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https://www.readbyqxmd.com/read/28743082/characterization-and-evaluation-of-nanoencapsulated-diethylcarbamazine-in-model-of-acute-hepatic-inflammation
#1
Gabriel Barros Rodrigues, Elquio Eleamen Oliveira, Francisco Jaime Bezerra Mendonça Junior, Laise Aline Martins Dos Santos, Wilma Helena de Oliveira, Maria Eduarda Rocha de França, Deniele Bezerra Lós, Brennda Martins Gabínio, Fábia Cristiane Melo Leite de Lira, Christina Alves Peixoto
Previous studies from our laboratory have demonstrated that Diethylcarbamazine (DEC) is a potent anti-inflammatory drug. The aim of the present study was to characterize the nanoencapsulation of DEC and to evaluate its effectiveness in a model of inflammation for the first time. C57BL/6 mice were divided into six groups: 1) Control; 2) Carbon tetrachloride (CCl4); 3) DEC 25mg/kg+CCl4; 4) DEC 50mg/kg+CCl4; 5) DEC-NANO 05mg/kg+CCl4 and 6) DEC-NANO 12.5mg/kg+CCl4. Liver fragments were stained with hematoxylin-eosin, and processed for Western blot, ELISA and immunohistochemistry...
July 22, 2017: International Immunopharmacology
https://www.readbyqxmd.com/read/28743058/oral-nanotherapeutics-redox-nanoparticles-attenuate-ultraviolet-b-radiation-induced-skin-inflammatory-disorders-in-kud-hr-hairless-mice
#2
Chitho P Feliciano, Yukio Nagasaki
The active participation of an anti-inflammatory drug in the biological pathways of inflammation is crucial for the achievement of beneficial and therapeutic effects. This study demonstrated the development of redox nanoparticles that can circulate in the blood at significantly high levels, thus increasing their efficacy as an oral treatment against the deleterious effects of reactive oxygen species (ROS) in an in vivo inflammatory skin model. To confirm the blood bioavailability of the nanoparticles, mice were injected with the nanoparticles solution (RNP(N)) via oral gavage...
July 12, 2017: Biomaterials
https://www.readbyqxmd.com/read/28743048/the-ketogenic-diet-in-patients-with-myoclonic-status-in-non-progressive-encephalopathy
#3
Roberto Caraballo, Francesca Darra, Gabriela Reyes, Marisa Armeno, Araceli Cresta, Graciela Mestre, Bernardo Dalla Bernardina
Myoclonic status in non-progressive encephalopathy (MSNPE) is characterized by the recurrence of long-lasting atypical status epilepticus associated with attention impairment and continuous polymorphous jerks, mixed with other complex abnormal movements, in infants suffering from a non-progressive encephalopathy. The ketogenic diet (KD) has been used as an alternative to antiepileptic drugs (AEDs) for patients with refractory epileptic encephalopathies. PURPOSE: In this study we assess the efficacy and tolerability of the KD in patients with MSNPE...
July 11, 2017: Seizure: the Journal of the British Epilepsy Association
https://www.readbyqxmd.com/read/28742644/update-on-sglt2-inhibitors-new-data-released-at-the-american-diabetes-association
#4
Sara Lee
Sodium-glucose cotransporter 2 (SGLT2) inhibitors are one of the newer classes of antiglycemic agents approved for the management of patients with type 2 diabetes mellitus. Due to their unique mechanism of action, SGLT2 inhibitors have shown to be beneficial beyond glucose control. The improvement in cardiovascular (CV) outcomes was first observed in the landmark EMPA-REG OUTCOMES study. Following these results, numerous CV outcome trials were designed to identify whether the beneficial CV and renal effects observed with empagliflozin are unique or a drug class effect...
September 2017: Critical Pathways in Cardiology
https://www.readbyqxmd.com/read/28742408/risk-competence-in-dealing-with-alcohol-and-other-drugs-in-adolescence
#5
Ede Nagy, Rolf Verres, Dennis Grevenstein
BACKGROUND: Adolescence is a critical phase for the development substance use patterns. We propose that individual competence in dealing with psychoactive substances is crucial for the development of healthy substance use behavior and prevention of substance misuse or addiction. OBJECTIVES: We present a new concept of health related skills in dealing with alcohol and other drugs in adolescence, its operationalization and validation. Our conception of risk competence (RICO) consists of the four major factors being Reflective, Informed, Self-Controlled and Life-Oriented, and their sub-facets...
July 25, 2017: Substance Use & Misuse
https://www.readbyqxmd.com/read/28742385/sequential-therapy-of-breast-cancer-cell-lines-with-vitamin-c-and-quercetin-improves-the-efficacy-of-chemotherapeutic-drugs
#6
Fatemeh Ramezani, Nasser Samadi, Zohreh Mostafavi-Pour
OBJECTIVE: Prevention by antioxidant agents including vitamin C (VC) and quercetin (QU), which are nontoxic, cost effective, and physiologically bioavailable, is a promising approach in breast cancer handling. The aim of this work is to investigate the influence of VC+QU on cytotoxicity profile of doxorubicin (DOX) plus paclitaxel (PAC) in breast cancer cells. METHODS: The effect of each drug on its own or in combination was evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay...
July 25, 2017: Nutrition and Cancer
https://www.readbyqxmd.com/read/28742190/the-research-on-the-influences-of-hyperthermal-perfusion-chemotherapy-combined-with-immunologic-therapy-on-the-immunologic-function-and-levels-of-circulating-tumor-cells-of-the-advanced-colorectal-cancer-patients-with-liver-metastasis
#7
J-J Sun, G-L Fan, X-G Wang, K Xu
OBJECTIVE: To investigated the influence of hyperthermal perfusion chemotherapy combined with immunologic therapy on the immunologic function and levels of circulating tumor cells of the advanced colorectal cancer patients with liver metastasis. PATIENTS AND METHODS: We enrolled 98 advanced colorectal cancer patients with liver metastasis that were admitted to this hospital for treatment and were randomly divided into two groups, the observation group (n = 49) and the control group (n = 49)...
July 2017: European Review for Medical and Pharmacological Sciences
https://www.readbyqxmd.com/read/28742113/addition-of-17-allylamino-17-demethoxygeldanamycin-to-a-suboptimal-caspofungin-treatment-regimen-in-neutropenic-rats-with-invasive-pulmonary-aspergillosis-delays-the-time-to-death-but-does-not-enhance-the-overall-therapeutic-efficacy
#8
Jeannine M Refos, Alieke G Vonk, Marian T Ten Kate, Kimberly Eadie, Henri A Verbrugh, Irma A J M Bakker-Woudenberg, Wendy W J van de Sande
Caspofungin (CAS) which is used as salvage therapy in patients with invasive pulmonary aspergillosis (IPA) inhibits the 1,3-β-D-glucan synthesis in Aspergillus fumigatus. Inhibiting 1,3-β-D-glucan synthesis induces a stress response and in an invertebrate model it was demonstrated that inhibiting this response with geldamycin enhanced the therapeutic efficacy of CAS. Since geldamycin itself is toxic to mammalians, the therapeutic efficacy of combining geldamycin with CAS was not studied in rodent models. Therefore in this study we investigated if the geldamycin derivate 17-(allylamino)-17-demethoxygeldanamycin (17-AAG) was able to enhance the therapeutic efficacy of CAS in vitro and in our IPA model in transiently neutropenic rats...
2017: PloS One
https://www.readbyqxmd.com/read/28741970/efficacy-and-safety-of-once-weekly-semaglutide-for-the-treatment-of-type-2-diabetes
#9
Xueying Tan, Xiaojing Cao, Minzhi Zhou, Ping Zou, Jingbo Hu
Type 2 diabetes is a chronic metabolic disease characterized by persistent hyperglycemia resulting from progressive deficient of insulin in patients with a background of insulin resistance. Current treatment algorithms recommended by American Diabetes Association/The European Association for the Study of Diabetes promote a patient-centered approach that takes into account a comprehensive consideration of pharmacological properties of drugs, including glucose-lowering action, effects on body weight, correction on multiple pathophysiologic defects, tolerability, and long-term safety...
July 25, 2017: Expert Opinion on Investigational Drugs
https://www.readbyqxmd.com/read/28741967/iglarlixi-a-titratable-once-daily-fixed-ratio-combination-of-basal-insulin-and-lixisenatide-for-intensifying-type-2-diabetes-management-for-patients-inadequately-controlled-on-basal-insulin-with-or-without-oral-agents
#10
Neil Skolnik, Renell S Dupree, Eric L Johnson
BACKGROUND: Achieving and maintaining glycemic control is important for people with type 2 diabetes (T2D) in order to reduce disease-related complications and mortality; however, about half of US patients fail to meet glycemic targets. iGlarLixi, a titratable fixed-ratio combination of insulin glargine 100 U/mL (iGlar) and lixisenatide for once-daily administration, was recently approved by the US Food and Drug Administration for use in adults with T2D inadequately controlled on basal insulin (<60 U daily) or lixisenatide...
July 25, 2017: Current Medical Research and Opinion
https://www.readbyqxmd.com/read/28741798/novel-orally-bioavailable-ezh1-2-dual-inhibitors-with-greater-antitumor-efficacy-than-an-ezh2-selective-inhibitor
#11
REVIEW
Daisuke Honma, Osamu Kanno, Jun Watanabe, Junzo Kinoshita, Makoto Hirasawa, Emi Nosaka, Machiko Shiroishi, Takeshi Takizawa, Isao Yasumatsu, Takao Horiuchi, Akira Nakao, Keisuke Suzuki, Tomonori Yamasaki, Katsuyoshi Nakajima, Miho Hayakawa, Takanori Yamazaki, Ajay Singh Yadav, Nobuaki Adachi
Polycomb repressive complex 2 (PRC2) methylates histone H3 lysine 27 and represses gene expression to regulate cell proliferation and differentiation. Enhancer of zeste homolog 2 (EZH2) or its close homolog EZH1 function as catalytic subunits of PRC2, so there are two PRC2 complexes containing either EZH2 or EZH1. Tumorigenic functions of EZH2 and its synthetic lethality with some subunits of SWItch/Sucrose Non-Fermentable (SWI/SNF) chromatin remodeling complexes have been observed. However, little is known about the function of EZH1 in tumorigenesis...
July 25, 2017: Cancer Science
https://www.readbyqxmd.com/read/28741391/clinical-implications-benefits-and-pitfalls-of-using-and-reversing-non-vitamin-k-antagonist-oral-anticoagulants
#12
Alexandra S Moss, Gerasimos Dimitropoulos, Gregory Y H Lip
The use of non-Vitamin K antagonist oral anticoagulant (NOAC) drugs is increasingly common in clinical practice. As compared to vitamin K antagonists they are more straightforward to initiate, require no hematological monitoring and offer potentially more stable therapeutic indices. Concern has been raised with regard to their safety profiles particularly in the context of acute reversal in major bleeding. Further issues pertain to patient concordance. Areas Covered: This review article aims to provide an overview of the current evidence relating to NOAC safety as well as the management of NOAC-related major bleeding with particular emphasis on reversal agents in use and in development following a selective literature review...
July 25, 2017: Expert Review of Hematology
https://www.readbyqxmd.com/read/28741382/sodium-glucose-co-transporter-2-inhibitor-luseogliflozin-in-the-management-of-type-2-diabetes-a-drug-safety-evaluation
#13
Daisuke Yabe, Yoshiyuki Hamamoto, Yusuke Seino, Hitoshi Kuwata, Takeshi Kurose, Yutaka Seino
Sodium glucose co-transporter-2 (SGLT2) inhibitors have been developed recently as a new class of anti-diabetic drug, and are becoming widely used in the management of type 2 diabetes (T2D). As these agents have a considerably different glucose-lowering mechanism from those of other anti-diabetic drugs, safe use of this drug class needs to be discussed based on data available from preapproval clinical trials as well as real-world studies. The SGLT2 inhibitor luseogliflozin was developed by Taisho Pharmaceutical Co...
July 25, 2017: Expert Opinion on Drug Safety
https://www.readbyqxmd.com/read/28741279/identification-of-lead-molecules-in-garcinia-mangostana-l-against-pancreatic-cholesterol-esterase-activity-an-in-silico-approach
#14
George Kadakasseril Varghese, Rini Abraham, Nisha N Chandran, Solomon Habtemariam
Hypercholesterolemia is one of the major risk factors for the development and progression of atherosclerosis. Hence, inhibitors of cholesterol absorption have been investigated for decades as a strategy to prevent and treat cardiovascular diseases associated with hypercholesterolemia. Cholesterol esterase (CEase) in pancreatic juice plays a vital role in the hydrolysis of dietary cholesterol esters to cholesterol and fatty acids. Since inhibition of CEase might lead to a reduction of cholesterol absorption, an attempt is made in this study to identify lead molecules of Garcinia mangostana by the in silico approach...
July 24, 2017: Interdisciplinary Sciences, Computational Life Sciences
https://www.readbyqxmd.com/read/28741274/cyclin-dependent-kinase-4-6-inhibitors-in-breast-cancer-palbociclib-ribociclib-and-abemaciclib
#15
REVIEW
Dorota Kwapisz
PURPOSE: The cyclin D-cyclin dependent kinase (CDK) 4/6-inhibitor of CDK4 (INK4)-retinoblastoma (Rb) pathway plays a crucial role in cell cycle progression and its dysregulation is an important contributor to endocrine therapy resistance. CDK4/6 inhibitors trigger cell cycle arrest in Rb protein (pRb)-competent cells. Recent years have seen the development of selective CDK4/6 inhibitors, which have delivered promising results of efficacy and manageable safety profiles. The main objective of this review is to discuss preclinical and clinical data to date, and ongoing clinical trials with palbociclib, ribociclib, and abemaciclib in breast cancer...
July 24, 2017: Breast Cancer Research and Treatment
https://www.readbyqxmd.com/read/28741150/eslicarbazepine-acetate-a-new-improvement-on-a-classic-drug-family-for-the-treatment-of-partial-onset-seizures
#16
REVIEW
Graciana L Galiana, Angela C Gauthier, Richard H Mattson
Eslicarbazepine acetate is a new anti-epileptic drug belonging to the dibenzazepine carboxamide family that is currently approved as adjunctive therapy and monotherapy for partial-onset (focal) seizures. The drug enhances slow inactivation of voltage-gated sodium channels and subsequently reduces the activity of rapidly firing neurons. Eslicarbazepine acetate has few, but some, drug-drug interactions. It is a weak enzyme inducer and it inhibits cytochrome P450 2C19, but it affects a smaller assortment of enzymes than carbamazepine...
July 24, 2017: Drugs in R&D
https://www.readbyqxmd.com/read/28741130/epigenetic-involvement-in-etiopathogenesis-and-implications-in-treatment-of-systemic-lupus-erythematous
#17
REVIEW
Arron Munggela Foma, Saeed Aslani, Jafar Karami, Ahmadreza Jamshidi, Mahdi Mahmoudi
BACKGROUND: Recent researches in the field of genetics have extended our knowledge through the discovery of genetic factors associated with autoimmune diseases (AID). Genetics by itself, however, cannot elucidate all the uncertainties encountered in the etiopathology of AID. On the other hand, incomplete harmony in the prevalence of AID in identical twins suggests that non-genetic factors may play an important role in determining the disease susceptibility. Besides, epigenetics, which is defined by changes in gene expression without a corresponding change in the DNA sequences, has come in to provide new awareness in the disease etiopathology by bridging the genetic and epigenetic factors...
July 24, 2017: Inflammation Research: Official Journal of the European Histamine Research Society ... [et Al.]
https://www.readbyqxmd.com/read/28741044/efficacy-and-tolerability-of-asenapine-compared-with-olanzapine-in-borderline-personality-disorder-an-open-label-randomized-controlled-trial
#18
Paola Bozzatello, Paola Rocca, Maria Uscinska, Silvio Bellino
BACKGROUND: Asenapine is a new second-generation antipsychotic that is understudied in borderline personality disorder (BPD). Only one study investigating the use of the drug in this indication (an open-label pilot study) has been conducted to date. OBJECTIVE: The present open-label, randomized, controlled trial aimed to evaluate the efficacy and tolerability of asenapine in comparison with olanzapine, the most broadly studied antipsychotic in BPD. METHODS: A total of 51 outpatients aged between 18 and 50 years with a diagnosis of BPD based on Diagnostic and Statistical Manual of Mental Disorders, Fifth Edition (DSM-5) criteria were assigned for 12 weeks to asenapine (5-10 mg/day) or olanzapine (5-10 mg/day)...
July 24, 2017: CNS Drugs
https://www.readbyqxmd.com/read/28740616/unlocking-the-potential-of-established-products-toward-new-incentives-rewarding-innovation-in-europe
#19
Gabrielle Nayroles, Sandrine Frybourg, Sylvie Gabriel, Åsa Kornfeld, Fernando Antoñanzas-Villar, Jaime Espín, Claudio Jommi, Nello Martini, Gérard de Pouvourville, Keith Tolley, Jürgen Wasem, Mondher Toumi
Background: Many established products (EPs - marketed for eight years or more) are widely used off-label despite little evidence on benefit-risk ratio. This exposes patients to risks related to safety and lack of efficacy, and healthcare providers to liability. Introducing new indications for EPs may represent a high societal value; however, manufacturers rarely invest in R&D for EPs. The objective of this research was to describe incentives and disincentives for developing new indications for EPs in Europe and to investigate consequences of current policies...
2017: Journal of Market Access & Health Policy
https://www.readbyqxmd.com/read/28740614/new-class-of-antitrypanosomal-agents-based-on-imidazopyridines
#20
Daniel G Silva, J Robert Gillespie, Ranae M Ranade, Zackary M Herbst, Uyen T T Nguyen, Frederick S Buckner, Carlos A Montanari, Michael H Gelb
The present work describes the synthesis of 22 new imidazopyridine analogues arising from medicinal chemistry optimization at different sites on the molecule. Seven and 12 compounds exhibited an in vitro EC50 ≤ 1 μM against Trypanosoma cruzi (T. cruzi) and Trypanosoma brucei (T. brucei) parasites, respectively. Based on promising results of in vitro activity (EC50 < 100 nM), cytotoxicity, metabolic stability, protein binding, and pharmacokinetics (PK) properties, compound 20 was selected as a candidate for in vivo efficacy studies...
July 13, 2017: ACS Medicinal Chemistry Letters
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