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https://www.readbyqxmd.com/read/29792023/fern-9-11-ene-2%C3%AE-3%C3%AE-diol-action-on-insulin-secretion-in-hyperglycemic-conditions
#1
Allisson Jhonatan Gomes Castro, Luisa Helena Cazarolli, Gabrielle Da Luz, Delsi Altenhofen, Hemily Batista Da Silva, Francieli Kanumfre Carvalho, Moacir Geraldo Pizzolatti, Fátima Rmb Silva
The objective of this study was to investigate the effect and the mechanism of action of fernenediol as insulin secretagogue. Wistar rats were treated with 0.1; 1 and 10 mg/kg fernenediol and then induced hyperglycemia by oral glucose. The glycaemia, insulin, LDH, calcium and hepatic glycogen were analyzed. Considering the intestine and pancreas as targets for the triterpene action, the duodenum was used to verify the influence of fernenediol on intestinal glycosidases. Additionally, pancreatic islets were used for studies of 14 C-deoxyglucose uptake and influx of 45 Ca2+ in hyperglycemic medium with/without fernenediol in the presence/absence of an inhibitor/activator of KATP channels, glibenclamide, diazoxide, nifedipine, calcium chelator (BAPTA- AM) and H-89 and ST the inhibitors of the PKA and PKC enzymes...
May 24, 2018: Biochemistry
https://www.readbyqxmd.com/read/29789532/ferroptosis-inducing-agents-compromise-in-vitro-human-islet-viability-and-function
#2
Antonio Bruni, Andrew R Pepper, Rena L Pawlick, Boris Gala-Lopez, Anissa F Gamble, Tatsuya Kin, Karen Seeberger, Gregory S Korbutt, Stefan R Bornstein, Andreas Linkermann, A M James Shapiro
Human islet transplantation has been hampered by donor cell death associated with the islet preparation procedure before transplantation. Regulated necrosis pathways are biochemically and morphologically distinct from apoptosis. Recently, ferroptosis was identified as a non-apoptotic form of iron-dependent regulated necrosis implicated in various pathological conditions. Mediators of islet oxidative stress, including glutathione peroxidase-4 (GPX4), have been identified as inhibitors of ferroptosis, and mechanisms that affect GPX4 function can impact islet function and viability...
May 22, 2018: Cell Death & Disease
https://www.readbyqxmd.com/read/29787771/inhibition-of-pten-protects-pc12-cells-against-oxygen-glucose-deprivation-induced-cell-death-through-mitoprotection
#3
Fereshteh Farajdokht, Gisou Mohaddes, Elham Karimi-Sales, Taiebeh Kafshdooz, Javad Mahmoudi, Seyed Mohsen Aberoumandi, Pouran Karimi
Mitochondria involve in the determination of ischemic neuronal cell fate through regulation of apoptotic and necrotic cell death. Phosphatase and tensin homolog (PTEN) protein negatively regulates Akt/PKB signaling which is the major cell survival pathway. The current study aimed to examine the impact of SF1670, a potent PTEN inhibitor, on mitochondria-mediated cell survival pathways in an in vitro stroke-like model. PC12 cells were exposed to one hour oxygen and glucose deprivation (OGD) followed by different time points of reperfusion (0, 30, 60, 120 and 180 min) and SF1670 treatments...
May 19, 2018: Brain Research
https://www.readbyqxmd.com/read/29782381/high-baseline-neutrophil-to-lymphocyte-ratio-predicts-worse-outcome-in-patients-with-metastatic-braf-positive-melanoma-treated-with-braf-and-mek-inhibitors
#4
Paweł Teterycz, Paulina Jagodzińska-Mucha, Bożena Cybulska-Stopa, Anna Mariuk-Jarema, Katarzyna Kozak, Hanna Koseła-Paterczyk, Anna M Czarnecka, Marcin Rajczykowski, Robert Dziura, Łukasz Galus, Jacek Mackiewicz, Tomasz Świtaj, Anna Klimczak, Slawomir Falkowski, Rafał Suwiński, Marek Ziobro, Iwona Ługowska, Piotr Rutkowski
Neutrophil-to-lymphocyte ratio (NLR) has been shown to be prognostic in several solid malignancies. There are limited data regarding its value during novel therapies in patients with melanoma. The aim of the study was to assess the practical utility of this ratio in patients with BRAF-mutant melanoma treated with a combination of BRAF and MEK inhibitors (BRAFi/MEKi). We included 215 patients with inoperable or metastatic melanoma who underwent BRAFi/MEKi treatment between October 2015 and June 2017. Baseline NLR and other complete blood count-derived inflammatory markers were tested for association with overall survival and progression-free survival in univariate and multivariate models...
May 18, 2018: Melanoma Research
https://www.readbyqxmd.com/read/29772481/vascular-peroxide-1-promotes-ox-ldl-induced-programmed-necrosis-in-endothelial-cells-through-a-mechanism-involving-%C3%AE-catenin-signaling
#5
Yin-Zhuang Zhang, Lei Wang, Jie-Jie Zhang, Xiao-Ming Xiong, Di Zhang, Xuan-Meng Tang, Xiu-Ju Luo, Qi-Lin Ma, Jun Peng
BACKGROUND AND AIMS: Vascular peroxidase 1 (VPO1) plays a key role in mediation of cardiovascular oxidative injury. This study aims to determine whether VPO1 can promote programmed necrosis of endothelial cells and the underlying mechanisms. METHODS AND RESULTS: Human umbilical vein endothelial cells (HUVECs) were incubated with oxidized low-density lipoprotein (ox-LDL, 100 μg/mL) for 48 h to induce cell injury, which showed an elevation in cell necrosis (reflected by the increased propidium iodide (PI) positive-staining cells, LDH release and decreased cell viability), concomitant with an increase in programmed necrosis-relevant proteins including receptor-interacting protein kinase 1/3 (RIPK1/3), p-RIPK3 and mixed lineage kinase domain like (MLKL); these phenomena were attenuated by necrostatin-1(Nec-1) and RIPK3 siRNA...
May 3, 2018: Atherosclerosis
https://www.readbyqxmd.com/read/29771406/bay-11-7082-induces-apoptosis-of-multiple-myeloma-u266-cells-through-inhibiting-nf-%C3%AE%C2%BAb-pathway
#6
Y Wang, X-L Zhang, C-M Sun
OBJECTIVE: To study the effects of BAY-11-7082 on proliferation and apoptosis of U266 cells and its mechanism of action. MATERIALS AND METHODS: Multiple myelomas U266 cells were cultured and divided into control group and gradient-concentration BAY-11-7082 groups (1 μmol/L, 2 μmol/L, 4 μmol/L and 8 μmol/L). Cells in BAY-11-7082 groups were treated with drugs in different concentrations for 4 h, while those in control group were added with an equal volume of solvent...
May 2018: European Review for Medical and Pharmacological Sciences
https://www.readbyqxmd.com/read/29767261/inhibition-of-mek-erk-stat3-signaling-in-oleuropein-treatment-inhibits-myocardial-ischemia-reperfusion
#7
Hong-Xu Jin, Yun-Hu Zhang, Ruo-Nan Guo, Su-Nuan Zhao
Studies have shown that oleuropein has antifungal, anti‑inflammatory, antiviral, antioxidant, anticancer and hypoglycemic functions. TTC solution staining was used to measure myocardial infarction size. A commercial kit was used to measure lactate dehydrogenase (LDH), creatinine kinase‑MB (CK‑MB), tumor necrosis factor‑α (TNF‑α), interleukin‑1β (IL‑1β), IL 6, superoxide dismutase (SOD), glutathione (GSH), malondialdehyde (MDA) and catalase levels. Western blot analysis was used to measure p53, p-MEK p-ERK and p‑IκBα protein expression...
May 11, 2018: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/29755548/ameliorative-effect-of-beraprost-sodium-on-celecoxib-induced-cardiotoxicity-in-rats
#8
Shafique Ahmad, Bibhu Prasad Panda, Mohammad Fahim, Neha Dhyani, Kiran Dubey
Selective COX-2 inhibitors are most widely used analgesic and anti-inflammatory drugs; however, its maximal use is highly associated with various serious abnormal cardiovascular events. Beraprost sodium (BPS), prostacyclin analogue has been shown to vasodilatory, antiplatelates, anti-inflmmatory, and antioxidant activity. The objective of the present study was to evaluate the effect of BPS on celecoxib cardiotoxicity in rats. Toxicity was induced in male Albino rats (250-280 g) by celecoxib (100 mg/kg/day)...
2018: Iranian Journal of Pharmaceutical Research: IJPR
https://www.readbyqxmd.com/read/29747595/the-search-for-a-melanoma-tailored-chemotherapy-in-the-new-era-of-personalized-therapy-a-phase-ii-study-of-chemo-modulating-temozolomide-followed-by-fotemustine-and-a-cooperative-study-of-goim-gruppo-oncologico-italia-meridionale
#9
Michele Guida, Stefania Tommasi, Sabino Strippoli, Maria Iole Natalicchio, Simona De Summa, Rosamaria Pinto, Antonio Cramarossa, Anna Albano, Salvatore Pisconti, Michele Aieta, Ruggiero Ridolfi, Amalia Azzariti, Gabriella Guida, Vito Lorusso, Giusepe Colucci
BACKGROUND: It is frequently asked whether chemotherapy can still play a role in metastatic melanoma considering the effectiveness of the available drugs today, including antiCTLA4/antiPD1 immunotherapy and antiBRAF/antiMEK inhibitors. However, only approximately half of patients respond to these drugs, and the majority progress after 6-11 months. Therefore, a need for other therapeutic options is still very much apparent. We report the first large trial of a sequential full dose of fotemustine (FM) preceded by a low dose of temozolomide (TMZ) as a chemo-modulator in order to inactivate the DNA repair action of O(6)-methylguanine DNA-methyltransferase (MGMT)...
May 10, 2018: BMC Cancer
https://www.readbyqxmd.com/read/29747052/oleanolic-acid-protects-against-cognitive-decline-and-neuroinflammation-mediated-neurotoxicity-by-blocking-secretory-phospholipase-a2-iia-activated-calcium-signals
#10
Leguo Zhang, Ruixue Xia, Jianpu Jia, Lixuan Wang, Kuo Li, Yanhua Li, Junling Zhang
Neuroinflammation causes neurotoxic injury and underlies the pathogenesis of neurodegenerative disorders including Alzheimer's disease (AD). Astrocytes are the predominant immunoregulatory cells in AD. Oleanolic acid (OA) is a promising anti-inflammatory therapeutic agent that can ameliorate cerebral damage in ischemic environments, but its role in AD remains poorly elucidated. Here, preconditioning with OA inhibited the transcription and secretion of inflammatory cytokines IL-6, TNF-α, and IL-1β in amyloid-beta peptide (Aβ)-activated astrocytes...
May 7, 2018: Molecular Immunology
https://www.readbyqxmd.com/read/29746779/energy-metabolism-drugs-block-triple-negative-breast-metastatic-cancer-cell-phenotype
#11
Silvia Cecilia Pacheco-Velazquez, Diana Xochiquetzal Robledo-Cadena, Ileana Hernández-Reséndiz, Juan Carlos Gallardo-Pérez, Rafael Moreno-Sánchez, Sara Rodríguez-Enríquez
To establish alternative targeted therapies against triple negative (TN) breast cancer, (1) the energy metabolism and (2) the sensitivity of cell growth, migration and invasiveness towards metabolic, canonical and NSAID inhibitors was analyzed in MDA-MB-231 and MDA-MB-468, two TN metastatic breast cancer cell lines, under both normoxia (21% O2) and hypoxia (0.1% O2). For comparative purposes, analysis was also carried out in the less-metastatic breast MCF-7 cancer cells. Under normoxia, oxidative phosphorylation (OxPhos) was significantly higher (2-times) in MDA-MB-468 than in MDA-MB-231 and MCF-7 whereas their glycolytic fluxes and OxPhos and glycolytic protein contents were all similar...
May 10, 2018: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29741915/the-role-of-microrna-1-targeting-mapk3-in-myocardial-ischemia-reperfusion-injury-in-rats-undergoing-sevoflurane-preconditioning-via-the-pi3k-akt-pathway
#12
Yun-Ling Hao, Hong-Cheng Fang, Hong-Lei Zhao, Xiao-Li Li, Ying Luo, Bao-Quan Wu, Ming-Jie Fu, Wei Liu, Jin-Jie Liang, Xie-Hui Chen
Recent studies have uncovered the vital roles played by microRNAs (miRNAs) in regulating cardiac injury. Amongst them, the cardiac enriched microRNA-1 (miR-1) has been extensively studied and proven to be detrimental to cardiac myocytes. Hence, the current study aims to explore whether miR-1 affects myocardial ischemia/reperfusion injury (MIRI) in rats undergoing sevoflurane preconditioning and the underlying mechanism. After successful model establishment, rats with MIRI were transfected with mimics or inhibitors of miR-1, or siRNA against MAPK3, and then were injected with sevoflurane...
May 9, 2018: American Journal of Physiology. Cell Physiology
https://www.readbyqxmd.com/read/29738843/transporter-dependent-cytotoxicity-of-antiviral-drugs-in-primary-cultures-of-human-proximal-tubular-cells
#13
Lawrence H Lash, Caroline A Lee, Clynn Wilker, Vishal Shah
The role of plasma membrane transporters in the nephrotoxicity of two antiretroviral drugs, cidofovir and tenofovir, was studied in primary cultures of human proximal tubular (hPT) cells. Cells were grown on Transwell filter inserts to maintain epithelial polarity and access to either the apical or basolateral plasma membrane. The function of relevant membrane transporters, organic anion transporter 1 and 3 (OAT1/3), P-glycoprotein (multidrug resistance protein-1; P-gp or MDR1), and organic cation transporter 2 (OCT2), was validated by measurements of apical-to-basolateral and basolateral-to-apical fluxes of furosemide, digoxin, and metformin, respectively...
May 5, 2018: Toxicology
https://www.readbyqxmd.com/read/29729269/ll-37-induced-human-osteoblast-cytotoxicity-and-permeability-occurs-independently-of-cellular-ll-37-uptake-through-clathrin-mediated-endocytosis
#14
Emma Anders, Sara Dahl, Daniel Svensson, Bengt-Olof Nilsson
The host defense peptide LL-37 is cytotoxic for bacteria but it has also been reported to reduce host cell viability through an intracellular mechanism. LL-37-evoked cytotoxicity may be involved in the loss of bone tissue in periodontitis which is an inflammatory disease characterized by high concentrations of LL-37 observed locally in the periodontal tissue at the inflammation process. Here, we showed that LL-37 reduced human osteoblast-like MG63 cell viability assessed by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and increased plasma membrane permeability determined by measuring intracellular Ca2+ levels and lactate dehydrogenase (LDH) release...
May 2, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29721178/extracellular-nicotinamide-phosphoribosyltransferase-enampt-is-a-novel-marker-for-patients-with-braf-mutated-metastatic-melanoma
#15
Valentina Audrito, Antonella Managò, Federica Zamporlini, Eliana Rulli, Federica Gaudino, Gabriele Madonna, Stefania D'Atri, Gian Carlo Antonini Cappellini, Paolo Antonio Ascierto, Daniela Massi, Nadia Raffaelli, Mario Mandalà, Silvia Deaglio
Metastatic melanoma carrying BRAF mutations represent a still unmet medical need as success of BRAF inhibitors is limited by development of resistance. Nicotinamide phosphoribosyltransferase (NAMPT) is a key enzyme in NAD biosynthesis. An extracellular form (eNAMPT) possesses cytokine-like functions and is up-regulated in inflammatory disorders, including cancer. Here we show that eNAMPT is actively released in culture supernatants of melanoma cell lines. Furthermore, cells that become resistant to BRAF inhibitors (BiR) show a significant increase of eNAMPT levels...
April 10, 2018: Oncotarget
https://www.readbyqxmd.com/read/29719506/araloside-c-prevents-hypoxia-reoxygenation-induced-endoplasmic-reticulum-stress-via-increasing-heat-shock-protein-90-in-h9c2-cardiomyocytes
#16
Yuyang Du, Min Wang, Xuesong Liu, Jingyi Zhang, Xudong Xu, Huibo Xu, Guibo Sun, Xiaobo Sun
Araloside C (AsC) is a cardioprotective triterpenoid compound that is mainly isolated from Aralia elata . This study aims to determine the effects of AsC on hypoxia-reoxygenation (H/R)-induced apoptosis in H9c2 cardiomyocytes and its underlying mechanisms. Results demonstrated that pretreatment with AsC (12.5 μM) for 12 h significantly suppressed the H/R injury in H9c2 cardiomyocytes, including improving cell viability, attenuating the LDH leakage and preventing cardiomyocyte apoptosis. AsC also inhibited H/R-induced ER stress by reducing the activation of ER stress pathways (PERK/eIF2α and ATF6), and decreasing the expression of ER stress-related apoptotic proteins (CHOP and caspase-12)...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29717767/bisphosfonate-matrix-metalloproteinase-inhibitors-for-the-treatment-of-periodontitis-an-in-vitro-study
#17
Marianna De Colli, Paolo Tortorella, Mariangela Agamennone, Cristina Campestre, Fulvio Loiodice, Amelia Cataldi, Susi Zara
Periodontitis is an inflammatory disease caused by anaerobic bacteria, including Porphyromonas gingivalis. Lipopolysaccharide (LPS)‑stimulated persistent inflammation is responsible for an increase in matrix metalloproteinase (MMP) expression, resulting in periodontal tissue destruction. The aim of the present study was to investigate synthesized bisphosphonic MMP inhibitors, in an in vitro model consisting of human gingival fibroblasts exposed to LPS, and to compare the biological responses to those induced by zoledronate (ZA), a commercial bisphosphonate...
April 25, 2018: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/29705352/apigenin-7-o-%C3%AE-d-6%C3%A2-p-coumaroyl-glucopyranoside-pretreatment-attenuates-myocardial-ischemia-reperfusion-injury-via-activating-ampk-signaling
#18
Yingda Feng, Yunyang Lu, Dan Liu, Wei Zhang, Juntian Liu, Haifeng Tang, Yanrong Zhu
AIMS: Apigenin-7-O-β-d-(-6″-p-coumaroyl)-glucopyranoside (APG) was considered as the major active compound derived from Clematis tangutica. Though we have demonstrated that APG exerts cardioprotective effects, the mechanism of APG-mediated cardioprotection remains largely unknown. Numerous studies indicate that endoplasmic reticulum stress (ERS) is a vital injury factor in myocardial ischemia reperfusion (MI/R). In this study, we mainly investigated whether modulation of the ERS and AMPK were involved in the cardioprotective action of APG during MI/R injury...
April 26, 2018: Life Sciences
https://www.readbyqxmd.com/read/29704006/intracellular-glycolysis-in-brown-adipose-tissue-is-essential-for-optogenetically-induced-nonshivering-thermogenesis-in-mice
#19
Jae Hoon Jeong, Ji Suk Chang, Young-Hwan Jo
Release of fatty acids from lipid droplets upon activation of the sympathetic nervous system (SNS) is a key step in nonshivering thermogenesis in brown adipose tissue (BAT). However, intracellular lipolysis appears not to be critical for cold-induced thermogenesis. As activation of the SNS increases glucose uptake, we studied whether intracellular glycolysis plays a role in BAT thermogenesis. To stimulate BAT-innervating sympathetic nerves in vivo, we expressed channelrhodopsin-2 (ChR2) in catecholaminergic fibers by crossbreeding tyrosine hydroxylase-Cre mice with floxed-stop ChR2 mice...
April 27, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29693750/protein-phosphatase-2a-mediates-js-k-induced-apoptosis-by-affecting-bcl-2-family-proteins-in-human-hepatocellular-carcinoma-hepg2-cells
#20
Ling Liu, Zile Huang, Jingjing Chen, Jiangang Wang, Shuying Wang
Protein phosphatase 2A (PP2A) is an important enzyme within various signal transduction pathways. The present study was investigated PP2A mediates JS-K-induced apoptosis by affecting Bcl-2 family protein. JS-K showed diverse inhibitory effects in five HCC cell lines, especially HepG2 cells. JS-K caused a dose- and time-dependent reduction in cell viability and increased in levels of LDH release. Meanwhile, JS-K- induced apoptosis was characterized by mitochondrial membrane potential reduction, Hoechst 33342+ /PI+ dual staining, release of cytochrome c (Cyt c), and activation of cleaved caspase-9/3...
April 25, 2018: Journal of Cellular Biochemistry
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