structure of the isolated compound was determined on the basis of various spectroscopic interpretations (UV, NMR, FTIR, and GC-MS-EI). This structure was submitted in the PubChem compound database (SID 249494133). SID 249494133 was carried out by density functional theory calculation to observe the chemical stability and electrostatic potential of this compound. The absorption, distribution, metabolism, excretion (ADME) property of this compound was predicted to evaluate the drug likeness and toxicity...
November 24, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/29170886/phase-ii-study-of-doxorubicin-and-thalidomide-in-patients-with-refractory-aggressive-fibromatosis
#16
Xin Liu, Huijie Wang, Xianghua Wu, Xiaonan Hong, Zhiguo Luo
Background To evaluate the efficacy and safety of doxorubicin (ADM) combined with thalidomide (THA) as a first-line treatment for patients with refractory aggressive fibromatosis (AF). Patients and Methods Eligible patients were treated with ADM 30 mg/m(2) on days 1-2 and THA 200 mg nightly on days 1-21 every 3 weeks for a maximum of six cycles. THA was then continued for a total of 1 year. The primary end point was response rate (RR). Results Fifteen patients were enrolled in the study. No patient had a complete response, but five patients had partial responses, resulting in a RR of 33%...
November 23, 2017: Investigational New Drugs
https://www.readbyqxmd.com/read/29169426/-knockdown-of-alox5-gene-promotes-apoptosis-of-k562-adm-cells
#17
Yujie Luo, Min Xu, Wenwan Gao, Kun Tao
Objective To investigate the effect of short hairpin RNA (shRNA) knockdown of arachidonate 5-lipoxygenase (Alox5) gene on the apoptosis of resistant chronic myeloid leukemia K562/ADM cells. Methods Three pairs of shRNA fragment targeting human Alox5 gene were synthesized and inserted into pGenesil-1 interference vector. Enzyme digestion and sequencing were performed to identify the recombinant plasmid pGenesil-1-shRNA-Alox5. The plasmid was then transfected into K562/ADM cells. Real-time quantitative PCR and Western blotting were used to detect the Alox5 mRNA and protein levels to get the best interference group...
October 2017: Xi Bao Yu Fen Zi Mian Yi Xue za Zhi, Chinese Journal of Cellular and Molecular Immunology
https://www.readbyqxmd.com/read/29168743/synthesis-and-anticandidal-activity-evaluation-of-new-benzimidazole-thiazole-derivatives
#18
Zafer Asım Kaplancıklı, Serkan Levent, Derya Osmaniye, Begüm Nurpelin Sağlık, Ulviye Acar Çevik, Betül Kaya Çavuşoğlu, Yusuf Özkay, Sinem Ilgın
Azole-based antifungal agents constitute one of the important classes of antifungal drugs. Hence, in the present work, 12 new benzimidazole-thiazole derivatives 3a-3l were synthesized to evaluate their anticandidal activity against C.albicans, C.glabrata, C.krusei, and C.parapsilopsis. The structures of the newly synthesized compounds 3a-3l were confirmed by IR, ¹H-NMR, (13)C-NMR, and ESI-MS spectroscopic methods. ADME parameters of synthesized compounds 3a-3l were predicted by an in-slico study and it was determined that all synthesized compounds may have a good pharmacokinetic profile...
November 23, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29166346/options-in-acellular-dermal-matrix-device-assembly
#19
Steven Sigalove
Prepectoral prosthetic breast reconstruction has become increasingly popular during the last several years. Original shortcomings and poor outcomes in the 1970s have been overcome with the use of the bioengineered breast concept-namely, use of improved form stable breast implants, autologous fat grafting, and acellular dermal matrices (ADMs). Careful use of these reconstructive tools combined with improved mastectomy skin flaps has lead to successful early outcomes. Prepectoral breast reconstruction mitigates the animation deformities and muscle tightness previously associated with dual-plane prosthetic breast reconstruction while at the same time producing reproducible and outstanding aesthetic outcomes...
December 2017: Plastic and Reconstructive Surgery
https://www.readbyqxmd.com/read/29166342/important-considerations-for-performing-prepectoral-breast-reconstruction
#20
Hani Sbitany
Prepectoral breast reconstruction has emerged as an excellent technique for postmastectomy reconstruction, as it allows for full preservation of a patient's pectoralis major muscle and chest wall function. This reduces pain, eliminates animation deformity, and results in high patient satisfaction. Safely performed prepectoral breast reconstruction requires a careful patient selection process before committing to the procedure, taking into account comorbidities, radiation status, and oncologic criteria such as tumor location and breast cancer stage...
December 2017: Plastic and Reconstructive Surgery
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"