вторник, 17 января 2012 г.

Games

Games


Slideshow 9.7.2 - Personalize your slide shows.. (Shareware)

Posted: 17 Jan 2012 03:48 AM PST



Slideshow is a very basic and easy-to-use slideshow and presentation tool for multimedia files, movies, sounds and images that allows you to quickly and easily create slideshow presentations and portfolios that can be distributed as freestanding programs for Mac and Windows or as movie files optimized for YouTube, CD-ROMs, the Web, iTunes, iPod, iOS (iPad, iPhone and iPhone 4) mobile devices and computers.

FAST TO LEARN AND EASY TO USE It is fast to learn and easy to use. Apimac Slideshow lets you personalize a presentation, adapting it to the most varied needs. You can create presentations and slideshows that can be manually or automatically controlled, you can personalize the presentation with colored backgrounds, use multiple soundtracks and show images and movies along with their names and custom text.

HANDLES A WIDE RANGE OF GRAPHIC AND MULTIMEDIA FORMATS Apimac Slideshow can handle a wide range of graphic and multimedia formats: QuickTime Movies, QuickTime VR Movies, MP3, MPEG, AutoDesk Animator (FLC), AIFF, AU, WAVE, DV, OpenDML audio files, and all the main graphic formats such as JPEG, TIFF, Pict, Photoshop, PNG, MacPaint, GIF, animated GIF, Windows Bitmap BMP and SGI.

MAKING SLIDESHOWS The program is the perfect tool to make your own slideshows of images and movies: just drag and drop files or folders on the main window and click Play or create a freestandig slideshow to distribuite to both Mac and Windows computers. What's more, the new release of this application sports the number one feature request from users: the ability to create movie files out of one slideshow presentation. Apimac Slideshow can create movie files optimized for: YouTube, Cellulars, Email, iPod, iPhone, iPad, iPod touch, the Web, CD-ROM, Apple TV and Computers.

MAKING PRESENTATIONS Creating slideshow presentations with Apimac Slideshow is easy: add photos and video, personalize the presentation environment with colored backgrounds and multiple soundtracks, then distribuite it or use it in your computer.

MAKING DIGITAL PORTFOLIOS Apimac Slideshow is the best tool for photographers, illustrators, architects to create digital portfolios of high-quality still images which can be destribuited on CD-ROMS and DVDs as Mac or Window free-standing application. During a presentation Apimac Slideshow is able to show the IPTC, EXIF, and ICC info tags along with the name of the file.

With Apimac Slideshow you can create slideshow presentations and portfolios that can be distributed as freestanding slideshow applications for either Mac or Windows. These stand-alone presentations are so easy to use that can be launched by just a simple double-click.

Apimac Slideshow is a must for anyone who wants to distribute presentations, portfolios or collections of movies and images on removable disks, CD-ROMs, DVDs or any other digital medium.

NOTES There are some Mac options not supported by Windows presentations: the MPEG-4 audio files are not supported (e.g. .m4a, .aac); the fade effect only works with accelerated graphic hardware and it fades the screen only about 50%.

INTERNET CONNECTION NOT REQUIRED The main features of the app does not require any Internet connection.

SUPPORT For any product information, please contact our support, we are happy to provide information about our software and technical assistance: www.apimac.com/support



Version 9.7.2:
  • Addressed all know bugs, Various code optimizations.


Mac OS X 10.5 or later

Download Now

Sensors, Vol. 12, Pages 1014-1034: Optimal Methods of RTK-GPS/Accelerometer Integration to Monitor the Displacement of Structures

Posted: 17 Jan 2012 12:00 AM PST

The accurate measurement of diverse displacements of structures is an important index for the evaluation of a structure's safety. In this study, a comparative analysis was conducted to determine the integrated RTK-GPS/accelerometer method that can provide the most precise structure displacement measurements. For this purpose, three methods of calculating the dynamic displacements from the acceleration data were comparatively analyzed. In addition, two methods of determining dynamic, static, and quasi-static displacements by integrating the displacements measured from the RTK-GPS system and the accelerometer were also comparatively analyzed. To ensure precise comparison results, a cantilever beam was manufactured onto which diverse types of displacements were generated to evaluate the measurement accuracy by method. Linear variable differential transformer (LVDT) measurements were used as references for the evaluation to ensure accuracy. The study results showed that the most suitable method of measuring the dynamic displacement with the accelerometer was to calculate the displacement by filtering and double-integrating the acceleration data using the FIR band-pass filter. The integration method that uses frequency-based displacement extraction was most appropriate for the integrated RTK-GPS/accelerometer method of comprehensively measuring the dynamic, static, and quasi-static displacements.

Sensors, Vol. 12, Pages 1002-1013: FBG Sensor for Contact Level Monitoring and Prediction of Perforation in Cardiac Ablation

Posted: 17 Jan 2012 12:00 AM PST

Atrial fibrillation (AF) is the most common type of arrhythmia, and is characterized by a disordered contractile activity of the atria (top chambers of the heart). A popular treatment for AF is radiofrequency (RF) ablation. In about 2.4% of cardiac RF ablation procedures, the catheter is accidently pushed through the heart wall due to the application of excessive force. Despite the various capabilities of currently available technology, there has yet to be any data establishing how cardiac perforation can be reliably predicted. Thus, two new FBG based sensor prototypes were developed to monitor contact levels and predict perforation. Two live sheep were utilized during the study. It was observed during operation that peaks appeared in rhythm with the heart rate whenever firm contact was made between the sensor and the endocardial wall. The magnitude of these peaks varied with pressure applied by the operator. Lastly, transmural perforation of the left atrial wall was characterized by a visible loading phase and a rapid signal drop-off correlating to perforation. A possible pre-perforation signal was observed for the epoxy-based sensor in the form of a slight signal reversal (12–26% of loading phase magnitude) prior to perforation (occurring over 8 s).

IJMS, Vol. 13, Pages 1006-1017: Photostability of Isovaline and its Precursor 5-Ethyl-5-methylhydantoin Exposed to Simulated Space Radiations

Posted: 17 Jan 2012 12:00 AM PST

Aqueous solutions of isovaline and its precursor molecule, 5-ethyl-5-methylhydantoin, were irradiated with ultraviolet and γ-ray photons, to evaluate their structural stability against space radiation. The degree of photolysis was measured and irradiation products were identified using chiral, reversed-phase and ion-exchange high-performance liquid chromatography. The experimental results show that the degree of photolysis of 5-ethyl-5-methylhydantoin is more significant than that of isovaline under ultraviolet light irradiation, while the results under γ-ray irradiation are the opposite. As the products of isovaline photolysis, aspartic acid, serine, glutamic acid and alanine were dominantly detected.

IJMS, Vol. 13, Pages 994-1005: Boesenbergia pandurata Attenuates Diet-Induced Obesity by Activating AMP-Activated Protein Kinase and Regulating Lipid Metabolism

Posted: 17 Jan 2012 12:00 AM PST

Obesity, a chronic metabolic disorder, is characterized by enlarged fat mass and dysregulation of lipid metabolism. The medicinal plant, Boesenbergia pandurata (Roxb.) Schltr., has been reported to possess anti-oxidative and anti-inflammatory properties; however, its anti-obesity activity is unexplored. The present study was conducted to determine whether B. pandurata extract (BPE), prepared from its rhizome parts, attenuated high-fat diet (HFD)-induced obesity in C57BL/6J mice. The molecular mechanism was investigated in 3T3-L1 adipocytes and HepG2 human hepatoma cells. BPE treatment decreased triglyceride accumulation in both 3T3-L1 adipocytes and HepG2 hepatocytes by activating AMP-activated protein kinase (AMPK) signaling and regulating the expression of lipid metabolism-related proteins. In the animal model, oral administration of BPE (200 mg/kg/day for 8 weeks) significantly reduced HFD-induced body weight gain without altering the amount of food intake. In addition, elevated serum levels of total cholesterol, low-density lipoprotein cholesterol, and triglycerides were suppressed by BPE administration. Fat pad masses were reduced in BPE-treated mice, as evidenced by reduced adipocyte size. Furthermore, BPE protected against the development of nonalcoholic fatty liver by decreasing hepatic triglyceride accumulation. BPE also activated AMPK signaling and altered the expression of lipid metabolism-related proteins in white adipose tissue and liver. Taken together, these findings indicate that BPE attenuates HFD-induced obesity by activating AMPK and regulating lipid metabolism, suggesting a potent anti-obesity agent.

IJMS, Vol. 13, Pages 977-993: Isoflurane Protects Against Human Endothelial Cell Apoptosis by Inducing Sphingosine Kinase-1 via ERK MAPK

Posted: 17 Jan 2012 12:00 AM PST

Endothelial dysfunction is a major clinical problem affecting virtually every patient requiring critical care. Volatile anesthetics are frequently used during the perioperative period and protect the heart and kidney against ischemia and reperfusion injury. We aimed to determine whether isoflurane, the most commonly used volatile anesthetic in the USA, protects against endothelial apoptosis and necrosis and the mechanisms involved in this protection. Human endothelial EA.hy926 cells were pretreated with isoflurane or carrier gas (95% room air + 5% CO2) then subjected to apoptosis with tumor necrosis factor-α or to necrosis with hydrogen peroxide. DNA laddering and in situ Terminal Deoxynucleotidyl Transferase Biotin-dUTP Nick-End Labeling (TUNEL) staining determined EA.hy926 cell apoptosis and percent LDH released determined necrosis. We also determined whether isoflurane modulates the expression and activity of sphingosine kinase-1 (SK1) and induces the phosphorylation of extracellular signal regulated kinase (ERK MAPK) as both enzymes are known to protect against cell death. Isoflurane pretreatment significantly decreased apoptosis in EA.hy926 cells as evidenced by reduced TUNEL staining and DNA laddering without affecting necrosis. Mechanistically, isoflurane induces the phosphorylation of ERK MAPK and increased SK1 expression and activity in EA.hy926 cells. Finally, selective blockade of SK1 (with SKI-II) or S1P1 receptor (with W146) abolished the anti-apoptotic effects of isoflurane. Taken together, we demonstrate that isoflurane, in addition to its potent analgesic and anesthetic properties, protects against endothelial apoptosis most likely via SK1 and ERK MAPK activation. Our findings have significant clinical implication for protection of endothelial cells during the perioperative period and patients requiring critical care.

IJMS, Vol. 13, Pages 961-976: Freshwater Plants Synthesize Sulfated Polysaccharides: Heterogalactans from Water Hyacinth (Eicchornia crassipes)

Posted: 17 Jan 2012 12:00 AM PST

Sulfated polysaccharides (SP) are found mainly in seaweeds and animals. To date, they have only been found in six plants and all inhabit saline environments. Furthermore, there are no reports of SP in freshwater or terrestrial plants. As such, this study investigated the presence of SP in freshwaters Eichhornia crassipes, Egeria densa, Egeria naja, Cabomba caroliniana, Hydrocotyle bonariensis and Nymphaea ampla. Chemical analysis identified sulfate in N. ampla, H. bonariensis and, more specifically, E. crassipes. In addition, chemical analysis, FT-IR spectroscopy, histological analysis, scanning electron microscopy (SEM) and energy-dispersive X-ray analysis (EDXA), as well as agarose gel electrophoresis detected SP in all parts of E. crassipes, primarily in the root (epidermis and vascular bundle). Galactose, glucose and arabinose are the main monosaccharides found in the sulfated polysaccharides from E. crassipes. In activated partial thromboplastin time (APTT) test, to evaluate the intrinsic coagulation pathway, SP from the root and rhizome prolonged the coagulation time to double the baseline value, with 0.1 mg/mL and 0.15 mg/mL, respectively. However, SP from the leaf and petiole showed no anticoagulant activity. Eichornia SP demonstrated promising anticoagulant potential and have been selected for further studies on bioguided fractionation; isolation and characterization of pure polysaccharides from this species. Additionally in vivo experiments are needed and are already underway.

IJMS, Vol. 13, Pages 943-960: Improvement of Thermal Stability via Outer-Loop Ion Pair Interaction of Mutated T1 Lipase from Geobacillus zalihae Strain T1

Posted: 17 Jan 2012 12:00 AM PST

Mutant D311E and K344R were constructed using site-directed mutagenesis to introduce an additional ion pair at the inter-loop and the intra-loop, respectively, to determine the effect of ion pairs on the stability of T1 lipase isolated from Geobacillus zalihae. A series of purification steps was applied, and the pure lipases of T1, D311E and K344R were obtained. The wild-type and mutant lipases were analyzed using circular dichroism. The Tm for T1 lipase, D311E lipase and K344R lipase were approximately 68.52 °C, 70.59 °C and 68.54 °C, respectively. Mutation at D311 increases the stability of T1 lipase and exhibited higher Tm as compared to the wild-type and K344R. Based on the above, D311E lipase was chosen for further study. D311E lipase was successfully crystallized using the sitting drop vapor diffusion method. The crystal was diffracted at 2.1 Å using an in-house X-ray beam and belonged to the monoclinic space group C2 with the unit cell parameters a = 117.32 Å, b = 81.16 Å and c = 100.14 Å. Structural analysis showed the existence of an additional ion pair around E311 in the structure of D311E. The additional ion pair in D311E may regulate the stability of this mutant lipase at high temperatures as predicted in silico and spectroscopically.

IJMS, Vol. 13, Pages 929-942: Effect of Enzymatic Treatment of Different Starch Sources on the in Vitro Rate and Extent of Starch Digestion

Posted: 17 Jan 2012 12:00 AM PST

Gelatinized wheat, potato and waxy maize starches were treated enzymatically in order to increase the degree of branching of the amylopectin fraction and thereby change the starch degradation profile towards a higher proportion of slowly digestible starch (SDS). The materials were characterized by single-pulse 1H HR-MAS NMR spectroscopy and in vitro digestion profile according to the Englyst procedure. Using various concentrations and incubation times with branching enzyme (EC 2.4.1.18) without or with additional treatment with the hydrolytic enzymes; β-amylase (EC 3.2.1.2), α-glucosidase (EC 3.2.1.20), or amyloglucosidase (EC 3.2.1.3) the proportion of α-(1-6) linkages was increased by up to a factor of 4.1, 5 and 5.8 in waxy maize, wheat and potato starches, respectively. The proportion of SDS was significantly increased when using hydrolytic enzymes after treatment with branching enzyme but it was only for waxy maize that the proportion of α-(1-6) bonds and the in vitro digestion profile was significantly correlated.

Polymers, Vol. 4, Pages 240-255: Conformational Effects in Non-Stoichiometric Complexes of Two Hyperbranched Molecules with a Linear Polyelectrolyte

Posted: 17 Jan 2012 12:00 AM PST

We report results from Brownian dynamics computer simulations of systems comprised by two terminally charged hyperbranched molecules preferentially branched in the periphery, with an oppositely charged linear chain of varying length. Comparison of the findings from the present study to stoichiometric counterparts and to analogous dendrimer-based complexes, reveal that the presence of the second hyperbranched molecule incurs significant changes in the conformational characteristics of both components of the complex. Instead of step-like changes in the average size and shape of the hyperbranched component that were noted in the previously studied stoichiometric systems, a rather smooth change is observed upon increase of the length of the linear component. In addition, a markedly different behavior is also noticed in the conformational characteristics of the linear chain when compared to that in similar dendrimer-based systems. The above findings are consistent with the higher degree of deformability of the peripherally branched molecules which allow appropriate rearrangements in shape in order to accommodate the favorable Coulombic interactions between the two components of the complex. This behavior offers new insight towards the design of more efficient hyperbranched-based systems which can take advantage of the multifunctionality and the structural properties of the highly branched polymer components.

Martian Chronicles, part two

Posted: 17 Jan 2012 02:13 AM PST

The StarShipSofa podcast has the second installment of Jeff Lane's reading of my YA novella The Martian Chronicles (here's part one). Lane does a great job with the reading. MP3 link.

This posting includes an audio/video/photo media file: Download Now

NetStatsBaseball 0.9.9 (updated)

Posted: 17 Jan 2012 01:35 AM PST

Polymers, Vol. 4, Pages 211-239: Internal Dynamics of Dendritic Molecules Probed by Pyrene Excimer Formation

Posted: 17 Jan 2012 12:00 AM PST

This review exposes the current poor understanding of the internal segmental chain dynamics of dendrimers in solution probed by monitoring the process of excimer formation between pyrene labels covalently attached to the chain ends of dendrimers. The review begins by covering the bases of fluorescence and the kinetics of pyrene excimer formation before describing a procedure based on the Model Free (MF) analysis that is used to analyze quantitatively the fluorescence decays acquired for dendrimers, the ends of which have been fully and covalently labeled with pyrene. Comparison of the various trends obtained by different research groups describing the efficiency of pyrene excimer formation with the generation number of dendrimers illustrates the lack of consensus between the few studies devoted to the topic. One possible reason for this disagreement might reside in the presence of minute amounts of unattached pyrene labels which act as potent fluorescent impurities and affect the analysis of the fluorescence spectra and decays in an uncontrolled manner. The review points out that the MF analysis of the fluorescence decays acquired with pyrene-labeled dendrimers enables one to account for the presence of unattached pyrene and to retrieve information about the internal segmental dynamics of the dendrimer. It provides guidelines that should enable future studies on pyrene-labeled dendrimers to yield results that are more straightforward to interpret.

Molecules, Vol. 17, Pages 884-896: Design, Synthesis and Antifibrotic Activities of Carbohydrate- Modified 1-(Substituted aryl)-5-trifluoromethyl-2(1H) Pyridones

Posted: 17 Jan 2012 12:00 AM PST

Pirfenidone, a pyridone compound, is an effective and novel antifibrotic agent. In this article, we describe the design, synthesis and activity evaluation of novel antifibrotic agents, 1-(substituted aryl)-5-trifluoromethyl-2(1H) pyridones modified with carbohydrate. Most of the title compounds exhibited comparable or better inhibitory activity than fluorofenidone. Notably, compound 19a demonstrated the highest cell-based inhibitory activity against NIH 3T3 (IC50 = 0.17 mM).

Molecules, Vol. 17, Pages 873-883: Novel Benzothiazole, Benzimidazole and Benzoxazole Derivatives as Potential Antitumor Agents: Synthesis and Preliminary in Vitro Biological Evaluation

Posted: 17 Jan 2012 12:00 AM PST

In a previous hit-to-lead research program targeting anticancer agents, two promising lead compounds, 1a and 1b, were found. However, the poor solubility of 1a and 1b made difficult further in vivo studies. To solve this problem, a lead optimization was conducted through introducing N-methyl-piperazine groups at the 2-position and 6-position. To our delight, the optimized analogue 1d showed comparable antiproliferative activity in vitro with better solubility, compared with 1a. Based on this result, the replacement of the benzothiazole scaffold with benzimidazole and benzoxazole moieties afforded 1f and 1g, whose activities were fundamentally retained. In the preliminary in vitro biological evaluation, the immunofluorescence staining of HCT116 cells indicated that 1d, 1f and 1g led to cytosolic vacuolization which was not induced by 1a at low micromolecular concentrations. These results suggest that these optimized compounds might potentially constitute a novel class of anticancer agents, which merit further studies.

Molecules, Vol. 17, Pages 861-872: Phytochemical Study and Anti-inflammatory, Antidiabetic and Free Radical Scavenger Evaluations of Krameria pauciflora Methanol Extract

Posted: 17 Jan 2012 12:00 AM PST

The plant Krameria pauciflora MOC et. Sessé ex DC. is used as an anti-inflammatory and antidiabetic in traditional medicine. The aim of this study was to evaluate the in vivo anti-inflammatory and antidiabetic effects of a methanol extract from the roots of K. pauciflora. Dichloromethane and ethyl acetate extracts obtained by partitioning the methanol extract were also evaluated. Complete methanol and dichloromethane extracts showed anti-inflammatory effects at 3 mg/kg. An anti-inflammatory effect similar to indomethacin (10 mg/kg) was observed when the methanol and dichloromethane extracts, which contain a cycloartane-type triterpene and an sterol, were administered orally at several doses (3, 10, 30 and 100 mg/kg), whereas no anti-inflammatory effect was observed at any dose for the ethyl acetate extract, which contains catechin-type flavonoids. The antidiabetic effect of each extract was also determined. An antihyperglycaemic effect was observed in diabetic rats, but no effect in normoglycaemic animals was observed when the methanol extract was administrated at 30 mg/kg. All of the extracts exhibited radical scavenger activity. Additionally, constituents from all of the extracts were identified by NMR. This article supports the use of K. pauciflora as an anti-inflammatory because it exhibits a similar effect to indomethacin. However, its antidiabetic effect is not completely clear, although it could be useful for preventing diabetic complications.

Default Folder X 4.4.8 - Enhances Open and Save dialogs.. (Shareware)

Posted: 16 Jan 2012 08:59 PM PST



Default Folder X attaches a toolbar to the right side of the Open and Save dialogs in any Mac OS X-native application. The toolbar gives you fast access to various folders and commands. You just click on the buttons to go to your favorite and recently used folders, manage the folders and files shown in the list, and make changes to your settings.

Default Folder also fixes a number of problems in Open and Save dialogs, "rebounding" back to the last selected file, putting the path listing back in the top menu, and correcting bugs in scrolling column views.

Check out the screencast by clicking here!

Features:

  • Directory assistant: You can access the contents of your recent, favorite, and open folders right from Default Folder X's toolbar. Its hierarchical pop-up menus expand as you mouse over them, letting you navigate your folders to get to your files. To work faster, you can assign a keyboard shortcut for all of your favorite folders. If an Open and Save dialog isn't open, then you can use Default Folder X's menu bar, Dock icon, or keyboard shortcuts.
  • Real time saving: If you're constantly saving things inside the same folder, Default Folder X can remember that folder for you. You can even set a different default folder for each application you use. That way, you'll already be in the right folder when you're working.
  • Finder management: Have you ever wanted to save a file to an open Finder window? Default Folder X lets you open up or save to any Finder window with a single click. It also lets you get info on, rename, and delete existing files, putting the Finder's power in every Open and Save dialog.
  • Instant Recall: To help you quickly return to folders you've recently used, Default Folder X remembers them for you. It can even rebound to the last file you used in all your recent folders. With Default Folder X, you'll never forget where you put something.
  • Spotlight on the spot: Mac OS X delivers amazing search capabilities with Spotlight, but adding your own search keywords requires a trip to the Finder's Get Info window or to an application like Tags, Fresh, or Tag Folders. No more! Default Folder X lets you add Spotlight keywords, OpenMeta tags, and Finder labels on the spot, while you're still in the Save dialog. It even remembers keywords you've used before and automatically completes them as you type.
  • Information central: Leopard delivers amazing previews with QuickLook, but in Open dialogs they're small and you can only see them in column view. With Default Folder X you get previews below every Open dialog, expanded to fill the available space. Need to see more detail? Click on the image and it zooms up to full size. And if you'd rather have words instead of pictures, Default Folder X delivers those details too. The file's size, the date you created and modified it, the Finder label, Spotlight comments, OpenMeta tags, access permissions - they're all there too.
  • Workflow without work: Rather than make you learn and set up a new application, Default Folder X blends into Mac OS X. Its pop-up menus and Finder integration will start saving you time immediately, and it will put your pre-existing Favorite folders in its toolbar right away. When you do decide to start customizing it, Default Folder X lets you set default folders and assign shortcuts right from its toolbar. Finally, effortless workflow.


Version 4.4.8:
  • Default Folder X's contextual menus are once again available in all Open and Save dialogs. Right-click or Control-click on any file in a file dialog to rename, delete, get info, or zip it.
  • Updated to work with all Open and Save dialogs in the latest version of Google Chrome.
  • Fixed a bug that caused file dialogs to hang when you used OS X's New Folder dialog.
  • Worked around a bug in OS X that could result in Default Folder X going to the wrong folder when the original was not available.
  • Corrected a bug that would cause the path popup menu in some Open dialogs to overlap the Spotlight search field.
  • Fixed a problem that prevented Default Folder X from opening its preferences on some machines.
  • Added support for DesktopShelves and QuickTime Player X.
  • Added IgnoreTheseFolders.plist inside Default Folder X to allow additional folders to be ignored when Default Folder X builds its recent folder list. Any folder that matches or is nested within the folders listed in the plist file will not be included in your Recent Folders menu. To add more folders, modify the file that's located here:
    ~/Library/PreferencePanes/Default Folder X.prefPane/Contents/Resources/Default Folder X.bundle/Contents/Resources/IgnoreTheseFolders.plist


Mac OS X 10.5 or later

Download Now

This posting includes an audio/video/photo media file: Download Now

Molecules, Vol. 17, Pages 851-860: Effect of Efavirenz on UDP-Glucuronosyltransferase 1A1, 1A4, 1A6, and 1A9 Activities in Human Liver Microsomes

Posted: 17 Jan 2012 12:00 AM PST

Efavirenz is a non-nucleoside reverse transcriptase inhibitor used for the treatment of human immunodeficiency virus type 1 infections. Drug interactions of efavirenz have been reported due to in vitro inhibition of CYP2C9, CYP2C19, CYP3A4, and UDP-glucuronosyltransferase 2B7 (UGT2B7) and in vivo CYP3A4 induction. The inhibitory potentials of efavirenz on the enzyme activities of four major UDP-glucuronosyltransferases (UGTs), 1A1, 1A4, 1A6, and 1A9, in human liver microsomes were investigated using liquid chromatography-tandem mass spectrometry. Efavirenz potently inhibited UGT1A4-mediated trifluoperazine N-glucuronidation and UGT1A9-mediated propofol glucuronidation, with Ki values of 2.0 and 9.4 μM, respectively. [I]/Ki ratios of efavirenz for trifluoperazine N-glucuronidation and propofol glucuronidation were 6.5 and 1.37, respectively. Efavirenz also moderately inhibited UGT1A1-mediated 17β-estradiol 3-glucuronidation, with a Ki value of 40.3 μM, but did not inhibit UGT1A6-mediated 1-naphthol glucuronidation. Those in vitro results suggest that efavirenz should be examined for potential pharmacokinetic drug interactions in vivo due to strong inhibition of UGT1A4 and UGT1A9.

Molecules, Vol. 17, Pages 843-850: Two Novel Naphthalene Glucosides and an Anthraquinone Isolated from Rumex dentatus and Their Antiproliferation Activities in Four Cell Lines

Posted: 17 Jan 2012 12:00 AM PST

An ethyl acetate extract of the roots of Rumex dentatus L. was investigated. Three compounds were identified by their spectroscopic data as chrysophanol (1), 6-methyl-7-acetyl-1, 8-dihydroxy-3-methoxy naphthalene-1-O-β-D(L)-glucoside (2) and 6-methyl-7-acetyl-1, 8-dihydroxy naphthalene-1-O-β-D(L)-glucoside (3) were found in the plant for the first time. Compounds 2 and 3 are novel compounds. Their antiproliferation activities were tested by the MTT assay in four cell lines (breast cancer MCF-7, gastric cancer 7901, melanoma A375 and oophoroma SKOV-3).

Awesome Tanks

Posted: 16 Jan 2012 11:56 PM PST

Lead your tank and cause as much mayhem and destruction as possible! Don't forget Upgrading your tank for improved abilities.

Комментариев нет:

Отправить комментарий