Antiprotozoal activity of azabicyclo-nonanes linked to tetrazole or sulfonamide cores

N-(Aminoalkyl)azabicyclo[3.2.2]nonanes possess antiplasmodial and antitrypanosomal activity. A series with terminal tetrazole or sulfonamido partial structure was prepared. The structures of all new compounds were confirmed by NMR and IR spectroscopy and by mass spectral data. A single crystal structure analysis enabled the distinction between isomers. The antiprotozoal activities were examined in vitro against strains of Plasmodium falciparum and Trypanosoma brucei rhodesiense (STIB 900). The most active sulfonamide and tetrazole derivates showed activities in the submicromolar range

Unexpected ring‑opening of 2,3‑dihydropyridines

The reaction of 2,3-dihydropyridines with sulfonyl halides surprisingly yielded open chain dienes with sulfonylimine structure. The products were specific out of several possible isomers and, therefore, a separation of isomers was not necessary. All new compounds were characterized using FT-IR spectroscopy, HRMS, and NMR spectroscopy. A bicyclic by-product from the reaction of a 2,3-dihydropyridine with mesyl chloride was isolated and its structure elucidated using a single X-ray crystal analysis. Some biological activities, like antimicrobial and cytotoxic properties were investigated

Transposon activation is a major driver in the genome evolution of cultivated olive trees ( Olea europaea L.)

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Identificación y relaciones genéticas de variedades de olivo en España mediante el uso de marcadores EST-SNPs

En España existe una gran riqueza varietal de olivo (Olea europaea subsp. europaea var europaea) que ha sido ampliamente caracterizada y evaluada. Aun así, varios estudios recientes han evidenciado la presencia de variedades locales de olivo desconocidas, poniendo de manifiesto la necesidad de profundizar en trabajos de prospección, conservación y caracterización varietal. Por ello, en los últimos años, se están llevando a cabo trabajos de prospección en diferentes puntos del país (Andalucía, Aragón, Cataluña y La Rioja). Dichos trabajos han permitido la localización de 290 olivos cultivados de interés y recogida de material vegetal para su posterior identificación. Dicho material ha sido discriminado mediante un conjunto de 96 EST-SNPs recientemente desarrollado en el Banco Mundial de Germoplasma de Olivo del IFAPA (BGMO, Córdoba). El empleo de los marcadores EST-SNPs permitió la identificación de un total de 154 nuevas variedades en las cuatro regiones prospectadas y la detección de casos de sinonimias y homonimias. Además, los marcadores empleados pusieron en evidencia la presencia de una variabilidad relativamente amplia con unos rangos de heterocigosidad esperada y observada de 0,31-0,5 y 0,29-0,81, y valores medios de 0,46 y 0,53, respectivamente. El estudio de las relaciones genéticas entre las variedades prospectadas y el conjunto de variedades nacionales conservadas en el BGMO reveló una clara agrupación de variedades andaluzas y variedades del norte de España, indicando de esta manera una posible selección local de variedades de olivo en nuestro país. En concordancia con estudios anteriores en olivo, estos resultados ponen de manifiesto la eficiencia del conjunto de 96 EST-SNPs para la identificación varietal en olivo y su utilidad para mejorar el manejo de colecciones de recursos genéticos del cultivo

Usefulness of a New Large Set of High Throughput EST-SNP Markers as a Tool for Olive Germplasm Collection Management

Germplasm collections are basic tools for conservation, characterization, and efficient use of olive genetic resources. The identification of the olive cultivars maintained in the collections is an important ongoing task which has been performed by both, morphological and molecular markers. In the present study, based on the sequencing results of previous genomic projects, a new set of 1,043 EST-SNP markers has been identified. In order to evaluate its discrimination capacity and utility in diversity studies, this set of markers was used in a representative number of accessions from 20 different olive growing countries and maintained at the World Olive Germplasm Collection of IFAPA Centre ‘Alameda del Obispo’ (Córdoba, Spain), one of the world’s largest olive germplasm bank. Thus, the cultivated material included: cultivars belonging to previously defined core collections by means of SSR markers and agronomical traits, well known homonymy cases, possible redundancies previously identified in the collection, and recently introduced accessions. Marker stability was tested in repeated analyses of a selected number of accessions, as well as in different trees and accessions belonging to the same cultivar. In addition, 15 genotypes from a cross ‘Picual’ × ‘Arbequina’ cultivars from the IFAPA olive breeding program and a set of 89 wild genotypes were also included in the study. Our results indicate that, despite their relatively wide variability, the new set of EST-SNPs displayed lower levels of genetic diversity than SSRs in the set of olive core collections tested. However, the EST-SNP markers displayed consistent and reliable results from different plant material sources and plant propagation events. The EST-SNPs revealed a clear cut off between inter- and intra-cultivar variation in olive. Besides, they were able to reliably discriminate among different accessions, to detect possible homonymy cases as well as efficiently ascertain the presence of redundant germplasm in the collection. Additionally, these markers were highly transferable to the wild genotypes. These results, together with the low genotyping error rates and the easy and fully automated procedure used to get the genotyping data, validate the new set of EST-SNPs as possible markers of choice for olive cultivar identification

On the origin of the invasive olives (Olea europaea L., Oleaceae).

The olive tree (Olea europaea) has successfully invaded several regions in Australia and Pacific islands. Two olive subspecies (subspp. europaea and cuspidata) were first introduced in these areas during the nineteenth century. In the present study, we determine the origin of invasive olives and investigate the importance of historical effects on the genetic diversity of populations. Four invasive populations from Australia and Hawaii were characterized using eight nuclear DNA microsatellites, plastid DNA markers as well as ITS-1 sequences. Based on these data, their genetic similarity with native populations was investigated, and it was determined that East Australian and Hawaiian populations (subsp. cuspidata) have originated from southern Africa while South Australian populations (subsp. europaea) have mostly derived from western or central Mediterranean cultivars. Invasive populations of subsp. cuspidata showed significant loss of genetic diversity in comparison to a putative source population, and a recent bottleneck was evidenced in Hawaii. Conversely, invasive populations of subsp. europaea did not display significant loss of genetic diversity in comparison to a native Mediterranean population. Different histories of invasion were inferred for these two taxa with multiple cultivars introduced restoring gene diversity for europaea and a single successful founder event and sequential introductions to East Australia and then Hawaii for cuspidata. Furthermore, one hybrid (cuspidata x europaea) was identified in East Australia. The importance of hybridizations in the future evolution of the olive invasiveness remains to be investigated