Tocotrienols inhibit human glutathione S-transferase P1-1

Tocotrienols inhibit human glutathione S-transferase P1-1. van Haaften RI, Haenen GR, Evelo CT, Bast A. Department of Pharmacology and Toxicology, Faculty of Medicine, Universiteit Maastricht, The Netherlands. [email protected] Tocopherols and tocotrienols are food ingredients that are believed to have a positive effect on health. The most studied property of both groups of compounds is their antioxidant action. Previously, we found that tocopherols and diverse tocopherol derivatives can inhibit the activity of human glutathione S-transferase P1-1 (GST P1-1). In this study we found that GST P1-1 is also inhibited, in a concentration-dependent manner, by alpha- and gamma-tocotrienol. The concentration giving 50% inhibition of GST P1-1 is 1.8 +/- 0.1 microM for alpha-tocotrienol and 0.7 +/- 0.1 microM for gamma-tocotrienol. This inhibition of GST P1-1 is noncompetitive with respect to both substrates CDNB and GSH. We also examined the 3D structure of GST P1-1 for a possible tocopherol/tocotrienol binding site. The enzyme contains a very hydrophobic pit-like structure where the phytyl tail of tocopherols and tocotrienols could fit in. Binding of tocopherol and tocotrienol to this hydrophobic region might lead to bending of the 3D structure. In this way tocopherols and tocotrienols can inhibit the activity of the enzyme; this inhibition can have far-reaching implications for human

Biotransformation pathway maps in WikiPathways enable direct visualization of drug metabolism related expression changes.

In recent decades, our knowledge of the genetics and functional genomics of drug-metabolizing enzymes has increased and a wealth of data on drug-related 'omics' has become available. Despite the availability of large amounts of biological information on xenobiotic biotransformation, the number of available biotransformation pathway maps that can easily be used for visualization of multiple omics data is limited. Here, we created integrated biotransformation pathway maps suitable for multiple omics analysis using PathVisio. The ease of visualizing data on these maps was demonstrated by using published microarray data from human hepatocyte-like cell models, exemplifying - where a sufficient capacity for metabolizing chemicals is a prerequisite for a suited model - how the biotransformation pathway maps can be used for model selection

From nanotechnology to nanomedicine: applications to cancer research

Scientific advances have significantly improved the practice of medicine by providing objective and quantitative means for exploring the human body and disease states. These innovative technologies have already profoundly improved disease detection, imaging, treatment and patient follow-up. Today's analytical limits are at the nanoscale level (one-billionth of a meter) enabling a detailed exploration at the level of DNA, RNA, proteins and metabolites which are in fact nano-objects. This translational review aims at integrating some recent advances from micro- and nano-technologies with high potential for improving daily oncology practice

Языковое своеобразие стихотворения Зульфии "Пришла весна, спрашивает о тебе"

В жизни и творчестве узбекской поэтессы Зульфии Исраиловой особую роль играет весна. Она родилась в первый день весны. Каждую весну с момента гибели спутника жизни поэта Хамида Олимджана, любившего эту пору, Зульфия посвящала ему стихотворение. Всего их пятьдесят. При цитировании документа, используйте ссылку http://essuir.sumdu.edu.ua/handle/123456789/3470