5-Substituted-2,2'-anhydrouridines, potent inhibitors of uridine phosphorylase.

abstract：:The phenolic glucoside gastrodin, a main constituent of a Chinese traditional herbal medicine, has been known to display several biological and pharmacological properties. However, the role and precise molecular mechanisms explaining how gastrodin suppresses the inflammatory response in septic cardiac dysfunction are ...

journal_title：Biochemical pharmacology

authors： Yang P,Han Y,Gui L,Sun J,Chen YL,Song R,Guo JZ,Xie YN,Lu D,Sun L

更新日期：2013-04-15 00:00:00

abstract：:Studies were performed to investigate the irreversible binding and oxidative metabolism of propranolol in human liver microsomes and the relationship of binding and metabolism to the polymorphic oxidation of debrisoquine. Incubation of microsomes with 14C-labelled propranolol in the presence of a NADPH-generating syst...

journal_title：Biochemical pharmacology

authors： Shaw L,Lennard MS,Tucker GT,Bax ND,Woods HF

更新日期：1987-07-15 00:00:00

abstract：:Although it is generally believed that thiazolidinediones ameliorate insulin resistance by lowering circulating free fatty acids, direct effects of these drugs in skeletal muscle may also contribute to their antidiabetic action. We report that troglitazone administration to mice for 1 day increased the protein express...

journal_title：Biochemical pharmacology

authors： Planavila A,Alegret M,Sánchez RM,Rodríguez-Calvo R,Laguna JC,Vázquez-Carrera M

更新日期：2005-04-15 00:00:00

abstract：:These in vitro studies indicate that N-oxidation of N-hydroxyamphetamine (NOHA) by rat liver homogenates yields phenylacetone oxime (PAOx) as the major metabolite. This oxidation was NADPH and oxygen dependent but was not appreciably increased in microsomes from phenobarbital-pretreated animals. The addition to micros...

journal_title：Biochemical pharmacology

authors： Matsumoto RM,Cho AK

更新日期：1982-01-01 00:00:00

abstract：:The enhanced nitric oxide (NO) and prostaglandin (PG) generation of activated macrophages is controlled by glucocorticoid-sensitive inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2), respectively. Negative feedback regulation of iNOS expression by the products of both pathways has been suggested, but...

journal_title：Biochemical pharmacology

authors： Pang L,Hoult JR

更新日期：1997-02-21 00:00:00

abstract：:Angiogenesis has emerged as a critical process for tumour progression. Identifying key pathways involved in the regulation and promotion of angiogenesis has resulted in the development of numerous approaches targeting pro-angiogenic signalling pathways. The most prominent and characterised pro-angiogenic pathway is th...

journal_title：Biochemical pharmacology

authors： Bridges EM,Harris AL

更新日期：2011-05-15 00:00:00

abstract：:Bufuralol hydroxylation activities of liver microsomal cytochrome P450 (P450) enzymes were studied in the rat; the reaction has been used widely in determining levels of liver microsomal P450 2D6, which shows debrisoquine-type genetic polymorphism in humans. Liver microsomes catalyzed the conversion of bufuralol to 1'...

journal_title：Biochemical pharmacology

authors： Mimura M,Yamazaki H,Sugahara C,Hiroi T,Funae Y,Shimada T

更新日期：1994-06-01 00:00:00

abstract：:Endotoxin (LPS) and interleukin-1 beta (IL-1 beta) increased the expression of tissue factor, a membrane-anchored glycoprotein that initiates blood coagulation on the surface of cultured human umbilical vein endothelial cells (HUVEC) and human monocyte/macrophages. On monocyte/macrophages, oleic acid strongly inhibite...

journal_title：Biochemical pharmacology

authors： Lalé A,Herbert JM

更新日期：1994-07-19 00:00:00

abstract：:The major metabolic products of the endogeneous catecholamine dopamine are its 3- and 4-O-sulphates which have also been implicated as intermediates in noradrenaline biosynthesis. Because of the unsatisfactory status of the literature concerning the synthesis, isolation, purity and characterisation of the dopamine O-s...

journal_title：Biochemical pharmacology

authors： Osikowska BA,Idle JR,Swinbourne FJ,Sever PS

更新日期：1982-07-01 00:00:00

abstract：:Sodium orthovanadate is known to promote glucose uptake in muscle and adipose tissues and has been suggested as a possible oral hypoglycemic agent. In addition, insulin-dependent diabetes has been shown to alter the hepatobiliary clearance of several drugs in rats. This study has determined whether orthovanadate, like...

journal_title：Biochemical pharmacology

authors： Watkins JB 3rd,Bauman ME,Beaty TM

更新日期：1993-12-14 00:00:00

abstract：:African trypanosomes, like Trypanosoma brucei, depend on antigenic variation to evade the immune response of the vertebrate host. An antigenic switch corresponds to the activation of a variable surface glycoprotein (VSG) gene from a large silent repertoire. Most switches require the duplicative transposition of a VSG ...

journal_title：Biochemical pharmacology

authors： Cornelissen AW,Michels PA,Borst P,Spanjer W,Versluijs-Broers JA,Van der Meer C,Farzaneh F,Shall S

更新日期：1985-12-01 00:00:00

abstract：:R-flurbiprofen, a non cyclooxygenase inhibiting non-steroidal anti-inflammatory drug (NSAID), has been found to inhibit tumor growth in various animal models. In vitro experiments have shown that this effect is based on the induction of a cell cycle block and apoptosis. Cell cycle inhibition has been explained by acti...

journal_title：Biochemical pharmacology

authors： Grösch S,Schilling K,Janssen A,Maier TJ,Niederberger E,Geisslinger G

更新日期：2005-03-01 00:00:00

abstract：:The underlying mechanism of the antiproliferative effect of S (simvastatin), a HMG-CoA reductase inhibitor, in vascular smooth muscle cells (SMC) is still poorly understood. In the present study, we used synchronized human SMC, isolated from left interior mammary artery, as an in vitro model to test the effects of S o...

journal_title：Biochemical pharmacology

authors： Nègre-Aminou P,van Erck M,van Leeuwen RE,Collard JG,Cohen LH

更新日期：2001-04-15 00:00:00

abstract：:The identification of proliferation/survival pathways constitutively activated by genetic alterations in multiple myeloma (MM), or sustained by the bone marrow (BM) microenvironment, provides novel opportunities for the development of targeted therapies. The deregulated function of protein tyrosine kinases plays a cri...

journal_title：Biochemical pharmacology

authors： Cassinelli G,Ronchetti D,Laccabue D,Mattioli M,Cuccuru G,Favini E,Nicolini V,Greco A,Neri A,Zunino F,Lanzi C

更新日期：2009-11-01 00:00:00

abstract：:The thiopurine drugs 6-mercaptopurine (6-MP) and 6-thioguanine (6-TG) are well-established agents for the treatment of leukaemia but their main modes of action are controversial. Thiopurine methyltransferase (TPMT) metabolises thiopurine drugs and influences their cytotoxic activity. TPMT, like DNA methyltransferases ...

journal_title：Biochemical pharmacology

authors： Hogarth LA,Redfern CP,Teodoridis JM,Hall AG,Anderson H,Case MC,Coulthard SA

更新日期：2008-10-15 00:00:00

abstract：:Naturally occurring amino acid substitutions conferring resistance to methotrexate (MTX) have been reported previously at codon positions 22 (leu-->arg, phe) and 31 (phe-->ser, trp) of mammalian dihydrofolate reductases (DHFR). To explore the character of other substitutions, a polymerase chain reaction (PCR)-assisted...

journal_title：Biochemical pharmacology

authors： Morris JA,McIvor RS

更新日期：1994-03-29 00:00:00

abstract：:On the basis of previous electrophysiological studies, it has been proposed that there are three main classes of excitatory amino acid receptor in the mammalian central nervous system, which are activated preferentially by kainic acid, quisqualic acid and N-methyl-D-aspartate respectively. Although the pharmacology of...

journal_title：Biochemical pharmacology

authors： Anand H,Roberts PJ,Badman G,Dixon AJ,Collins JF

更新日期：1986-02-01 00:00:00

abstract：:ICRF-193 [meso-2,3-bis(3,5-dioxopiperazine-1-yl)butane], a bisdioxopiperazine compound, has been shown to be a catalytic inhibitor of DNA topoisomerase II by stabilizing the enzyme in the form of a closed "protein clamp," an intermediate form in the catalytic cycle (Roca et al., Proc Natl Acad Sci USA 91: 1781-1785, 1...

journal_title：Biochemical pharmacology

authors： Sato M,Ishida R,Narita T,Kato J,Ikeda H,Fukazawa H,Andoh T

更新日期：1997-09-01 00:00:00

abstract：:The metabolism of alpha,alpha,beta,beta- tetradeutero -N,N -dimethyltryptamine ( D4DMT ) in rat brain in vivo as a function of time and dose was examined. Quantification of D4DMT and its respective deutero-metabolites was accomplished using gas chromatographic/mass spectrometric/selected ion monitoring/isotope dilutio...

journal_title：Biochemical pharmacology

authors： Barker SA,Beaton JM,Christian ST,Monti JA,Morris PE

更新日期：1984-05-01 00:00:00

abstract：:We have previously reported that Gen-27, a newly synthesized flavonoid, exhibits anticancer effects against human colorectal cancer cells. In this study, we investigated the anticancer effects in human breast cancer cell lines and its underlying mechanisms. We demonstrated that Gen-27 inhibited the growth and prolifer...

journal_title：Biochemical pharmacology

authors： Tao L,Wei L,Liu Y,Ding Y,Liu X,Zhang X,Wang X,Yao Y,Lu J,Wang Q,Hu R

更新日期：2017-02-01 00:00:00

abstract：:A series of trifluoromethanesulfonamides (TFMS) was synthesized and tested for uncoupling activity in rat liver mitochondria. With succinate as the mitochondrial substrate, and the respiratory control index (RCI) as an indicator of their uncoupling ability, we found that all of the TFMS tested were uncouplers of oxida...

journal_title：Biochemical pharmacology

authors： McCracken RO,Carr AW,Stillwell WH,Lipkowitz KB,Boisvenue R,O'Doherty GO,Wickiser DI

更新日期：1993-05-05 00:00:00

abstract：:In order to elucidate the role of mitochondrial dysfunction in paracetamol-induced hepatotoxicity, the effects of paracetamol on the oxygen consumption and ATP content of the isolated perfused rat liver were correlated with parameters of hepatic viability and hepatotoxicity. Paracetamol at 5 g/L reduced the oxygen con...

journal_title：Biochemical pharmacology

authors： Strubelt O,Younes M

更新日期：1992-07-07 00:00:00

abstract：:A voluminous number of evidence suggests that an increased consumption of fruit and vegetables is a relatively easy and practical strategy to reduce significantly the incidence of chronic diseases, such as cancer, cardiovascular diseases and other aging-related pathologies. This review will critically discuss the appl...

journal_title：Biochemical pharmacology

authors： Russo GL

更新日期：2007-08-15 00:00:00

abstract：:Treatment of red blood cells with the copper (II) ascorbate system causes increased lipid peroxidation, increased membrane microviscosity, and phospholipid translocation with a concurrent decrease in cytosolic catalase and glutathione peroxidase activities. All these changes are prevented if the cells are treated with...

journal_title：Biochemical pharmacology

authors： Chattopadhyay A,Choudhury TD,Bandyopadhyay D,Datta AG

更新日期：2000-02-15 00:00:00

abstract：:Chronic administration of the beta-adrenergic receptor agonist isoproterenol (5 mg/200 g animal for 10 days) resulted in rat parotid and submandibular gland hypertrophy, and it induced synthesis of a series of proline-rich proteins (PRPs) and glycoproteins. Treated parotid glands additionally exhibit an increase in ac...

journal_title：Biochemical pharmacology

authors： Wells DJ,Humphreys-Beher MG

更新日期：1985-12-15 00:00:00

abstract：:EM012, a semisynthetic phthalideisoquinoline alkaloid, has been recently found to target microtubules and possess anti-cancer activity. In this study, we evaluated the effects of EM012 in combination with the classic microtubule-targeting agent paclitaxel. Our results demonstrated that EM012 enhanced the anti-prolifer...

journal_title：Biochemical pharmacology

authors： Zhou J,Liu M,Aneja R,Chandra R,Joshi HC

更新日期：2004-12-15 00:00:00

abstract：:The effects of beta 1- and beta 1 + beta 2-antagonists on the myocardial adaptation to exercise training were investigated in male Sprague-Dawley rats randomly divided into trained (treadmill, 1 hr/day, 5 days/week for 10 weeks at 27 m/min, 15% grade) without drug (TC), sedentary without drug (SC), trained treated wit...

journal_title：Biochemical pharmacology

authors： Ji LL,Stratman FW,Lardy HA

更新日期：1987-10-15 00:00:00

abstract：:The intraperitoneal injection of methylglyoxal bis(cyclohexylamidinohydrazone) (MGBC), an inhibitor of S-adenosylmethionine decarboxylase and spermidine synthase, markedly increased (7-fold of the basal level at 4 hr) ornithine decarboxylase (ODC) activity in normal mouse liver. ODC activity was also increased 2.5-fol...

journal_title：Biochemical pharmacology

authors： Hibasami H,Maekawa S,Murata T,Nakashima K

更新日期：1988-11-01 00:00:00

abstract：:CYP2C19 (formerly known as CYP2C75), highly homologous to human CYP2C19, has been identified in cynomolgus and rhesus macaques, non-human primate species widely used in drug metabolism studies. CYP2C19 is predominantly expressed in liver and encodes a functional drug-metabolizing enzyme. Genetic variants in human CYP2...

journal_title：Biochemical pharmacology

authors： Uno Y,Matsushita A,Shukuya M,Matsumoto Y,Murayama N,Yamazaki H

更新日期：2014-09-15 00:00:00

abstract：:Osteoarthritis is the most prevalent musculoskeletal disorder and one for which there is no disease modifying therapy available at present. Our current understanding of the disease mechanism of osteoarthritis is limited owing to a lacuna of knowledge about the development and maintenance of articular cartilage that is...

journal_title：Biochemical pharmacology

authors： Jaswal AP,Bandyopadhyay A

更新日期：2019-07-01 00:00:00