Microsomes

Publication Title: 
Die Pharmazie

In an effort to identify a new chemopreventive agent, the present study was conducted to investigate the role of T. chebula in the prevention of ferric nitrilotriacetic acid (Fe- NTA) induced oxidative stress and renal tumorigenesis in Wistar rats. A single application of Fe-NTA (9 mg Fe/kg body weight, intraperitoneally) significantly induced oxidative stress and elevated the marker parameters of tumor promotion. However, the pretreatment of animals with different doses of T.

Author(s): 
Prasad, L.
Khan, T. H.
Jahangir, T.
Sultana, S.
Publication Title: 
Meat Science

Conjugated linoleic acid, a fatty acid found in milk fat and ruminant meat is one of the functional food components. Modifying fatty acid composition so as to increase CLA and other beneficial PUFA/MUFA level and reducing SFA levels might be a key to enhance the neutraceutical and therapeutic value of ruminant-derived food products.

Author(s): 
Rana, Madhu Suman
Tyagi, A.
Hossain, Sk Asraf
Tyagi, A. K.
Publication Title: 
The Journal of Pharmacology and Experimental Therapeutics

The purpose of this study was to determine the importance of intestinal disposition in the first-pass metabolism of flavonoids. A four-site perfused rat intestinal model, rat liver and intestinal microsomes, Caco-2 cell microsomes, and the Caco-2 cell culture model were used. In the four-site model, approximately 28% of perfused aglycones are absorbed (approximately 450 nmol/30 min). Both absorption and subsequent excretion of metabolites were rapid and site-dependent (p < 0.05).

Author(s): 
Chen, Jun
Lin, Huimin
Hu, Ming
Publication Title: 
Drug Metabolism and Disposition: The Biological Fate of Chemicals

Oxycodone undergoes N-demethylation to noroxycodone and O-demethylation to oxymorphone. The cytochrome P450 (P450) isoforms capable of mediating the oxidation of oxycodone to oxymorphone and noroxycodone were identified using a panel of recombinant human P450s. CYP3A4 and CYP3A5 displayed the highest activity for oxycodone N-demethylation; intrinsic clearance for CYP3A5 was slightly higher than that for CYP3A4. CYP2D6 had the highest activity for O-demethylation. Multienzyme, Michaelis-Menten kinetics were observed for both oxidative reactions in microsomes prepared from five human livers.

Author(s): 
Lalovic, Bojan
Phillips, Brian
Risler, Linda L.
Howald, William
Shen, Danny D.
Publication Title: 
The Journal of Pharmacology and Experimental Therapeutics

Aspirin (acetylsalicylic acid) and clopidogrel are two major antithrombogenic agents that are widely used for the treatment and prevention of cerebro- and cardiovascular conditions such as stroke. Combined use produces enhanced therapeutic effect. Aspirin and clopidogrel both are esters, and hydrolysis leads to decreased or inactivated therapeutic activity. The aim of the study was to determine whether aspirin and clopidogrel are hydrolyzed by the same enzyme(s), thus reciprocally prolonging the antithrombogenic activity.

Author(s): 
Tang, Man
Mukundan, Madhu
Yang, Jian
Charpentier, Nathan
LeCluyse, Edward L.
Black, Chris
Yang, Dongfang
Shi, Deshi
Yan, Bingfang
Publication Title: 
The Journal of Pharmacology and Experimental Therapeutics

Oseltamivir is the main medicine recommended by the World Health Organization in anticipation of next influenza pandemic. This anti-influenza viral agent is an ester prodrug, and the antiviral activity is achieved by its hydrolytic metabolite: oseltamivir carboxylate. In this study, we report that the hydrolytic activation is catalyzed by carboxylesterase human carboxylesterase (HCE) 1. Liver microsomes rapidly hydrolyzed oseltamivir, but no hydrolysis was detected with intestinal microsomes or plasma.

Author(s): 
Shi, Deshi
Yang, Jian
Yang, Dongfang
LeCluyse, Edward L.
Black, Chris
You, Li
Akhlaghi, Fatemeh
Yan, Bingfang
Publication Title: 
Diabetes

OBJECTIVE: Human adenovirus type 36 (Ad-36) increases adiposity but improves insulin sensitivity in experimentally infected animals. We determined the ability of Ad-36 to increase glucose uptake by human primary skeletal muscle (HSKM) cells. RESEARCH DESIGN AND METHODS: The effect of Ad-36 on glucose uptake and cell signaling was determined in HSKM cells obtained from type 2 diabetic and healthy lean subjects. Ad-2, another human adenovirus, was used as a negative control. Gene expression and proteins of GLUT1 and GLUT4 were measured by real-time PCR and Western blotting.

Author(s): 
Wang, Zhong Q.
Cefalu, William T.
Zhang, Xian H.
Yu, Yongmei
Qin, Jianhua
Son, Leslie
Rogers, Pamela M.
Mashtalir, Nazar
Bordelon, Justin R.
Ye, Jianping
Dhurandhar, Nikhil V.
Publication Title: 
Bioorganic & Medicinal Chemistry

Silymarin, an extract of the seeds of milk thistle (Silybum marianum), is used as an herbal remedy, particularly for hepatoprotection. The main chemical constituents in silymarin are seven flavonolignans. Recent studies explored the non-selective methylation of one flavonolignan, silybin B, and then tested those analogues for cytotoxicity and inhibition of both cytochrome P450 (CYP) 2C9 activity in human liver microsomes and hepatitis C virus infection in a human hepatoma (Huh7.5.1) cell line. In general, enhanced bioactivity was observed with the analogues.

Author(s): 
Althagafy, Hanan S.
Graf, Tyler N.
Sy-Cordero, Arlene A.
Gufford, Brandon T.
Paine, Mary F.
Wagoner, Jessica
Polyak, Stephen J.
Croatt, Mitchell P.
Oberlies, Nicholas H.
Publication Title: 
Molecular Pharmacology

Germander, a plant used in folk medicine, caused an epidemic of cytolytic hepatitis in France. In about half of these patients, a rechallenge caused early recurrence, suggesting an immunoallergic type of hepatitis. Teucrin A (TA) was found responsible for the hepatotoxicity via metabolic activation by CYP3A. In this study, we describe the presence of anti-microsomal epoxide hydrolase (EH) autoantibodies in the sera of patients who drank germander teas for a long period of time.

Author(s): 
De Berardinis, V.
Moulis, C.
Maurice, M.
Beaune, P.
Pessayre, D.
Pompon, D.
Loeper, J.
Publication Title: 
Mutagenesis

Scientific information regarding plants used in folk medicine in the form of teas and their effect on human health or on genetic material has been the subject of many different types of investigation. The antimutagenic activity of two plants Maytenus ilicifolia and Peltastes peltatus, both rich in compounds of the flavonoid and tannin groups and frequently employed in folk medicine, was studied.

Author(s): 
Horn, Rubem Cesar
Vargas, Vera Maria Ferrão

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