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https://www.readbyqxmd.com/read/28230794/structural-determinant-and-its-underlying-molecular-mechanism-of-stpc2-related-to-anti-angiogenic-activity
#1
Min Hu, Ning Cui, Zhixiang Bo, Feixiang Xiang
In this study, we aimed to use different strategies to further uncover the anti-angiogenic molecular mechanism of a fucoidan-like polysaccharide STPC2, isolated from brown alga Sargassum thunbergii. A desulfated derivative, STPC2-DeS, was successfully prepared and identified. The native polysaccharide and desulfated product were subjected to evaluate their anti-angiogenic effects. In the tube formation assay, STPC2 showed dose-dependent inhibition. In addition, STPC2 could distinctly inhibit the permeation of HUVEC cells into the lower chamber...
February 21, 2017: Marine Drugs
https://www.readbyqxmd.com/read/28230176/antithrombotic-therapy-for-patients-with-stemi-undergoing-primary-pci
#2
REVIEW
Francesco Franchi, Fabiana Rollini, Dominick J Angiolillo
Antithrombotic therapy, including antiplatelet and anticoagulant agents, is the cornerstone of pharmacological treatment to optimize clinical outcomes in patients with ST-segment elevation myocardial infarction (STEMI) undergoing primary percutaneous coronary intervention (PPCI). Intravenous anticoagulant drugs available for PPCI include the indirect thrombin inhibitors unfractionated heparin and low-molecular-weight heparin, and the direct thrombin inhibitor bivalirudin. Intravenous antiplatelet drugs mainly include glycoprotein IIb/IIIa inhibitors and the P2Y12-receptor inhibitor cangrelor...
February 23, 2017: Nature Reviews. Cardiology
https://www.readbyqxmd.com/read/28230084/highly-potent-antimicrobial-peptides-from-n-terminal-membrane-binding-region-of-e-coli-mreb
#3
Karabi Saikia, Yalavarthi Durga Sravani, Vibin Ramakrishnan, Nitin Chaudhary
Microbial pathogenesis is a serious health concern. The threat escalates as the existing conventional antimicrobials are losing their efficacy against the evolving pathogens. Peptides hold promise to be developed into next-generation antibiotics. Antimicrobial peptides adopt amphipathic structures that could selectively bind to and disrupt the microbial membranes. Interaction of proteins with membranes is central to all living systems and we reasoned that the membrane-binding domains in microbial proteins could be developed into efficient antimicrobials...
February 23, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28229330/the-involvement-of-the-myelin-associated-inhibitors-and-their-receptors-in-cns-plasticity-and-injury
#4
REVIEW
Anthony G Boghdadi, Leon Teo, James A Bourne
The limited capacity for the central nervous system (CNS) to repair itself was first described over 100 years ago by Spanish neuroscientist Ramon Y. Cajal. However, the exact mechanisms underlying this failure in neuronal regeneration remain unclear and, as such, no effective therapeutics yet exist. Numerous studies have attempted to elucidate the biochemical and molecular mechanisms that inhibit neuronal repair with increasing evidence suggesting that several inhibitory factors and repulsive guidance cues active during development actually persist into adulthood and may be contributing to the inhibition of repair...
February 22, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/28228690/human-cytomegalovirus-interleukin-10-enhances-matrigel-invasion-of-mda-mb-231-breast-cancer-cells
#5
Cendy A Valle Oseguera, Juliet V Spencer
BACKGROUND: While some risk factors for breast cancer are well-known, the influence of other factors, particularly virus infection, remains unclear. Human cytomegalovirus (HCMV) is widespread in the general population, and both molecular and epidemiological evidence has indicated links between HCMV and breast cancer. The HCMV protein cmvIL-10 is a potent suppressor of immune function that has also been shown to promote proliferation and migration of breast cancer cells. In this study, the impact of cmvIL-10 on tumor cell invasion through a simulated basement membrane was investigated...
2017: Cancer Cell International
https://www.readbyqxmd.com/read/28228097/alkaloid-extracts-from-combretum-zeyheri-inhibit-the-growth-of-mycobacterium-smegmatis
#6
Tafadzwa Nyambuya, Ruvimbo Mautsa, Stanley Mukanganyama
BACKGROUND: Current tuberculosis regimens have failed to combat the issue of drug resistance and ethno medicines may represent a possible source of antimycobacterial agents. Combretum species are well known in African traditional medicines and used for various ailments including pneumonia, venereal diseases like syphilis, mental problems, relief of sore throats and colds, fever, and chest coughs associated with tuberculosis. Alkaloids function as either hydrogen-acceptor or hydrogen-donor in hydrogen bonding critical for the interaction between targets thus, potentiating effects of curative agents on diseases...
February 23, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28228088/aryl-heteroaryl-substituted-celecoxib-derivatives-as-cox-2-inhibitors-synthesis-anti-inflammatory-activity-and-molecular-docking-studies
#7
Golla Madhava, Katla Venkata Ramana, Saddala Madhu Sudhana, Devineni Subba Rao, Kuntrapakam Hema Kumar, Valluru Lokanatha, Asupatri Usha Rani, Chamarthi Naga Raju
BACKGROUND: Cyclooxygenase (COX-2) inhibitors have been developed to provide better anti-inflammatory and analgesic efficacy than those of traditional NSAIDs. Several compounds having selective COX-2 inhibitors such as SC-558, Celecoxib, Rofecoxib, Valdecoxib and Etoricoxib are marketed as new generation NSAIDs and block the production of prostaglandins (PGs) in inflammatory cells. New anti-inflammatory dynamic agents with improved potency and safety profile are still needed. OBJECTIVE: As a part of our continuation research work towards the synthesis of anti-inflammatory agents, the synthesis of N-substituted aryl/heteroaryl-pyrazole-1yl benzene sulfonamide (Celecoxib) derivatives, and evaluated their anti-inflammatory activity in both methods in vitro and in vivo, and molecular docking study on COX-2 enzyme will be discussed in this study...
February 20, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28228001/fabrication-of-progesterone-loaded-nanofibers-for-the-drug-delivery-applications-in-bovine
#8
Chitra Karuppannan, Mehnath Sivaraj, J Ganesh Kumar, Rangasamy Seerangan, S Balasubramanian, Dhinakar Raj Gopal
Progesterone is a potent drug for synchronization of the estrus and ovulation cycles in bovine. At present, the estrus cycle of bovine is controlled by the insertion of progesterone-embedded silicone bands. The disadvantage of nondegradable polymer inserts is to require for disposal of these bands after their use. The study currently focuses on preparation of biodegradable progesterone-incorporated nanofiber for estrus synchronization. Three different concentrations (1.2, 1.9, and 2.5 g) of progesterone-impregnated nanofibers were fabricated using electrospinning...
December 2017: Nanoscale Research Letters
https://www.readbyqxmd.com/read/28226206/exploration-of-the-innate-immune-system-of-styela-clava-zn-2-binding-enhances-the-antimicrobial-activity-of-the-tunicate-peptide-clavanin-a
#9
Samuel A Juliano, Scott Pierce, James A DeMayo, Marcy J Balunas, Alfredo M Angeles-Boza
Tunicates have been used as primitive models for understanding cell mediated and humoral immunity. Clavanin A (ClavA) is a potent antimicrobial peptide produced by the solitary tunicate Styela clava. In this work, we demonstrate that ClavA utilizes Zn(2+) ions to potentiate its antimicrobial activity. A reduced concentration at which the peptide inhibits the growth of bacteria and an increase in the rate of killing is observed in the presence of Zn(2+). Membrane depolarization, β-galactosidase leakage and potassium leakage assays indicate that ClavA is membrane active, forms small pores, but induces cell death by targeting an intracellular component...
February 22, 2017: Biochemistry
https://www.readbyqxmd.com/read/28225264/fatty-acid-comprising-lysine-conjugates-anti-mrsa-agents-that-display-in-vivo-efficacy-by-disrupting-biofilms-with-no-resistance-development
#10
Mohini Mohan Konai, Jayanta Haldar
Methicillin-resistant Staphylococcus aureus (MRSA) have developed resistance to antibiotics of last resort such as vancomycin, linezolid and daptomycin. Additionally, their biofilm forming capability has set an alarming situation in the treatment of bacterial infections. Herein we report the potency of fatty acid comprising lysine conjugates as novel anti-MRSA agents, which were not only capable of killing growing planktonic MRSA at low concentration (MIC = 3.1-6.3 µg/mL), but also displayed potent activity against non-dividing stationary phase cells...
February 22, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/28225079/multiple-sodium-channel-isoforms-mediate-the-pathological-effects-of-pacific-ciguatoxin-1
#11
Marco C Inserra, Mathilde R Israel, Ashlee Caldwell, Joel Castro, Jennifer R Deuis, Andrea M Harrington, Angelo Keramidas, Sonia Garcia-Caraballo, Jessica Maddern, Andelain Erickson, Luke Grundy, Grigori Y Rychkov, Katharina Zimmermann, Richard J Lewis, Stuart M Brierley, Irina Vetter
Human intoxication with the seafood poison ciguatoxin, a dinoflagellate polyether that activates voltage-gated sodium channels (NaV), causes ciguatera, a disease characterised by gastrointestinal and neurological disturbances. We assessed the activity of the most potent congener, Pacific ciguatoxin-1 (P-CTX-1), on NaV1.1-1.9 using imaging and electrophysiological approaches. Although P-CTX-1 is essentially a non-selective NaV toxin and shifted the voltage-dependence of activation to more hyperpolarising potentials at all NaV subtypes, an increase in the inactivation time constant was observed only at NaV1...
February 22, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28225005/autophagy-protects-against-palmitic-acid-induced-apoptosis-in-podocytes-in-vitro
#12
Xu-Shun Jiang, Xue-Mei Chen, Jiang-Min Wan, Hai-Bo Gui, Xiong-Zhong Ruan, Xiao-Gang Du
Autophagy is a highly conserved degradation process that is involved in the clearance of proteins and damaged organelles to maintain intracellular homeostasis and cell integrity. Type 2 diabetes is often accompanied by dyslipidemia with elevated levels of free fatty acids (FFAs). Podocytes, as an important component of the filtration barrier, are susceptible to lipid disorders. The loss of podocytes causes proteinuria, which is involved in the pathogenesis of diabetic nephropathy. In the present study, we demonstrated that palmitic acid (PA) promoted autophagy in podocytes...
February 22, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28220599/identification-of-laminin-%C3%AE-5-short-arm-peptides-active-for-endothelial-cell-attachment-and-tube-formation
#13
Yamato Kikkawa, Yumika Sugawara, Nozomi Harashima, Shogo Fujii, Kazuki Ikari, Jun Kumai, Fumihiko Katagiri, Kentaro Hozumi, Motoyoshi Nomizu
Laminin-511, a major component of endothelial basement membrane, consists of α5, β1, and γ1 chains. The short arm region of the α5 chain is a structural feature of endothelial laminins. In this study, we identified active sequences for human umbilical vein endothelial cells (HUVECs) using recombinant proteins and synthetic peptides. The short arm of the α5 chain contains three globular domains [laminin N-terminal globular domain, laminin 4 domain a, and laminin 4 domain b (LN, L4a, and L4b)] and three rod-like elements [laminin epidermal growth factor-like domain a, b, and c (LEa, LEb, and LEc)]...
February 21, 2017: Journal of Peptide Science: An Official Publication of the European Peptide Society
https://www.readbyqxmd.com/read/28216467/nmr-and-esr-study-of-amphotericin-b-interactions-with-various-binary-phosphatidylcholine-phosphatidylglycerol-membranes
#14
J C Debouzy, L Mehenni, D Crouzier, M Lahiani-Skiba, G Nugue, M Skiba
Several biologically relevant phospholipids are considered as potential excipients for IV administration liposome's formulation of AMB (Biopharmaceututics Classification System Class IV). On the basis of in vivo bioavaibility studies, DMPC and DMPG were ranked as the first potent encapsulation enhancers for this model drug, especially if one expects to target DMPG rich systems as pulmonary surfactant. Subsequently, dispersions (multilayers) of DMPC, DMPG or in binary systems with various molar ratios were prepared with or without AMB (molar ratios AMB/lipid) and further investigated using the (1)H-,(31)P-NMR methods...
February 16, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28214967/increased-atrial-%C3%AE-adrenergic-receptors-and-grk-2-gene-expression-can-play-a-fundamental-role-in-heart-failure-after-repair-of-congenital-heart-disease-with-cardiopulmonary-bypass
#15
Marcela Silva Oliveira, Fabio Carmona, Walter V A Vicente, Paulo H Manso, Karina M Mata, Mara Rúbia Celes, Erica C Campos, Simone G Ramos
Surgeries to correct congenital heart diseases are increasing in Brazil and worldwide. However, even with the advances in surgical techniques and perfusion, some cases, especially the more complex ones, can develop heart failure and death. A retrospective study of patients who underwent surgery for correction of congenital heart diseases with cardiopulmonary bypass (CPB) in a university tertiary-care hospital that died, showed infarction in different stages of evolution and scattered microcalcifications in the myocardium, even without coronary obstruction...
February 18, 2017: Pediatric Cardiology
https://www.readbyqxmd.com/read/28214344/neferine-potentiates-the-antitumor-effect-of-cisplatin-in-human-lung-adenocarcinoma-cells-via-a-mitochondria-mediated-apoptosis-pathway
#16
Kalai Selvi Sivalingam, Poornima Paramasivan, Ching Feng Weng, Viswanadha Vijaya Padma
Cisplatin is one of the most potent chemotherapeutic agents for the treatment of many types of solid tumors but its efficacy is often limited by the development of resistance and dose limiting toxicity. Neferine is an alkaloid isolated from seed embryo of Nelumbo nucifera, it has recently been shown to have anticancer effects in various human cancer cell lines. The present investigation is designed to study the chemosensitizing ability of neferine with cisplatin in A549 cells. Neferine potentiates the cisplatin induced apoptosis through the exploration of characteristic apoptotic morphological changes, induced sub-G0/G1 cell cycle arrest, ROS hypergeneration, significant loss of cellular antioxidant enzymes as well as loss of mitochondrial membrane potential (ΔΨM)...
February 18, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28213729/alpha-tocopherol-transfer-protein-%C3%AE-ttp-is-expressed-in-endometrial-carcinoma-and-is-correlated-with-figo-stage-and-5-year-survival
#17
Sabine Heublein, Thomas Vrekoussis, Ronny Etzl, Daisy Rotzoll, Christina Kuhn, Gesine Faigle, Iordanis Navrozoglou, Theodore Stefos, Antonis Makrigiannakis, Udo Jeschke
BACKGROUND: Increased oxidative stress plays an important role in cancer development. Vitamin E is considered a potent anti-oxidant and its transfer protein αTTP facilitates its cellular delivery. We hypothesize that αTTP could be present in and have an impact on endometrial cancer. MATERIALS AND METHODS: Ishikawa endometrial cancer cells were treated with BSO and AAPH to mimick oxidative stress conditions. αTTP was detected by immunocytochemistry and western blot...
February 17, 2017: Journal of Cancer Research and Clinical Oncology
https://www.readbyqxmd.com/read/28213701/ursolic-acid-mediated-changes-in-glycolytic-pathway-promote-cytotoxic-autophagy-and-apoptosis-in-phenotypically-different-breast-cancer-cells
#18
Anna Lewinska, Jagoda Adamczyk-Grochala, Ewa Kwasniewicz, Anna Deregowska, Maciej Wnuk
Plant-derived pentacyclic triterpenotids with multiple biological activities are considered as promising candidates for cancer therapy and prevention. However, their mechanisms of action are not fully understood. In the present study, we have analyzed the effects of low dose treatment (5-20 µM) of ursolic acid (UA) and betulinic acid (BA) on breast cancer cells of different receptor status, namely MCF-7 (ER(+), PR(+/-), HER2(-)), MDA-MB-231 (ER(-), PR(-), HER2(-)) and SK-BR-3 (ER(-), PR(-), HER2(+)). UA-mediated response was more potent than BA-mediated response...
February 17, 2017: Apoptosis: An International Journal on Programmed Cell Death
https://www.readbyqxmd.com/read/28213307/enhanced-toxicity-to-the-cyanobacterium-microcystis-aeruginosa-by-low-dosage-repeated-exposure-to-the-allelochemical-n-phenyl-1-naphthylamine
#19
Y N Gao, F J Ge, L P Zhang, Y He, Z Y Lu, Y Y Zhang, B Y Liu, Q H Zhou, Z B Wu
It has been puzzling whether and how a plant could exert a strong allelopathic inhibition to the target organisms by releasing low concentrations of allelochemicals. Plant allelochemicals have been proposed to be released continuously, however, direct evidence from specific allelochemicals is urgently required. In the present study, the toxicity of allelochemical N-phenyl-1-naphthylamine (NPN) towards the cyanobacterium Microcystis aeruginosa by two different exposure patterns was compared. One was low-dosage repeated exposure (LRE), in which 50  μg L(-1) NPN was repeatedly dosed to simulate the continual release of allelochemicals, and the other one was high-dosage single exposure (HSE) as per the routine toxicity assay...
January 21, 2017: Chemosphere
https://www.readbyqxmd.com/read/28213276/engineering-approaches-in-sirna-delivery
#20
Anna Angela Barba, Sara Cascone, Diego Caccavo, Gaetano Lamberti, Gianluca Chiarappa, Michela Abrami, Gabriele Grassi, Mario Grassi, Giovanna Tomaiuolo, Stefano Guido, Valerio Brucato, Francesco Carfì Pavia, Giulio Ghersi, Vincenzo La Carrubba, Roberto Andrea Abbiati, Davide Manca
siRNAs are very potent drug molecules, able to silence genes involved in pathologies development. siRNAs have virtually an unlimited therapeutic potential, particularly for the treatment of inflammatory diseases. However, their use in clinical practice is limited because of their unfavorable properties to interact and not to degrade in physiological environments. In particular they are large macromolecules, negatively charged, which undergo rapid degradation by plasmatic enzymes, are subject to fast renal clearance/hepatic sequestration, and can hardly cross cellular membranes...
February 14, 2017: International Journal of Pharmaceutics
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