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Biochemical Pharmacology

Chao Liu, Jianing Wang, Yan Yang, Xiuting Liu, Yubing Zhu, Jianjun Zou, Sishi Peng, Thi Ha Le, Yu Chen, Shuli Zhao, Bangshun He, Qiongyu Mi, Xu Zhang, Qianming Du
Previous studies reported that Ginsenoside Rd (Rd) had anti-inflammatory and anti-cancer effects. However, the molecular mechanism underlying the inhibition effect of Rd on colitis in mice hasn't been clarified clearly. Here, in our study, we detected the effects of Rd on dextran sulfate sodium (DSS)-induced murine colitis, and found that oral administration of Rd dose-dependently alleviated DSS-induced body weight loss, colon length shortening and colonic pathological damage with lower myeloperoxidase (MPO) and inducible nitric oxide synthase (iNOS) activities and higher glutathione level...
July 13, 2018: Biochemical Pharmacology
Mohammed Benkheil, Jan Paeshuyse, Johan Neyts, Matthias Van Haele, Tania Roskams, Sandra Liekens
HCV is a major risk factor for hepatocellular carcinoma (HCC). HCC development in chronically infected HCV patients has until now been attributed to persistent inflammation and interference of viral proteins with host cell signaling. Since activation of the epidermal growth factor receptor (EGFR) presents a crucial step in HCV entry, we aimed at investigating whether EGFR signaling may contribute to the pathogenesis of HCV-related HCC. By applying microarray analysis, we generated a gene expression signature for secreted proteins in HCV-infected hepatoma cells...
July 13, 2018: Biochemical Pharmacology
Sebastián Zagmutt, Paula Mera, M Carmen Soler-Vázquez, Laura Herrero, Dolors Serra
The current obesity epidemic is a major worldwide health and economic burden. In the modern environment, an increase in the intake of high-fat and high-sugar foods plays a crucial role in the development of obesity by disrupting the mechanisms governing food intake and energy balance. Food intake and whole-body energy balance are regulated by the central nervous system through a sophisticated neuronal network located mostly in the hypothalamus. In particular, the hypothalamic arcuate nucleus (ARC) is a fundamental center that senses hormonal and nutrient-related signals informing about the energy state of the organism...
July 13, 2018: Biochemical Pharmacology
Xueyan Zhou, Yun Zhao, Juan Wang, Xi Wang, Chunxia Chen, Di Yin, Feng Zhao, Jiale Yin, Meng Guo, Longzhen Zhang, Lei Du, Bei Zhang, Xiaoxing Yin
Estrogen plays a pivotal role in the pathological development of breast cancer. Resveratrol has chemo-preventive effects against breast cancer, whereas, the mechanism of antitumor activities of resveratrol remains unanswered. In this study, we showed that estrogen homeostasis profile was disturbed in both breast cancer patients and in experimental breast cancer model rats, with carcinogenic catechol estrogens significantly accumulated in the mammary tissues. UDP-glucuronosyltransferase 1A8 (UGT1A8) is an important phase II drug-metabolizing enzymes which involved in the metabolism of catechol estrogens...
July 12, 2018: Biochemical Pharmacology
Xiaosa Wu, Han-Shen Tae, Yen-Hua Huang, David J Adams, David J Craik, Quentin Kaas
The ribbon isomer of α-conotoxin AuIB has 10-fold greater potency than the wild-type globular isomer at inhibiting nicotinic acetylcholine receptors (nAChRs) in rat parasympathetic neurons, and unlike its globular isoform, ribbon AuIB only targets a specific stoichiometry of the α3β4 nAChR subtype. Previous electrophysiological recordings of AuIB indicated that ribbon AuIB binds to the α3(+)α3(-) interface within the nAChR extracellular domain, which is displayed by the (α3)3 (β4)2 stoichiometry but not by (α3)2 (β4)3 ...
July 12, 2018: Biochemical Pharmacology
Elena Mariotto, Roberta Bortolozzi, Ilaria Volpin, Davide Carta, Valentina Serafin, Benedetta Accordi, Giuseppe Basso, Pilar Luque Navarro, Luisa Carlota López-Cara, Giampietro Viola
Choline kinase alpha 1 (ChoKα1) has recently become an interesting therapeutic target since its overexpression has been associated to tumorigenesis in many cancers. Nevertheless, little is known regarding hematological malignancies. In this manuscript, we investigated the effect of a novel and selective ChoKα inhibitor EB-3D in T acute lymphoblastic leukemia (T-ALL). The effect of EB-3D was evaluated in a panel of T-leukemia cell lines and ex-vivo primary cultures derived from pediatric T-ALL patients. We also evaluated in detail, using Reverse Phase Protein Array (RPPA), protein phosphorylation level changes in T-ALL cells upon treatment...
July 11, 2018: Biochemical Pharmacology
Ariel D Quiroga, Richard Lehner
Excessive triacylglycerol (TG) accumulation is the distinctive feature of obesity. In the liver, sustained TG accretion leads to nonalcoholic fatty liver disease (NAFLD), eventually progressing to non-alcoholic steatohepatitis (NASH) and cirrhosis, which is associated with complications including hepatic failure, hepatocellular carcinoma and death. Pharmacological interventions are actively pursued to prevent lipid accumulation in hepatocytes and, therefore, to ameliorate the associated pathophysiological conditions...
July 10, 2018: Biochemical Pharmacology
Ching-Yi Tsai, Kuang-Yu Dai, Chi Fang, Jacqueline C C Wu, Samuel H H Chan
Despite great advances in contemporary medicine, brain death still remains enigmatic and its cellular and molecular mechanisms unsettled. This review summarizes recent findings that substantiate the notion that PTEN/FLJ10540/PI3K/Akt cascade, the classical tumorigenic signaling pathway, is actively engaged in experimental brain stem death. These results were based on a clinically relevant animal model that employs the pesticide mevinphos as the experimental insult in Sprague-Dawley rats to mimic brain stem death in patients died of organophosphate poisoning...
July 3, 2018: Biochemical Pharmacology
Yunduan Song, Yaxian Wu, Xiaozong Li, Yao Shen, Yunhe Ding, Hongbo Zhu, Fangfang Liu, Kaikai Yu, Lei Sun, Feng Qian
Asthma is one of the most common pulmonary diseases that threatens human life because of lack of effective medicines. Protostemonine (PSN), an active alkaloid extracted from the roots of Stemona sesslifolia, has anti-inflammatory effects on acute lung injury and acute liver failure. However, it has not been defined whether PSN alleviates asthmatic inflammation. Here, we reported that PSN inhibits pulmonary eosinophil infiltration, goblet cell hyperplasia, mucus secretion, IgE and Th2 cytokine (IL-4, IL-5, IL-13 and IL-33) production by using DRA (dust mites, ragweed and aspergillus)-induced murine asthma model...
July 2, 2018: Biochemical Pharmacology
Vijaya L Damaraju, Michelle Kuzma, Carol E Cass, Charles T Putman, Michael B Sawyer
Tyrosine kinase inhibitors (TKIs) have advanced cancer treatment and prognosis but have also resulted in adverse effects such as fatigue, diarrhea, hypothyroidism, and other toxicities. We investigated TKI effects on skeletal muscle as a possible explanation of TKI induced fatigue. Changes in mitochondrial function due to inhibition of oxidative phosphorylation complexes, generation of superoxides, and inhibition of key transporters involved in uptake of glucose and/or nucleosides may result in alteration of energy metabolism and/or mitochondrial function...
July 2, 2018: Biochemical Pharmacology
Daniela Impellizzeri, Rosalba Siracusa, Marika Cordaro, Alessio Filippo Peritore, Enrico Gugliandolo, Giuseppe Mancuso, Angelina Midiri, Rosanna Di Paola, Salvatore Cuzzocrea
Interleukin (IL)-1 and IL-18 belong to the IL-1 family of ligands, and their receptors are members of the IL-1 receptor family. Both cytokines drive an extensive range of pro-inflammatory networks in many cell types using common signal transduction cascades. Anyway, differences in signaling pathways exist. With this aim in mind, we investigated by using transgenic mice the mechanisms through the simultaneous deficiency of both IL-1β and IL-18 could be more protective compared to blocking the single cytokine IL-1β or IL-18 during colitis...
June 28, 2018: Biochemical Pharmacology
Pankaj Pandey, Narayan D Chaurasiya, Babu L Tekwani, Robert J Doerksen
The endocannabinoid system plays an important role in the pathophysiology of various neurological disorders, such as anxiety, depression, neurodegenerative diseases, and schizophrenia; however, little information is available on the coupling of the endocannabinoid system with the monoaminergic systems in the brain. In the present study, we tested four endocannabinoids and two anandamide analogs for inhibition of recombinant human MAO-A and -B (monoamine oxidase). Virodhamine inhibited both MAO-A and -B (IC50 values of 38...
June 26, 2018: Biochemical Pharmacology
Alexander J Kvist, Kajsa P Kanebratt, Anna Walentinsson, Henrik Palmgren, Matthew O'Hara, Anders Björkbom, Linda C Andersson, Marie Ahlqvist, Tommy B Andersson
Primary human hepatocytes (PHH), HepaRG™, HepG2, and two sources of induced pluripotent stem cell (iPSC) derived hepatocytes were characterized regarding gene expression and function of key hepatic proteins, important for the metabolic fate of drugs. The gene expression PCA analysis showed a distance between the two iPSC derived hepatocytes as well as the HepG2 and HepaRG™ cells to the three PHH donors and PHH pool, which were clustered more closely together. Correlation-based hierarchical analysis clustered HepG2 close to the stem cell derived hepatocytes both when the expression of 91 genes related to liver function or only cytochrome P450 (P450) genes were analyzed indicating the non-liver feature and a similar low P450 profile in these cell models...
June 25, 2018: Biochemical Pharmacology
Ting Song, Minhang Zhang, Peng Liu, Zhenyu Xue, Yudan Fan, Zhichao Zhang
Targeting Bcl-2 with ABT-199 (Venetoclax) shows limited single-agent activity against many cancers in both preclinical and clinical investigations. Combination therapies have attracted great attention. The principal purpose of this study was to investigate the mechanism of synergism between ABT-199 and paclitaxel. Moreover, we analyzed the biomarker to identify tumors which are most likely to respond to this combination. We evaluated the effect of this combination in a panel of nine cancer cell lines including cervical cancer, lung cancer, ovarian cancer, lymphoma, leukemia and breast cancer...
June 25, 2018: Biochemical Pharmacology
Chenfan Duan, Yanzhuo Liu, Ying Li, Honglei Chen, Xiaoxiao Liu, Xuewei Chen, Jiang Yue, Xiaoyang Zhou, Jing Yang
Sulfasalazine (SF) promotes remyelination and improves the outcome of multiple sclerosis (MS) patients. However, the underlining mechanism remains elusive. Here, we examined whether SF blocks microglia switching to a pro-inflammatory M1-like phenotype through a competing endogenous RNA (ceRNA) effects in cuprizone-induced demyelination. The microglia reprogramming effects of SF in the mice model of cuprizone-induced demyelination was measured by histological, immunohistochemical and molecular biological methods...
June 23, 2018: Biochemical Pharmacology
Yasuhiro Uno, Rika Takahira, Norie Murayama, Yu Ishii, Yoshinori Ikenaka, Mayumi Ishizuka, Hiroshi Yamazaki, Shinichi Ikushiro
UDP-glucuronosyltransferases (UGTs) are drug-metabolizing enzymes essential for the metabolism of endogenous substrates and xenobiotics. Molecular characteristics of UGTs have been extensively investigated in humans, but in cynomolgus macaques, a non-human primate species widely used in drug metabolism studies, remain to be investigated. In this study, 12 UGT1A cDNAs (UGT1A1, 1A2, 1A4A, 1A4B, 1A5A, 1A5B, 1A5C, 1A6, 1A7, 1A8, 1A9, and 1A10) were isolated and characterized in cynomolgus macaques. UGT1A5C cDNA did not contain a complete coding region due to nonsense mutations, and was excluded from further analysis...
June 23, 2018: Biochemical Pharmacology
Emil Jakobsen, Sofie C Lange, Jens V Andersen, Claus Desler, Henriette Kihl, Michaela C Hohnholt, Malin H Stridh, Lene J Rasmussen, Helle S Waagepetersen, Lasse K Bak
Soluble adenylate cyclase (sAC) is a non-plasma membrane-bound isoform of the adenylate cyclases signaling via the canonical second messenger, 3',5'-cyclic AMP (cAMP). sAC is involved in key physiological processes such as insulin release, sperm motility, and energy metabolism. Thus, sAC has attracted interest as a putative drug target and attempts have been made to develop selective inhibitors. Since sAC has a binding constant for its substrate, ATP, in the millimolar range, reductions in mitochondrial ATP production may be part of the mechanism-of-action of sAC inhibitors and the potential of these compounds to study the physiological outcomes of inhibition of sAC might be severely hampered by this...
June 22, 2018: Biochemical Pharmacology
Alex J Félix, Carlos J Ciudad, Véronique Noé
PolyPurine Reverse Hoogsteen (PPRH) hairpins constitute a relatively new pharmacological agent for gene silencing that has been applied for a growing number of gene targets. Previously we reported that specific PPRHs against the antiapoptotic gene survivin were able to decrease viability of PC3 prostate cancer cells by increasing apoptosis, while not acting on HUVEC non-tumoral cells. These PPRHs were efficient both in vitro and in vivo. In the present work, we performed a functional pharmacogenomics study on the effects of specific and unspecific hairpins against survivin...
June 22, 2018: Biochemical Pharmacology
Jeffrey M Witkin, Ryan A Shenvi, Xia Li, Scott D Gleason, Julie Weiss, Denise Morrow, John T Catow, Mark Wakulchik, Masaki Ohtawa, Hai-Hua Lu, Michael D Martinez, Jeffrey M Schkeryantz, Timothy S Carpenter, Felice C Lightstone, Rok Cerne
The 'neurotrophic sesquiterpenes' refer to a group of molecules derived from the Illicium genus of flowering plant. They display neurotrophic effects in cultured neuron preparations and have been suggested to be cognitive enhancers and potential therapeutics for neurodegenerative disorders and dementias. Recent synthetic advances generated sufficient quantities of jiadifenolide for in vivo investigation into its biological effects. Jiadifenolide did not induce convulsions in mice nor did it enhance or diminish convulsions induced by pentylenetetrazole...
June 22, 2018: Biochemical Pharmacology
Sandra Blasco-Benito, Marta Seijo-Vila, Miriam Caro-Villalobos, Isabel Tundidor, Clara Andradas, Elena García-Taboada, Jeff Wade, Stewart Smith, Manuel Guzmán, Eduardo Pérez-Gómez, Mara Gordon, Cristina Sánchez
Breast cancer is the second leading cause of death among women. Although early diagnosis and development of new treatments have improved their prognosis, many patients present innate or acquired resistance to current therapies. New therapeutic approaches are therefore warranted for the management of this disease. Extensive preclinical research has demonstrated that cannabinoids, the active ingredients of Cannabis sativa, trigger antitumor responses in different models of cancer. Most of these studies have been conducted with pure compounds, mainly Δ9 -tetrahydrocannabinol (THC)...
June 22, 2018: Biochemical Pharmacology
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