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https://www.readbyqxmd.com/read/28604588/docosahexaenoic-acid-induces-expression-of-heme-oxygenase-1-and-nad-p-h-quinone-oxidoreductase-through-activation-of-nrf2-in-human-mammary-epithelial-cells
#1
Hye-Yoon Bang, Sin-Aye Park, Soma Saeidi, Hye-Kyung Na, Young-Joon Surh
Docosahexaenoic acid (DHA), an ω-3 fatty acid abundant in fish oils, has diverse health beneficial effects, such as anti-oxidative, anti-inflammatory, neuroprotective, and chemopreventive activities. In this study, we found that DHA induced expression of two representative antioxidant/cytoprotective enzymes, heme oxygenase-1 (HO-1) and NAD(P)H:quinone oxidoreductase (NQO1), in human mammary epithealial (MCF-10A) cells. DHA-induced upregulation of these enzymes was accompanied by enhanced translocation of the redox-sensitive transcription factor Nrf2 into the nucleus and its binding to antioxidant response element...
June 10, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28570591/statin-and-rottlerin-small-molecule-inhibitors-restrict-colon-cancer-progression-and-metastasis-via-macc1
#2
Manisha Juneja, Dennis Kobelt, Wolfgang Walther, Cynthia Voss, Janice Smith, Edgar Specker, Martin Neuenschwander, Björn-Oliver Gohlke, Mathias Dahlmann, Silke Radetzki, Robert Preissner, Jens Peter von Kries, Peter Michael Schlag, Ulrike Stein
MACC1 (Metastasis Associated in Colon Cancer 1) is a key driver and prognostic biomarker for cancer progression and metastasis in a large variety of solid tumor types, particularly colorectal cancer (CRC). However, no MACC1 inhibitors have been identified yet. Therefore, we aimed to target MACC1 expression using a luciferase reporter-based high-throughput screening with the ChemBioNet library of more than 30,000 compounds. The small molecules lovastatin and rottlerin emerged as the most potent MACC1 transcriptional inhibitors...
June 2017: PLoS Biology
https://www.readbyqxmd.com/read/28539656/pkc-%C3%AE-isoform-plays-a-crucial-role-in-tat-tlr4-signalling-pathway-to-activate-nf-%C3%AE%C2%BAb-and-cxcl8-production
#3
Manutea Serrero, Rémi Planès, Elmostafa Bahraoui
HIV-1 Tat protein induces the production of CXCL8 chemokine in a TLR4/MD2 and PKC dependent manner. The objective of this study was to understand whether these two pathways were distinct or constituted a single common pathway, and to determine the nature of the PKC isoforms involved and their interrelation with the activation of NF-κB and CXCL8 gene product expression. Here, we show that Tat-induced CXCL8 production is essentially dependent on the activation of PKC delta isoform, as shown a) by the capacity of PKC delta dominant negative (DN), and Rottlerin, a selective PKC delta pharmacological inhibitor, to inhibit Tat-induced CXCL8 production and b) by the ability of the constitutively active (CAT) isoform of PKC delta to induce CXCL8 production in a HEK cell line in the absence of Tat stimulation...
May 24, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28535942/gallic-acid-increases-atrial-natriuretic-peptide-secretion-and-mechanical-dynamics-through-activation-of-pkc
#4
Xia Liu, Ying Zhang, Lan Hong, Chun-Ji Han, Bo Zhang, Shuai Zhou, Cheng-Zhe Wu, Li-Ping Liu, Xun Cui
AIMS: Gallic acid (GA) protects against myocardial ischemia-reperfusion (I/R) injury, prevents cardiac hypertrophy and fibrosis, and has anti-inflammatory activity in the heart. However, its effects in regulating atrial natriuretic peptide (ANP) secretion are unknown. The aim of this study was to determine the function of GA in regulating ANP secretion and atrial dynamics in rat atria. KEY FINDINGS: GA (0.01, 0.05, and 0.1μmol/L) significantly increased atrial ANP secretion and induced positive inotropy dose-dependently...
May 20, 2017: Life Sciences
https://www.readbyqxmd.com/read/28513986/pleiotropic-effects-of-chronic-phorbol-ester-treatment-to-improve-glucose-transport-in-insulin-resistant-cardiomyocytes
#5
Christelle Viglino, Bahareh Khoramdin, Guillaume Praplan, Christophe Montessuit
Stimulation of glucose transport is an important determinant of myocardial susceptibility to ischemia and reperfusion. Stimulation of glucose transport is markedly impaired in cardiomyocytes exposed to free fatty acids (FFA). Deactivation of the Focal Adhesion Kinase (FAK) by FFA contributes to glucose transport impairment, and could be corrected by chronic treatment with the phorbol ester TPA. However, TPA must have effects in addition to FAK reactivation to restore stimulated glucose transport. Chronic treatment with TPA improved basal and stimulated glucose transport in FFA-exposed, but not in control cardiomyocytes...
May 17, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28455500/rottlerin-mediated-inhibition-of-toxoplasma-gondii-growth-in-bewo-trophoblast-like-cells
#6
Francesca Ietta, Emanuela Maioli, Elena Daveri, Juliana Gonzaga Oliveira, Rafaela José da Silva, Roberta Romagnoli, Laura Cresti, Anna Maria Avanzati, Luana Paulesu, Bellisa de Freitas Barbosa, Angelica de Oliveira Gomes, José Roberto Mineo, Eloisa Amália Vieira Ferro
Autophagy is a crucial and physiological process for cell survival from yeast to mammals, including protozoan parasites. Toxoplasma gondii, an intracellular parasite, typically exploits autophagic machinery of host cell; however host cell upregulates autophagy to combat the infection. Herein we tested the efficacy of Rottlerin, a natural polyphenol with autophagic promoting properties, against Toxoplasma infection on the chorioncarcinoma-derived cell line BeWo. We found that Rottlerin, at sub-toxic doses, induced morphological and biochemical alterations associated with autophagy and decreased Toxoplasma growth in infected cells...
April 28, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28423559/rottlerin-as-a-novel-chemotherapy-agent-for-adrenocortical-carcinoma
#7
Yi Zhu, Minjie Wang, Xu Zhao, Lei Zhang, Yigao Wu, Bangqi Wang, Weilie Hu
Adrenocortical carcinoma (ACC) is a rare, but aggressive endocrine malignancy with a generally poor clinical outcome. There is no effective therapy for advanced and metastatic ACC. In our study, we found that an existing drug (rottlerin) exerted its tumour-suppressive function in ACC. Specifically, rottlerin inhibited cellular proliferation of ACC cell lines (NCI-H295R and SW-13) in a dose- and time-dependent manner. We also found that rottlerin induced cell apoptosis and promoted G0/G1 cell cycle arrest in ACC cell lines...
April 4, 2017: Oncotarget
https://www.readbyqxmd.com/read/28373608/protein-kinase-c-%C3%AE-signaling-regulates-glucagon-secretion-from-pancreatic-islets
#8
Kiyotake Yamamoto, Hiroyuki Mizuguchi, Natsumi Tokashiki, Makoto Kobayashi, Motoyuki Tamaki, Youichi Sato, Hiroyuki Fukui, Aiko Yamauchi
Accumulating evidence supports the "glucagonocentric hypothesis", in which antecedent α-cell failure and inhibition of glucagon secretion are responsible for diabetes progression. Protein kinase C (PKC) is involved in glucagon secretion from α-cells, although which PKC isozyme is involved and the mechanism underlying this PKC-regulated glucagon secretion remains unknown. Here, the involvement of PKCδ in the onset and progression of diabetes was elucidated. Immunofluorescence studies revealed that PKCδ was expressed and activated in α-cells of STZ-induced diabetic model mice...
2017: Journal of Medical Investigation: JMI
https://www.readbyqxmd.com/read/28373118/synergism-between-pkc%C3%AE-regulators-hypericin-and-rottlerin-enhances-apoptosis-in-u87-mg-glioma-cells-after-light-stimulation
#9
Matus Misuth, Denis Horvath, Pavol Miskovsky, Veronika Huntosova
BACKGROUND: Gliomas belong to the most infiltrative types of tumors. Photodynamic therapy (PDT) can be applied to regulate glioma cell proliferation. The inhibitors of PKCs are very promising drugs that can mediate glioma cells apoptosis in PDT. Hypericin is one of PKCs regulators, and thanks to its physicochemical properties it can be used in PDT. Rottlerin is also considered to be the PKCδ inhibitor. Its implementation in PDT may significantly influence glioma cells response to PDT...
March 31, 2017: Photodiagnosis and Photodynamic Therapy
https://www.readbyqxmd.com/read/28286125/n-propyl-gallate-suppresses-lipopolysaccharide-induced-inducible-nitric-oxide-synthase-activation-through-protein-kinase-c%C3%AE-mediated-up-regulation-of-heme-oxygenase-1-in-raw264-7-macrophages
#10
Wookwang Jeon, Seong Ji Park, Byung-Chul Kim
n-Propyl gallate is a synthetic phenolic antioxidant with potential anti-inflammatory effects. However, the underlying mechanism remains largely unknown. In the present study, we showed that n-propyl gallate increases the expression and activity of the heme oxygenase-1 (HO-1), a stress-inducible protein with potent anti-inflammatory activity, in RAW264.7 macrophages. The inhibition of the HO-1 activity by treatment with zinc (II) protoporphyrin IX (ZnPP) or by knockdown of the HO-1 expression with small interference RNA significantly reversed the inhibitory effect of n-Propyl gallate on activations of nuclear factor-κB (NF-κB) and inducible nitric oxide synthase (iNOS) induced by lipopolysaccharide (LPS)...
April 15, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28182013/duodenal-glp-1-signaling-regulates-hepatic-glucose-production-through-a-pkc-%C3%AE-dependent-neurocircuitry
#11
Mengliu Yang, Jinzhi Wang, Shaobo Wu, Lei Yuan, Xiaodong Zhao, Chaohong Liu, Jing Xie, Yanjun Jia, Yerui Lai, Allan Zijian Zhao, Guenther Boden, Ling Li, Gangyi Yang
Intestinal glucagon-like peptide-1 (GLP-1) is a hormone that stimulates insulin secretion and acts as a neuropeptide to control glucose homeostasis, but little is known whether intestinal GLP-1 has any effect in the control of hepatic glucose production (HGP). Here we found that intraduodenal infusion of GLP-1 activated duodenal PKC-δ, lowered HGP and was accompanied by a decrease in hepatic expression of gluconeogenic enzymes and an increase in hepatic insulin signaling in rats. However, gut co-infusion of either the GLP-1 receptor antagonist Ex-9, or the PKC-δ inhibitor rottlerin with GLP-1, negated the ability of gut GLP-1 to lower HGP and to increase hepatic insulin signaling during clamps...
February 9, 2017: Cell Death & Disease
https://www.readbyqxmd.com/read/28161478/identification-of-tg100-115-as-a-new-and-potent-trpm7-kinase-inhibitor-which-suppresses-breast-cancer-cell-migration-and-invasion
#12
Chiman Song, Yeonju Bae, JinJoo Jun, Hyomin Lee, Nam Doo Kim, Kyung-Bok Lee, Wooyoung Hur, Jae-Yong Park, Taebo Sim
BACKGROUND: Transient receptor potential melastatin 7 (TRPM7) regulates breast cancer cell proliferation, migration, invasion and metastasis in its ion channel- and kinase domain-dependent manner. The pharmacological effects of TRPM7 ion channel inhibitors on breast cancer cells have been studied, but little is known about the effects of TRPM7 kinase domain inhibitors due to lack of potent TRPM7 kinase inhibitors. METHODS: Screening was performed by using TRPM7 kinase assay...
April 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28101215/rottlerin-induced-autophagy-leads-to-apoptosis-in-bladder-cancer-cells
#13
Ping Qi, Zhenhua He, Lixiu Zhang, Yuan Fan, Zhiping Wang
It has been well-established that apoptosis contributes to cancer cell death; however, the role of autophagy in cancer cell death remains unclear. The aim of the present study was to investigate the effects of rottlerin, a traditional Indian medicine, on cell growth inhibition and autophagy in EJ human bladder carcinoma cells in vitro. Cell viability, measured by MTT assay, was found to be suppressed in a dose- and time-dependent manner. In addition, apoptosis was significantly increased in cells treated with rottlerin, as indicated by increased annexin V-fluorescein isothiocyanate/propidium iodide staining and changes in the cell cycle distribution that indicated blockage at G1 phase...
December 2016: Oncology Letters
https://www.readbyqxmd.com/read/27999199/rottlerin-exhibits-antitumor-activity-via-down-regulation-of-taz-in-non-small-cell-lung-cancer
#14
Zhe Zhao, Nana Zheng, Lixia Wang, Yingying Hou, Xiuxia Zhou, Zhiwei Wang
Rottlerin, a polyphenolic compound derived from Mallotus philipinensis, has been reported to exhibit anti-tumor activities in a variety of human malignancies including NSCLC (non-small cell lung cancer). TAZ (transcriptional co-activator with PDZ-binding motif), one of the key activators in Hippo pathway, has been characterized as an oncoprotein. Therefore, inhibition of TAZ could be useful for the treatment of human cancers. In the current study, we aimed to explore whether rottlerin inhibits the expression of TAZ in NSCLC, leading to its anti-cancer activity...
January 31, 2017: Oncotarget
https://www.readbyqxmd.com/read/27997884/the-natural-plant-product-rottlerin-activates-kv7-1-kcne1-channels
#15
Veronika Matschke, Ilaria Piccini, Janina Schubert, Eva Wrobel, Florian Lang, Johann Matschke, Elsie Amedonu, Sven G Meuth, Timo Strünker, Nathalie Strutz-Seebohm, Boris Greber, Jürgen Scherkenbeck, Guiscard Seebohm
BACKGROUND/AIMS: Acquired as well as inherited channelopathies are disorders that are caused by altered ion channel function. A family of channels whose malfunction is associated with different channelopathies is the Kv7 K+ channel family; and restoration of normal Kv7 channel function by small molecule modulators is a promising approach for treatment of these often fatal diseases. METHODS: Here, we show the modulation of Kv7 channels by the natural compound Rottlerin heterologously expressed in Xenopus laevis oocytes and on iPSC cardiomyocytes overexpressing Kv7...
2016: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/27939242/ex4-stabilizes-and-activates-nrf2-via-pkc%C3%AE-contributing-to-the-prevention-of-oxidative-stress-induced-pancreatic-beta-cell-damage
#16
Mi-Hwi Kim, Eung-Hwi Kim, Hye Seung Jung, Dongki Yang, Eun-Young Park, Hee-Sook Jun
Oxidative stress in pancreatic beta cells can inhibit insulin secretion and promote apoptotic cell death. Exendin-4 (EX4), a glucagon-like peptide-1 receptor agonist, can suppress beta cell apoptosis, improve beta cell function and protect against oxidative damage. In this study, we investigated the molecular mechanisms for antioxidative effects of EX4 in pancreatic beta cells. INS-1 cells, a rat insulinoma cell line, were pretreated with EX4 and exposed to palmitate or H2O2. Reactive oxygen species (ROS) production, and glutathione and insulin secretion were measured...
January 15, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/27923483/regulation-of-membrane-type-1-matrix-metalloproteinase-activity-and-intracellular-localization-in-clinical-thoracic-aortic-aneurysms
#17
John S Ikonomidis, Elizabeth K Nadeau, Adam W Akerman, Robert E Stroud, Rupak Mukherjee, Jeffrey A Jones
OBJECTIVE: Membrane type-1 matrix metalloproteinase (MT1-MMP) is elevated during thoracic aortic aneurysm (TAA) development in mouse models, and plays an important role in the activation of matrix metalloproteinase (MMP)-2 and the release of matrix- bound transforming growth factor-β. In this study, we tested the hypothesis that MT1-MMP is subject to protein kinase C (PKC)-mediated regulation, which alters intracellular trafficking and activity with TAAs. METHODS: Levels of MMP-2, native and phosphorylated MT1-MMP, and PKC-δ were measured in aortic tissue from patients with small TAAs (<5 cm; n = 8) and large TAAs (>6...
March 2017: Journal of Thoracic and Cardiovascular Surgery
https://www.readbyqxmd.com/read/27889758/stimulation-of-suicidal-erythrocyte-death-by-rottlerin
#18
Morena Mischitelli, Mohamed Jemaà, Mustafa Almasry, Caterina Faggio, Florian Lang
BACKGROUND/AIMS: The phytochemical polyphenol rottlerin is a potent activator of diverse Ca2+ -sensitive K+ channels. Those channels play a decisive role in the execution of eryptosis, the suicidal death of erythrocytes, which is characterized by cell shrinkage and cell membrane scrambling with phosphatidylserine translocation to the erythrocyte surface. Signaling involved in the stimulation of eryptosis includes increase of cytosolic Ca2+ activity ([Ca2+]i) and ceramide. The present study explored, whether rottlerin induces eryptosis and, if so, to test for the involvement of Ca2+ entry and ceramide...
2016: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/27822410/rottlerin-exhibits-anti-cancer-effect-through-inactivation-of-s-phase-kinase-associated-protein-2-in-pancreatic-cancer-cells
#19
Jingna Su, Lixia Wang, Xuyuan Yin, Zhe Zhao, Yingying Hou, Xiantao Ye, Xiuxia Zhou, Zhiwei Wang
Rottlerin, a natural product isolated from Mallotus philippinensis, has been characterized as an effective chemoprevention agent in inhibiting tumor cell growth. Although multiple studies have revealed the role of rottlerin in tumorigenesis, the molecular mechanism of rottlerin-mediated anti-tumor activity has not been fully elucidated. It has been reported that Skp2 (S-phase kinase associated protein 2) plays an oncogenic role in human malignancies, indicating that inactivation of Skp2 could be a promising approach for the treatment of cancers...
2016: American Journal of Cancer Research
https://www.readbyqxmd.com/read/27799485/protein-kinase-c%C3%AE-suppresses-autophagy-to-induce-kidney-cell-apoptosis-in-cisplatin-nephrotoxicity
#20
Dongshan Zhang, Jian Pan, Xudong Xiang, Yu Liu, Guie Dong, Man J Livingston, Jian-Kang Chen, Xiao-Ming Yin, Zheng Dong
Nephrotoxicity is a major adverse effect in cisplatin chemotherapy, and renoprotective approaches are unavailable. Recent work unveiled a critical role of protein kinase Cδ (PKCδ) in cisplatin nephrotoxicity and further demonstrated that inhibition of PKCδ not only protects kidneys but enhances the chemotherapeutic effect of cisplatin in tumors; however, the underlying mechanisms remain elusive. Here, we show that cisplatin induced rapid activation of autophagy in cultured kidney tubular cells and in the kidneys of injected mice...
April 2017: Journal of the American Society of Nephrology: JASN
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