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Molecular and Cellular Biochemistry

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https://www.readbyqxmd.com/read/27909846/benzimidazole-inhibitors-of-protein-kinase-ck2-potently-inhibit-the-activity-of-atypical-protein-kinase-rio1
#1
Konrad Kubiński, Maciej Masłyk, Andrzej Orzeszko
Benzimidazole derivatives of 5,6-dichlorobenzimidazole 1-β-D-ribofuranoside (DRB) comprise the important class of protein kinase CK2 inhibitors. Depending on the structure, benzimidazoles inhibit CK2 with different selectivity and potency. Besides CK2, the compounds can inhibit, with similar activity, other classical eukaryotic protein kinases (e.g. PIM, DYRK, and PKD). The present results show that a majority of the most common CK2 inhibitors can affect the atypical kinase Rio1 in a nanomolar range. Kinetic data confirmed the mode of action of benzimidazoles as typical ATP-competitive inhibitors...
December 1, 2016: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/27896594/global-cerebral-ischemia-due-to-circulatory-arrest-insights-into-cellular-pathophysiology-and-diagnostic-modalities
#2
REVIEW
Santosh K Sanganalmath, Purva Gopal, John R Parker, Richard K Downs, Joseph C Parker, Buddhadeb Dawn
Circulatory arrest (CA) remains a major unresolved public health problem in the United States; the annual incidence of which is ~0.50 to 0.55 per 1000 population. Despite seminal advances in therapeutic approaches over the past several decades, brain injury continues to be the leading cause of morbidity and mortality after CA. In brief, CA typically results in global cerebral ischemia leading to delayed neuronal death in the hippocampal pyramidal cells as well as in the cortical layers. The dynamic changes occurring in neurons after CA are still unclear, and predicting these neurological changes in the brain still remains a difficult issue...
November 28, 2016: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/27896593/biochemical-and-oxidative-stress-markers-in-the-liver-and-kidneys-of-rats-submitted-to-different-protocols-of-anabolic-steroids
#3
Guilherme Lopes Dornelles, Andressa Bueno, Juliana Sorraila de Oliveira, Aleksandro Schafer da Silva, Raqueli Teresinha França, Cássia Bagolin da Silva, Márcia Silveira Netto Machado, Letícia do Santos Petry, Fátima Husein Abdalla, Cibele Lima Lhamas, Cinthia Melazzo de Andrade
The objective of this study was to evaluate the effects of different protocols (P1, P2, and P3) of boldenone undecylenate (BU) and stanozolol (ST) on markers of liver and kidney function and variables of oxidative stress in these organs. For this, 54 male Wistar rats were divided into nine groups of six animals each. Each animal received intramuscularly 5.0 mg kg(-1) of BU or ST once a week for 4 weeks (P1); 2.5 mg kg(-1) of BU or ST once a week for 8 weeks (P2); and 1.25 mg kg(-1) of BU or ST once a week for 12 weeks (P3)...
November 28, 2016: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/27885584/wt1-and-nphs2-gene-mutation-analysis-and-clinical-management-of-steroid-resistant-nephrotic-syndrome
#4
Aravind Selvin Kumar Ramanathan, Murali Vijayan, Srilakshmi Rajagopal, Padmaraj Rajendiran, Prabha Senguttuvan
Nephrotic syndrome (NS) is a kidney disease predominantly present in children with idiopathic condition; final stage of the disease progresses into end-stage renal disease. Generally, NS is treated using standard steroid therapy, however; most of the children are steroid sensitive and about 15-20% are non-responders (SRNS). Non-responsiveness of these children would be a risk with the possibility of mutational changes in podocyte genes (NPHS1, NPHS2, WT1, PLCE1). The mutation in podocyte genes is associated with SRNS...
November 25, 2016: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/27882442/the-effects-of-zofenopril-on-cardiac-function-and-pro-oxidative-parameters-in-the-streptozotocin-induced-diabetic-rat-heart
#5
Petar Ristic, Ivan Srejovic, Tamara Nikolic, Isidora Stojic, Dragana Ristic, Vladimir Zivkovic, Vladimir Lj Jakovljevic
Diabetes mellitus is a chronic condition that continues to increase in both incidence and prevalence. Renin-Angiotensin-Aldosterone System is one of the main modulators of chronic hyperglycaemia and, thus, its influence on tissues. Hyperglycaemia-induced oxidative stress is an important factor in diabetic cardiomyopathy. The present study was carried out on 24 adult male Wistar albino rats (8-week-old and with body masses of 190 ± 10 g). We evaluated the influence of acute administration of zofenopril on ex vivo myocardial function from rats with streptozotocin-induced diabetes mellitus, with a special emphasis on cardiodynamic and oxidative stress parameters in diabetic rat hearts...
November 24, 2016: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/27882441/regioselective-synthesis-and-biological-studies-of-novel-1-aryl-3-5-bis-het-aryl-pyrazole-derivatives-as-potential-antiproliferative-agents
#6
Hanumappa Ananda, Kothanahally S Sharath Kumar, Mayilaadumveettil Nishana, Mahesh Hegde, Mrinal Srivastava, Raghava Byregowda, Bibha Choudhary, Sathees C Raghavan, Kanchugarakoppal S Rangappa
Pyrazole moiety represents an important category of heterocyclic compound in pharmaceutical and medicinal chemistry. The novel 1-aryl-3, 5-bis (het) aryl pyrazole derivatives were synthesized with complementary regioselectivity. The chemical structures were confirmed by IR, (1)H NMR, (13)C NMR, and mass spectral analysis. The chemical entities were screened in various cancer cell lines to assess their cell viability activity. Results showed that the compound 3-(1-(4-bromophenyl)-5-phenyl-1H-pyrazol-3-yl) pyridine (5d) possessed maximum cytotoxic effect against breast cancer and leukemic cells...
November 24, 2016: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/27878499/therapeutic-potential-of-adam17-modulation-in-gastric-cancer-through-regulation-of-the-egfr-and-tnf-%C3%AE-signalling-pathways
#7
Jinbing Sun, Jianlong Jiang, Kuangyi Lu, Qiao Chen, Danhao Tao, Zhong Chen
A disintegrin and metalloproteinase 17 (ADAM17) is highly expressed in various tumours and affects tumour progression. In this study, ADAM17 expression in 60 gastric cancer and 20 normal gastric mucosal tissues was assessed using immunohistochemistry. ADAM17 expression was higher in gastric cancer tissues than in normal gastric mucosal tissues (P < 0.0005). A significant relationship was identified between ADAM17 expression and the depth of tumour invasion, metastasis, and carcinoma stage. Furthermore, the effects of ADAM17 knockdown on the proliferation, cell invasion, and apoptosis of human gastric carcinoma cells (SGC-7901) were determined...
November 22, 2016: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/27873143/regulation-of-rac1-gtpase-activity-by-quinine-through-g-protein-and-bitter-taste-receptor-t2r4
#8
Crystal Sidhu, Appalaraju Jaggupilli, Prashen Chelikani, Rajinder P Bhullar
Rac1 belongs to the Rho family of small GTPases and regulates actin cytoskeleton reorganization. T2R4 is a bitter taste receptor belonging to the G protein-coupled receptor family of proteins. In addition to mediating bitter taste perception from the tongue, T2R4s are found in extra-oral tissues, e.g., nasal epithelium, airways, brain, testis suggesting a much broader physiological function for these receptors. Anti-malarial drug and a bitter tasting compound, quinine, is a known agonist for T2R4, whereas BCML (Nα,Nα-Bis(carboxymethyl)-L-lysine) acts as an inverse agonist...
November 22, 2016: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/27868170/protein-kinases-mechanisms-and-downstream-targets-in-inflammation-mediated-obesity-and-insulin-resistance
#9
REVIEW
Kalyana C Nandipati, Saravanan Subramanian, Devendra K Agrawal
Obesity-induced low-grade inflammation (metaflammation) impairs insulin receptor signaling. This has been implicated in the development of insulin resistance. Insulin signaling in the target tissues is mediated by stress kinases such as p38 mitogen-activated protein kinase, c-Jun NH2-terminal kinase, inhibitor of NF-kB kinase complex β (IKKβ), AMP-activated protein kinase, protein kinase C, Rho-associated coiled-coil containing protein kinase, and RNA-activated protein kinase. Most of these kinases phosphorylate several key regulators in glucose homeostasis...
November 21, 2016: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/27868169/articulatin-d-induces-apoptosis-via-activation-of-caspase-8-in-acute-t-cell-leukemia-cell-line
#10
Ruchi Mishra, Mrinal K Das, Savita Singh, Radhey Shyam Sharma, Sadhna Sharma, Vandana Mishra
Leukemia is among the most aggressive and prevalent human malignant carcinoma. Chemotherapy is the preferred therapeutic strategy; however, recurrence of cancer and non-selective cytotoxicity are the major concerns. Unlike synthetic chemotherapeutic agents, mistletoe ribosome-inactivating protein (RIP) displays anti-tumor function in various types of cancers. However, its effect on leukemia cells is little explored. In this study, we assessed the impact of Viscum articulatum RIP (Articulatin-D) on the survival of acute T-cell leukemia cells and the involved molecular and cellular mechanisms...
November 21, 2016: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/27864727/post-translational-modification-by-acetylation-regulates-the-mitochondrial-carnitine-acylcarnitine-transport-protein
#11
Nicola Giangregorio, Annamaria Tonazzi, Lara Console, Cesare Indiveri
The carnitine/acylcarnitine transporter (CACT; SLC25A20) mediates an antiport reaction allowing entry of acyl moieties in the form of acylcarnitines into the mitochondrial matrix and exit of free carnitine. The transport function of CACT is crucial for the β-oxidation pathway. In this work, it has been found that CACT is partially acetylated in rat liver mitochondria as demonstrated by anti-acetyl-lys antibody immunostaining. Acetylation was reversed by the deacetylase Sirtuin 3 in the presence of NAD(+). After treatment of the mitochondrial extract with the deacetylase, the CACT activity, assayed in proteoliposomes, increased...
November 18, 2016: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/27854077/prohibitin-confers-cytoprotection-against-iso-induced-hypertrophy-in-h9c2-cells-via-attenuation-of-oxidative-stress-and-modulation-of-akt-gsk-3%C3%AE-signaling
#12
Debabrata Chowdhury, Dinesh Kumar, Utpal Bhadra, Tangutur Anjana Devi, Manika Pal Bhadra
Numerous hypertrophic stimuli, including β-adrenergic agonists such as isoproterenol (ISO), result in generation of reactive oxygen species (ROS) and alteration in the mitochondrial membrane potential (Δψ) leading to oxidative stress. This process is well associated with phosphorylation of thymoma viral proto-oncogene Akt (Ser473) and glycogen synthase kinase-3β (Gsk-3β) (Ser9), with resultant inactivation of Gsk-3β. In the present study, we found that the protective defensive role of prohibitin (PHB) against ISO-induced hypertrophic response in rat H9c2 cells is via attenuation of oxidative stress-dependent signaling pathways...
November 16, 2016: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/27854076/dodeca-2-e-4-e-dienoic-acid-isobutylamide-enhances-glucose-uptake-in-3t3-l1-cells-via-activation-of-akt-signaling
#13
Kyeong-Mi Choi, Wonkyun Kim, Jin Tae Hong, Hwan-Soo Yoo
Dodeca-2(E),4(E)-dienoic acid isobutylamide (DDI), an alkamide derived from the plant Echinacea purpurea, promotes adipocyte differentiation and activates peroxisome proliferator-activated receptor γ, which is associated with enhanced insulin sensitivity. In the present study, we investigated whether DDI may increase glucose uptake through activation of the insulin signaling pathway in 3T3-L1 adipocytes. DDI increased insulin-stimulated glucose uptake, and expression and translocation of glucose transporter 4 in adipocytes treated with sub-optimal levels of insulin...
November 16, 2016: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/27854075/benzimidazole-derivative-m084-extends-the-lifespan-of-caenorhabditis-elegans-in-a-daf-16-foxo-dependent-way
#14
Ai-Jun Ding, Gui-Sheng Wu, Bin Tang, Xuechuan Hong, Michael X Zhu, Huai-Rong Luo
With the growth of aging population, there is increasing demand to develop strategy to improve the aging process and aging-related diseases. Benzimidazole and its derivatives are crucial heterocyclic backbone of many drugs and compounds with diverse therapeutic applications, including alleviation of aging-related diseases. Here, we investigate if the benzimidazole derivative n-butyl-[1H]-benzimidazol-2-amine (M084), a novel inhibitor of TRPC4 and TRPC5 channels and antidepressant, could affect the lifespan of Caenorhabditis elegans (C...
November 16, 2016: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/27854074/resveratrol-and-its-methoxy-derivatives-modulate-the-expression-of-estrogen-metabolism-enzymes-in-breast-epithelial-cells-by-ahr-down-regulation
#15
Barbara Licznerska, Hanna Szaefer, Marcin Wierzchowski, Hanna Sobierajska, Wanda Baer-Dubowska
Our earlier studies have shown that compared to resveratrol, its analogs with ortho-methoxy substituents exert stronger antiproliferative and proapoptotic activity. Since estrogens are considered the major risk factors of breast carcinogenesis, the aim of this study was to evaluate the effect of 3,4,2'-trimethoxy (3MS), 3,4,2',4'-tetramethoxy (4MS), and 3,4,2',4',6'-pentamethoxy (5MS) trans-stilbenes on the constitutive expression of the enzymes involved in estrogen metabolism, as well as receptors: AhR and HER2 in breast epithelial cell line MCF10A...
November 16, 2016: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/27854073/altered-extracellular-atp-adp-and-amp-hydrolysis-in-blood-serum-of-sedentary-individuals-after-an-acute-aerobic-moderate-exercise-session
#16
Cesar Eduardo Jacintho Moritz, Bruno Costa Teixeira, Liliana Rockenbach, Alvaro Reischak-Oliveira, Emerson André Casali, Ana Maria Oliveira Battastini
Nucleotidases participate in the regulation of physiological and pathological events, such as inflammation and coagulation. Exercise promotes distinct adaptations, and can influence purinergic signaling. In the present study, we investigated soluble nucleotidase activities in the blood serum of sedentary young male adults at pre- and post-acute moderate aerobic exercise. In addition, we evaluated how this kind of exercise could influence adenine nucleotide concentrations in the blood serum. Sedentary individuals were submitted to moderate aerobic exercise on a treadmill; blood samples were collected pre- and post-exercise, and serum was separated for analysis...
November 16, 2016: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/27854072/sh003-enhances-paclitaxel-chemosensitivity-in-mcf-7-pax-breast-cancer-cells-through-inhibition-of-mdr1-activity
#17
Hyeong Sim Choi, Sung-Gook Cho, Min Kyoung Kim, Hee Jae Lee, Seung Hee Moon, Hee Jae Jang, Seong-Gyu Ko
Paclitaxel is an anti-cancer drug for treating cancer, but paclitaxel resistance is reported in cancer cells. Multidrug resistance (MDR) is related with the epithelial-to-mesenchymal transition (EMT) mechanism, which plays a key role in cancer metastasis. Moreover, EMT mechanism is connected to tamoxifen resistance in breast cancer cells. Consequently, oncologists are interested in finding new MDR1 inhibitors originating from herbal medicines to have less side-effect. Here, we investigated an inhibition effect of SH003 on MDR1 activity in paclitaxel-resistant MCF-7/PAX breast cancer cells...
November 16, 2016: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/27848074/induction-of-autophagy-by-salidroside-through-the-ampk-mtor-pathway-protects-vascular-endothelial-cells-from-oxidative-stress-induced-apoptosis
#18
Xiang-Tao Zheng, Zi-Heng Wu, Ye Wei, Ju-Ji Dai, Guan-Feng Yu, FengLai Yuan, Le-Chi Ye
Vascular endothelial cells are highly sensitive to oxidative stress, and this is one of the mechanisms by which widespread endothelial dysfunction is induced in most cardiovascular diseases and disorders. However, how these cells can survive in oxidative stress environments remains unclear. Salidroside, a traditional Chinese medicine, has been shown to confer vascular protective effects. We aimed to understand the role of autophagy and its regulatory mechanisms by treating human umbilical vein endothelial cells (HUVECs) with salidroside under oxidative stress...
November 15, 2016: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/27844252/effect-of-puerarin-on-transcriptome-of-astrocyte-during-oxygen-glucose-deprivation-reoxygenation-injury
#19
Shuyong Wei, Jie Tong, Qiang Xue, Yang Liu, Xiaoyu Xu
Stroke is a serious disease with complex pathomechanism and limited therapeutic effect in clinic. Our previous research has found obvious therapeutic effect of Puerarin (Pur) on stroke injury of rat. The aim of this study is to investigate the transcriptome changes of oxygen-glucose deprivation/reoxygenation (OGD/R)-injured astrocytes before and after the intervention of Pur. Cells activity and apoptosis detection indicated that the activity of OGD/R-injured astrocytes was improved, and the apoptosis was ameliorated by Pur...
November 14, 2016: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/27844251/characterisation-of-neuroprotective-efficacy-of-modified-poly-arginine-9-r9-peptides-using-a-neuronal-glutamic-acid-excitotoxicity-model
#20
Adam B Edwards, Ryan S Anderton, Neville W Knuckey, Bruno P Meloni
In a recent study, we highlighted the importance of cationic charge and arginine residues for the neuroprotective properties of poly-arginine and arginine-rich peptides. In this study, using cortical neuronal cultures and an in vitro glutamic acid excitotoxicity model, we examined the neuroprotective efficacy of different modifications to the poly-arginine-9 peptide (R9). We compared an unmodified R9 peptide with R9 peptides containing the following modifications: (i) C-terminal amidation (R9-NH2); (ii) N-terminal acetylation (Ac-R9); (iii) C-terminal amidation with N-terminal acetylation (Ac-R9-NH2); and (iv) C-terminal amidation with D-amino acids (R9D-NH2)...
November 14, 2016: Molecular and Cellular Biochemistry
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