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https://www.readbyqxmd.com/read/28926928/curcumin-inhibited-growth-of-human-melanoma-a375-cells-via-inciting-oxidative-stress
#1
Wang Liao, Wei Xiang, Fei-Fei Wang, Rui Wang, Yan Ding
Curcumin, a polyphenol compound, possesses potent pharmacological properties in preventing cancers, which make it as a potential anti-cancer mediator. However, it is still unknown that whether Curcumin induced melanoma A375 cell was associated with oxidative stress. Here, we firstly found a fascinating result that Curcumin could reduce the proliferation and induced apoptosis of human melanoma A375 cells. Meanwhile, IC50 of Curcumin on A375 cells is 80μM at 48h. In addition, Curcumin caused oxidative stress through inducing further ROS burst, decreasing GSH, and wrecking mitochondria membrane potential (MMP), which were reversed by ROS inhibitor N-acetylcysteine (NAC)...
September 15, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28925877/4-aryl-heteroaryl-4h-fused-pyrans-as-anti-proliferative-agents-design-synthesis-and-biological-evaluation
#2
Dinesh Kumar, Gurpreet Singh, Pooja Sharma, Arem Quayum, Girish Mahajan, M J Mintoo, Shashank Kumar Singh, Dilip Manikrao Mondhe, Pms Bedi, Subheet K Jain, Girish Kumar Gupta
The current study is focused on the design and synthesis of 4-aryl/heteroaryl-4H-fused pyrans as anti-proliferative agents. All the synthesized molecules were screened against a panel of human carcinoma cell lines. Significant inhibition was exhibited by the compounds against HCT-116 (Colon) and PC-3 (Prostate) cell lines while A-549 (Lung) cell lines, MiaPaCa-2 (Pancreatic) cell lines and HL-60 (Leukemia Cancer) cell lines were almost resistant to the exposure of the test compounds. Compound FP-(v)n displayed noteworthy cytotoxicity towards HCT-116 malignant cells with IC50 value of 0...
September 18, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28923840/apoptotic-bodies-elicit-gas6-mediated-migration-of-axl-expressing-tumor-cells
#3
Annelien Jm Zweemer, Cory B French, Joshua Mesfin, Simon Gordonov, Aaron S Meyer, Douglas A Lauffenburger
Metastases are a major cause of cancer mortality. AXL, a receptor tyrosine kinase (RTK) aberrantly expressed in many tumors, is a potent oncogenic driver of metastatic cell motility and has been identified as broadly relevant in cancer drug resistance. Despite its frequent association with changes in cancer phenotypes, the precise mechanism leading to AXL activation is incompletely understood. In addition to its ligand growth arrest specific-6 (Gas6), activation of AXL requires the lipid moiety phosphatidylserine (PS)...
September 18, 2017: Molecular Cancer Research: MCR
https://www.readbyqxmd.com/read/28923386/structure-based-design-synthesis-and-biological-evaluation-of-withaferin-a-analogues-as-potent-apoptotic-inducers
#4
Gabriel G Llanos, Liliana M Araujo, Ignacio A Jiménez, Laila M Moujir, Jaime Rodríguez, Carlos Jiménez, Isabel L Bazzocchi
Apoptosis inducers represent an attractive approach for the discovery and development of anticancer agents. Herein, we report on the development by molecular fine tuning of a withaferin A-based library of 63 compounds (2-64), 53 of them reported for the first time. Their antiproliferative evaluation on HeLa, A-549 and MCF-7 human tumor cell lines identified fifteen analogues displaying higher activity (IC50 values ranging 0.3-4.8 μM) than the lead (IC50 values ranging 1.3-10.1 μM) either in lag or log growth phases...
September 6, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28919780/the-role-and-significance-of-vegfr2-regulatory-t-cells-in-tumor-immunity
#5
REVIEW
Panrong Zhu, Chenxi Hu, Kaiyuan Hui, Xiaodong Jiang
Tumor development is closely related to angiogenesis, and VEGFR2 plays an important role in tumor angiogenesis. It is broadly expressed in the blood vessels, especially in the microvessels of tumor tissues. Furthermore, VEGFR2 is detected on the surface of the cell membrane in various immune cells, such as dendritic cells, macrophages, and regulatory T cells (Tregs). Tregs, which are one of the key negative regulatory factors in tumor immune microenvironments, show high-level expression of VEGFR2 which participates in the regulation of immunosuppressive function...
2017: OncoTargets and Therapy
https://www.readbyqxmd.com/read/28918572/spot-light-on-skeletal-muscles-optogenetic-stimulation-to-understand-and-restore-skeletal-muscle-function
#6
Tobias van Bremen, Thorsten Send, Philipp Sasse, Tobias Bruegmann
Damage of peripheral nerves results in paralysis of skeletal muscle. Currently, the only treatment option to restore proper function is electrical stimulation of the innervating nerve or of the skeletal muscles directly. However this approach has low spatial and temporal precision leading to co-activation of antagonistic muscles and lacks cell-type selectivity resulting in pain or discomfort by stimulation of sensible nerves. In contrast to electrical stimulation, optogenetic methods enable spatially confined and cell-type selective stimulation of cells expressing the light sensitive channel Channelrhodopsin-2 with precise temporal control over the membrane potential...
September 16, 2017: Journal of Muscle Research and Cell Motility
https://www.readbyqxmd.com/read/28918125/iodinated-chlorin-p6-copper-complex-induces-anti-proliferative-effect-in-oral-cancer-cells-through-elevation-of-intracellular-reactive-oxygen-species
#7
Paromita Sarbadhikary, Alok Dube
We investigated the anticancer chemotoxicity of previously reported iodinated chlorin p6 copper complex (ICp6-Cu), a novel chlorophyll derivative in which copper is attached to the side chain carboxylate groups via coordination. Human oral carcinoma cells NT8e, 4451 and the non-cancerous keratinocyte HaCaT cells were treated with ICp6-Cu for 48 h in dark and cell viability, proliferation and morphological alterations were examined. ICp6-Cu showed pronounced cytotoxicity in cancer cells with IC50 ∼40 μM, whereas, the viability of HaCaT cells was not affected...
September 13, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28917448/in-vitro-antitumor-activity-of-novel-benzimidazole-based-cu-ii-complexes
#8
Jiyong Hu, Yan Guo, Jin'an Zhao, Junshuai Zhang
Four benzimidazole-based Cu(II) complexes: Cu2(p-2-bmp)2Br4 (1), Cu2(p-2-bmp)2Cl4 (2), Cu2(p-2-bmb)2(DMF)2Br4·(CHCl3) (3), and Cu(p-2-bmb)(NO3)2·(CHCl3) (4) were isolated and characterized, where p-2-bmp is 1-((2-(pyridine-2-yl)-1H-benzoimidazol-1-yl)methyl)-1H-pyridine and p-2-bmb is 1-((2-(pyridin-2-yl)-1-benzoimidazol-1-yl)methyl)-1H-benzotriazole. Complexes 1 and 2 have binuclear configurations, 3 has a mononuclear structure, and 4has a one-dimensional (1-D) chain skeleton. To evaluate their potential anticancer effects on human carcinoma cells, anti-proliferation, DNA binding and cleavage, and apoptosis elicitation were examined...
September 5, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28916341/design-synthesis-and-biological-evaluation-of-benzamide-and-phenyltetrazole-derivatives-with-amide-and-urea-linkers-as-bcrp-inhibitors
#9
Nehaben A Gujarati, Leli Zeng, Pranav Gupta, Zhe-Sheng Chen, Vijaya L Korlipara
Breast cancer resistant protein (BCRP/ABCG2), a 72kDa plasma membrane transporter protein is a member of ABC transporter superfamily. Increased expression of BCRP causes increased efflux and therefore, reduced intracellular accumulation of many unrelated chemotherapeutic agents leading to multidrug resistance (MDR). A series of 31 benzamide and phenyltetrazole derivatives with amide and urea linkers has been synthesized to serve as potential BCRP inhibitors in order to overcome BCRP-mediated MDR. The target derivatives were tested for their cytotoxicity and reversal effects in human non-small cell lung cancer cell line H460 and mitoxantrone resistant cell line H460/MX20 using the MTT assay...
September 7, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28914418/spermidine-rescues-proximal-tubular-cells-from-oxidative-stress-and-necrosis-after-ischemic-acute-kidney-injury
#10
Jinu Kim
Kidney ischemia and reperfusion injury (IRI) is associated with a high mortality rate, which is attributed to tubular oxidative stress and necrosis; however, an effective approach to limit IRI remains elusive. Spermidine, a naturally occurring polyamine, protects yeast cells against aging through the inhibition of oxidative stress and necrosis. In the present study, spermidine supplementation markedly attenuated increases in plasma creatinine concentration and tubular injury score after IRI. In addition, exogenous spermidine potently inhibited oxidative stress, especially lipid peroxidation after IRI in kidneys and exposure to hydrogen peroxide in kidney proximal tubular cells, suppressing plasma membrane disruption and necrosis...
September 15, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28912103/membrane-perturbing-activities-and-structural-properties-of-the-frog-skin-derived-peptide-esculentin-1a-1-21-nh2-and-its-diastereomer-esc-1-21-1c-correlation-with-their-antipseudomonal-and-cytotoxic-activity
#11
Maria Rosa Loffredo, Anirban Ghosh, Nicole Harmouche, Bruno Casciaro, Vincenzo Luca, Annalisa Bortolotti, Floriana Cappiello, Lorenzo Stella, Anirban Bhunia, Burkhard Bechinger, Maria Luisa Mangoni
Antimicrobial peptides (AMPs) represent new alternatives to cope with the increasing number of multi-drug resistant microbial infections. Recently, a derivative of the frog-skin AMP esculentin-1a, Esc(1-21), was found to rapidly kill both the planktonic and biofilm forms of the Gram-negative bacterium Pseudomonas aeruginosa with a membrane-perturbing activity as a plausible mode of action. Lately, its diastereomer Esc(1-21)-1c containing two d-amino acids i.e. (D)Leu14 and (D)Ser17 revealed to be less cytotoxic, more stable to proteolytic degradation and more efficient in eradicating Pseudomonas biofilm...
September 11, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28912099/antimicrobial-peptides-are-degraded-by-the-cytosolic-proteases-of-human-erythrocytes
#12
Charles G Starr, William C Wimley
Well-studied and promising antimicrobial peptides (AMPs), with potent bactericidal activity, in vitro, have yet to have a significant impact in human medicine beyond topical applications. We previously showed that interactions of AMPs with concentrated human erythrocytes inhibit many of them, and suggested that screens and assays should be done in their presence to mimic host cell inhibition. Here, we use AMPs to characterize the activity of proteases that are associated with human erythrocytes. The representative AMPs, ARVA and indolicidin, are degraded significantly during incubation with dilute, washed erythrocytes and yield a variety of degradation products, suggesting significant exopeptidase activity...
September 11, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28904355/highly-potent-antimicrobial-modified-peptides-derived-from-the-acinetobacter-baumannii-phage-endolysin-lysab2
#13
Shih-Yi Peng, Ren-In You, Meng-Jiun Lai, Nien-Tsung Lin, Li-Kuang Chen, Kai-Chih Chang
The increase in the prevalence of multidrug-resistant Acinetobacter baumannii (MDRAB) strains is a serious public health concern. Antimicrobial peptides (AMPs) are a possible solution to this problem. In this study, we examined whether AMPs could be derived from phage endolysins. We synthesized four AMPs based on an amphipathic helical region in the C-terminus of endolysin LysAB2 encoded by the A. baumannii phage ΦAB2. These peptides showed potent antibacterial activity against A. baumannii (minimum inhibitory concentration, 4-64 μM), including some MDR and colistin-resistant A...
September 13, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28903409/acetyl-lupeolic-acid-inhibits-akt-signaling-and-induces-apoptosis-in-chemoresistant-prostate-cancer-cells-in-vitro-and-in-vivo
#14
Claudia Schmidt, Cornelia Loos, Lu Jin, Michael Schmiech, Christoph Q Schmidt, Menna El Gaafary, Tatiana Syrovets, Thomas Simmet
The triterpenoid acetyl-lupeolic acid (ac-LA) isolated from the oleogum resin of Boswellia carterii reduced the viability of a panel of cancer cell lines more efficiently than lupeol. There was no detectable intracellular conversion of ac-LA to lupeol and vice versa. In contrast to docetaxel, ac-LA did not induce selection of treatment-resistant cancer cells. By various parameters including DNA fragmentation, ac-LA was shown to induce apoptosis in androgen-independent PC-3 cells, whereas in MDA-MB-231 breast cancer cells, ac-LA led to cell accumulation in the G2/M phase of the cell cycle, but not to apoptosis...
August 15, 2017: Oncotarget
https://www.readbyqxmd.com/read/28902888/dendrimer-based-selective-autophagy-induction-rescues-%C3%AE-f508-cftr-and-inhibits-pseudomonas-aeruginosa-infection-in-cystic-fibrosis
#15
Scott Mackenzie Brockman, Manish Bodas, David Silverberg, Ajit Sharma, Neeraj Vij
BACKGROUND: Cystic Fibrosis (CF) is a genetic disorder caused by mutation(s) in the CF-transmembrane conductance regulator (Cftr) gene. The most common mutation, ΔF508, leads to accumulation of defective-CFTR protein in aggresome-bodies. Additionally, Pseudomonas aeruginosa (Pa), a common CF pathogen, exacerbates obstructive CF lung pathology. In the present study, we aimed to develop and test a novel strategy to improve the bioavailability and potentially achieve targeted drug delivery of cysteamine, a potent autophagy-inducing drug with anti-bacterial properties, by developing a dendrimer (PAMAM-DEN)-based cysteamine analogue...
2017: PloS One
https://www.readbyqxmd.com/read/28902165/development-of-novel-nrf2-are-inducers-bearing-pyrazino-2-1-a-isoquinolin-scaffold-with-potent-in-vitro-efficacy-and-enhanced-physicochemical-properties
#16
Hongbin Dai, Qiong Jiao, Tian Liu, Qidong You, Zhengyu Jiang
Pyrazino[2,1-a]isoquinolin analogues were reported as potent activators of Nrf2/ARE signaling both in vitro and in vivo by our group. In this study, we simplified the ring system to investigate the functions of various parts of the pyrazino[2,1-a]isoquinolin scaffold. We proved that the tetrahydroisoquinoline was not essential for activity and the pyrido[1,2-a]pyrazin analogues 3b and 3g retained the cellular Nrf2/ARE activation activity. Besides, this simplification significantly enhanced water solubility and membrane permeability, indicating that these compounds are more favourable for the further development of therapeutic agents around Nrf2 activation...
September 13, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28898776/effect-of-electro-activated-solutions-of-sodium-acetate-and-sodium-propionate-on-geosmin-producing-streptomyces-avermitilis-strain
#17
Viacheslav Liato, Mohammed Aïder
Electro-activated solutions of salts of weak organic acids are defined as novel potent disinfecting agents that can be used in the agri-food industry. The aim of the present work is to study and understand the destruction mechanism of electro-activated solutions of sodium acetate (EAA) and sodium propionate (EAP) against Streptomyces avermitilis spores. The results of antibacterial activity showed high bacteriostatic effect for all the tested solutions, including sodium hypochlorite used as positive control...
September 6, 2017: Chemosphere
https://www.readbyqxmd.com/read/28895404/exosomes-of-human-mesenchymal-stem-stromal-medicinal-signaling-cells-a-review
#18
U Altanerova, J Jakubechova, V Repiska, C Altaner
In this review, we intend to explore the potential therapeutic effects of exosomes released from mesenchymal stem/stromal cells (MSCs). MSCs gained credibility as a therapeutic tool due to their potential to differentiate into many cell types like osteoblasts, chondrocytes, adipocytes, muscular, endothelial, cardiovascular, and neurogenic cells. They possess potent wound healing activity due to their immunosuppressive and anti-inflammatory properties. MSCs are tested in large number of clinical trials for treatment of diseases, which do not have adequate therapy at present...
September 12, 2017: Neoplasma
https://www.readbyqxmd.com/read/28894024/the-synergistic-antimicrobial-effects-of-novel-bombinin-and-bombinin-h-peptides-from-the-skin-secretion-of%C3%A2-bombina-orientalis
#19
Jie Xiang, Mei Zhou, Yuxin Wu, Tianbao Chen, Chris Shaw, Lei Wang
Bombinin and bombinin H are two antimicrobial peptide (AMP) families initially discovered from the skin secretion of Bombina that share the same biosynthetic precursor-encoding cDNAs, but have different structures and physicochemical properties. Insight into their possible existing relationship lead us to perform the combination investigations into their anti-infectious activities. In this work, we report the molecular cloning and functional characterisation of two novel AMPs belonging to bombinin and bombinin H families from secretions of Bombina orientalis Their mature peptides (BHL-bombinin and bombinin HL), coded by single open-reading frame (ORF), were chemically synthesised along with an analogue peptide that replaced L-leucine with D-leucine from the 2nd position of the N-terminus (bombinin HD)...
September 11, 2017: Bioscience Reports
https://www.readbyqxmd.com/read/28893782/aminoglycoside-concentrations-required-for-synergy-with-carbapenems-against-pseudomonas-aeruginosa-determined-via-mechanistic-studies-and-modeling
#20
Rajbharan Yadav, Jürgen B Bulitta, Elena K Schneider, Beom Soo Shin, Tony Velkov, Roger L Nation, Cornelia B Landersdorfer
This study aimed to systematically identify the aminoglycoside concentrations required for synergy with a carbapenem and characterize the permeabilizing effect of aminoglycosides on the outer membrane of Pseudomonas aeruginosa Monotherapies and combinations of four aminoglycosides and three carbapenems were studied against P. aeruginosa strain AH298-GFP in 48 h static-concentration time-kill studies (SCTK) (inoculum; 10(7.6) CFU/mL). The outer membrane permeabilizing effect of tobramycin alone and in combination with imipenem was characterized via electron micrographs, confocal imaging and the nitrocefin assay...
September 11, 2017: Antimicrobial Agents and Chemotherapy
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