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https://www.readbyqxmd.com/read/29656443/biological-evaluation-of-selected-3-4-dihydro-2-1h-quinoxalinones-and-3-4-dihydro-1-4-benzoxazin-2-ones-molecular-docking-study
#1
Jelena Petronijević, Nenad Janković, Tatjana P Stanojković, Nenad Joksimović, Nađa Đ Grozdanić, Milan Vraneš, Aleksandar Tot, Zorica Bugarčić
In order to investigate new potential therapeutically active agents, we investigated the biological properties of two small libraries of quinoxalinones and 1,4-benzoxazin-2-ones. The results obtained showed that compounds 5, 9-11 have good cytotoxic activity against HeLa cells where the lowest IC50 value (10.46 ± 0.82 μM/mL) was measured for compound 10. Additionally, the most active compounds (5, 9-11) showed much better selectivity for MRC-5 cells (up to 17.4) compared to cisplatin. In vitro evaluation of the inhibition of the enzyme α-glucosidase showed that compounds 10 and 11 exert significant inhibition of the enzyme at 52...
April 14, 2018: Archiv der Pharmazie
https://www.readbyqxmd.com/read/29656376/human-genetics-of-sclerosing-bone-disorders
#2
REVIEW
Raphaël De Ridder, Eveline Boudin, Geert Mortier, Wim Van Hul
PURPOSE OF REVIEW: The group of sclerosing bone disorders encompasses a variety of disorders all marked by increased bone mass. In this review, we give an overview of the genetic causes of this heterogeneous group of disorders and briefly touch upon the value of these findings for the development of novel therapeutic agents. RECENT FINDINGS: Advances in the next-generation sequencing technologies are accelerating the molecular dissection of the pathogenic mechanisms underlying skeletal dysplasias...
April 14, 2018: Current Osteoporosis Reports
https://www.readbyqxmd.com/read/29656298/high-expression-of-peroxiredoxin-1-is-associated-with-epithelial-mesenchymal-transition-marker-and-poor-prognosis-in-gastric-cancer
#3
Wei Yu, Jing Wu, Zhong-Liang Ning, Qiao-Yu Liu, Rui-Liang Quan
BACKGROUND Recent studies show that peroxiredoxin 1 (Prdx1) contributes to the progression and poor prognosis of carcinoma through multiple mechanisms. However, there is little information on its expression and prognostic value in gastric cancer. This study investigated the expression of Prdx1 in gastric cancer, along with evaluating its clinical-pathological and prognostic importance. MATERIAL AND METHODS A total of 189 pairs of gastric cancer and paracarcinomatous tissues were assessed for Prdx1 expression and its association with clinical characteristics...
April 15, 2018: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
https://www.readbyqxmd.com/read/29656030/post-stroke-depression-the-sequelae-of-cerebral-stroke
#4
REVIEW
Jyotirekha Das, G K Rajanikant
Post-stroke depression (PSD) is the most common mental health issue, afflicting around 33% of stroke survivors. PSD has a negative impact on the rehabilitation, recuperation of motor and cognitive deficits following stroke and significantly increases the chances of relapsing neurovascular events. It has been demonstrated that biological and psychological factors have a significant role in PSD. Numerous endeavors have been made to discover the risk factors and predictors of PSD. Screening and diagnosis also have gained attention; however, a suitable tool is yet to be developed...
April 12, 2018: Neuroscience and Biobehavioral Reviews
https://www.readbyqxmd.com/read/29655702/4-2-4-chlorophenyl-1-4-chlorophenyl-amino-ethyl-benzene-1-3-diol-is-a-potential-agent-for-gout-therapy-as-a-dual-inhibitor-of-xod-and-nlrp3
#5
Mengze Zhou, Suning Li, Ling Song, Qinghua Hu, Wentao Liu
BACKGOUND: Gout is an inflammatory arthritis characterized by abrupt self-limiting attacks of inflammation caused by precipitation of monosodium urate crystals (MSU) in the joint. Both anti-hyperuricemia and anti-inflammation could be gout therapeutic strategies, whereas ideal drugs for gout treatment are deficient. PURPOSE: 4-(2-(4-chlorophenyl)-1-((4-chlorophenyl)amino)ethyl)benzene-1, 3-diol (CBED) was obtained from a cluster of deoxybenzoins derivatives synthesized by our research group with potent anti-hyperuricemic and anti-inflammatory activities, which was expected to be a dual inhibitor of xanthine oxidase (XOD) and NOD-like receptor protein 3 (NLRP3)...
March 15, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/29655682/pristimerin-a-naturally-occurring-triterpenoid-attenuates-tumorigenesis-in-experimental-colitis-associated-colon-cancer
#6
Ju-Hyung Park, Jin-Kyung Kim
BACKGROUND: Pristimerin is a quinonemethide triterpenoid with anti-cancer, anti-angiogenic, anti-inflammatory and anti-protozoal activity. However, the therapeutic role of pristimerin in colitis-associated colorectal carcinogenesis is unknown. PURPOSE: We sought to examine the therapeutic effects of pristimerin on colitis-associated colon cancer induced in mice using azoxymethane (AOM)/dextran sulfate sodium (DSS). The goal was to identify the potential mechanism of action underlying the pharmacological activity of pristimerin...
March 15, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/29655681/anti-inflammatory-activity-of-khayandirobilide-a-from-khaya-senegalensis-via-nf-%C3%AE%C2%BAb-ap-1-and-p38-mapk-nrf2-ho-1-signaling-pathways-in-lipopolysaccharide-stimulated-raw-264-7-and-bv-2-cells
#7
Miao-Miao Zhou, Wen-Yan Zhang, Rui-Jun Li, Chao Guo, Shan-Shan Wei, Xiao-Meng Tian, Jun Luo, Ling-Yi Kong
BACKGROUND: Immunocytes-involved inflammation is considered to modulate the damage in various diseases. Herein, novel therapeutics suppressing over-activation of immunocytes could prove an effective strategy to prevent inflammation-related diseases. PURPOSE: The objective of this study is to evaluate the anti-inflammatory activity of Khayandirobilide A (KLA), a new andirobin-type limonoid with modified furan ring isolated from the Khaya senegalensis (Desr.) A. Juss...
March 15, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/29653141/dual-mechanism-of-type-vii-collagen-transfer-by-bone-marrow-mesenchymal-stem-cell-extracellular-vesicles-to-recessive-dystrophic-epidermolysis-bullosa-fibroblasts
#8
Jeffrey McBride, Luis Rodriguez-Menocal, Ambar Candanedo, Wellington Guzman, Marta Garcia-Contreras, Evangelos Badiavas
Recessive dystrophic epidermolysis bullosa (RDEB) is a severe blistering disease resulting from a lack of type VII collagen production. Recent clinical trials have shown efficacy of bone marrow-derived mesenchymal stem cells (BM-MSCs) in the treatment of epidermolysis bullosa, including improved basement membrane restructuring and cutaneous wound healing. The mechanism as to how type VII collagen is transferred from donor stem cell to recipient RDEB cells has not been defined. Here, we submit the model that BM-MSC-derived extracellular vesicles serve at least two roles: 1) to help transport type VII collagen within the extracellular space; and 2) to feed RDEB fibroblasts with messenger RNA that codes for type VII collagen, resulting in COL7A1 translation and synthesis of type VII collagen alpha chain proteins by RDEB fibroblasts...
April 10, 2018: Biochimie
https://www.readbyqxmd.com/read/29652968/-therapeutic-monitoring-of-antimicrobial-agents-in-pediatrics-review-based-on-latin-american-experiences
#9
Brenda Zylbersztajn, Marlon Barraza, Juan P Torres, Jorge Morales
This review summarizes recommendations of therapeutic monitoring of three antimicrobials based in regional data: vancomycin, amikacin and voriconazole in pediatric population. Regional evidence agrees with international literature regarding the requirement of higher daily doses than 40 mg/kg/day of vancomycin, as well as with the possibility of use one daily doses of amikacin and to recommend higher doses of voriconazole compared to the initially recommended doses of 8 mg/kg/day. Local data on the pharmacokinetic/pharmacodynamic behavior of various antimicrobials in pediatrics are of great value for dosing adjustment in our pediatric population...
2018: Revista Chilena de Infectología: órgano Oficial de la Sociedad Chilena de Infectología
https://www.readbyqxmd.com/read/29652864/honey-bee-as-alternative-medicine-to-treat-eleven-multidrug-resistant-bacteria-causing-urinary-tract-infection-during-pregnancy
#10
Mabrouka Bouacha, Hayette Ayed, Nedjoud Grara
Medicinal benefits of honey bee have been recognized in the medical community since ancient times as a remedy for many diseases and infections. This study aimed to investigate the in vitro susceptibility of 11 multidrug-resistant bacterial strains, isolated from urinary tract infections of pregnant women, to six honey samples collected from different localities in the east of Algeria. The evaluation of the antibacterial activity was performed by the well method followed by the broth dilution method using two-fold dilutions of each honey sample ranging from 2...
April 13, 2018: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/29652700/overall-disability-sum-score-for-clinical-assessment-of-neurological-involvement-in-eosinophilic-granulomatosis-with-polyangiitis
#11
Roberto Padoan, Maddalena Marconato, Mara Felicetti, Francesco Cinetto, Mariachiara Cerchiaro, Francesca Rizzo, Renzo Marcolongo, Leonardo Punzi, Carlo Agostini, Franco Schiavon
AIM: The aim of this study was to verify the application of Overall Disability Sum Score (ODSS) for standardized clinical assessment of neurological involvement in patients with eosinophilic granulomatosis with polyangiitis (EGPA) and its correlation with treatment response and long-term outcomes. METHODS: Consecutive EGPA patients referred to our tertiary vasculitis center were retrospectively evaluated. Patients' neurological damage and disability were systematically assessed with Vasculitis Damage Index and ODSS...
April 13, 2018: Journal of Clinical Rheumatology: Practical Reports on Rheumatic & Musculoskeletal Diseases
https://www.readbyqxmd.com/read/29652421/arterial-hypertension-after-age-65-from-epidemiology-and-pathophysiology-to-therapy-do-we-know-where-we-stand
#12
Jerzy Gąsowski, Karolina Piotrowicz, Franz H Messerli
Arterial hypertension is a prevalent disease with great harming potential. After the age of 55 years the remaining lifetime risk of hypertension amounts to 90%. Despite the constant advances some important issues such as the cut-off blood pressure for the initiation of antihypertensive therapy or the therapeutic goal are debated. In this review, we present - based on the available literature - the current concepts concerning the pathophysiology, epi-demiology and antihypertensive therapy in patients aged 65 years or older...
2018: Kardiologia Polska
https://www.readbyqxmd.com/read/29652200/bursera-copallifera-extracts-have-cytotoxic-and-migration-inhibitory-effects-in-breast-cancer-cell-lines
#13
Fabiola Domínguez, Paola Maycotte, Adilene Acosta-Casique, Sofía Rodríguez-Rodríguez, Diego A Moreno, Federico Ferreres, Juan Carlos Flores-Alonso, María Guadalupe Delgado-López, Martín Pérez-Santos, Maricruz Anaya-Ruiz
Plants from the Bursera genus are widely distributed in the tropical dry forests of Mexico. In traditional medicine, extracts from different species of Bursera have been used for a wide range of biological activities, including the treatment of cancer-related symptoms. Compounds present in the Bursera genus include lignans, flavonoids, steroids, short-chain aliphatic alkanes, acetates, alcohols, ketones, and terpenoids. In some instances, secondary metabolites of these classes of compounds may induce cytotoxicity, and therefore we sought to investigate the effects of B...
April 1, 2018: Integrative Cancer Therapies
https://www.readbyqxmd.com/read/29652045/-the-medical-recreational-and-balneotherapeutic-regions-of-the-krasnoyarsk-territory
#14
N K Dzhabarova, N G Sidorina, I N Smirnova, A A Kokhanenko, N G Klopotova
BACKGROUND: the creation of the efficient system of the spa and health resort-based health care for the population of the entire territory of the Russian Federation requires the systematic evaluation and protection of the natural resources of country as a basis for the further development of the health resort and recreation facilities in different regions. AIM: The objective of the present study was to estimate the possibilities of expansion of the health resort and recreational activities based on the rational exploitation of the natural resources of the medical-recreational and balneotherapeutic areas of the Krasnoyarsk Territory...
April 9, 2018: Voprosy Kurortologii, Fizioterapii, i Lechebnoĭ Fizicheskoĭ Kultury
https://www.readbyqxmd.com/read/29652040/-the-physical-and-chemical-properties-of-the-skin-and-the-action-of-therapeutic-physical-factors
#15
V S Ulashchik
This article discusses the importance of the physical and chemical properties of the skin subjected to the action of the therapeutic physical factors. The author presents the data illustrating the influence of alterations in skin permeability on the penetration of medicinal substances into the organs and tissues of the body under conditions of application of various physico-pharmacological methods based on the use of chemical ingredients of peloid therapy and other balneotherapeutic technologies. The effectiveness of skin permeability is known to be of special importance in the context of physical therapy since it determines the action of its individual components...
April 9, 2018: Voprosy Kurortologii, Fizioterapii, i Lechebnoĭ Fizicheskoĭ Kultury
https://www.readbyqxmd.com/read/29651898/the-effectiveness-of-therapeutic-strategies-for-patients-with-radiculopathy-a-network-meta-analysis
#16
Xiaoyu Zhang, Zhiqiang Zhang, Jianzhong Wen, Jie Lu, Yingchun Sun, Dechun Sang
Objectives The aim of this network meta-analysis is to assess the effectiveness of therapeutic strategies for patients with radiculopathy, including physical, medical, surgical, and other therapies. Methods We electronically searched electronic databases including PubMed and Embase for randomized controlled trials. The response rate and visual analog scale of pain change were considered as primary outcomes. The outcomes were measured by odds ratio (OR) value and corresponding 95% credible intervals (CrIs) or standardized mean difference (MD) with 95% CrIs...
January 2018: Molecular Pain
https://www.readbyqxmd.com/read/29651884/kinetic-and-structural-studies-on-the-interactions-of-torpedo-californica-acetylcholinesterase-with-two-donepezil-like-rigid-analogues
#17
Rosanna Caliandro, Alessandro Pesaresi, Luca Cariati, Antonio Procopio, Manuela Oliverio, Doriano Lamba
Acetylcholinesterase inhibitors were introduced for the symptomatic treatment of Alzheimer's disease (AD). Among the currently approved inhibitors, donepezil (DNP) is one of the most preferred choices in AD therapy. The X-ray crystal structures of Torpedo californica AChE in complex with two novel rigid DNP-like analogs, compounds 1 and 2, have been determined. Kinetic studies indicated that compounds 1 and 2 show a mixed-type inhibition against TcAChE, with Ki values of 11.12 ± 2.88 and 29.86 ± 1...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/29651883/lncrna-dancr-promotes-lung-cancer-by-sequestering-mir-216a
#18
Qiang Zhen, Li-Na Gao, Ren-Feng Wang, Wei-Wei Chu, Ya-Xiao Zhang, Xiao-Jian Zhao, Bao-Lei Lv, Jia-Bao Liu
BACKGROUND: Long noncoding RNAs (lncRNAs) are a new class of cancer regulators. Here, we aimed to investigate the diagnostic and therapeutic values of an lncRNA, differentiation antagonizing noncoding RNA (DANCR), in lung cancer. METHODS: Real-time polymerase chain reaction was used to compare DANCR levels in normal and cancerous lung tissues as well as lung cancer cells. Lentiviral transduction was used to induce DANCR overexpression or silencing in vitro, followed by monitoring cell proliferation, colony formation, and changes in microRNA-216a (miR-216a) expression...
January 2018: Cancer Control: Journal of the Moffitt Cancer Center
https://www.readbyqxmd.com/read/29651698/mitogenic-activity-of-artocarpus-lingnanensis-lectin-and-its-apoptosis-induction-in-jurkat-t-cells
#19
Linjie Zeng, Lu Li, Qiyan Zeng, Yong Deng, Lijun Yin, Liejun Liao
Lectins are a class of carbohydrate-binding proteins or glycoproteins and used in the purification and characterization of glycoproteins according to their specificity to carbohydrates. In the present study, the mitogenic activity of Artocarpus lingnanensis lectin (ALL) and its apoptosis induction in Jurkat T cells were explored. MTT assay revealed strong mitogenic potential of ALL. Meanwhile, the anti-cancer activity of ALL was also explored using the human leukemic Jurkat T cell line. ALL exhibited strong binding affinity (97%) to the cell membrane, which could be effectively inhibited by N-acetyl-D-galactosaminide (NAD)...
April 12, 2018: Journal of Natural Medicines
https://www.readbyqxmd.com/read/29651562/the-evaluation-of-e-faecalis-colonies-dissolution-ability-of-sodium-hypochlorite-in-microenvironment-by-a-novel-device
#20
Xiaoqiang Sun, Shaorong Li, Shujing Wang, Chunxiong Luo, Benxiang Hou
Enterococcus faecalis(E. faecalis) is a common microorganism could be isolated from the infected canals, especially in the case of refractory apical periodontitis. Due to its ability to invade the dentinal tubules and highly resistant to antimicrobial strategies, the thorough debridement of E.faecalis is hard to achieve. And that may be one of the reasons to cause reinfection and therapeutic failure. According to the anatomy of dentinal tubules published before and the results of our team previous work, we designed six types of microtubes with different sizes...
April 12, 2018: Biomedical Microdevices
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