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https://www.readbyqxmd.com/read/28821158/synthesis-characterization-bioactivity-and-potential-application-of-phenolic-acid-grafted-chitosan-a-review
#1
REVIEW
Jun Liu, Huimin Pu, Shuang Liu, Juan Kan, Changhai Jin
In recent years, increasing attention has been paid to the grafting of phenolic acid onto chitosan in order to enhance the bioactivity and widen the application of chitosan. Here, we present a comprehensive overview on the recent advances of phenolic acid grafted chitosan (phenolic acid-g-chitosan) in many aspects, including the synthetic method, structural characterization, biological activity, physicochemical property and potential application. In general, four kinds of techniques including carbodiimide based coupling, enzyme catalyzed grafting, free radical mediated grafting and electrochemical methods are frequently used for the synthesis of phenolic acid-g-chitosan...
October 15, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28820058/editorial-neurodegenerative-disorders-synthesis-drug-delivery-strategies-and-biological-evaluation-of-new-therapeutic-agents
#2
EDITORIAL
Antonio Di Stefano, Marcella Reale
No abstract text is available yet for this article.
2017: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28820051/bisthiourea-derivatives-of-dipeptide-conjugated-benzo-d-isoxazole-as-a-new-class-of-therapeutics-synthesis-and-molecular-docking-studies
#3
H K Kumara, D M Suyoga Vardhan, J Shiva Kumar, D Channe Gowda
We have synthesized a series of bisthiourea derivatives of dipeptides (Lys/lys-Asp and Lys/lys-Trp) conjugated benzo[d]isoxazole and the structures of synthesized compounds were confirmed by correlating their physical and spectroscopic data with earlier data. The molecules 1-24 were examined for their in vitro anti-inflammatory activity by employing human erythrocyte suspension test and it was found that the IC50 values of 9, 12, 21 and 24 were lower than the IC50 of standard references indomethacin and ibuprofen...
August 16, 2017: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28819698/sublethal-effects-of-pyrethroid-and-neonicotinoid-insecticides-on-iphiseiodes-zuluagai-denmark-and-muma-mesostigmata-phytoseiidae
#4
Odimar Zanuzo Zanardi, Gabriela Pavan Bordini, Aline Aparecida Franco, Cynthia Renata Oliveira Jacob, Pedro Takao Yamamoto
The predator mite Iphiseiodes zuluagai Denmark & Muma is an important biological-control agent of mite pests, and it is one of the most common species found in citrus orchards. This study assessed, under laboratory conditions, the toxicity and duration of the harmful effects of five insecticides, the three pyrethroids deltamethrin, esfenvalerate and lambda-cyhalothrin, and the two neonicotinoids imidacloprid and thiamethoxam on I. zuluagai. Furthermore, we estimated the life-table parameters of the predator...
August 17, 2017: Ecotoxicology
https://www.readbyqxmd.com/read/28819543/diosmin-attenuates-methotrexate-induced-hepatic-renal-and-cardiac-injury-a-biochemical-and-histopathological-study-in-mice
#5
Mohamed M Abdel-Daim, Hesham A Khalifa, Abdelrahman Ibrahim Abushouk, Mohamed A Dkhil, Saleh A Al-Quraishy
The current study was designed to investigate the beneficial role of diosmin, a biologically active flavonoid, against methotrexate- (MTX-) induced hepatic, renal, and cardiac injuries in mice. Male Swiss albino mice received a single intraperitoneal injection of MTX (at 20 mg/kg, body weight) either alone or in combination with oral diosmin (at 50 or 100 mg/kg body weight, for 10 days). Serum was used to evaluate tissue injury markers, while hepatic, renal, and cardiac tissue samples were obtained for determination of antioxidant activity as well as histopathological examination...
2017: Oxidative Medicine and Cellular Longevity
https://www.readbyqxmd.com/read/28819273/enhanced-anaerobically-digested-swine-wastewater-treatment-by-the-composite-of-polyaluminum-chloride-pac-and-bacillus-megatherium-g106-derived-eps
#6
Junyuan Guo, Yang Huang, Cheng Chen, Yu Xiao, Jing Chen, Biyu Jian
A strain was isolated from biological sludge to produce EPS by using anaerobically digested swine wastewater (ADSW). Potential of the EPS in ADSW treatment were discussed. Results showed that the optimal fermentation medium for EPS production was determined as 4 g K2HPO4, 2 g KH2PO4, and 2 g sucrose dissolved in 1 L ADSW. After fermentation for 60 h, 2.98 g EPS with main backbone of polysaccharides can be extracted from 1 L of fermentation broth. The EPS showed good performances in ADSW treatment, after conditioned by this EPS, removal efficiencies of COD, ammonia, and TP reached 70...
August 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28819220/nosema-ceranae-fipronil-and-their-combination-compromise-honey-bee-reproduction-via-changes-in-male-physiology
#7
Guillaume Kairo, David G Biron, Faten Ben Abdelkader, Marc Bonnet, Sylvie Tchamitchian, Marianne Cousin, Claudia Dussaubat, Boris Benoit, André Kretzschmar, Luc P Belzunces, Jean-Luc Brunet
The honey bee is threatened by biological agents and pesticides that can act in combination to induce synergistic effects on its physiology and lifespan. The synergistic effects of a parasite/pesticide combination have been demonstrated on workers and queens, but no studies have been performed on drones despite their essential contribution to colony sustainability by providing semen diversity and quality. The effects of the Nosema ceranae/fipronil combination on the life traits and physiology of mature drones were examined following exposure under semi-field conditions...
August 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28818768/novel-gomisin-b-analogues-as-potential-cytotoxic-agents-design-synthesis-biological-evaluation-and-docking-studies
#8
B Poornima, Bandi Siva, A Venkanna, G Shankaraiah, Nishant Jain, Dharmendra Kumar Yadav, Sanjeev Misra, K Suresh Babu
As part of pharmacological-phytochemical integrated studies on medicinal flora, Gomisin B (1) was isolated as major phytochemical lead from schisandra grandiflora, a plant traditionally used in different Asian systems of medicine. A series of 1,2,3-triazoles derivatives were synthesized at the C-7' position of the gomisin B core through diastereoselective Michael addition followed by regioselective Huisgen 1,3-dipolar cycloaddition reactions. All these triazolyl derivatives (5a-5q) were well characterized using modern spectroscopic techniques and evaluated for their anti-cancer activity against a panel of five human cancerous cell-lines...
August 1, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28818767/recent-advances-of-pyrazole-containing-derivatives-as-anti-tubercular-agents
#9
Zhi Xu, Chuan Gao, Qing-Cheng Ren, Xu-Feng Song, Lian-Shun Feng, Zao-Sheng Lv
One-third of the world's population infected tuberculosis (TB), and more than 1 million deaths annually. The co-infection between the mainly pathogen Mycobacterium tuberculosis (MTB) and HIV, and the incidence of drug-resistant TB, multi-drug resistant TB, extensively drug-resistant TB as well as totally drug-resistant TB have further aggravated the mortality and spread of this disease. Thus, there is an urgent need to develop novel anti-TB agents against both drug-susceptible and drug-resistant TB. The wide spectrum of biological activities and successful utilization of pyrazole-containing drugs in clinic have inspired more and more attention towards this kind of heterocycles...
August 3, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28818745/a-systematic-review-on-the-role-of-eicosanoid-pathways-in-rheumatoid-arthritis
#10
REVIEW
Malvina Hoxha
BACKGROUND: Rheumatoid arthritis is characterized by the production of eicosanoids, cytokines, adhesion molecules, infiltration of T and B lymphocytes in the synovium and oxygen reduction accompanied by the cartilage degradation. Eicosanoids are responsible for the progressive destruction of cartilage and bone, however neither steroids, nor the non steroidal anti-inflammatory drugs (NSAIDs), cannot slow down cartilage and bone destruction providing only symptomatic improvement. The current rheumatoid arthritis treatment options include mainly the use of disease-modifying anti-rheumatic drugs, the corticosteroids, the NSAIDs and biological agents...
August 14, 2017: Advances in Medical Sciences
https://www.readbyqxmd.com/read/28818671/incidence-and-risk-of-cardiotoxicity-in-cancer-patients-treated-with-targeted-therapies
#11
REVIEW
Matteo Santoni, Federico Guerra, Alessandro Conti, Alessandra Lucarelli, Silvia Rinaldi, Laura Belvederesi, Alessandro Capucci, Rossana Berardi
BACKGROUND: Cardiotoxicityis a serious side effect of molecularly targeted agents. The purpose of this study was to evaluate the incidence and Relative Risk (RR) of developing all-grade and high-grade cardiotoxicity in patients with solid tumors receiving targeted agents through a revised meta-analysis of available clinical trials. METHODS: The scientific literature regarding cardiotoxicity was extensively analyzed using MEDLINE, PubMed, Embase and Cochrane Central Register of Controlled Trials (CENTRAL)...
July 28, 2017: Cancer Treatment Reviews
https://www.readbyqxmd.com/read/28818421/erbb-signaling-antagonist-ameliorates-behavioral-deficit-induced-by-phencyclidine-pcp-in-mice-without-affecting-metabolic-syndrome-markers
#12
Hagar Tadmor, Idit Golani, Ravid Doron, Ilana Kremer, Alon Shamir
Schizophrenia is a severe syndrome that affects about 1% of the world population. Since the mid-1950s, antipsychotics have been used to treat schizophrenia with preference for treating positive symptoms; however, their tolerance level is low, there are numerous side effects, and only some patients respond to the treatment. Antipsychotic medications that are more effective, better tolerated, and with fewer adverse effects are urgently needed. Given the accumulating evidence of the role filled by the ErbB signaling network in the biology of the dopamine, GABA, and glutamate systems, and in the etiology of schizophrenia, we hypothesized that the ErbB network is a candidate for development of a novel agent through which various symptoms of schizophrenia and other psychiatric disorders might be treated...
August 14, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/28818362/two-year-follow-up-of-crohn-s-patients-substituted-to-certolizumab-anti-tnfa-therapy-savant-2
#13
Andrew Motlis, Moheb Boktor, Paul Jordan, Urska Cvek, Marjan Trutschl, J Steven Alexander
The effectiveness of ant-TNF 'biologic' therapy in is well supported in the management of moderate to severe Crohn's Disease (CD). Our first 'SAVANT' study was to our knowledge the first study report one- year outcomes in patients (n=60) who switched from previous anti-TNFa treatment to Cimzia/Certolizumab. This current study (SAVANT 2) follows up on longer term outcomes and provides additional clinical and biochemical data that may contribute to therapeutic responses. This IRB approved study was a retrospective analysis of the initial patients included in SAVANT 1...
August 9, 2017: Pathophysiology: the Official Journal of the International Society for Pathophysiology
https://www.readbyqxmd.com/read/28816409/genistein-represses-pepck-c-expression-in-an-insulin-independent-manner-in-hepg2-cells-and-in-alloxan-induced-diabetic-mice
#14
Barilin Dkhar, Kitboklang Khongsti, Daiahun Thabah, Donkupar Syiem, Kapaettu Satyamoorthy, Bidyadhar Das
Genistein has been reported to exert beneficial effects on type 2 diabetes mellitus (T2DM); however, the underlying molecular mechanisms involved therein have not been clearly elucidated. To address this question, the effect of the genistein on the expression of phosphoenolpyruvate carboxykinase (PEPCK), and glucose production in HepG2 cells and in alloxan-induced diabetic mice was investigated. HepG2 cells were exposed to diferrent concentration of genistein in presence or absence of modulators, and the expression of cytosolic PEPCK (PEPCK-C) and the signalling pathways was studied...
August 17, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28816107/fishing-anti-inflammatories-from-known-drugs-in-silico-repurposing-design-synthesis-and-biological-evaluation-of-bisacodyl-analogues
#15
Maité Sylla-Iyarreta Veitía, Dany Siverio Mota, Vanessa Lerari, Marta Marín, Rosa M Giner, Liliana Vicet Muro, Yankier Rivero Guerra, Françoise Dumas, Clotilde Ferroud, Peter A M de Witte, Alexander D Crawford, Vicente J Arán, Yovani Marrero Ponce
Herein is described in silico repositioning, design, synthesis, biological evaluation and structure-activity relationship (SAR) of an original class of anti-inflammatory agents based on a polyaromatic pharmacophore structurally related to bisacodyl (BSL) drug used in therapeutic as laxative. We describe the potential of TOMOCOMD-CARDD methods to find out new anti-inflammatory drug-like agents from a diverse series of compounds using the total and local atom based bilinear indices as molecular descriptors. The models obtained were validated by biological studies, identifying BSL as the first anti-inflammatory lead-like using in silico repurposing from commercially available drugs...
August 17, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28815923/biophysical-screening-of-a-focused-library-for-the-discovery-of-cyp121-inhibitors-as-novel-antimycobacterials
#16
Christian Brengel, Andreas Thomann, Alexander Schifrin, Giuseppe Allegretta, Ahmed A M Kamal, Joerg Haupenthal, Isabell Schnorr, Sang Hyun Cho, Scott Gary Franzblau, Martin Empting, Jens Eberhard, Rolf W Hartmann
The development of novel antimycobacterial agents against Mycobacterium tuberculosis (Mtb) is urgently required due to the appearance of multi-drug resistance (MDR) combined with a complicated long-term treatment. CYP121 was shown to be a promising novel target for inhibition of mycobacterial growth. In this study, we describe the rational discovery of new CYP121 inhibitors by a systematic screening based on biophysical and microbiological methods. Best hits originating from only one structural class gave first information about molecular motifs required for binding and activity...
August 16, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28815872/a-multimethod-computational-simulation-approach-for-investigating-mitochondrial-dynamics-and-dysfunction-in-degenerative-aging
#17
Timothy E Hoffman, Katherine J Barnett, Lyle Wallis, William H Hanneman
Research in biogerontology has largely focused on the complex relationship between mitochondrial dysfunction and biological aging. In particular, the mitochondrial free radical theory of aging (MFRTA) has been well accepted. However, this theory has been challenged by recent studies showing minimal increases in reactive oxygen species (ROS) as not entirely deleterious in nature, and even beneficial under the appropriate cellular circumstances. To assess these significant and nonintuitive observations in the context of a functional system, we have taken an in silico approach to expand the focus of the MFRTA by including other key mitochondrial stress response pathways, as they have been observed in the nematode Caenorhabditis elegans...
August 16, 2017: Aging Cell
https://www.readbyqxmd.com/read/28815806/evaluation-in-zebrafish-model-of-the-toxicity-of-rhodamine-b-conjugated-crotamine-a-peptide-potentially-useful-for-diagnostics-and-therapeutics
#18
Judy Yuet-Wa Chan, Hefeng Zhou, Yiu Wa Kwan, Shun Wan Chan, Gandhi Radis-Baptista, Simon Ming-Yuen Lee
Crotamine is defensin-like cationic peptide from rattlesnake venom that possesses anticancer, antimicrobial, and antifungal properties. Despite these promising biological activities, toxicity is a major concern associated with the development of venom-derived peptides as therapeutic agents. In the present study, we used zebrafish as a system model to evaluate the toxicity of rhodamine B-conjugated (RhoB) crotamine derivative. The lethal toxic concentration of RhoB-crotamine was as low as 4 μM, which effectively kill zebrafish larvae in less than 10 min...
August 16, 2017: Journal of Biochemical and Molecular Toxicology
https://www.readbyqxmd.com/read/28815424/hexamermis-popilliae-n-sp-nematoda-mermithidae-parasitizing-the-japanese-beetle-popillia-japonica-newman-coleoptera-scarabaeidae-in-italy
#19
Giuseppe Mazza, Francesco Paoli, Agostino Strangi, Giulia Torrini, Leonardo Marianelli, Giuseppino Sabbatini Peverieri, Francesco Binazzi, Giovanni Bosio, Stefano Sacchi, Claudia Benvenuti, Davide Venanzio, Emanuela Giacometto, Pio F Roversi, George O Poinar
A new species of mermithid nematode, Hexamermis popilliae n. sp. (Nematoda: Mermithidae) is described from the Japanese beetle Popillia japonica Newman in Italy, an area of new introduction for this invasive pest. The combination of the following characters separates H. popilliae from other members of the genus Hexamermis Steiner, 1924: adult head obtuse; amphidial pouches slightly posterior to lateral head papillae in female but adjacent to lateral head papillae in males; amphidial openings large, well developed; amphidial pouches elliptical in females and oblong in males; cuticular vulvar cone well developed, vulvar lips greatly reduced or lacking, vagina curved at tip where meeting uteri, without reverse bend (not S-shaped), spicules slightly curved, with a slight bend in the basal portion, approximately equal to body width at cloaca...
August 16, 2017: Systematic Parasitology
https://www.readbyqxmd.com/read/28815334/clinical-characteristics-of-patient-selection-and-imaging-predictors-of-outcome-in-solid-tumors-treated-with-checkpoint-inhibitors
#20
REVIEW
Sabrina Rossi, Luca Toschi, Angelo Castello, Fabio Grizzi, Luigi Mansi, Egesta Lopci
The rapidly evolving knowledge on tumor immunology and the continuous implementation of immunotherapy in cancer have recently led to the FDA and EMA approval of several checkpoint inhibitors as immunotherapic agents in clinical practice. Anti-CTLA-4, anti-PD-1, and anti-PDL-1 antibodies are becoming standard of care in advanced melanoma, as well as in relapsed or metastatic lung and kidney cancer, demonstrating higher and longer response compared to standard chemotherapy. These encouraging results have fostered the evaluation of these antibodies either alone or in combination with other therapies in several dozen clinical trials for the treatment of multiple tumor types...
August 16, 2017: European Journal of Nuclear Medicine and Molecular Imaging
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