Search results for "synthesi"
showing 10 items of 2904 documents
Gene expression is stronger associated with behaviour than with age and fertility in ant workers
2018
AbstractThe ecological success of social insects is based on division of labour, not only between queens and workers, but also among workers. Whether a worker tends the brood or forages is strongly influenced by age, fertility and nutritional status, with brood carers being younger, more fecund and corpulent. Here, we experimentally disentangle behaviour from age and fertility inTemnothorax longispinosusant workers and analyse how these parameters are linked to whole-body gene expression. Our transcriptome analysis reveals four times more genes associated with behaviour than with age and only few fertility-associated genes. Brood carers exhibited an upregulation of genes involved in lipid b…
Data from: A revision of Sesuvium (Aizoaceae, Sesuvioideae)
2017
Sesuvium and Cypselea are closely related succulent genera within the Sesuvioideae (Aizoaceae). Since Cypselea is nested in Sesuvium in molecular studies and both genera share traits separating them from other members of the subfamily, we propose to include Cypselea in Sesuvium. Sesuvium (incl. Cypselea) comprises 14 species and is distributed worldwide with centres of diversity in southern Africa and North and Central America. Sesuvium comprises erect to procumbent herbs with opposite leaves that often bear conspicuous sheath-like lateral appendages on the petioles (pseudostipules). These and the many-seeded capsules are diagnostic traits, separating Sesuvium from the closely related gener…
Organochromium complexes - labelled aminoglycoside antibiotics derived from kanamycin A and tobramycin. Synthesis, structural characterization and us…
1993
Abstract The synthesis of metallocenic derivatives of aminoglycoside antibiotics, i. e. kanamycin A and tobramycin, is described. The organometallic-labelled compounds have been obtained from the reaction between the polyaminodrugs and organochromium esters of N-hydroxysuccinimide. The reaction proceeded selectively at the 6′-N position, as might be deduced both from the mass and the pH-dependent 13 C-NMR spectra. The procedure could be regarded as generally useful for the metallolabelling of aminoglycoside antibiotics. As an example of application a competitive immunoassay based on the use of these labels is proposed.
In vivo evaluation of the interaction between the Escherichia coli IGP synthase subunits using the Bacterial Two-Hybrid system
2020
ABSTRACT Histidine biosynthesis is one of the most characterized metabolic routes for its antiquity and its central role in cellular metabolism; indeed, it represents a cross-road between nitrogen metabolism and de novo synthesis of purines. This interconnection is due to the activity of imidazole glycerol phosphate synthase, a heterodimeric enzyme constituted by the products of two his genes, hisH and hisF, encoding a glutamine amidotransferase and a cyclase, respectively. Despite their interaction was suggested by several in vitro experiments, their in vivo complex formation has not been demonstrated. On the contrary, the analysis of the entire Escherichia coli interactome performed using…
Modular Solid-Phase Synthesis of Antiprotozoal Barnesin Derivatives
2020
Here, we applied and optimized a solid support (SP)-based Horner-Wadsworth-Emmons reagent to prepare SP-bound vinylogous amino acids. Subsequent SP-based peptide synthesis, global deprotection, and chemical modifications yielded 14 lipodipeptides carrying vinylogous amino acids, including the natural product barnesin A (1). Biological evaluation revealed that several synthesized derivatives show micromolar to nanomolar inhibitory activity against papain-like cysteine proteases, human cathepsin L, and rhodesain.
Synthesis and biological evaluation of sphingosine kinase 2 inhibitors with anti-inflammatory activity.
2019
The synthesis of inhibitors of SphK2 with novel structural scaffolds is reported. These compounds were designed from a molecular modeling study, in which the molecular interactions stabilizing the different complexes were taken into account. Particularly interesting is that 7‐bromo‐2‐(2‐phenylethyl)‐2,3,4,5‐tetrahydro‐1,4‐epoxynaphtho[1,2‐b]azepine, which is a selective inhibitor of SphK2, does not exert any cytotoxic effects and has a potent anti‐inflammatory effect. It was found to inhibit mononuclear cell adhesion to the dysfunctional endothelium with minimal impact on neutrophil–endothelial cell interactions. The information obtained from our theoretical and experimental study can be us…
Structure, Biosynthesis, and Bioactivity of Photoditritide from Photorhabdus temperata Meg1
2019
A new cyclic peptide photoditritide (1), containing two rare amino acid d-homoarginine residues, was isolated from Photorhabdus temperata Meg1 after the nonribosomal peptide synthetase encoding gene pdtS was activated via promoter exchange. The structure of 1 was elucidated by HR-MS and NMR experiments. The absolute configurations of amino acids were determined according to the advanced Marfey's method after hydrolysis of 1. Bioactivity testing of 1 revealed potent antimicrobial activity against Micrococcus luteus with an MIC value of 3.0 μM and weak antiprotozoal activity against Trypanosoma brucei rhodesiense with an IC50 value of 13 μM. Additionally, the biosynthetic pathway of 1 was als…
Design, synthesis, DNA-binding and cytotoxicity evaluation of new potential combilexines
2002
Combilexines, compounds in which a DNA intercalator is linked to a minor groove binding component, interact with the DNA in a sequence specific manner to yield in most cases compounds with anticancer activity. A series of new compounds closely related to netropsin in which the two components were linked by an amide group was synthesised as potential combilexines. As some of these compounds showed cytotoxic activity in vitro, an attempt was made to rationalise their mechanism of action. The DNA binding characteristics of the carboxamides were evaluated by thermal denaturation experiments and by ethidium bromide displacement assay. Their ability to inhibit the topoisomerase I was also determi…
Stereoselective Synthesis of the Antiprotozoal Lactone Passifloricin A and Seven Isomers Thereof
2004
The conjugated delta-lactone passifloricin A, a natural product with antiprotozoal activity, and seven isomers thereof have been synthesized in enantiopure form. It has been shown in this way that the proposed structure for the natural compound was erroneous. The correct structure is now evidenced. Key steps of the syntheses were asymmetric Brown-type aldehyde allylations and ring-closing metatheses.
Correction: Total synthesis of two potent anti-inflammatory macrolactones of the oxacyclododecindione type
2015
Correction for ‘Total synthesis of two potent anti-inflammatory macrolactones of the oxacyclododecindione type’ by Johannes Tauber et al., Org. Biomol. Chem., 2015, 13, 7813–7821.