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https://www.readbyqxmd.com/read/29332356/%C3%AE-aescin-shows-potent-antiproliferative-activity-in-osteosarcoma-cells-by-inducing-autophagy-ros-generation-and-mitochondrial-membrane-potential-loss
#1
Zhao-Rui Liu, Li-Zhi Sun, Tang-Hong Jia, Dao-Fu Jia
PURPOSE: Osteosarcoma is one of the frequent bone tumor affecting mainly children and is associated with considerable mortality. The limited availability of anticancer drugs and less efficacious treatment options have led to poor survival rates of patients with osteosarcoma. Therefore, there is need to look for more viable treatment options and against this backdrop, natural products may prove handy. Therefore the aim of the present study was to evaluate the anticancer activity of a natural product of plant origin, β-aescin, against U2OS human osteosarcoma cells...
November 2017: Journal of B.U.ON.: Official Journal of the Balkan Union of Oncology
https://www.readbyqxmd.com/read/29332353/aesculetin-6-7-dihydroxycoumarin-exhibits-potent-and-selective-antitumor-activity-in-human-acute-myeloid-leukemia-cells-thp-1-via-induction-of-mitochondrial-mediated-apoptosis-and-cancer-cell-migration-inhibition
#2
Jian Gong, Wei-Guo Zhang, Xiao-Fen Feng, Mei-Juan Shao, Chao Xing
PURPOSE: The main target of the present research was to examine the antitumor properties of aesculetin in human acute myeloid leukemia cancer cells (THP-1) and peripheral blood mono-nucleated cells (PBMCs) (used as normal cell line model) along with the determination of its effects on induction of apoptosis, inhibition of cancer cell migration and changes in Bcl-2/Bax protein expressions. METHODS: MTT colorimetric bioassay was performed to study the impact of this natural compound on cytotoxicity of both cell types...
November 2017: Journal of B.U.ON.: Official Journal of the Balkan Union of Oncology
https://www.readbyqxmd.com/read/29331805/synthesis-characterization-and-anticancer-activity-in%C3%A2-vitro-and-in%C3%A2-vivo-evaluation-of-an-iridium-iii-polypyridyl-complex
#3
Qiao-Yan Yi, Dan Wan, Bing Tang, Yang-Jie Wang, Wen-Yao Zhang, Fan Du, Miao He, Yun-Jun Liu
An iridium (III) complex [Ir(ppy)2(BDPIP)]PF6 (Ir-1) was reported to show high anticancer activity and may be used as a potent anticancer drug. In the current study, we designed and synthesized a novel iridium (III) complex and evaluated its potential inhibitory effect on the cancer cell growth in vitro and in vivo. This complex was found to display high cytotoxic activity in vitro and in vivo against A549 cell with a low IC50 value of 3.6 ± 0.3 μM and inhibiting percentage of tumor growth is 63.84% compared with the control...
December 1, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29331753/an-iridium-iii-complex-as-potent-anticancer-agent-induces-apoptosis-and-autophagy-in-b16%C3%A2-cells-through-inhibition-of-the-akt-mtor-pathway
#4
Bing Tang, Dan Wan, Yang-Jie Wang, Qiao-Yan Yi, Bo-Hong Guo, Yun-Jun Liu
A new ligand THPDP (THPDP = 11-(6,7,8,9-tetrahydrophenazin-2-yl)dipyrido[3,2-a:2',3'-c]phenazine) and its iridium(III) complex [Ir(ppy)2(THPDP)]PF6 (Ir-1) was synthesized and characterized by elemental analysis, IR, ESI-MS, 1H NMR and 13C NMR. The cytotoxicity in vitro of the complex against cancer cells B16, A549, Eca-109, SGC-7901, BEL-7402 and normal NIH 3T3 cell lines was evaluated using MTT method. The IC50 values of the complex toward B16, A549 and Eca-109 cells are 1.0 ± 0.02, 1.4 ± 0...
December 30, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29327480/membrane-active-peptide-pv3-efficiently-eradicates-multidrug-resistant-pseudomonas-aeruginosa-in-a-mouse-model-of-burn-infection
#5
Hamed Memariani, Delavar Shahbazzadeh, Jean-Marc Sabatier, Kamran Pooshang Bagheri
The aim of this study was to evaluate the topical bactericidal activity of peptide PV3 against a MDR isolate of Pseudomonas aeruginosa in a mouse model of burn infection. The structural analysis of PV3 by circular dichroism spectroscopy indicated a low peptide helical content in water, whereas a high helical content was observed in the presence of the more hydrophobic 50% (v/v) trifluoroethanol/water buffer. A confocal microscopy analysis indicated that the main action of PV3 occurred at the membrane of bacteria...
January 12, 2018: APMIS: Acta Pathologica, Microbiologica, et Immunologica Scandinavica
https://www.readbyqxmd.com/read/29324251/potential-role-of-plasmodium-falciparum-exported-protein-1-in-the-chloroquine-mode-of-action
#6
Andreas Martin Lisewski, Joel Patrick Quiros, Monica Mittal, Nagireddy Putluri, Arun Sreekumar, Jesper Z Haeggström, Olivier Lichtarge
In the human malaria parasite Plasmodium falciparum, membrane glutathione S-transferases (GST) have recently emerged as potential cellular detoxifying units and as drug target candidates with the artemisinin (ART) class of antimalarials inhibiting their activity at single-digit nanomolar potency when activated by iron sources such as cytotoxic hematin. Here we put forward the hypothesis that the membrane GST Plasmodium falciparum exported protein 1 (PfEXP1, PF3D7_1121600) might be directly involved in the mode of action of the unrelated antimalarial 4-aminoquinoline drug chloroquine (CQ)...
December 27, 2017: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/29323103/oridonin-exerts-anticancer-effect-on-osteosarcoma-by-activating-ppar-%C3%AE-and-inhibiting-nrf2-pathway
#7
Ying Lu, Yang Sun, Jianwei Zhu, Lisha Yu, Xiubo Jiang, Jie Zhang, Xiaochen Dong, Bo Ma, Qi Zhang
Osteosarcoma is the most common high-grade human primary malignant bone sarcoma with lower survival in the past decades. Oridonin, a bioactive diterpenoid isolated from Rabdosia rubescens, has been proved to possess potent anti-cancer effects. However, its potential mechanism still remains not fully clear nowadays. In this study, we investigated the anticancer effect of oridonin on human osteosarcoma and illuminated the underlying mechanisms. In vitro, oridonin inhibited the cell viability of various osteosarcoma cells...
January 11, 2018: Cell Death & Disease
https://www.readbyqxmd.com/read/29321581/a-ruthenium-based-5-fluorouracil-complex-with-enhanced-cytotoxicity-and-apoptosis-induction-action-in-hct116-cells
#8
Valdenizia Rodrigues Silva, Rodrigo S Corrêa, Luciano de Souza Santos, Milena Botelho Pereira Soares, Alzir Azevedo Batista, Daniel Pereira Bezerra
Combination of multifunctionalities into one compound is a rational strategy in medicinal chemical design, and have often been used with metallodrug-based compounds. In the present study, we synthesized a novel ruthenium-based 5-fluorouracil complex [Ru(5-FU)(PPh3)2(bipy)]PF6 (PPh3 = triphenylphosphine; and bipy = 2,2'-bipyridine) with enhanced cytotoxicity in different cancer cells, and assessed its apoptosis induction action in human colon carcinoma HCT116 cells. The complex was characterized by infrared, cyclic voltammetry, molar conductance measurements, elemental analysis, NMR experiments and X-ray crystallographic analysis...
January 10, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29321334/mechanism-of-hiv-1-resistance-to-an-electronically-constrained-%C3%AE-helical-peptide-membrane-fusion-inhibitor
#9
Xiyuan Wu, Zixuan Liu, Xiaohui Ding, Danwei Yu, Huamian Wei, Bo Qin, Yuanmei Zhu, Huihui Chong, Sheng Cui, Yuxian He
SC29EK is an electronically constrained α-helical peptide HIV-1 fusion inhibitor highly effective against both wild-type and enfuvirtide (T20)-resistant viruses. In this study, we focused on investigating the mechanism of HIV-1 resistance to SC29EK by two approaches. First, SC29EK-escaping HIV-1 variants were selected and characterized. Three mutant viruses, which possessed two (E43K/E49A) or three (Q39R/N43K/N126K, N43K/E49A/N126K) amino acid substitutions in the N- and C-terminal repeat regions of gp41 were identified as conferring high resistance to SC29EK and cross-resistance to the first-generation (T20, C34) and newly-designed (sifuvirtide, MT-SC29EK, 2P23) fusion inhibitors...
January 10, 2018: Journal of Virology
https://www.readbyqxmd.com/read/29321064/the-role-of-ace2-angiotensin-1-7-and-mas1-receptor-axis-in-glucocorticoid-induced-intrauterine-growth-restriction
#10
Elham Ghadhanfar, Aseel Alsalem, Shaimaa Al-Kandari, Jumana Naser, Fawzi Babiker, Maie Al-Bader
BACKGROUND: Plasma and urine levels of the potent vasodilator Ang-(1-7) are elevated in mid and late pregnancy and are correlated with elevated placental angiogenesis, fetal blood flow, and rapid fetal growth. We hypothesized that Ang-(1-7), its receptor (Mas1) and the enzymes involved in Ang-(1-7) production (ACE2 and Membrane metallo-endopeptidase; MME) are down regulated in response to glucocorticoid administration contributing to IUGR. METHODS: Pregnant female Sprague-Dawley rats were injected with dexamethasone (DEX; 0...
December 29, 2017: Reproductive Biology and Endocrinology: RB&E
https://www.readbyqxmd.com/read/29320716/distinct-roles-of-systemic-and-local-actions-of-insulin-on-pancreatic-%C3%AE-cells
#11
Takumi Kitamoto, Kenichi Sakurai, Eun Young Lee, Koutaro Yokote, Domenico Accili, Takashi Miki
OBJECTIVE: Pancreatic β-cell mass and function are critical in glucose homeostasis. Their regulatory mechanisms have been studied principally under experimental conditions of reduced β-cell numbers, such as β-cell ablation and partial pancreatectomy. In the present study, we generated an opposite mouse model with an excessive amount of ectopic β-cells, and analyzed its consequence on β-cell mass and survival. METHODS: Mice underwent sub-renal transplantation (SRT) of pseudo-islets generated from a pancreatic β-cell line MIN6 or intra-pancreatic transplantation (IPT) of MIN6 cells, and morphological and functional changes of their endocrine pancreata were analyzed...
January 7, 2018: Metabolism: Clinical and Experimental
https://www.readbyqxmd.com/read/29320578/the-potent-effect-of-mycolactone-on-lipid-membranes
#12
Milène Nitenberg, Anaïs Bénarouche, Ofelia Maniti, Estelle Marion, Laurent Marsollier, Julie Géan, Erick J Dufourc, Jean-François Cavalier, Stéphane Canaan, Agnès P Girard-Egrot
Mycolactone is a lipid-like endotoxin synthesized by an environmental human pathogen, Mycobacterium ulcerans, the causal agent of Buruli ulcer disease. Mycolactone has pleiotropic effects on fundamental cellular processes (cell adhesion, cell death and inflammation). Various cellular targets of mycolactone have been identified and a literature survey revealed that most of these targets are membrane receptors residing in ordered plasma membrane nanodomains, within which their functionalities can be modulated...
January 10, 2018: PLoS Pathogens
https://www.readbyqxmd.com/read/29317197/structural-determinants-of-phorbol-ester-binding-activity-of-the-c1a-and-c1b-domains-of-protein-kinase-c-theta
#13
Agnes Czikora, Satyabrata Pany, Youngki You, Amandeep S Saini, Nancy E Lewin, Gary A Mitchell, Adelle Abramovitz, Noemi Kedei, Peter M Blumberg, Joydip Das
The PKC isozymes represent the most prominent family of signaling proteins mediating response to the ubiquitous second messenger diacylglycerol. Among them, PKCθ is critically involved in T-cell activation. Whereas all the other conventional and novel PKC isoforms have twin C1 domains with potent binding activity for phorbol esters, in PKCθ only the C1b domain possesses potent binding activity, with little or no activity reported for the C1a domain. In order to better understand the structural basis accounting for the very weak ligand binding of the PKCθ C1a domain, we assessed the effect on ligand binding of twelve amino acid residues which differed between the C1a and C1b domains of PKCθ...
January 6, 2018: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/29316337/a-novel-enediyne-integrated-antibody-drug-conjugate-shows-promising-anti-tumor-efficacy-against-cd30-lymphomas
#14
Rong Wang, Liang Li, Shenghua Zhang, Yi Li, Xiaofei Wang, Qingfang Miao, Yongsu Zhen
CD30 is a 120-kDa type I trans-membrane glycoprotein belonging to the tumor necrosis factor (TNF) receptor superfamily. Overexpression of CD30 has been reported in Hodgkin lymphoma (HL) and anaplastic large cell lymphoma (ALCL). CD30-targeted treatment with antibody-drug conjugates (ADCs) can lead to promising clinical benefit. Lidamycin (LDM), consisting of an apoprotein LDP and an active enediyne chromaphore AE, is a member of the enediyne antibiotic family and one of the most potent antitumor agents. AE and LDP can be dissociated and reconstituted under certain conditions in vitro...
January 9, 2018: Molecular Oncology
https://www.readbyqxmd.com/read/29315210/isoaaptamine-induces-t-47d-cells-apoptosis-and-autophagy-via-oxidative-stress
#15
Chih-Fung Wu, Man-Gang Lee, Mohamed El-Shazly, Kuei-Hung Lai, Seng-Chung Ke, Chiang-Wen Su, Shou-Ping Shih, Ping-Jyun Sung, Ming-Chang Hong, Zhi-Hong Wen, Mei-Chin Lu
Aaptos is a genus of marine sponge which belongs to Suberitidae and is distributed in tropical and subtropical oceans. Bioactivity-guided fractionation of Aaptos sp. methanolic extract resulted in the isolation of aaptamine, demethyloxyaaptamine, and isoaaptamine. The cytotoxic activity of the isolated compounds was evaluated revealing that isoaaptamine exhibited potent cytotoxic activity against breast cancer T-47D cells. In a concentration-dependent manner, isoaaptamine inhibited the growth of T-47D cells as indicated by short-(MTT) and long-term (colony formation) anti-proliferative assays...
January 9, 2018: Marine Drugs
https://www.readbyqxmd.com/read/29315015/tumor-specific-t-cells-engineered-to-overcome-tumor-immune-evasion-induce-clinical-responses-in-patients-with-relapsed-hodgkin-lymphoma
#16
Catherine M Bollard, Tamara Tripic, Conrad Russell Cruz, Gianpietro Dotti, Stephen Gottschalk, Vicky Torrano, Olga Dakhova, George Carrum, Carlos A Ramos, Hao Liu, Meng-Fen Wu, Andrea N Marcogliese, Cecilia Barese, Youli Zu, Daniel Y Lee, Owen O'Connor, Adrian P Gee, Malcolm K Brenner, Helen E Heslop, Cliona M Rooney
Purpose Transforming growth factor-β (TGF-β) production in the tumor microenvironment is a potent and ubiquitous tumor immune evasion mechanism that inhibits the expansion and function of tumor-directed responses; therefore, we conducted a clinical study to discover the effects of the forced expression of a dominant-negative TGF-β receptor type 2 (DNRII) on the safety, survival, and activity of infused tumor-directed T cells. Materials and Methods In a dose escalation study, eight patients with Epstein Barr virus-positive Hodgkin lymphoma received two to 12 doses of between 2 × 107 and 1...
January 9, 2018: Journal of Clinical Oncology: Official Journal of the American Society of Clinical Oncology
https://www.readbyqxmd.com/read/29313547/the-p-type-atpase-inhibiting-potential-of-polyoxotungstates
#17
Nadiia Gumerova, Lukáš Krivosudský, Gil Fraqueza, Joscha Breibeck, Emir Al-Sayed, Elias Tanuhadi, Aleksandar Bijelic, Juan Fuentes, Manuel Aureliano, Annette Rompel
Polyoxometalates (POMs) are transition metal complexes that exhibit a broad diversity of structures and properties rendering them promising for biological purposes. POMs are able to inhibit a series of biologically important enzymes, including phosphatases, and thus are able to affect many biochemical processes. In the present study, we analyzed and compared the inhibitory effects of nine different polyoxotungstates (POTs) on two P-type ATPases, Ca2+-ATPase from skeletal muscle and Na+/K+-ATPase from basal membrane of skin epithelia...
January 9, 2018: Metallomics: Integrated Biometal Science
https://www.readbyqxmd.com/read/29312593/shikonin-induces-ros-based-mitochondria-mediated-apoptosis-in-colon-cancer
#18
Wenquan Liang, Jianxin Cui, Kecheng Zhang, Hongqing Xi, Aizhen Cai, Jiyang Li, Yunhe Gao, Chong Hu, Yi Liu, Yixun Lu, Ning Wang, Xiaosong Wu, Bo Wei, Lin Chen
Colon cancer is the third most common malignancy worldwide, and chemotherapy is a widely used strategy in clinical therapy. Chemotherapy-resistant of colon cancer is the main cause of recurrence and progression. Novel drugs with efficacy and safety in treating colon cancer are urgently needed. Shikonin, a naphthoquinone derived from the roots of the herbal plant Lithospermum erythrorhizon, has been determined to be a potent anti-tumor agent. The aim of the present study was to detect the underlying anti-tumor mechanism of shikonin in colon cancer...
December 12, 2017: Oncotarget
https://www.readbyqxmd.com/read/29311306/mechanism-specific-assay-design-facilitates-the-discovery-of-nav1-7-selective-inhibitors
#19
Tania Chernov-Rogan, Tianbo Li, Gang Lu, Henry Verschoof, Kuldip Khakh, Steven W Jones, Maureen H Beresini, Chang Liu, Daniel F Ortwine, Steven J McKerrall, David H Hackos, Daniel Sutherlin, Charles J Cohen, Jun Chen
Many ion channels, including Nav1.7, Cav1.3, and Kv1.3, are linked to human pathologies and are important therapeutic targets. To develop efficacious and safe drugs, subtype-selective modulation is essential, but has been extremely difficult to achieve. We postulate that this challenge is caused by the poor assay design, and investigate the Nav1.7 membrane potential assay, one of the most extensively employed screening assays in modern drug discovery. The assay uses veratridine to activate channels, and compounds are identified based on the inhibition of veratridine-evoked activities...
January 8, 2018: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/29311064/high-content-screening-of-mmv-pathogen-box-for-plasmodium-falciparum-digestive-vacuole-disrupting-molecules-reveals-valuable-starting-points-for-drug-discovery
#20
Jie Xin Tong, Rajesh Chandramohanadas, Kevin Shyong-Wei Tan
Plasmodium falciparum infections leading to malaria have severe clinical manifestations and high mortality rates. Chloroquine (CQ), a former mainstay of malaria chemotherapy, has been rendered ineffective due to the emergence of wide-spread resistance. Recent studies, however, have unveiled a novel mode of action in which low micromolar levels of CQ permeabilized the parasite's digestive vacuole (DV) membrane, leading to calcium efflux, mitochondrial depolarization and DNA degradation. These phenotypes implicate the DV as an alternative target of CQ and suggests that DV disruption is an attractive target for exploitation through the screening for DV-disruptive antimalarials...
January 8, 2018: Antimicrobial Agents and Chemotherapy
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