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https://www.readbyqxmd.com/read/29475164/thiazolidinediones-as-antidiabetic-agents-a-critical-review
#1
REVIEW
M J Nanjan, Manal Mohammed, B R Prashantha Kumar, M J N Chandrasekar
Thiazolidinediones (TZDs) or Glitazones are an important class of insulin sensitizers used in the treatment of Type 2 diabetes mellitus (T2DM). TZDs were reported for their antidiabetic effect through antihyperglycemic, hypoglycemic and hypolipidemic agents. In time, these drugs were known to act by increasing the transactivation activity of Peroxisome Proliferators Activated Receptors (PPARs). The clinically used TZDs that suffered from several serious side effects and hence withdrawn/updated later, were full agonists of PPAR-γ and potent insulin sensitizers...
February 12, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29475156/potent-hydrazone-derivatives-targeting-esophageal-cancer-cells
#2
Ling-Yu Li, Jia-Di Peng, Wenjuan Zhou, Hui Qiao, Xin Deng, Zhou-Hua Li, Ji-Deng Li, Yun-Dong Fu, Song Li, Kai Sun, Hong-Min Liu, Wen Zhao
Hydrazone and their derivatives are a series of highly active molecules, which are widely used as lead compounds for the research and development of new anti-cancer drugs. In this study, 20 compounds were synthesized, based on this scaffold and their in vitro cytotoxicity against 6 cancer cell lines, including EC9706, SMMC-7721, MCF7, PC3, MGC-803 and EC109 was tested. Among them, compound 6p, showed strong anti-proliferative activities on esophageal carcinoma cells: EC9706 and EC109 with IC50 values of 1...
February 14, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29475141/quercetin-enhances-chemotherapeutic-effect-of-doxorubicin-against-human-breast-cancer-cells-while-reducing-toxic-side-effects-of-it
#3
Shizheng Li, Song Yuan, Qian Zhao, Bo Wang, Xiuyan Wang, Kun Li
Doxorubicin (Dox) is an efficient drug for breast cancer chemotherapy, however, its toxic side effects on non-tumor tissues, especially on myocardial cells, sometimes limit its clinical application. Therefore, it is necessary to develop a new drug, which can be combined with Dox to potentiate the anti-tumor effect of Dox at a lower concentration and attenuate the toxic side effects of it. Quercetin (Que) has anti-tumor activity in addition to its protective effects on various cells. By preparing human non-tumoral MCF-10A mammary cells, human breast cancer MCF-7 and MDA-MB-231 cells and human myocardial AC16 cells, here, we wanted to evaluate whether Que might represent such an agent and investigate its possible mechanisms of potentiating the anti-tumor effect of Dox at a lower concentration...
February 20, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29475016/dual-functionalized-nanoparticles-loaded-microbubbles-for-enhancement-of-drug-uptake
#4
Yingjia Li, Xia Zhang, Wanxian Luo, Dongxiao Wang, Li Yang, Jianguo Wang, Li Zhang, Shiyu Zhang, Shuyi Luo, Ying Wang
The application of microbubble (MB)-assisted ultrasound (US) can combine the advantages of real-time imaging and targeted drug delivery. However, the drug loading capacity of MB is limited restricting its application in antitumor procedure. In contrast, nanoparticles (NPs) can carry drugs more efficiently, but adverse side effect induced by unspecific accumulation can not be ignored. Herein, we developed a dual-functionalized NP loaded MB to investigate its potential feasibility for tumor-targeted drug delivery...
February 5, 2018: Ultrasonics
https://www.readbyqxmd.com/read/29474707/immune-relevant-models-for-ocular-inflammatory-diseases
#5
Brian C Gilger
Ocular inflammatory diseases, such as dry eye and uveitis, are common, painful, difficult to treat, and may result in vision loss or blindness. Ocular side effects from the use of antiinflammatory drugs (such as corticosteroids or nonsteroidal antiinflammatories) to treat ocular inflammation have prompted development of more specific and safer medications to treat inflammatory and immune-mediated diseases of the eye. To assess the efficacy and safety of these new therapeutics, appropriate immune-relevant animal models of ocular inflammation are needed...
February 21, 2018: ILAR Journal
https://www.readbyqxmd.com/read/29474272/an-update-in-the-initial-management-of-paediatric-status-epilepticus
#6
Ben Lawton, Tessa Davis, Henry Goldstein, Andrew Tagg
PURPOSE OF REVIEW: Over the last 2 years, algorithms for the optimal management of status epilepticus have changed, as the medical community has recognized the need to terminate seizures in status in a timely manner. Recent research has evaluated the different choices of benzodiazepine and has given consideration to second-line treatment options. RECENT FINDINGS: There has been a move to examine alternatives to phenytoin (such as levetiracetam and lacosamide) as second-line agents...
February 22, 2018: Current Opinion in Pediatrics
https://www.readbyqxmd.com/read/29473868/oncotargeting-by-vesicular-stomatitis-virus-vsv-advances-in-cancer-therapy
#7
REVIEW
Suman Bishnoi, Ritudhwaj Tiwari, Sharad Gupta, Siddappa N Byrareddy, Debasis Nayak
Modern oncotherapy approaches are based on inducing controlled apoptosis in tumor cells. Although a number of apoptosis-induction approaches are available, site-specific delivery of therapeutic agents still remain the biggest hurdle in achieving the desired cancer treatment benefit. Additionally, systemic treatment-induced toxicity remains a major limiting factor in chemotherapy. To specifically address drug-accessibility and chemotherapy side effects, oncolytic virotherapy (OV) has emerged as a novel cancer treatment alternative...
February 23, 2018: Viruses
https://www.readbyqxmd.com/read/29473765/antimicrobial-molecules-in-the-lung-formulation-challenges-and-future-directions-for-innovation
#8
Arcadia Woods, Khondaker Miraz Rahman
Inhaled antimicrobials have been extremely beneficial in treating respiratory infections, particularly chronic infections in a lung with cystic fibrosis. The pulmonary delivery of antibiotics has been demonstrated to improve treatment efficacy, reduce systemic side effects and, critically, reduce drug exposure to commensal bacteria compared with systemic administration, reducing selective pressure for antimicrobial resistance. This review will explore the specific challenges of pulmonary delivery of a number of differing antimicrobial molecules, and the formulation and technological approaches that have been used to overcome these difficulties...
February 23, 2018: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29473531/diabetic-complications-and-insight-into-antidiabetic-potentialities-of-ethno-medicinal-plants-a-review
#9
Muhammad Bilal, Muhammad Sarfaraz Iqbal, Syed Bilal Shah, Tahir Rasheed, Hafiz M N Iqbal
BACKGROUND: The naturally inspired treatment options for several disease conditions and human-health related disorders such as diabetes mellitus have gained considerable research interest. In this context, naturally occurring plants and herbs with medicinal functionalities have gained special place than ever before in the current medicinal world. OBJECTIVE: The objective of this review is to extend the current knowledge in the clinical field related to the diabetic complications...
February 21, 2018: Recent Patents on Inflammation & Allergy Drug Discovery
https://www.readbyqxmd.com/read/29473291/bayesian-approach-for-assessing-noninferiority-in-a-three-arm-trial-with-binary-endpoint
#10
Santu Ghosh, Ram C Tiwari, Samiran Ghosh
With the recent advancement in many therapeutic areas, quest for better and enhanced treatment options is ever increasing. While the "efficacy" metric plays the most important role in this development, emphasis on other important clinical factors such as less intensive side effects, lower toxicity, ease of delivery, and other less debilitating factors may result in the selection of treatment options, which may not beat current established treatment option in terms efficacy, yet prove to be desirable for subgroups of patients...
February 22, 2018: Pharmaceutical Statistics
https://www.readbyqxmd.com/read/29473233/highly-augmented-drug-loading-and-stability-of-micellar-nanocomplexes-composed-of-doxorubicin-and-poly-ethylene-glycol-green-tea-catechin-conjugate-for-cancer-therapy
#11
Kun Liang, Joo Eun Chung, Shu Jun Gao, Nunnarpas Yongvongsoontorn, Motoichi Kurisawa
Low drug loading and instability in blood circulation are two key challenges that impede the successful clinical translation of nanomedicine, as they result in only marginal therapeutic efficacy and toxic side effects associated with premature drug leakage, respectively. Herein, highly stable and ultrahigh drug loading micellar nanocomplexes (MNCs) based on the self-assembly of the anticancer drug doxorubicin (DOX) and a poly(ethylene glycol)-epigallocatechin-3-O-gallate (EGCG) conjugate are developed. The formation of these MNCs is facilitated by strong favorable intermolecular interactions between the structurally similar aromatic EGCG and DOX molecules, which impart exceptionally high drug-loading capability of up to 88% and excellent thermodynamic and kinetic stability...
February 23, 2018: Advanced Materials
https://www.readbyqxmd.com/read/29473131/searching-for-new-drugs-for-chagas-diseases-triazole-analogs-display-high-in-vitro-activity-against-trypanosoma-cruzi-and-low-toxicity-toward-mammalian-cells
#12
Robson Xavier Faria, Daniel Tadeu Gomes Gonzaga, Paulo Anastácio Furtado Pacheco, André Luis Almeida Souza, Vitor Francisco Ferreira, Fernando de Carvalho da Silva
Chagas disease is one of the most relevant endemic diseases in Latin America caused by the flagellate protozoan Trypanosoma cruzi. Nifurtimox and benzonidazole are the drugs used in the treatment of this disease, but they commonly are toxic and present severe side effects. New effective molecules, without collateral effects, has promoted the investigation to develop new lead compounds with to advance for clinical trials. Previously, 3-nitro-1H-1,2,4-triazole-based amines and 1,2,3-triazoles demonstrated significant trypanocidal activity against T...
February 23, 2018: Journal of Bioenergetics and Biomembranes
https://www.readbyqxmd.com/read/29473096/influence-of-gemcitabine-chemotherapy-on-the-microbiota-of-pancreatic-cancer-xenografted-mice
#13
Concetta Panebianco, Kaarel Adamberg, Madis Jaagura, Massimiliano Copetti, Andrea Fontana, Signe Adamberg, Kaia Kolk, Raivo Vilu, Angelo Andriulli, Valerio Pazienza
BACKGROUND AND AIMS: Pancreatic ductal adenocarcinoma (PDAC) represents the fourth cause of cancer-related death. We aimed to evaluate whether gemcitabine treatment shapes the gut microbiota in a model of PDAC xenografted mice. MATERIALS AND METHODS: Pancreatic cancer xenograft mice were subjected to gemcitabine injection once per week for 3 weeks to assess the tumor volume as compared to control mice injected with normal saline solution. The composition of fecal microbiota, the activation of NF-kB pathway in cancer tissues and the serum metabolomics were further analyzed...
February 22, 2018: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/29473075/monascin-inhibits-il-1%C3%AE-induced-catabolism-in-mouse-chondrocytes-and-ameliorates-murine-osteoarthritis
#14
Gang Zheng, Yu Zhan, Qian Tang, Tianhe Chen, Fanghong Zheng, Haoli Wang, Jianle Wang, Dengying Wu, Xiaobing Li, Ying Zhou, Xiaobin Wang, Yaosen Wu, Yifei Zhou, Huazi Xu, Naifeng Tian, Xiaolei Zhang
Osteoarthritis (OA) is an age-related degenerative disease and is the fourth major cause of disability, but there are no effective therapies because of its complex pathology and the side effects of the drugs. Previous research demonstrated that inflammation and ECM degradation play major roles in OA development. Monascin is an azaphilonoid pigment extracted from Monascus-fermented rice with a potential anti-inflammatory effect reported in various preclinical studies. In the present study, we investigated the protectiveness of monascin on interleukin (IL)-1β-induced mouse chondrocytes and surgical destabilization of the medial meniscus mouse (DMM) OA models...
February 23, 2018: Food & Function
https://www.readbyqxmd.com/read/29473044/cardiotoxicity-of-anticancer-therapeutics
#15
REVIEW
Jerry Dong, Hong Chen
As cancer therapeutics continues to improve and progress, the adverse side effects associated with anticancer treatments have also attracted more attention and have become extensively explored. Consequently, the importance of posttreatment follow-ups is becoming increasingly relevant to the discussion. Contemporary treatment methods, such as tyrosine kinase inhibitors, anthracycline chemotherapy, and immunotherapy regimens are effective in treating different modalities of cancers; however, these reagents act through interference with DNA replication or prevent DNA repair, causing endothelial dysfunction, generating reactive oxygen species, or eliciting non-specific immune responses...
2018: Frontiers in Cardiovascular Medicine
https://www.readbyqxmd.com/read/29472768/effect-of-zhen-qi-fu-zheng-granules-on-the-bone-marrow-depression-model-induced-by-zidorf
#16
Mingsan Miao, Lihua Cao, Ming Bai, Gangling Chen
Zidorf is a commonly used drug for the treatment of AIDS, the most common side effects of AZT was bone marrow depression. Therefore, we investigated the effects of Zhen Qi Fu Zheng (AQFZ) granules on the model of bone marrow depression induced by AZT. We showed that the high, medium and low doses of AQFZ granules could increase the number of WBC in the mice model induced by AZT, and the difference was significant ( P  < 0.01) compared with the model group. Each dose of AQFZ granules can increase the thymus cortex thickness, the number of thymus lymphocytes, spleen nodule size, the number of lymphocytes in the spleen ( P  < 0...
February 2018: Saudi Journal of Biological Sciences
https://www.readbyqxmd.com/read/29471963/-hepatotoxicity-of-tyrosine-kinase-inhibitors-mechanisms-involved-and-practical-implications
#17
REVIEW
Dominique Béchade, Camille Chakiba, Marie Desjardin, Yves Bécouarn, Marianne Fonck
Tyrosine kinase inhibitors (TKIs) are used for the targeted treatment of solid cancers. TKIs produce a variable incidence of liver adverse events (5-25%) which can progress to severe liver injury in a minority of patients if treatment is maintained despite ongoing injury. This risk requires careful patient management to maintain treatment benefit without harm. This review highlights the various mechanisms of idiosyncratic hepatotoxicity, the formation of reactive metabolites and how this leads to toxicity. These critical events depend of the drug-specific characteristics of each TKI and the patient risk factors, especially genetic characterization...
February 19, 2018: Bulletin du Cancer
https://www.readbyqxmd.com/read/29471839/controlled-education-of-patients-after-stroke-ceops-nurse-led-multimodal-and-long-term-interventional-program-involving-a-patient-s-caregiver-to-optimize-secondary-prevention-of-stroke-study-protocol-for-a-randomized-controlled-trial
#18
Anne-Marie Mendyk, Alain Duhamel, Yannick Bejot, Didier Leys, Laurent Derex, Olivier Dereeper, Olivier Detante, Pierre-Yves Garcia, Olivier Godefroy, Francisco Macian Montoro, Jean-Philippe Neau, Sébastien Richard, Thierry Rosolacci, Igor Sibon, Denis Sablot, Serge Timsit, Mathieu Zuber, Charlotte Cordonnier, Régis Bordet
BACKGROUND: Setting up a follow-up secondary prevention program after stroke is difficult due to motor and cognitive impairment, but necessary to prevent recurrence and improve patients' quality of life. To involve a referent nurse and a caregiver from the patient's social circle in nurse-led multimodal and long-term management of risk factors after stroke could be an advantage due to their easier access to the patient and family. The aim of this study is to compare the benefit of optimized follow up by nursing personnel from the vascular neurology department including therapeutic follow up, and an interventional program directed to the patient and a caregiving member of their social circle, as compared with typical follow up in order to develop a specific follow-up program of secondary prevention of stroke...
February 22, 2018: Trials
https://www.readbyqxmd.com/read/29471572/-cardiovascular-medication-in-elderly-patients
#19
Robert H G Schwinger
Elderly people show increased probability to develop atherosclerotic diseases; in consequence heart failure - most often following coronary heart disease - as well as atrial fibrillation is more common. Following guidelines may lead to polypharmacy, i. e. use of more than 5 drugs daily. Thus, drug interactions as well as side effects become more likely; especially in elderly patients reduced kidney function has to be taken into account. Only drugs which have shown to prolong life or to reduce symptoms in controlled clinical trials should be used...
February 2018: Deutsche Medizinische Wochenschrift
https://www.readbyqxmd.com/read/29471399/from-genome-wide-association-studies-to-mendelian-randomization-novel-opportunities-for-understanding-cardiovascular-disease-causality-pathogenesis-prevention-and-treatment
#20
Marianne Benn, Børge G Nordestgaard
The Mendelian randomization approach is an epidemiologic study design incorporating genetic information into traditional epidemiologic studies to infer causality of biomarkers, risk factors, or lifestyle factors on disease risk. Mendelian randomization studies often draw on novel information generated in genome-wide association studies on causal associations between genetic variants and a risk factor or lifestyle factor. Such information can then be used in a largely unconfounded study design free of reverse causation to understand if and how risk factors and lifestyle factors cause cardiovascular disease...
February 19, 2018: Cardiovascular Research
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