Lipase‐Catalyzed Kinetic Resolution of Novel Antifungal N‐Substituted Benzimidazole Derivatives

A series of new N‐substituted benzimidazole derivatives was synthesized and their antifungal activity against Candida albicans was evaluated. The chemical step included synthesis of appropriate ketones containing benzimidazole ring, reduction of ketones to the racemic alcohols, and acetylation of alcohols to the esters. All benzimidazole derivatives were obtained with satisfactory yields and in relatively short times. All synthesized compounds exhibit significant antifungal activity against Candida albicans 900028 ATCC (% cell inhibition at 0.25 μg concentration > 98%). Additionally, racemic mixtures of alcohols were separated by lipase‐catalyzed kinetic resolution. In the enzymatic step a transesterification reaction was applied and the influence of a lipase type and solvent on the enantioselectivity of the reaction was studied. The most selective enzymes were Novozyme SP 435 and lipase Amano AK from Pseudomonas fluorescens (E > 100). Chirality 28:347–354, 2016. © 2016 Wiley Periodicals, Inc.     

Macular retinal thickness and flow density change by optical coherence tomography angiography after posterior scleral reinforcement

Optical coherence tomography angiography(Angio-OCT) has introduced a new non-invasive, quantitative method to assess superficial and deep capillary networks of the retina. In this study, we investigated macular retinal thickness and flow density change following posterior scleral reinforcement(PSR) surgery, using an RTVue XR Avanti Angio-OCT, in patients with pathological myopia. A total of 13 patients with pathological myopia were recruited and all patients completed the 6 months follow-up visit. Data from 22 eyes were used in this study. The mean age was 36.23±15.29 years, and 43%(n=6) were men.Spherical equivalent refractive error(SE) ranged from –8.0 to –24.0 D. Postoperative axial length, best-corrected visual acuity and SE did not change significantly at each follow-up, compared with pre-operative measures(P0.05). Postoperative flow density of superficial and deep retinal layers at each sector did not change significantly at each follow-up, compared with preoperative measures(P0.05). However, we found significant decrease in retinal thickness of parafovea-inferior sector after PSR surgery(P0.01), indicating potential relaxation of vitreofoveal traction after PSR surgery.     

Absence of estrogen receptor beta leads to abnormal adipogenesis during early tendon healing by an up‐regulation of PPARγ signalling

Achilles tendon injury is one of the challenges of sports medicine, the aetiology of which remains unknown. For a long time, estrogen receptor β (ERβ) has been known as a regulating factor of the metabolism in many connective tissues, such as bone, muscle and cartilage, but little is known about its role in tendon. Recent studies have implicated ERβ as involved in the process of tendon healing. Tendon‐derived stem cells (TDSCs) are getting more and more attention in tendon physiological and pathological process. In this study, we investigated how ERβ played a role in Achilles tendon healing. Achilles tendon injury model was established to analyse how ERβ affected on healing process in vivo. Cell proliferation assay, Western blots, qRT‐PCR and immunocytochemistry were performed to investigate the effect of ERβ on TDSCs. Here, we showed that ERβ deletion in mice resulted in inferior gross appearance, histological scores and, most importantly, increased accumulation of adipocytes during the early tendon healing which involved activation of peroxisome proliferator‐activated receptor γ (PPARγ) signalling. Furthermore, in vitro results of ours confirmed that the abnormity might be the result of abnormal TDSC adipogenic differentiation which could be partially reversed by the treatment of ERβ agonist LY3201. These data revealed a role of ERβ in Achilles tendon healing for the first time, thereby providing a new target for clinical treatment of Achilles tendon injury.     

The Accumulation of Risk and Essential Elements in Edible Mushrooms Chlorophyllum rhacodes,Suillus grevillei,Imleria badia,and Xerocomellus chrysenteron Growing in the Czech Republic

Risk and essential elements were determined in fruiting bodies of wild growing edible mushrooms Chlorophyllum rhacodes, Suillus grevillei, Imleria badia, and Xerocomellus chrysenteron collected in an unpolluted site in South Bohemia, the Czech Republic. The elements were also determined in underlying soils and the bioconcentration factors were calculated. The analyses revealed that C. rhacodes accumulated Ag, Cu, Rb, Se, Zn, As, Cd, and Tl. On the other hand, S. grevillei accumulated Cd, Rb, Ag, Se, and Cs. I. badia and X. chrysenteron strongly accumulated Rb, Cs, and Ag; these species showed the ability to accumulate Cu and Zn as well. Contents of detrimental Cr^VI were in all cases below the quantification limit (0.003 mg kg^?1 dry matter). Studied mushroom species (mainly C. rhacodes) accumulated some toxic elements. However, no considerable effect on human health is expected since they are usually consumed as a delicacy and do not represent a major component of diet.     

The P2-receptor-mediated Ca2+ signalosome of the human pulmonary endothelium - implications for pulmonary arterial hypertension

Purinergic Signalling - Dysfunction of the pulmonary endothelium is associated with most lung diseases. Extracellular nucleotides modulate a plethora of endothelial functions in the lung such as...     

Proteomic Profiling of Mouse Helper T Cell Differentiation

Helper T cell differentiation is a key process in the regulation of adaptive immune responses. Here, mouse Th1 and Th2 cells are profiled using high‐throughput proteomics to increase the understanding of the molecular biology of Th differentiation to support the design of prophylactic and therapeutic intervention strategies for (infectious) diseases. Protein profiling of Th1/Th2 differentiated cells results in the quantification of almost 6000 proteins of which 41 are differentially expressed at FDR < 0.1, and 19 at the FDR < 0.05 level, respectively. Differential protein expression analysis identifies a number of the expected canonical Th differentiation markers, and gene set analysis using the REACTOME database and a hypergeometric test (FDR < 0.05) confirms that helper T cell pathways are the top sets that are differentially expressed. Additionally, by network analysis, many differentially expressed proteins are associated with the Th1 and Th2 pathways. Data are available via PRIDE database with identifier PXD004532.