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31.
Abstract An enantioselective approach towards the synthesis of optically pure cyclohexene nucleosides 3 has been developed starting from (R)-carvone. The key steps are the regio- and stereoselective hydroboration of an exo double bond, the selective reduction of an enone intermediate and introduction of a base moiety by Mitsunobu reaction. Conformational analysis showed that the adenine base adopts predominantly in a pseudo-axial position. 相似文献
32.
Erik De Clercq Arthur Van Aerschot Piet Herdewijn Masanori Baba Rudi Pauwels Jan Balzarini 《Nucleosides, nucleotides & nucleic acids》2013,32(5-6):659-671
Abstract Among the purine and pyrimidine 2′,3′-dideoxynucleosides, 2′,3′-didehydro-2′,3′-dideoxynucleosides, 3′-azido-2′,3′-dideoxynucleosides and 3′-fluoro-2′,3′-dideoxynucleosides, several congeners have been identified which achieve a potent and selective inhibition of HIV-1 replication in vitro. 相似文献
33.
André B. P. van Kuilenburg Heinz-Josef Klumpen Anneke M. Westermann Lida Zoetekouw Piet J. M. Bakker Henk-Jan Guchelaar 《Nucleosides, nucleotides & nucleic acids》2013,32(6-7):726-732
Dihydropyrimidine dehydrogenase (DPD) plays a pivotal role in the metabolism of 5-fluorouracil (5FU). In patients treated with capecitabine or 5FU combined with other chemotherapeutic drugs, DPD activity in peripheral blood mononuclear cells was increased in patients experiencing grade I/II neutropenia. In contrast, decreased DPD activity proved to be associated with grade I/II dermatological toxicity, including hand-foot syndrome. Thus, patients with a low-normal or high-normal DPD activity proved to be at risk of developing mild toxicity upon treatment with 5FU-based chemotherapy, demonstrating the important role of DPD in the etiology of toxicity associated with 5FU and the catabolites of 5FU. 相似文献
34.
Ilse Verheggen Arthur Van Aerschot Jef Rozenski Gerard Janssen Erik De Clercq Piet Herdewijn 《Nucleosides, nucleotides & nucleic acids》2013,32(1-3):325-335
Abstract 1,5-Anhydrohexitol congeners of AZT, D4T and DDC were synthesized. These compounds did not show anti-HIV activity. 相似文献
35.
Sergey N. Mikhailov Erik De Clercq Piet Herdewijn 《Nucleosides, nucleotides & nucleic acids》2013,32(7-8):1323-1334
Abstract The previously developed method for the preparation of 2′-O-D-ribofuranosyl-nucleosides is extended to ribosylation of 2′-deoxynucleosides. The scope and limitations of this reaction are discussed. 相似文献
36.
37.
Rational use of Jatropha curcas L. in food and medicine: from toxicity problems to safe applications
Muhamad Insanu Chryssa Dimaki Richard Wilkins John Brooker Piet van der Linde Oliver Kayser 《Phytochemistry Reviews》2013,12(1):107-119
Jatropha curcas L. has become an important plant for biorefinery and production of biodiesel. From its ethnobotanical use, the plant is known for several activities which are associated with high toxicity. The latest development in engineering technology enables detoxification of native oil and other parts of the plant for new pharmaceutical purposes. Hence a revised look to the rich metabolic spectra of partly structurally rare secondary compound becomes an interesting field of research to be explored. In this review, we discuss recent developments in the technology of detoxification process and give insight about how this ethnomedicinal plant can be applied to new fields of experimental medicine. The review highlights recent data on biological activities and discusses concepts and strategies for turning a poison plant into a valuable crop with high pharmaceutical potential. 相似文献
38.
Markus Möst Adam Petrusek Ruben Sommaruga Petr Jan Juračka Miroslav Slusarczyk Marina Manca Piet Spaak 《Hydrobiologia》2013,715(1):51-62
The occurrence of members of the highly diverse Daphnia longispina complex in Southern and Central Asian high-mountain lakes has been recognized for more than a century. Until now, however, no molecular data have been available for these populations inhabiting the “Roof of the World.” Here, we present the first identification for D. gr. longispina from that region based on a molecular phylogeny. Our findings show that alpine lakes in the Pamir and Himalaya mountains host populations of widespread species of the complex, for which these are the highest known localities. A spineless morph from the Himalaya region, previously labeled as D. longispina var. aspina, was clustering tightly with D. dentifera, while a population from the Pamir mountain range was grouped with D. longispina. In addition, we analyzed ecological data available for lakes in the Khumbu region (Himalaya) to investigate ecological preferences of non-pigmented D. gr. longispina. The identified factors can at least partly be related to avoidance of high UV conditions by this species. We conclude that the widespread species D. dentifera and D. longispina also colonized the Asian high-mountain lakes, and identify the need for further research to trace the possible effect of rapid environmental changes in this region on the diversity and ecology of high-altitude Daphnia populations. 相似文献
39.
This study compares the relative influences of physiography and anthropogenic pressures on river biota at catchment, riparian corridor, and reach scales. Environmental data, catchment and riparian corridor land use, anthropogenic modifications and biological data were compiled for 301 French sites sampled from 2005 to 2008. First, relationships between anthropogenic pressures and fish and macroinvertebrate assemblages were analysed using redundancy analysis. Second, the influences of physiography and the three scales of human pressures on biological assemblages were measured using variance partitioning. Distributions of fish and macroinvertebrate taxa along the pressure gradients agreed with bio-ecological knowledge. At the reach scale, assemblage variability among the 301 French sites was related to the presence of an impoundment and to poor water quality, while at larger scales it was linked to a gradient from forest to agricultural covers. In addition, a large proportion of the explained variability in assemblage composition was related to complex interactions among factors (~40%) and to physiographic variables (~30%). Furthermore, our results highlight that catchment land use better reflects local water quality impairments than hydromorphological degradations. Finally, this study supports the idea that human pressure effects on river communities are linked at several spatial scales and must be considered jointly. 相似文献
40.
Joleen Masschelein Wesley Mattheus Ling-Jie Gao Pieter Moons Rob Van Houdt Birgit Uytterhoeven Chris Lamberigts Eveline Lescrinier Jef Rozenski Piet Herdewijn Abram Aertsen Chris Michiels Rob Lavigne 《PloS one》2013,8(1)
Serratia plymuthica strain RVH1, initially isolated from an industrial food processing environment, displays potent antimicrobial activity towards a broad spectrum of Gram-positive and Gram-negative bacterial pathogens. Isolation and subsequent structure determination of bioactive molecules led to the identification of two polyamino antibiotics with the same molecular structure as zeamine and zeamine II as well as a third, closely related analogue, designated zeamine I. The gene cluster encoding the biosynthesis of the zeamine antibiotics was cloned and sequenced and shown to encode FAS, PKS as well as NRPS related enzymes in addition to putative tailoring and export enzymes. Interestingly, several genes show strong homology to the pfa cluster of genes involved in the biosynthesis of long chain polyunsaturated fatty acids in marine bacteria. We postulate that a mixed FAS/PKS and a hybrid NRPS/PKS assembly line each synthesize parts of the backbone that are linked together post-assembly in the case of zeamine and zeamine I. This interaction reflects a unique interplay between secondary lipid and secondary metabolite biosynthesis. Most likely, the zeamine antibiotics are produced as prodrugs that undergo activation in which a nonribosomal peptide sequence is cleaved off. 相似文献