Comparison of pharmacokinetic and pharmacodynamic profiles of aspirin following oral gavage and diet dosing in rats.


:Aspirin is one of the oldest drugs and has been purported to have multiple beneficial effects, including prevention of cardiovascular disease and cancer, in addition to its original indication for treatment of inflammation, fever and pain. In cancer chemoprevention studies using animal models, two methods of aspirin administration have been employed: oral gavage and diet. The untested assumption was that exposure and the resultant pharmacological effects are similar for these two administration methods when dosing is normalized on the basis of mg/kg body weight/day. This study examined and compared time-dependent plasma and colon mucosal concentrations of aspirin metabolite salicylate (aspirin concentrations were below level of quantification), plasma thromboxane B(2) concentrations, and colon mucosal prostaglandin E(2) concentration following these two different dosing paradigms in rats. Diet dosing yielded relatively constant plasma and colon salicylate concentration vs. time profiles. On the other hand, oral gavage dosing led to a rapid peak followed by a fast decline in salicylate concentration in both plasma and colon. Nevertheless, the exposure as measured by the area under plasma or colon concentration-time curve of salicylate was linearly related to dose irrespective of the dosing method. Linear relationships were also observed between colon and plasma salicylate areas under the curve and between colon prostaglandin E(2) and plasma thromboxane B(2) areas under the curve. Therefore, more easily accessible plasma salicylate and thromboxane B(2) concentrations were representative of the salicylate exposure and prostaglandin E(2) pharmacodynamic biomarker in the target colon, respectively.


Chem Biol Interact


Kapetanovic IM,Bauer KS,Tessier DM,Lindeblad MO,Zakharov AD,Lubet R,Lyubimov A




Has Abstract


2009-05-15 00:00:00














  • Conjugation of benzo[a]pyrene metabolites by freshwater green alga Selenastrum capricornutum.

    abstract::Benzo[a]pyrene (BaP) undergoes metabolic transformation in mammals via oxidative, hydrolytic, and conjugative processes; however, little is known concerning BaP conjugation in freshwater algae. It has been shown in this laboratory that BaP is metabolized by Selenastrum capricornutum via a dioxygenase pathway. This stu...

    journal_title:Chemico-biological interactions

    pub_type: 杂志文章


    authors: Warshawsky D,Keenan TH,Reilman R,Cody TE,Radike MJ

    更新日期:1990-01-01 00:00:00

  • The effects of indole-3-acetic acid on human and horse serum butyrylcholinesterase.

    abstract::Butyrylcholinesterase (BChE) constitutes the first line defense in the serum of higher organisms and is a marker for toxic exposure. Indole-3-acetic acid (IAA) is a major plant growth hormone of the auxin class, affecting cell enlargement, and differentiation. As a result of the industrial usage, this agrochemical is ...

    journal_title:Chemico-biological interactions

    pub_type: 杂志文章


    authors: Bodur E,Cokugras AN

    更新日期:2005-12-15 00:00:00

  • Sulfated polysaccharides from the edible marine algae Padina tetrastromatica attenuates isoproterenol-induced oxidative damage via activation of PI3K/Akt/Nrf2 signaling pathway - An in vitro and in vivo approach.

    abstract::The reactive oxygen species (ROS) induced oxidative stress is an inevitable factor for the pathogenesis of cardiovascular diseases. The edible marine algae-derived sulfated polysaccharides gained special attention as novel bioactive compounds having potential pharmacological activities. The present study evaluated in ...

    journal_title:Chemico-biological interactions

    pub_type: 杂志文章


    authors: V S L,Rauf AA,Kurup GM

    更新日期:2019-08-01 00:00:00

  • Salidroside attenuates colistin-induced neurotoxicity in RSC96 Schwann cells through PI3K/Akt pathway.

    abstract::Neurotoxicity is a key dose-limiting factor for colistin therapy. This study aimed to investigate the protective effect of Salidroside on colistin-induced neurotoxicity in RSC96 Schwann cells and the underlying mechanisms. After Salidroside (12.5, 25, 50 μg/mL) treatment for 2 h, the cells were cultured with 250 μg/mL...

    journal_title:Chemico-biological interactions

    pub_type: 杂志文章


    authors: Lu Z,Jiang G,Chen Y,Wang J,Muhammad I,Zhang L,Wang R,Liu F,Li R,Qian F,Li J

    更新日期:2017-06-01 00:00:00

  • Transient induction of increased aldehyde dehydrogenase 3A1 levels in cultured human breast (adeno)carcinoma cell lines via 5'-upstream xenobiotic, and electrophile, responsive elements is, respectively, estrogen receptor-dependent and -independent.

    abstract::Transient up-regulation of ALDH3A1, CYP1A1 and CYP1B1 transcription by transient exposure to aryl hydrocarbon receptor (AhR) ligands, e.g. 3-methylcholanthrene, is via transient transactivation of xenobiotic responsive elements (XRE) present in the 5'-upstream regions of these genes. Others have shown that AhR ligand-...

    journal_title:Chemico-biological interactions

    pub_type: 杂志文章


    authors: Sládek NE

    更新日期:2003-02-01 00:00:00

  • Overview of lipid peroxidation products and hepatic protein modification in alcoholic liver disease.

    abstract:OBJECTIVES:Oxidative stress is one component of alcoholic liver disease (ALD) that is manifested in the peroxidation of cellular lipids producing the electrophile, 4-hydroxynonenal (4-HNE). This electrophile is proposed to modify essential cellular proteins resulting in loss of protein function and cellular homeostasis...

    journal_title:Chemico-biological interactions

    pub_type: 杂志文章,评审


    authors: Smathers RL,Galligan JJ,Stewart BJ,Petersen DR

    更新日期:2011-06-30 00:00:00

  • Glutathione depletion, lipid peroxidation, DNA double-strand breaks and the cytotoxicity of 2-bromo-3-(N-acetylcystein-S-yl)hydroquinone in rat renal cortical cells.

    abstract::The mechanisms involved in the cytotoxicity of 2-bromo-3-(N-acetylcystein-S-yl)hydroquinone, a model compound for hydroquinone derived mercapturic acids, were investigated in rat renal proximal tubule cells. 2-Bromo-3-(N-acetylcystein-S-yl)hydroquinone induced a time- and concentration-dependent decrease in cell viabi...

    journal_title:Chemico-biological interactions

    pub_type: 杂志文章


    authors: Vamvakas S,Bittner D,Koob M,Glück S,Dekant W

    更新日期:1992-08-14 00:00:00

  • In vitro skin decontamination of the organophosphorus pesticide Paraoxon with nanometric cerium oxide CeO2.

    abstract::Organophosphorus compounds (OP), which mainly penetrate via the percutaneous pathway, represent a threat for both military and civilians. Body surface decontamination is vital to prevent victims poisoning. The development of a cost-effective formulation, which could be efficient and easy to handle in case of mass cont...

    journal_title:Chemico-biological interactions

    pub_type: 杂志文章


    authors: Salerno A,Devers T,Bolzinger MA,Pelletier J,Josse D,Briançon S

    更新日期:2017-04-01 00:00:00

  • Target cells for methylsulphonyl-2,6-dichlorobenzene in the olfactory mucosa in mice.

    abstract::Previously we reported that methylsulphonyl-2,6-dichlorobenzene, 2, 6-(diCl-MeSO(2)-B), was irreversibly bound to the olfactory mucosa of mice and induced necrosis of the Bowman's glands with subsequent neuroepithelial degeneration and detachment. In this study, autoradiography and histopathology were used to determin...

    journal_title:Chemico-biological interactions

    pub_type: 杂志文章


    authors: Bahrami F,van Hezik C,Bergman A,Brandt I

    更新日期:2000-10-16 00:00:00

  • Lack of effect of glutathione depletion on cytotoxicity, mutagenicity and DNA damage produced by doxorubicin in cultured cells.

    abstract::Since endogenous glutathione (GSH), the main non-protein intracellular thiol compound, is known to provide protection against reactive radical species, its depletion by diethylmaleate (DEM) was used to assess the role of free radical formation mediated by doxorubicin in DNA damage, cytotoxicity and mutagenicity of the...

    journal_title:Chemico-biological interactions

    pub_type: 杂志文章


    authors: Capranico G,Babudri N,Casciarri G,Dolzani L,Gambetta RA,Longoni E,Pani B,Soranzo C,Zunino F

    更新日期:1986-02-01 00:00:00

  • Race to arsenal COVID-19 therapeutics: Current alarming status and future directions.

    abstract::The on-going pandemic of COVID-19 wreaked by a viral infection of SARS-CoV-2, has generated a catastrophic plight across the globe. Interestingly, one of the hallmarks of COVID-19 is the so-called 'cytokine storm' due to attack of SARS-Cov-2 in the lungs. Considering, mesenchymal stem cells (MSCs) therapy could contri...

    journal_title:Chemico-biological interactions

    pub_type: 杂志文章,评审


    authors: Dubey AK,Singh A,Prakash S,Kumar M,Singh AK

    更新日期:2020-12-01 00:00:00

  • Arginase purified from endophytic Pseudomonas aeruginosa IH2: Induce apoptosis through both cell cycle arrest and MMP loss in human leukemic HL-60 cells.

    abstract::Arginase is a therapeutic enzyme for arginine-auxotrophic cancers but their low anticancer activity, less proteolytic tolerance and shorter serum half-life are the major shortcomings. In this study, arginase from Pseudomonas aeruginosa IH2 was purified to homogeneity and estimated as 75 kDa on native-PAGE and 37 kDa o...

    journal_title:Chemico-biological interactions

    pub_type: 杂志文章


    authors: Husain I,Bala K,Wani A,Makhdoomi U,Malik F,Sharma A

    更新日期:2017-08-25 00:00:00

  • Beneficial effects of Murraya koenigii leaves on antioxidant defense system and ultra structural changes of pancreatic beta-cells in experimental diabetes in rats.

    abstract::Oxidative stress and oxidative damage to tissues are common end points of chronic diseases such as atherosclerosis, diabetes, and rheumatoid arthritis. Oxidative stress in diabetes coexists with a reduction in the antioxidant status, which can further increase the deleterious effects of free radicals. The aim of the p...

    journal_title:Chemico-biological interactions

    pub_type: 杂志文章


    authors: Arulselvan P,Subramanian SP

    更新日期:2007-01-30 00:00:00

  • Gastroprotective potential of risperidone, an atypical antipsychotic, against stress and pyloric ligation induced gastric lesions.

    abstract::Risperidone has been used in some stress disorders and may be potentially protective against stress-induced gastric lesions. Thus, the aim of the present study is to investigate, whether risperidone, a D(2) receptor and 5-HT(2A) receptor antagonist, would be able to result in gastroprotective effect in stress-induced ...

    journal_title:Chemico-biological interactions

    pub_type: 杂志文章


    authors: Saxena B,Krishnamurthy S,Singh S

    更新日期:2011-04-25 00:00:00

  • Accumulation and elimination of macromolecular lesions in susceptible and non-susceptible rat tissues after repeated administration of trans-4-acetylaminostilbene.

    abstract::Trans-4-acetylaminostilbene (trans-AAS) is a potent carcinogen and quite specifically produces sebaceous gland tumors, predominantly in the Zymbal's gland of rats. It is also acutely toxic to the rat glandular stomach. Recent results have shown that these target tissues are not notably exposed to reactive metabolites ...

    journal_title:Chemico-biological interactions

    pub_type: 杂志文章


    authors: Hilpert D,Neumann HG

    更新日期:1985-06-01 00:00:00

  • Caffeine does not bind covalently to liver microsomes from different animal species and to proteins and DNA from perfused rat liver.

    abstract::Caffeine was found not to bind covalently to liver microsomal proteins from mice, rats and rabbits. Microsomes metabolized caffeine only to a limited extent, the highest rate (about 2% of the substrate concentration) being obtained with rabbit microsomal preparations. The rat liver perfusion technique represents a goo...

    journal_title:Chemico-biological interactions

    pub_type: 杂志文章


    authors: Szczawinska K,Ginelli E,Bartosek I,Gambazza C,Pantarotto C

    更新日期:1981-03-15 00:00:00

  • MicroRNA-621 inhibits cell proliferation and metastasis in bladder cancer by suppressing Wnt/β-catenin signaling.

    abstract::Increasing evidence has shown that dysregulation of microRNA-621 (miR-621) is demonstrated to be associated with several cancers. However, the role of miR-621 in bladder cancer (BCa) remains unclear. Herein, we aimed to study the expression pattern, biological function, and molecular mechanism of miR-621 in BCa. First...

    journal_title:Chemico-biological interactions

    pub_type: 杂志文章


    authors: Tian H,Wang X,Lu J,Tian W,Chen P

    更新日期:2019-08-01 00:00:00

  • Structure-function relationships of the alpha/beta-hydrolase fold domain of neuroligin: a comparison with acetylcholinesterase.

    abstract::The neuroligins are postsynaptic cell adhesion proteins whose extracellular domain belongs to the alpha/beta-hydrolase fold family of proteins, a family characterized through the enzyme acetylcholinesterase (AChE) and other enzymes with various substrate specificities. Neuroligin associations with the pre-synaptic neu...

    journal_title:Chemico-biological interactions

    pub_type: 杂志文章


    authors: Leone P,Comoletti D,Taylor P,Bourne Y,Marchot P

    更新日期:2010-09-06 00:00:00

  • Protective effect of allyl methyl disulfide on acetaminophen-induced hepatotoxicity in mice.

    abstract::Multiple sulfur compounds of garlic have shown versatile medicinal activities in the prevention and treatment of various diseases. Allyl methyl disulfide (AMDS) was identified as one of the bioactive components in fresh garlic paste in our previous study. The purpose of this study was to investigate the hepatoprotecti...

    journal_title:Chemico-biological interactions

    pub_type: 杂志文章


    authors: Zhang Y,Zhang F,Wang K,Liu G,Yang M,Luan Y,Zhao Z

    更新日期:2016-04-05 00:00:00

  • 2,3,7,8-Tetrachlorodibenzo-p-dioxin alters melatonin metabolism in fish hepatocytes.

    abstract::Pineal hormone melatonin is an important regulator of endocrine and circadian rhythms in vertebrates. Since liver is assumed to be the major organ in the metabolism of this indole hormone, we investigated the effect of the known Ah-receptor agonist, 2,3,7, 8-tetrachlorodibenzo-p-dioxin (TCDD) on melatonin metabolism i...

    journal_title:Chemico-biological interactions

    pub_type: 杂志文章


    authors: Pesonen M,Korkalainen M,Laitinen JT,Andersson TB,Vakkuri O

    更新日期:2000-06-01 00:00:00

  • Andrographolide could inhibit human colorectal carcinoma Lovo cells migration and invasion via down-regulation of MMP-7 expression.

    abstract::Andrographolide (Andro), a diterpenoid lactone isolated from a traditional herbal medicine Andrographis paniculata, is known to possess multiple pharmacological activities. In our previous study, Andro had been shown to have potent anti-cancer activity against human colorectal carcinoma Lovo cells by inhibiting cell-c...

    journal_title:Chemico-biological interactions

    pub_type: 杂志文章


    authors: Shi MD,Lin HH,Chiang TA,Tsai LY,Tsai SM,Lee YC,Chen JH

    更新日期:2009-08-14 00:00:00

  • Differentiation of human placental BeWo cells by the environmental contaminant benzo(a)pyrene.

    abstract::Polycyclic aromatic hydrocarbons (PAHs) such as benzo(a)pyrene (BaP) are widely-distributed environmental contaminants known to exert toxic effects in various tissues, including placenta. PAHs have notably been shown to inhibit proliferation of trophoblastic cells. The present study was designed to determine whether P...

    journal_title:Chemico-biological interactions

    pub_type: 杂志文章


    authors: Le Vee M,Kolasa E,Jouan E,Collet N,Fardel O

    更新日期:2014-03-05 00:00:00

  • DNA damage and repair in epithelial (mucous) cells and crypt cells from isolated colon.

    abstract::Colon epithelium is made up of two general classes of cells, surface cells which are post-mitotic and crypt cells which contain the proliferative population. Their relative vulnerability to environmental damage and ability to perform DNA repair are important issues in colon carcinogenesis. DNA damage and repair was st...

    journal_title:Chemico-biological interactions

    pub_type: 杂志文章


    authors: Kulkarni MS,Yielding KL

    更新日期:1985-01-01 00:00:00

  • NADH fluorescence lifetime analysis of the effect of magnesium ions on ALDH2.

    abstract::Aldehyde dehydrogenase 2 (ALDH2) catalyzes oxidation of toxic aldehydes to carboxylic acids. Physiologic levels of Mg(2+) ions influence ALDH2 activity in part by increasing NADH binding affinity. Traditional fluorescence measurements monitor the blue shift of the NADH fluorescence spectrum to study ALDH2-NADH interac...

    journal_title:Chemico-biological interactions

    pub_type: 杂志文章


    authors: Gonnella TP,Leedahl TS,Karlstad JP,Picklo MJ

    更新日期:2011-05-30 00:00:00

  • [6]-Gingerol induces reactive oxygen species regulated mitochondrial cell death pathway in human epidermoid carcinoma A431 cells.

    abstract::Since skin cancer incidence and prevalence is constantly rising up the charts despite all efforts, search for newer, better agents for protection and treatment is required. Ginger (Zingiber officinale Roscoe), a monocotyledonous herb, is widely used as a herbal medicine, given the presence of homologous phenolic keton...

    journal_title:Chemico-biological interactions

    pub_type: 杂志文章


    authors: Nigam N,Bhui K,Prasad S,George J,Shukla Y

    更新日期:2009-09-14 00:00:00

  • Subunit communication in tetrameric class 2 human liver aldehyde dehydrogenase as the basis for half-of-the-site reactivity and the dominance of the oriental subunit in a heterotetramer.

    abstract::Data has been published showing that in heterotetrameric liver mitochondrial aldehyde dehydrogenase composed of the active (E487) and the inactive Oriental-variant (K487) subunit, the Oriental variant was dominant and caused the inactivation of the E487 subunit. The published structures of the enzyme showed that the g...

    journal_title:Chemico-biological interactions

    pub_type: 杂志文章


    authors: Weiner H,Wei B,Zhou J

    更新日期:2001-01-30 00:00:00

  • An evolutionary perspective on the first disulfide bond in members of the cholinesterase-carboxylesterase (COesterase) family: Possible outcomes for cholinesterase expression in prokaryotes.

    abstract::Within the alpha/beta hydrolase fold superfamily of proteins, the COesterase group (carboxylesterase type B, block C, cholinesterases …) diverged from the other groups through simultaneous integration of an N-terminal, first disulfide bond and a significant increase in the protein mean size. This first disulfide bond ...

    journal_title:Chemico-biological interactions

    pub_type: 杂志文章


    authors: Chatonnet A,Brazzolotto X,Hotelier T,Lenfant N,Marchot P,Bourne Y

    更新日期:2019-08-01 00:00:00

  • The diversity of microbial aldo/keto reductases from Escherichia coli K12.

    abstract::The genome of Escherichia coli K12 contains 9 open reading frames encoding aldo/keto reductases (AKRs) that are differentially regulated and sequence diverse. A significant amount of data is available for the E. coli AKRs through the availability of gene knockouts and gene expression studies, which adds to the biochem...

    journal_title:Chemico-biological interactions

    pub_type: 杂志文章


    authors: Lapthorn AJ,Zhu X,Ellis EM

    更新日期:2013-02-25 00:00:00

  • Mechanistic evaluation of gastroprotective effects of Kangfuxin on ethanol-induced gastric ulcer in mice.

    abstract::This study was designed to evaluate the gastroprotective effect of Kangfuxin (KFX), a Chinese patent medicine constituent isolated from American cockroach, on ethanol-induced gastric ulcer in mice and to elucidate the potential mechanisms of the effect involved. According to the results, mice treated with alcohol appe...

    journal_title:Chemico-biological interactions

    pub_type: 杂志文章


    authors: Shen Y,Sun J,Niu C,Yu D,Chen Z,Cong W,Geng F

    更新日期:2017-08-01 00:00:00

  • Biologically active aromatic retinoids bearing azido photoaffinity-labeling groups and their binding to cellular retinoic acid-binding protein.

    abstract::Retinoids bearing azido photoaffinity-labeling groups (azidoretinoids) have potential as probes for investigating the molecular mechanisms of action of all-trans-retinoic acid (RA) as mediated by its cellular retinoic acid-binding protein (CRABP) and nuclear receptor proteins. Two new azidoretinoids, 3-azido-4-[2-(5,6...

    journal_title:Chemico-biological interactions

    pub_type: 杂志文章


    authors: Sani BP,Wille JJ Jr,Dawson MI,Hobbs PD,Bupp J,Rhee S,Chao WR,Dorsky A,Morimoto H

    更新日期:1990-01-01 00:00:00