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Ginsenoside Compound K (GCK) is the main metabolite of natural protopanaxadiol ginsenosides with diverse pharmacological effects. Gut microbiota contributes to the biotransformation of GCK, while the effect of gut microbiota on the pharmacokinetics of GCK in vivo remains unclear. To illustrate the role of gut microbiota in GCK metabolism in vivo, a systematic investigation of the pharmacokinetics of GCK in specific pathogen free (SPF) and pseudo-germ-free (pseudo-GF) rats were conducted. Pseudo-GF rats were treated with non-absorbable antibiotics. Liquid chromatography tandem mass spectrometry (LC–MS/MS) was validated for the quantification of GCK in rat plasma. Compared with SPF rats, the plasma concentration of GCK significantly increased after the gut microbiota depleted. The results showed that GCK absorption slowed down, Tmax delayed by 3.5 h, AUC0-11 increased by 1.3 times, CLz/F decreased by 0.6 times in pseudo-GF rats, and Cmax was 1.6 times higher than that of normal rats. The data indicated that gut microbiota played an important role in the pharmacokinetics of GCK in vivo. [ABSTRACT FROM AUTHOR]

Objective: Pleural effusion is common problem, but the rapid and reliable diagnosis for specific pathogenic effusions are lacking. This study aimed to identify the diagnosis based on clinical variables to differentiate pleural tuberculous exudates from other pleural effusions. We also investigated the role of renin-angiotensin system (RAS) and matrix metalloproteinase (MMPs) in the pathogenesis of pleural exudates.Experimental design: The major components in RAS and extracellular matrix metabolism, including angiotensin converting enzyme (ACE), ACE2, MMP-2 and MMP-9 activities, were measured and compared in the patients with transudative (n = 45) and exudative (n = 80) effusions. The exudative effusions were come from the patients with tuberculosis (n = 20), pneumonia (n = 32), and adenocarcinoma (n = 28).Results: Increased ACE and equivalent ACE2 activities, resulting in a significantly increased ACE/ACE2 ratio in exudates, were detected compared to these values in transudates. MMP-9 activity in exudates was significantly higher than that in transudates. The significant correlation between ACE and ACE2 activity that was found in transudates was not found in exudates. Advanced analyses showed significantly increased ACE and MMP-9 activities, and decreased ACE2 activity in tuberculous pleural effusions compared with those in pneumonia and adenocarcinoma effusions. The results indicate that increased ACE and MMP-9 activities found in the exudates were mainly contributed from a higher level of both enzyme activities in the tuberculous pleural effusions.Conclusion: Interplay between ACE and ACE2, essential functions in the RAS, and abnormal regulation of MMP-9 probably play a pivotal role in the development of exudative effusions. Moreover, the ACE/ACE2 ratio combined with MMP-9 activity in pleural fluid may be potential biomarkers for diagnosing tuberculous pleurisy.

Rare circulating tumor cells (CTCs) are always harvested with large numbers of white blood cells (WBCs) by current CTC isolation techniques, which influences the accuracy of CTC‐related gene and protein analysis. Therefore, it is very urgent to develop a method for efficient isolation of CTCs with high purity. In this work, we fabricated a reversibly assembled interface by layer‐by‐layer assembly of biotinylated poly‐(L‐lysine‐graft‐ethylene glycol) (PLL‐g‐PEG‐biotin), streptavidin, and CTC‐specific antibody on a three‐dimensional conductive scaffold, and further embedded it into a customized microchip for CTC capture. The assembled multilayers increased the roughness of the scaffold, which improved the capture efficiency. Importantly, the PLL‐g‐PEG‐biotin covalently coupled with CTCs could be detached from the scaffold by electrostatic repulsion, and the released CTCs could be recaptured on the conductive scaffold via electrostatic attraction while the WBCs were continuously drifted away. This reversible capture and release strategy significantly improved the purity of CTCs, and pure CTCs were obtained from cancer patients' blood samples for gene mutation assay, which will be of great significance for assisting cancer diagnosis and treatment in a noninvasive way. [ABSTRACT FROM AUTHOR]

The syntheses of several new 7-azaindolyl-, indolyl-, and 3-methylindolyl-functionalized starburst molecules that contain either a 1,3,5-triazine, a benzene, a 2,4,6-triphenyl-2,4,6-triazine, a 1,3,5-triphenylbenzene, a 2,4,6-tris(biphenyl)-1,3,5-triazine, or a 1,3,5-tris(biphenyl)benzene core have been achieved. The synthetic methods used for these new compounds involve mostly Ullmann condensation and Suzuki coupling reactions. The thermal properties of the new molecules have been found to be highly dependent on the molecular weight and the central core. Glass transition temperatures greater than 150 °C were observed for the large starburst molecules based on the 2,4,6-tris(biphenyl)-1,3,5-triazine or the 1,3,5-tris(biphenyl)benzene core. The new starburst molecules are luminescent in the violet-blue region in solution and in the solid state. The emission energy and the quantum efficiency were found to be highly dependent on the central core and the functional group. In general, the triazine-based molecules were found to have a smaller HOMO-LUMO energy gap than the benzene-based analogues. The triphenyltriazine- or triphenylbenzene-based molecules were found to display a higher emission quantum efficiency than the large tris(biphenyl)triazine- or tris(biphenyl)benzene-based molecules. Key words: 7-azaindolyl, indolyl derivative, triazine and benzene cores, starburst molecule, blue luminescence. On a realise la synthese de plusieurs nouvelles molecules a base d'indolyle, de 3-methylindolye et de 7-azaindolyle fonctionnalises qui donnent l'impression d'une explosion d'etoiles et qui contiennent comme partie centrale une 1,3,5-triazine, un benzene, un 2,4,6-triphenyl-2,4,6-triazine, un 1,3,5-triphenylbenzene, un 2,4,6-tris(biphenyl)-1,3,5-triazine ou un 1,3,5-tris(biphenyl)benzene. Les methodes de synthese utilisees pour ces nouveaux produits impliquent principalement des reactions de condensation de Ullmann et de couplage de Suzuki. On a trouve que les proprietes des nouvelles molecules dependent fortement du poids moleculaire et de la nature de la partie centrale. On a observe des temperatures de transition de verre superieures a 150 °C pour les grosses molecules qui donnent l'impression d'une explosion d'etoiles a base d'une partie centrale de 2,4,6-tris(biphenyl)-1,3,5-triazine ou de 1,3,5-tris(biphenyl)benzene. Tant en solution qu'a l'etat solide, les nouvelles molecules qui donnent l'impression d'une explosion d'etoiles sont luminescentes dans la region du violet-bleu. On a trouve que l'energie d'emission et l'efficacite quantique dependent fortement de la nature de la partie centrale et du groupe fonctionnel. On a trouve que, en general, l'ecart entre les energies des orbitales moleculaires hautes occupees (HO) et basses vacantes (BV) des molecules a base de triazine sont plus faibles que celles de leurs analogues a base de benzene. On a observe que les efficacites quantiques d'emission des molecules a base de triphenyltriazine ou de triphenylbenzene sont plus grandes que celles des molecules a base de tris(biphenyl)triazine ou de tris(biphenyl)benzene. Mots cles : 7-azaindolyle, derive de l'indolyle, partie centrale a base de triazine et de benzene, molecule qui donne l'impression d'une explosion d'etoiles, luminescence bleue. [Traduit par la Redaction], Introduction Starburst or star-shaped molecules have been shown to have the tendency to form amorphous films with a relatively high [T.sub.g], a property that is highly desired for applications of [...]