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rottlerin

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https://www.readbyqxmd.com/read/29739836/inhibition-of-pkc%C3%AE-reduces-amyloid-%C3%AE-levels-and-reverses-alzheimer-disease-phenotypes
#1
Ying Du, Yingjun Zhao, Chuan Li, Qiuyang Zheng, Jing Tian, Zhuyi Li, Timothy Y Huang, Wei Zhang, Huaxi Xu
β-amyloid protein (Aβ) plays a central role in the pathogenesis of Alzheimer disease (AD). Aβ is generated from sequential cleavage of amyloid precursor protein (APP) by β-site APP-cleaving enzyme 1 (BACE1) and the γ-secretase complex. Although activation of some protein kinase C (PKC) isoforms such as PKCα and ε has been shown to regulate nonamyloidogenic pathways and Aβ degradation, it is unclear whether other PKC isoforms are involved in APP processing/AD pathogenesis. In this study, we report that increased PKCδ levels correlate with BACE1 expression in the AD brain...
May 8, 2018: Journal of Experimental Medicine
https://www.readbyqxmd.com/read/29659148/hydrogen-sulphide-increases-pulmonary-veins-and-atrial-arrhythmogenesis-with-activation-of-protein-kinase-c
#2
Chao-Shun Chan, Yung-Kuo Lin, Yu-Hsun Kao, Yao-Chang Chen, Shih-Ann Chen, Yi-Jen Chen
Hydrogen sulphide (H2 S), one of the most common toxic air pollutants, is an important aetiology of atrial fibrillation (AF). Pulmonary veins (PVs) and left atrium (LA) are the most important AF trigger and substrate. We investigated whether H2 S may modulate the arrhythmogenesis of PVs and atria. Conventional microelectrodes and whole-cell patch clamp were performed in rabbit PV, sinoatrial node (SAN) or atrial cardiomyocytes before and after the perfusion of NaHS with or without chelerythrine (a selective PKC inhibitor), rottlerin (a specific PKC δ inhibitor) or KB-R7943 (a NCX inhibitor)...
April 16, 2018: Journal of Cellular and Molecular Medicine
https://www.readbyqxmd.com/read/29545132/non-conventional-rottlerin-anticancer-properties
#3
REVIEW
Maioli E, Daveri E, Maellaro E, Ietta F, Cresti L, Valacchi G
In the past few years, we focused the interest on rottlerin, an old/new natural substance that, over the time, has revealed a number of cellular and molecular targets, all potentially implicated in the fight against cancer. Past and recent literature well demonstrated that rottlerin is an inhibitor of enzymes, transcription factors and signaling molecules that control cancer cell life and death. Although the rottlerin anticancer activity has been mainly ascribed to apoptosis and/or autophagy induction, recent findings unveiled the existence of additional mechanisms of toxicity...
March 12, 2018: Archives of Biochemistry and Biophysics
https://www.readbyqxmd.com/read/29505790/berberine-alleviates-hepatic-lipid-accumulation-by-increasing-abca1-through-the-protein-kinase-c-%C3%AE-pathway
#4
Hui Liang, Yutong Wang
Abnormal lipid metabolism may contribute to the pathogenesis of non-alcoholic steatohepatitis (NASH). The ATP-binding cassette transporter A1 (ABCA1) protein mediates the transport of cholesterol and phospholipids from cells to apolipoprotein A-I (apoA-I) to generate nascent HDL particles. Previous studies revealed that the overexpression of ABCA1 alleviated hepatic lipid levels by modifying lipid transport. Here, we examined the effect of berberine (BBR) on ABCA1 in QSG-7701 hepatocytes and in mice. BBR decreased hepatic cholesterol and triglyceride levels...
April 6, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29468562/pkc%C3%AE-knockout-mice-are-protected-from-dextromethorphan-induced-serotonergic-behaviors-in-mice-involvements-of-downregulation-of-5-ht-1a-receptor-and-upregulation-of-nrf2-dependent-gsh-synthesis
#5
Hai-Quyen Tran, Youngho Lee, Eun-Joo Shin, Choon-Gon Jang, Ji Hoon Jeong, Akihiro Mouri, Kuniaki Saito, Toshitaka Nabeshima, Hyoung-Chun Kim
We investigated whether a specific serotonin (5-HT) receptor-mediated mechanism was involved in dextromethorphan (DM)-induced serotonergic behaviors. We firstly observed that the activation of 5-HT1A receptor, but not 5-HT2A receptor, contributed to DM-induced serotonergic behaviors in mice. We aimed to determine whether the upregulation of 5-HT1A receptor induced by DM facilitates the specific induction of certain PKC isoform, because previous reports suggested that 5-HT1A receptor activates protein kinase C (PKC)...
February 22, 2018: Molecular Neurobiology
https://www.readbyqxmd.com/read/29410069/in-vitro-identification-of-mitochondrial-oxidative-stress-production-by-time-resolved-fluorescence-imaging-of-glioma-cells
#6
Silvia Tomkova, Matus Misuth, Lenka Lenkavska, Pavol Miskovsky, Veronika Huntosova
Oxidative phosphorylation and glycolysis are important features, by which cells could bypass oxidative stress. The level of oxidative stress, and the ability of cells to promote oxidative phosphorylation or glycolysis, significantly determined proliferation or cell demise. In the present work, we have employed selective mitochondrial probe MitoTracker™ Orange CMTM/Ros (MTO) to estimate the level of oxidative stress in cancer cells at different stressed conditions. MTO is partially sensitive to decrease of mitochondrial membrane potential and to reactive oxygen species (ROS) generated in mitochondria...
April 2018: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/29325900/orexin-b-modulates-synaptic-transmission-of-rod-bipolar-cells-in-rat-retina
#7
Gong Zhang, Xiao-Hua Wu, Guo-Zhong Xu, Shi-Jun Weng, Xiong-Li Yang, Yong-Mei Zhong
Orexin-A, -B play a crucial role in arousal and feeding by activating two G-protein-coupled receptors: orexin receptor 1 (OX1 R) and orexin receptor 2 (OX2 R). Orexins, along with orexin receptors, are expressed in retinal neurons, and they have been shown to differentially modulate excitatory AMPA receptors of amacrine and ganglion cells in the inner retina. In this work we report that orexin-B modulates the activity of rod bipolar cells (RBCs) located in the outer retina of rat. Intravitreal injection of orexin-B increased the amplitude of the scotopic electroretinographic b-wave, a reflection of RBC activity, recorded in vivo...
May 1, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29203243/rottlerin-upregulates-ddx3-expression-in-hepatocellular-carcinoma
#8
Zhong Wang, Gen-Hai Shen, Jia-Ming Xie, Bin Li, Quan-Gen Gao
Rottlerin has been reported to exert its anti-tumor activity in various types of human cancers. However, the underlying molecular mechanism has not been fully elucidated. In the current study, we explored whether rottlerin exhibits its tumor suppressive function in hepatocellular carcinoma cells. Our MTT assay results showed that rottlerin inhibited cell growth in hepatocellular carcinoma cells. Moreover, we found that rottlerin induced cell apoptosis and caused cell cycle arrest at G1 phase. Furthermore, our wound healing assay result demonstrated that rottlerin retarded cell migration in hepatocellular carcinoma cells...
January 1, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29115596/rottlerin-inhibits-cell-growth-induces-apoptosis-and-cell-cycle-arrest-and-inhibits-cell-invasion-in-human-hepatocellular-carcinoma
#9
Jichan Shi, Hongye Ning, Guiqing He, Yitong Huang, Zhengxing Wu, Lingling Jin, Xiangao Jiang
Rottlerin, a polyphenolic compound, has been demonstrated to exhibit antitumor activity in various types of human cancer. Several studies have revealed that rottlerin exerts its anticancer function through PKC‑dependent and independent pathways. The transcriptional co‑activator with PDZ‑binding motif (TAZ) oncopreotein is an important molecule in regulation of the Hippo pathway in human cancer. The present study investigated whether rottlerin has a tumor suppressive role via inhibiting the expression of TAZ, using cell viability assay, apoptosis and cell cycle analyses, western blot analysis and Tanswell invasion assay...
January 2018: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29058908/intracellular-fate-of-nanoparticles-with-polydopamine-surface-engineering-and-a-novel-strategy-for-exocytosis-inhibiting-lysosome-impairment-based-cancer-therapy
#10
Li Ding, Xianbing Zhu, Yiling Wang, Bingyang Shi, Xiang Ling, Houjie Chen, Wenhao Nan, Austin Barrett, Zilei Guo, Wei Tao, Jun Wu, Xiaojun Shi
Polydopamine (PDA) coating as a bioinspired strategy for nanoparticles (NPs) has been extensively applied in cancer theranostics. However, a cellular-level understanding of nano-biointeraction of these PDA-coated NPs (PDNPs), which drives the fate of them and acts as a critical step to determine their efficacy, still remains unknown. Herein, we utilized the representative mesoporous silica NPs (MSNs) to be coated with PDA and study their nano-bioactivities in cancer cells. HeLa cell line was utilized as a model in this study...
November 8, 2017: Nano Letters
https://www.readbyqxmd.com/read/29054523/glandular-hair-constituents-of-mallotus-philippinensis-muell-fruit-act-as-tyrosinase-inhibitors-insights-from-enzyme-kinetics-and-simulation-study
#11
Hridya Hemachandran, Fagun Jain, Sankari Mohan, Thirumal Kumar D, George Priya Doss C, Siva Ramamoorthy
The glandular hair extracts from the fruit rind of Mallotus philippinensis Muell. is employed to treat various skin infections, however the anti-tyrosinase activity remains unknown. Hence the present study inspected on the anti-melanogenic activity of M. philippinensis constituents. Lineweaver Burk plot revealed mixed inhibition for Rottlerin; non-competitive type of inhibition for mallotophilippen A and B respectively. Thermodynamic studies resulted in static quenching forming ground state complex with higher binding constant temperature dependently...
February 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29048618/dual-action-of-nsc606985-on-cell-growth-and-apoptosis-mediated-through-pkc%C3%AE-in-prostatic-cancer-cells
#12
Xin Wang, Chen Tan, Guo Wang, Jing-Jing Cai, Li-Ping Wang, Julianne Imperato-McGinley, Yuan-Shan Zhu
Chemotherapy is a vital therapeutic strategy for castration-resistant prostate cancer (CRPC). We have previously shown that NSC606985 (NSC), a camptothecin (CPT) analog, induced cell apoptosis via interacting with topoisomerase I (Topo I) in prostate cancer cells. In the present study, the effect and mechanism of CPT analogs in LAPC4 cells were investigated. LAPC-4 cells were treated with NSC, CPT, and topotecan. Cell proliferation, apoptosis, and protein kinase Cδ (PKCδ) subcellular activation were measured at different doses and time-points, with or without PKCδ inhibition or knockdown of PKCδ expression...
November 2017: International Journal of Oncology
https://www.readbyqxmd.com/read/29036789/protein-kinase-c-%C3%AE-dependent-regulation-of-ubiquitin-proteasome-system-function-in-breast-cancer
#13
Si Sun, Qi Wu, Junlong Song, Shengrong Sun
Besides the crucial role of hyperinsulinemia in the development of breast cancer with Type 2 diabetes mellitus (T2DM), it has been shown that hyperglycemia could contribute to promote cancer progression. A remarkable association within hyperglycemia, PKCδ and Ubiquitin-proteasome system (UPS) has been reported, suggesting that PKCδ may mediate high glucose-induced UPS activation in breast cancer cells. Although the independent effects of PKCδ or UPS on breast cancer and T2DM are increasingly supported by experimental evidence, the complex interactional link between PKCδ and UPS is still unclear...
December 12, 2017: Cancer Biomarkers: Section A of Disease Markers
https://www.readbyqxmd.com/read/28994806/solubility-of-hydrophobic-compounds-in-aqueous-solution-using-combinations-of-self-assembling-peptide-and-amino-acid
#14
Shaun Pacheco, Shan-Yu Fung, Mingyao Liu
Self-assembling peptides (SAPs) are promising vehicles for the delivery of hydrophobic therapeutics for clinical applications; their amphipathic properties allow them to dissolve hydrophobic compounds in the aqueous environment of the human body. However, self-assembling peptide solutions have poor blood compatibility (e.g., low osmolarity), hindering their clinical application through intravenous administrations. We have recently developed a generalized platform for hydrophobic drug delivery, which combines SAPs with amino acid solutions (SAP-AA) to enhance drug solubility and increase formulation osmolarity to reach the requirements for clinical uses...
September 20, 2017: Journal of Visualized Experiments: JoVE
https://www.readbyqxmd.com/read/28983628/long-intergenic-noncoding-rna-p21-mediates-oxidized-ldl%C3%A2-induced-apoptosis-and-expression-of-lox%C3%A2-1-in-human-coronary-artery-endothelial-cells
#15
Tao Zhou, Xiaofang Chen
Atherosclerosis is the most common pathological cause of cardiovascular diseases, and endothelial dysfunction has a vital role. It has been suggested that inhibiting endothelial cell apoptosis induced by oxidized low‑density lipoprotein (ox‑LDL), an essential atherosclerotic factor, is a potential novel therapeutic strategy against atherosclerosis. Previous studies have revealed that endothelial lectin‑like ox‑LDL receptor‑1 (LOX‑1) and long intergenic noncoding RNA p21 (lincRNA‑p21) may serve as therapeutic targets for atherosclerosis and associated cardiovascular disorders...
December 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28977931/inhibition-of-notch-1-pathway-is-involved-in-rottlerin-induced-tumor-suppressive-function-in-nasopharyngeal-carcinoma-cells
#16
Yingying Hou, Shaoyan Feng, Lixia Wang, Zhe Zhao, Jingna Su, Xuyuan Yin, Nana Zheng, Xiuxia Zhou, Jun Xia, Zhiwei Wang
Recent studies have revealed that rottlerin is a natural chemical drug to exert its anti-cancer activity. However, the molecular mechanisms of rottlerin-induced tumor suppressive function have not been fully elucidated. Notch signaling pathway has been characterized to play a crucial role in tumorigenesis. Therefore, regulation of Notch pathway could be beneficial for the treatment of human cancer. The aims of our current study were to explore whether rottlerin could suppress Notch-1 expression, which leads to inhibition of cell proliferation, migration and invasion in nasopharyngeal carcinoma cells...
September 22, 2017: Oncotarget
https://www.readbyqxmd.com/read/28895644/relaxin-inhibits-cardiac-fibrosis-in-diabetic-rats-roles-of-protein-kinase-c%C3%AE
#17
Ping Wang, Meng Li, Lei Dong, Hui Chen, Wei Su, Yu-Peng Wang
Relaxin (Rlx) is known to antagonize diabetic cardiac fibrosis. However, its mechanism is poorly understood. Protein kinase Cδ (PKCδ) plays a crucial role in diabetic cardiomyopathy (DCM). This study explored the involvement of PKCδ in Rlx's capacity of suppressing cardiac fibrosis in a rat model of type 2 diabetes mellitus (DM). Type 2 DM of 8-week-old male Sprague-Dawley (SD) rats was induced by a high-fat diet and the injection of streptozocin (STZ, 40 mg/kg). Fourteen-week-old rats with DM and rats in control group which were pre-treated for 1 week with human recombinant relaxin (rhRlx, 30 μg/kg...
September 11, 2017: Experimental and Clinical Endocrinology & Diabetes
https://www.readbyqxmd.com/read/28880029/fluorescence-labelling-of-extracellular-vesicles-using-a-novel-thiol-based-strategy-for-quantitative-analysis-of-cellular-delivery-and-intracellular-traffic
#18
H D Roberts-Dalton, A Cocks, J M Falcon-Perez, E J Sayers, J P Webber, P Watson, A Clayton, A T Jones
Extracellular vesicles, including exosomes, are naturally derived nanovesicles generated in and released by numerous cell types. As extracellular entities they have the capacity to interact with neighbouring cells and distant tissues and affect physiological processes as well as being implicated in numerous diseases including tumorigenesis and neurodegeneration. They are also under intense investigation as delivery vectors for biotherapeutics. The ways in which EVs interact with recipient cells to influence cell physiology and deliver a macromolecular payload are at the early stages of exploration...
September 21, 2017: Nanoscale
https://www.readbyqxmd.com/read/28801242/oxidant-species-are-involved-in-t-b-mediated-erk1-2-phosphorylation-that-activates-p53-p21-axis-to-promote-kshv-lytic-cycle-in-pel-cells
#19
Roberta Gonnella, Shivangi Yadav, Maria Saveria Gilardini Montani, Marisa Granato, Roberta Santarelli, Alessia Garufi, Gabriella D'Orazi, Alberto Faggioni, Mara Cirone
KSHV is a gammaherpesvirus strongly associated to human cancers such as Primary Effusion Lymphoma (PEL) and Kaposi's Sarcoma. The naturally virus-infected tumor cells usually display latent infection since a minority of cells undergoes spontaneous viral replication. The lytic cycle can be induced in vitro upon appropriate stimuli such as TPA (T), alone or in combination with butyrate (B), (T/B). In previous studies, Protein Kinase C (PKC) δ, Extracellular Signal-regulated Kinase1/2 (ERK1/2) and p53-p21 axis have been separately reported to play a role in KSHV reactivation from latency...
August 8, 2017: Free Radical Biology & Medicine
https://www.readbyqxmd.com/read/28723653/inhibition-of-notch-1-pathway-is-involved-in-rottlerin-induced-tumor-suppressive-function-in-nasopharyngeal-carcinoma-cells
#20
Yingying Hou, Shaoyan Feng, Lixia Wang, Zhe Zhao, Jingna Su, Xuyuan Yin, Nana Zheng, Xiuxia Zhou, Jun Xia, Zhiwei Wang
Recent studies have revealed that rottlerin is a natural chemical drug to exert its anti-cancer activity. However, the molecular mechanisms of rottlerin-induced tumor suppressive function have not been fully elucidated. Notch signaling pathway has been characterized to play a crucial role in tumorigenesis. Therefore, regulation of Notch pathway could be beneficial for the treatment of human cancer. The aims of our current study were to explore whether rottlerin could suppress Notch-1 expression, which leads to inhibition of cell proliferation, migration and invasion in nasopharyngeal carcinoma cells...
July 8, 2017: Oncotarget
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