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

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

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..

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

Synthesis and x-ray investigation of nitrocalix[4]quinone

The method of selective oxidation of simply accessible dihydroxy-dypropoxycalix[4]arene to nitrocalixmonoquinone by mixture of 75% nitric acid and glacial acetic acid was developed. The nitrocalixmonoquinone is prospective as synthone for design of optical sensors and redox-sensitive bio-active compounds. The nitrocalix[4]monoquinone exist a partial cone conformation.Розроблений метод селективного окиснення легкодоступного дигідроксидипропоксикалікс[4]арену сумішшю 75% азотної та льодяної оцтової кислоти, яке приводить до утворення нітрокалікс[4]монохінону — синтону для отримання оптичних сенсорів та редокс-чутливих біологічно активних речовин. Молекула нітрокалікс[4]монохінону існує в конформації частковий конус.Разработан метод селективного окисления легкодоступного дигидроксидипропоксикаликс[4]арена смесью 75% азотной и ледяной уксусной кислот, которое приводит к нитрокаликс[4]монохинону — синтону для получения оптических сенсоров и редокс-чувствительных биологически активных веществ. Молекула нитрокаликс[4]монохинона существует в конформации частичный конус

Influence of the nature of the solvent of crystallization on X-ray crystal structures of para-azidomethyltetrahydroxy-calix 4 arene

1 - ArticleThree different molecular structures of a para-azidomethyltetrahydroxy-calix[4]arene have been determined by single X-ray diffraction studies on crystals obtained from different solvent conditions. Among them, one structure also contains a water molecule and a toluene molecules although the two others are composed purely of para-azidomethyltetrahydroxy-calix[4]arene molecules. A comparative study of the three crystal structures in relation with solvent conditions and a global study of the azido moieties are presented. (C) 2011 Elsevier B.V. All rights reserved

Plasticity of the inner cell mass in mouse blastocyst is restricted by the activity of FGF/MAPK pathway

Abstract In order to ensure successful development, cells of the early mammalian embryo must differentiate to either trophectoderm (TE) or inner cell mass (ICM), followed by epiblast (EPI) or primitive endoderm (PE) specification within the ICM. Here, we deciphered the mechanism that assures the correct order of these sequential cell fate decisions. We revealed that TE-deprived ICMs derived from 32-cell blastocysts are still able to reconstruct TE during in vitro culture, confirming totipotency of ICM cells at this stage. ICMs isolated from more advanced blastocysts no longer retain totipotency, failing to form TE and generating PE on their surface. We demonstrated that the transition from full potency to lineage priming is prevented by inhibition of the FGF/MAPK signalling pathway. Moreover, we found that after this first restriction step, ICM cells still retain fate flexibility, manifested by ability to convert their fate into an alternative lineage (PE towards EPI and vice versa), until peri-implantation stage

Synthesis and structure of dipyrido-1,4-dithiins

Synthesis, properties and reactions of two isomeric dipyrido-1,4-dithiins of the C-2h and C-2v symmetry are described. Their structure detennination and identification are based on spectroscopic methods (H-1 and C-13 NMR, HETCOR, gHMBC and MS), physical properties (mp and R-f), the 1,4-dithiin ring opening reactions and finally X-Ray analysis. A very unusual type of the Smiles rearrangement (S -> S, the pyridyl group migrates from one sulfur atom to another) during the 1,4-dithiin ring opening with sodium methanethiolate enabling isomerization of dithiin with the C-2h symmetry to dithiin with the C-2v symmetry is found