Host-guest complexes of local anesthetics with cucurbit[6]uril and para-sulphonatocalix[8]arene in the solid state

© 2017 Elsevier B.V. Here we describe the host-guest inclusion complexes of local anesthetic drugs with two macrocyclic hosts cucurbit[6]uril and para-sulphonatocalix[8] arene in the solid state. The anesthetic agents used in the co-crystallization with the supramolecular hosts are lidocaine, procaine, procainamide, prilocaine and proparacaine. Both macrocycles encapsulate the alkylammonium moieties of anestetics guests into their cavities although the mechanism of complexation, host-guest stoichiometry and geometry differ depending on the nature of the supramolecular host

The solid-state structures of organic salts formed by calix[4]arene dihydroxyphosphonic acid with nucleic bases cations: adeninium, cytosinium, guaninium and uracilium

© 2018 Informa UK Limited, trading as Taylor & Francis Group. Calix[4]arene dihydroxyphosphonic acid has been demonstrated to possess an interesting range of biological properties, including atypical anti-cancer activity. The robustness of calix[4]arene dihydroxyphosphonic acid and its ubiquitous dimeric motif offers perspectives for pre-defined solid state complexation with small molecules. In the current article we describe co-crystals (organic salts) of calix[4]arene dihydroxyphosphonic acid with four nucleic base cations: adeninium, cytosinium, guaninium and uracilium. A number of characteristic interactions between the components in the four co-crystals are pointed out also using the Hirshfeld surface analysis. All the four co-crystals are based on layers of calix[4]arene dimers, alternating with layers of nucleic acid molecules. Two of the reported crystal structures (cytosinium and guaninium) are 1D channel-type structures, while the two others (adeninium and uracilium) represent 2D channel-type structures. In three out of four reported structures, interactions between the cations of nucleic bases are present generating 1D chains of cations. A constant motif is that the nucleic base is present in a type of cavity formed by one aromatic ring and a phosphonic acid moiety

Brg1 Is Required for Cdx2-Mediated Repression of Oct4 Expression in Mouse Blastocysts

During blastocyst formation the segregation of the inner cell mass (ICM) and trophectoderm is governed by the mutually antagonistic effects of the transcription factors Oct4 and Cdx2. Evidence indicates that suppression of Oct4 expression in the trophectoderm is mediated by Cdx2. Nonetheless, the underlying epigenetic modifiers required for Cdx2-dependent repression of Oct4 are largely unknown. Here we show that the chromatin remodeling protein Brg1 is required for Cdx2-mediated repression of Oct4 expression in mouse blastocysts. By employing a combination of RNA interference (RNAi) and gene expression analysis we found that both Brg1 Knockdown (KD) and Cdx2 KD blastocysts exhibit widespread expression of Oct4 in the trophectoderm. Interestingly, in Brg1 KD blastocysts and Cdx2 KD blastocysts, the expression of Cdx2 and Brg1 is unchanged, respectively. To address whether Brg1 cooperates with Cdx2 to repress Oct4 transcription in the developing trophectoderm, we utilized preimplantation embryos, trophoblast stem (TS) cells and Cdx2-inducible embryonic stem (ES) cells as model systems. We found that: (1) combined knockdown (KD) of Brg1 and Cdx2 levels in blastocysts resulted in increased levels of Oct4 transcripts compared to KD of Brg1 or Cdx2 alone, (2) endogenous Brg1 co-immunoprecipitated with Cdx2 in TS cell extracts, (3) in blastocysts Brg1 and Cdx2 co-localize in trophectoderm nuclei and (4) in Cdx2-induced ES cells Brg1 and Cdx2 are recruited to the Oct4 promoter. Lastly, to determine how Brg1 may induce epigenetic silencing of the Oct4 gene, we evaluated CpG methylation at the Oct4 promoter in the trophectoderm of Brg1 KD blastocysts. This analysis revealed that Brg1-dependent repression of Oct4 expression is independent of DNA methylation at the blastocyst stage. In toto, these results demonstrate that Brg1 cooperates with Cdx2 to repress Oct4 expression in the developing trophectoderm to ensure normal development

Generation of Induced Pluripotent Stem Cells from the Prairie Vole

The vast majority of animals mate more or less promiscuously. A few mammals, including humans, utilize more restrained mating strategies that entail a longer term affiliation with a single mating partner. Such pair bonding mating strategies have been resistant to genetic analysis because of a lack of suitable model organisms. Prairie voles are small mouse-like rodents that form enduring pair bonds in the wild as well as in the laboratory, and consequently they have been used widely to study social bonding behavior. The lack of targeted genetic approaches in this species however has restricted the study of the molecular and neural circuit basis of pair bonds. As a first step in rendering the prairie vole amenable to reverse genetics, we have generated induced pluripotent stem cell (IPSC) lines from prairie vole fibroblasts using retroviral transduction of reprogramming factors. These IPSC lines display the cellular and molecular hallmarks of IPSC cells from other organisms, including mice and humans. Moreover, the prairie vole IPSC lines have pluripotent differentiation potential since they can give rise to all three germ layers in tissue culture and in vivo. These IPSC lines can now be used to develop conditions that facilitate homologous recombination and eventually the generation of prairie voles bearing targeted genetic modifications to study the molecular and neural basis of pair bond formation

Influence of type and content of fat on acoustic properties of shortbread

Celem pracy było badanie wpływu rodzaju i udziału tłuszczu w recepturze ciastek kruchych na ich właściwości akustyczne. Stosowano margarynę (80,0% tł.) i masło śmietankowe (82,0% tł.), o udziale w recepturze od 19,2 do 82,0% w stosunku do mąki. Przeprowadzono pomiary zawartości i aktywności wody ciastek oraz ich ocenę sensoryczną, metodą punktową. Rejestrację emisji akustycznej (EA) generowanej podczas testu trójpunktowego łamania materiału z prędkością 20 mm·min-1, wykonano techniką kontaktową. Dźwięk analizowano w zakresie częstotliwości od 1 do 18 kHz. Analizowano deskryptory emisji akustycznej (liczbę zdarzeń EA, energię akustyczną, energię zdarzenia EA, maksymalną energię zdarzenia EA, czas trwania dźwięku, amplitudę, współczynnik nachylenia charakterystyki widmowej) oraz parametry sensoryczne (głośność, twardość, jakość ogólną, smak). Wykonano analizę statystyczną uzyskanych wyników metodą składowych głównych (PCA). Rodzaj i udział tłuszczu w recepturze ciastek wpływały na ich właściwości akustyczne. Ciastka z margaryną generowały dźwięki o wyższej energii w paśmie częstotliwości niskich 1-3 kHz i wysokich 13-14 kHz, niż ciastka z masłem śmietankowym, które emitowały dźwięki w paśmie częstotliwości: 1-2 kHz i 15-16 kHz. Zastosowanie statystycznej metody wielowymiarowej PCA do analizy danych pozwoliło na wyodrębnienie dwóch grup ciastek różniących się właściwościami akustycznymi. Grupę ciastek o udziale tłuszczu w recepturze od 19,5 do 32,0% oraz grupę o udziale tłuszczu od 52,8 do 82,0%. Wyższy udział tłuszczu w recepturze ciastek spowodował generację małej liczby zdarzeń, o krótkim czasie trwania i o niskiej energii zdarzenia. Malała również amplituda dźwięku, zaś współczynnik nachylenia charakterystyki widmowej nie wykazywał jednoznacznej tendencji zmian. Ciastka o większym udziale tłuszczu w recepturze postrzegano jako smaczniejsze oraz uzyskały wyższą ogólną ocenę sensoryczną niż ciastka z mniejszym udziałem tłuszczu. Do badania tekstury ciastek kruchych można stosować metodę pomiaru emisji akustycznej generowanej podczas ich łamania.The aim of this study was to investigate how the type and the share of fat in the shortbread recipe influences the acoustic properties. Margarine (80% fat) and butter (82% fat) were used, in an amounts from 19.2 to 82.0% relative to flour. Measurements of water content and water activity of shortbread were taken, and sensory evaluation was performed with the scoring method. Acoustic emission (EA) generated during the three-point breaking test of the material at a speed of 20 mm min-1 was registered with the contact technique. The sound was analysed in the frequency range from 1 to 18 kHz. Analysis was performed of the acoustic descriptors: number of AE events, acoustic energy, energy of one AE event, the maximum of one AE event, sound duration, amplitude, partition power spectrum slope, and of sensory parameters: loudness, hardness, overall quality, flavour. Statistical analysis of results was conducted with the principal components method (PCA). The type and the share of fat in the shortbread recipe affected the acoustic characteristics. Shortbread with margarine generated sounds of higher energy than shortbread with butter. The spectral characteristic of the AE signal presented activity in 1-3 kHz and 13-14 kHz for shortbread with margarine, and in 1-2 kHz and 15-16 kHz for shortbread with butter. Analysis of the acoustic descriptors of shortbread performed with the statistical method of principal component (PCA) allowed the separation of two groups of shortbread with different acoustic properties. A group with fat content in the shortbread recipe from 19.5 to 32.0%, and a group with fat share from 52.8 to 82.0%. The higher share of fat in the shortbread recipe caused the generation of a small number of events of short duration and low energy of event. Shortbread with the higher share of fat in the recipe were perceived as tastier and received higher sensory scores overall than shortbread with the lower the share of fat in the recipe. The method of registering acoustic emission during the breaking can be used for instrumental texture evaluation of shortbread

One-Day Preliminary National Consultation on Access to Patented Knowledge "Patents and Platform Technologies: Understanding Implications for Research and Development in Malaria and Tuberculosis"

Mr. Linu Mathew Philip, Executive Director, Centad warmly welcomed all distinguished resource people and delegates attending the consultation. He began the introduction by stating the importance of platform technology as an inter-phase to access medicine, in a time when pathogens were getting more resilient and there are fewer technologies to take on these issues. Mr. Philip also mentioned about Centad‟s dreams of access to medicines by taking on the policy issues effectively and aggressively. To make policies enable in such a way that people can have access to medicines and access to innovations, adding that technologies can find a good solution to these existing disease and the diseases that maybe coming in the course of time..