Abstract：
:Mechanism of interaction of non-steroidal anti-inflammatory drugs, celecoxib and valdecoxib with human serum albumin has been studied using fluorescence spectroscopic technique. There was only one high affinity site on serum albumin for both the drugs with association constants of the order of 10(4) in the case of celecoxib and 10(5) in the case of valdecoxib. Thermodynamic parameters for the binding indicated that hydrogen bonding interactions are predominantly involved in the binding of these drugs to human serum albumin. Binding studies in the presence of hydrophobic probe, 1-anilinonaphthalene-8-sulfonate (ANS) suggested that the mode of interaction of drugs and ANS with HSA is different and hydrophobic interactions are not primarily involved in the binding. Studies carried out in the presence of site-specific probe showed that drugs are bound at site II and phenolic oxygen of (411)Tyr is involved in binding. Stern-Volmer analysis of the quenching data indicated that predominantly static quenching mechanism is operative and the tryptophan residues of albumin are fully accessible to celecoxib and only partially accessible to valdecoxib. The presence of salt caused a decrease in the association constant and significant increase in the concentration of free drug.
journal_name
Pharmacol Resjournal_title
Pharmacological researchauthors
Seedher N,Bhatia Sdoi
10.1016/j.phrs.2006.02.008subject
Has Abstractpub_date
2006-08-01 00:00:00pages
77-84issue
2eissn
1043-6618issn
1096-1186pii
S1043-6618(06)00035-1journal_volume
54pub_type
杂志文章abstract：:Bleomycin (BLM) is a drug used to treat different types of neoplasms. BLM's most severe adverse effect is lung toxicity, which induces remodeling of lung architecture and loss of pulmonary function, rapidly leading to death. While its clinical role as an anticancer agent is limited, its use in experimental settings is...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2015.04.012
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abstract：:By the use of combined radioreceptor binding and autoradiographic techniques we attempted to analyse the biochemical characteristics and the anatomical localization of GABA-B receptors in sections of rat circle of Willis and pialarachnoid arteries. 3H-GABA in the presence of 40 microM isoguvacine and 2.5 mM CaCl2 was ...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/1043-6618(90)90731-r
更新日期：1990-05-01 00:00:00
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journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.2000.0702
更新日期：2000-10-01 00:00:00
abstract：:Stem cell mediated cardiac repair is an exciting and controversial area of cardiovascular research that holds the potential to produce novel, revolutionary therapies for the treatment of heart disease. Extensive investigation to define cell types contributing to cardiac formation, homeostasis and regeneration has prod...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2017.06.007
更新日期：2018-01-01 00:00:00
abstract：:Novel therapeutic strategies are needed to address and to solve the emerging problem of hypoxia-induced resistance to anticancer drugs. N-(4-Hydroxyphenyl)retinamide (4-HPR) exhibits potent anticancer and chemopreventive activities, but its inefficiency under hypoxia, through undetermined mechanisms, may contribute to...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2010.07.002
更新日期：2010-11-01 00:00:00
abstract：:Oxylipins (OXLs) are bioactive molecules generated by the oxidation of fatty acids that promote the resolution of acute inflammation and prevent chronic inflammatory processes through molecular mechanisms that are not well known. We have previously reported the anti-inflammatory activity of microalgae-derived OXLs and...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2017.10.009
更新日期：2018-02-01 00:00:00
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journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.1997.0151
更新日期：1997-04-01 00:00:00
abstract：:In China, child and adolescent pediatricians often face challenges in treating children with the appropriate medications. Within the last 8 years, the Chinese government has already initiated a series of policies to promote development of age-appropriate medicines for children. In this study,we introduced the current ...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2019.104412
更新日期：2019-10-01 00:00:00
abstract：:It has been suggested that hypertension results from a loss of immunological tolerance and the resulting autoimmunity may be an important underlying factor of its pathogenesis. This stems from the observations that many of the features involved in autoimmunity are also implicated in hypertension. Furthermore, the unde...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2016.09.008
更新日期：2016-11-01 00:00:00
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journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2019.03.023
更新日期：2019-05-01 00:00:00
abstract：:The present study was undertaken to characterize the interactions between nonsteroidal anti-inflammatory drugs and the alpha(2)-adrenoceptor agonist clonidine in an acute nociceptive test. The writhing test was selected as a model of acute visceral pain. Isobolograms were constructed to assess the interactions of clon...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2004.02.008
更新日期：2004-09-01 00:00:00
abstract：:Isoxanthohumol (IXN), a prenylated flavonoid from hops, exhibits diverse biological activities, e.g. antitumor, antiinflammatory, antioxidant and antiangiogenic. In this study, the effect of IXN is evaluated on two melanoma cell lines with dissimilar molecular background, B16 and A375. The treatment of both cell lines...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2016.01.011
更新日期：2016-03-01 00:00:00
abstract：BACKGROUND AND OBJECTIVES:Thymidylate synthase (TS) expression levels appear to be related to response to 5-fluorouracil-(5-FU)-based chemotherapy in colorectal cancer (CRC) patients. Three polymorphisms have been proposed as modulators of TS expression: a tandemly repeated sequence (2R/3R) in the 5' UTR, a SNP (G>C) w...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2011.04.006
更新日期：2011-09-01 00:00:00
abstract：:Metastatic cancers account for more than 90% of cancer mortality. The metastasis of all cancers is critically mediated by enzymes that degrade extracellular matrix. Aggressive tumors are characterized by an imbalance between enzymes that degrade ECM and endogenous inhibitors of the enzymes. Matrix metalloproteinases (...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2010.11.003
更新日期：2011-02-01 00:00:00
abstract：:Curcumin, a bioactive polyphenol, is a yellow pigment of the Curcuma longa (turmeric) plant. Curcumin has many pharmacologic effects including antioxidant, anti-carcinogenic, anti-obesity, anti-angiogenic and anti-inflammatory properties. Recently, it has been found that curcumin affects lipid metabolism, and subseque...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2017.02.008
更新日期：2017-05-01 00:00:00
abstract：:The molecular complexity of human breast cancer (BC) renders the clinical management of the disease challenging. Long non-coding RNAs (lncRNAs) are promising biomarkers for BC patient stratification, early detection, and disease monitoring. Here, we identified the involvement of the long intergenic non-coding RNA 0108...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2020.105249
更新日期：2020-11-01 00:00:00
abstract：:Purine release and prostaglandin (PG) outflow were simultaneously evaluated from untreated glial primary cultures of rat striatum, at rest and under field electrical stimulation. Purine release was also assayed from sister cultured cells in which a suitable pharmacological treatment with 1 x 10(-6) M dexamethasone or ...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/s1043-6618(89)80005-2
更新日期：1989-05-01 00:00:00
abstract：:Most cancer cells generate energy through aerobic glycolysis to enable their rapid growth and proliferation, which is a phenomenon known as Warburg effect. Inhibition of aerobic glycolysis reduces lactate and ATP generation in cancer cells, and ultimately kills tumor cells. Increasing evidence suggests that wogonin, a...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2018.07.011
更新日期：2018-09-01 00:00:00
abstract：:The most frequent cause of mortality and morbidity in industrialized countries is coronary artery disease (CAD), which in Europe alone is responsible for around two million deaths per year. In 2001 it accounted for about 260,000 hospital discharges in Italy. The costs of CAD treatment in Italy--which were borne by the...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2006.04.002
更新日期：2006-08-01 00:00:00
abstract：:Inflammation plays a key role in tumor promotion and development. Indeed, cyclooxygenase-2 (COX-2) expression is strongly associated with different types of cancer. An emerging class of compounds with significant anti-inflammatory properties is the hydrogen sulfide-releasing non-steroidal anti-inflammatory drugs (H2S-...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2016.10.019
更新日期：2016-12-01 00:00:00
abstract：:The potential for modulating gene expression by the use of antisense oligonucleotides has become increasingly interesting in recent years. Antisense oligonucleotides are complementary nucleic acid fragments that hybridize to target sequences within RNA to form a DNA-RNA duplex, resulting in the block of translation of...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1006/phrs.1997.0227
更新日期：1997-09-01 00:00:00
abstract：:Melanoma is a highly invasive and metastatic cancer with high mortality rates and chemoresistance. Around 50% of melanomas are driven by activating mutations in BRAF that has led to the development of potent anti-BRAF inhibitors. However resistance to anti-BRAF therapy usually develops within a few months and conseque...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2017.08.018
更新日期：2017-11-01 00:00:00
abstract：:Chronic stress can lead to depression due to elevated levels of stress hormones such as glucocorticoid. This is accompanied by an increase in reactive oxygen species (ROS) levels in the brain, which can cause dendritic spine loss and atrophy in neurons, followed by memory loss. Dicaffeoylquinic acids (diCQAs) are natu...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2020.105252
更新日期：2020-11-01 00:00:00
abstract：:The antiepileptic drug vigabatrin (GVG) is known to decrease significantly the serum concentration of concurrently administered phenytoin (PHT) in epileptic patients. To assess a possible mechanism for this interaction, the effect of GVG on the intestinal absorption of PHT was investigated by means of circulation expe...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/s1043-6618(05)80133-1
更新日期：1992-09-01 00:00:00
abstract：:The aqueous extract from aerial parts of Artemisia copa Phil. (Compositae), was evaluated for antinociceptive activity using writhing, formalin, and hot-plate tests in mice. A dose-related antinociceptive response was obtained in the writhing test at doses of 500 and 1000 mg/kg p.o. (percentage of inhibition 23.3 and ...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2003.12.016
更新日期：2004-07-01 00:00:00
abstract：:The metabolism of arachidonic acid by cytochrome P450 (CYP) epoxygenases generates epoxyeicosatrienoic acids (EETs) which affect numerous cellular process including Ca(2+) signaling and the activity of Ca(2+)-dependent K(+) channels. The expression of the CYP epoxygenase(s) that generate EETs in endothelial cells is n...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2003.11.016
更新日期：2004-06-01 00:00:00
abstract：:Combination antiretroviral therapy reduces morbidity and mortality in HIV infected patients. However, the cure of HIV infection is hindered by the persistence of the latent HIV reservoir. Latency reversing agents (LRAs) are developed to target the HIV latently infected cells for HIV reactivation. In addition to revers...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2018.10.023
更新日期：2019-01-01 00:00:00
abstract：:In the present study the effect of ketamine on the contractions caused by propoxur and phoxim on the isolated guinea pig ileum was investigated. Ketamine was found able to inhibit in a concentration-dependent manner the contractile responses of the ileum to propoxur and phoxim, while it did not significantly modify th...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/1043-6618(94)80003-0
更新日期：1994-08-01 00:00:00
abstract：:Regulatory T cells (Tregs) modulate ongoing immune responses to prevent autoimmunity in healthy bodies and inhibit effective anti-tumor immunity responses in tumor patients, leading to tumor progression. The function of Tregs in tumor immunity suggests that elimination of Tregs in the host may enhance the anti-tumor i...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2020.104659
更新日期：2020-03-01 00:00:00
abstract：:Heparin-binding protein (HBP; CAP37/azurocidin) is secreted from neutrophil leukocytes early during inflammation and plays a central role in early capillary leakage and extravasation of neutrophils. Furthermore, HBP is chemotactic towards monocytes and lymphocytes and protects against stress-induced apoptosis, e.g. in...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2005.01.004
更新日期：2005-06-01 00:00:00
