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https://www.readbyqxmd.com/read/28182013/duodenal-glp-1-signaling-regulates-hepatic-glucose-production-through-a-pkc-%C3%AE-dependent-neurocircuitry
#1
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
#2
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...
February 1, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28101215/rottlerin-induced-autophagy-leads-to-apoptosis-in-bladder-cancer-cells
#3
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
#4
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
#5
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
#6
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...
December 7, 2016: 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
#7
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...
November 14, 2016: Journal of Thoracic and Cardiovascular Surgery
https://www.readbyqxmd.com/read/27889758/stimulation-of-suicidal-erythrocyte-death-by-rottlerin
#8
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
#9
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
#10
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...
October 31, 2016: Journal of the American Society of Nephrology: JASN
https://www.readbyqxmd.com/read/27783407/efficient-pkc-inhibitor-screening-achieved-using-a-quantitative-ce-lif-assay
#11
Binh Thanh Nguyen, Min Park, Jae-Chul Pyun, Young Sook Yoo, Min-Jung Kang
An assay for protein kinase C delta (PKCδ) activity based on the quantification of a synthetic substrate using capillary electrophoresis with laser-induced fluorescence detection was developed. The peptides labeled with fluorescein isothiocyanate F-ERK (where ERK is extracellular signal-regulated kinase) and the phosphorylated form, P-F-ERK, were utilized for the method development and validation. The migration time of F-ERK and P-F-ERK were 6.3 ± 0.1 and 8.7 ± 0.2 min, respectively. LOD and LOQ values of F-ERK were 2 and 6 ng/mL and those of P-F-ERK were 4 and 12 ng/mL...
December 2016: Electrophoresis
https://www.readbyqxmd.com/read/27749013/high-motivation-for-exercise-is-associated-with-altered-chromatin-regulators-of-monoamine-receptor-gene-expression-in-the-striatum-of-selectively-bred-mice
#12
Michael Saul, Petra Majdak, Samuel Perez, Matthew Reilly, Theodore Garland, Justin S Rhodes
Though exercise is critical for health, many lack the motivation to exercise, and it is unclear how motivation might be increased. To uncover the molecular underpinnings of increased motivation for exercise, we analyzed the transcriptome of the striatum in four mouse lines selectively bred for high voluntary wheel running and four non-selected control lines. The striatum was dissected and RNA was extracted and sequenced from four individuals of each line. We found multiple genes and gene systems with strong relationships to both selection and running history over the previous 6 days...
October 17, 2016: Genes, Brain, and Behavior
https://www.readbyqxmd.com/read/27688248/synergistic-protective-effect-of-paeoniflorin-and-%C3%AE-ecdysterone-against-rotenone-induced-neurotoxicity-in-pc12-cells
#13
Han Liu, Chunlei Yu, Tianjiao Xu, Xiaojie Zhang, Miaoxian Dong
There are several factors, like oxidative stress and neurons loss, involving neurodegenerative diseases such as Parkinson's disease (PD). The combination of antioxidant and anti-apoptotic agent is becoming a promising approach to fight against PD. This study evaluates the hypothesis that paeoniflorin (PF) and β-ecdysterone (β-Ecd) synergize to protect PC12 cells against toxicity induced by PD-related neurotoxin rotenone. The combination of PF and β-Ecd, hereafter referred to as the PF/β-Ecd, at suboptimal concentrations increased the viability of rotenone-exposed PC12 cells in a synergistic manner...
September 29, 2016: Apoptosis: An International Journal on Programmed Cell Death
https://www.readbyqxmd.com/read/27665842/staurosporine-enhances-atra-induced-granulocytic-differentiation-in-human-leukemia-u937-cells-via-the-mek-erk-signaling-pathway
#14
Lei Shi, Xiang-Qin Weng, Yan Sheng, Jing Wu, Ming Ding, Xun Cai
Although all-trans retinoic acid (ATRA) is regarded as a prominent example of differentiation therapy, it is not effective for the treatment of other subtypes of acute myeloid leukemia (AML) beyond acute promyelocytic leukemia (APL). Therefore, new strategies need to be explored to extend the efficacy of ATRA-based therapy to non-APL AML patients. In the present study, staurosporine, a protein kinase C (PKC) pan-inhibitor, exhibited synergism with ATRA to promote granulocytic differentiation in poorly ATRA-sensitive U937 cells but not in ATRA unresponsive K562 and Kasumi cells...
November 2016: Oncology Reports
https://www.readbyqxmd.com/read/27626499/rottlerin-inhibits-cell-growth-and-invasion-via-down-regulation-of-cdc20-in-glioma-cells
#15
Lixia Wang, Yingying Hou, Xuyuan Yin, Jingna Su, Zhe Zhao, Xiantao Ye, Xiuxia Zhou, Li Zhou, Zhiwei Wang
Rottlerin, isolated from a medicinal plant Mallotus phillippinensis, has been demonstrated to inhibit cellular growth and induce cytoxicity in glioblastoma cell lines through inhibition of calmodulin-dependent protein kinase III. Emerging evidence suggests that rottlerin exerts its antitumor activity as a protein kinase C inhibitor. Although further studies revealed that rottlerin regulated multiple signaling pathways to suppress tumor cell growth, the exact molecular insight on rottlerin-mediated tumor inhibition is not fully elucidated...
September 12, 2016: Oncotarget
https://www.readbyqxmd.com/read/27623093/pkc%C3%AE-knockout-mice-are-protected-from-para-methoxymethamphetamine-induced-mitochondrial-stress-and-associated-neurotoxicity-in-the-striatum-of-mice
#16
Eun-Joo Shin, Duy-Khanh Dang, Hai-Quyen Tran, Yunsung Nam, Ji Hoon Jeong, Young Hun Lee, Kyung Tae Park, Yong Sup Lee, Choon-Gon Jang, Jau-Shyong Hong, Toshitaka Nabeshima, Hyoung-Chun Kim
Para-methoxymethamphetamine (PMMA) is a para-ring-substituted amphetamine derivative sold worldwide as an illegal psychotropic drug. Although PMMA use has been reported to lead to severe intoxication and even death, little is known about the mechanism(s) by which PMMA exerts its neurotoxic effects. Here we found that PMMA treatment resulted in phosphorylation of protein kinase Cδ (PKCδ) and subsequent mitochondrial translocation of cleaved PKCδ. PMMA-induced oxidative stress was more pronounced in mitochondria than in the cytosol...
September 10, 2016: Neurochemistry International
https://www.readbyqxmd.com/read/27606614/periodic-mechanical-stress-activates-pkc%C3%AE-dependent-egfr-mitogenic-signals-in-rat-chondrocytes-via-pi3k-akt-and-erk1-2
#17
Peng He, Nan Shen, Gongming Gao, Xuefeng Jiang, Huiqing Sun, Dong Zhou, Nanwei Xu, Luming Nong, Kewei Ren
BACKGROUND/AIMS: The present study aimed to analyze the mechanisms by which periodic mechanical stress is translated into biochemical signals, and to verify the important role of signaling molecules including phosphatidylinositol-3-kinase (PI3K)-Akt, protein kinase C (PKC), and epidermal growth factor receptor (EGFR) in chondrocyte proliferation. The effects of periodic mechanical stress on the mitogenesis of chondrocytes have been studied extensively in recent years. However, the mechanisms underlying the ability of chondrocytes to sense and respond to periodic mechanical stress need further investigation...
2016: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/27590028/spring-viraemia-of-carp-virus-enters-grass-carp-ovary-cells-via-clathrin-mediated-endocytosis-and-macropinocytosis
#18
Ling Shao, Jiuru Zhao, Haiqiang Zhang
Spring viraemia of carp virus (SVCV) is the causative pathogen of the outbreaks of an acute haemorrhagic and contagious viraemia responsible for the significant mortality in several cyprinid species. However, the endocytic pathway(s) and their regulatory molecules have not been characterized for SVCV. Here, using a combination of specific pharmacological inhibitors, transmission electron microscopy, immunofluorescence microscopy and real-time quantitative PCR, we found that SVCV entered grass carp ovary cells via clathrin-mediated endocytosis and macropinocytosis in a low-pH-dependent manner...
November 2016: Journal of General Virology
https://www.readbyqxmd.com/read/27582552/rottlerin-exerts-its-anti-tumor-activity-through-inhibition-of-skp2-in-breast-cancer-cells
#19
Xuyuan Yin, Yu Zhang, Jingna Su, Yingying Hou, Lixia Wang, Xiantao Ye, Zhe Zhao, Xiuxia Zhou, Yali Li, Zhiwei Wang
Studies have investigated the tumor suppressive role of rottlerin in carcinogenesis. However, the molecular mechanisms of rottlerin-induced anti-tumor activity are largely unclear. Skp2 (S-phase kinase associated protein 2) has been validated to play an oncogenic role in a variety of human malignancies. Therefore, inactivation of Skp2 could be helpful for the treatment of human cancers. In the current study, we explore whether rottlerin could inhibit Skp2 expression, leading to inhibition of cell growth, migration and invasion in breast cancer cells...
October 11, 2016: Oncotarget
https://www.readbyqxmd.com/read/27498028/protein-kinase-c-%C3%AE-inhibitor-rottlerin-inhibits-growth-and-survival-of-mycobacteria-exclusively-through-shikimate-kinase
#20
Sapna Pandey, Aditi Chatterjee, Swati Jaiswal, Sanjay Kumar, Ravishankar Ramachandran, Kishore K Srivastava
The molecular bases of disease provide exceptional prospect to translate research findings into new drugs. Nevertheless, to develop new and novel chemical entities takes huge amount of time and efforts, mainly due to the stringent processes. Therefore, drug repurposing is one of such strategies which is being used in recent times to identify new pharmacophores. The essential first step in discovery of the specific inhibitor with low toxicity is the identification and elucidation of pathways exclusive to target pathogen...
September 16, 2016: Biochemical and Biophysical Research Communications
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