WHO technical report series, ISSN 0512-3054 959
viii, 105 s. : tab. ; 24 cm
- MeSH
- akrylamidy toxicita MeSH
- arsen toxicita MeSH
- furany toxicita MeSH
- hodnocení rizik MeSH
- kontaminace potravin analýza MeSH
- perchloráty toxicita MeSH
- rtuť toxicita MeSH
- trichotheceny toxicita MeSH
- Konspekt
- Potravinářský průmysl
- NLK Obory
- toxikologie
- zemědělství a potravinářství
- NLK Publikační typ
- publikace WHO
- Klíčová slova
- psychogenní stres, perzistující organické látky, bromované spalovače hoření,
- MeSH
- diabetes mellitus 2. typu MeSH
- dioxiny škodlivé účinky toxicita MeSH
- dospělí * MeSH
- epidemiologické monitorování MeSH
- furany škodlivé účinky toxicita MeSH
- inzulinová rezistence MeSH
- látky znečišťující životní prostředí škodlivé účinky MeSH
- lidé MeSH
- obezita * etiologie MeSH
- organické látky klasifikace škodlivé účinky MeSH
- pesticidy škodlivé účinky toxicita MeSH
- psychický stres MeSH
- rizikové faktory MeSH
- tuková tkáň MeSH
- životní styl MeSH
- znečištění životního prostředí škodlivé účinky MeSH
- Check Tag
- dospělí * MeSH
- lidé MeSH
In an attempt to improve specific biological functions of cytokinins routinely used in plant micropropagation, 33 6-benzylamino-9-tetrahydropyran-2-ylpurine (THPP) and 9-tetrahydrofuran-2-ylpurine (THFP) derivatives, with variously positioned hydroxy and methoxy functional groups on the benzyl ring, were prepared. The new derivatives were prepared by condensation of 6-chloropurine with 3,4-dihydro-2H-pyran or 2,3-dihydrofuran and then by the condensation of these intermediates with the corresponding benzylamines. The prepared compounds were characterized by elemental analyses, TLC, HPLC, melting point determinations, CI+ MS and (1)H NMR spectroscopy. The cytokinin activity of all the prepared derivatives was assessed in three classical cytokinin bioassays (tobacco callus, wheat leaf senescence and Amaranthus bioassay). The derivatives 6-(3-hydroxybenzylamino)-9-tetrahydropyran-2-ylpurine (3) and 6-(3-hydroxybenzylamino)-9-tetrahydrofuran-2-ylpurine (23) were selected, because of the high affinity of their parent compound meta-topolin (mT, 6-(3-hydroxybenzylamino)purine) to cytokinin receptors, as model compounds for studying their perception by the receptors CRE1/AHK4 and AHK3 in a bacterial assay. Both receptors perceived these two derivatives less well than they perceived the parent compound. Subsequently, the susceptibility of several new derivatives to enzyme degradation by cytokinin oxidase/dehydrogenase was studied. Substitution of tetrahydropyran-2-yl (THP) at the N(9) position decreased the turnover rates of all new derivatives to some extent. To provide a practical perspective, the cytotoxicity of the prepared compounds against human diploid fibroblasts (BJ) and the human cancer cell lines K-562 and MCF-7 was also assayed in vitro. The prepared compounds showed none or marginal cytotoxicity compared to the corresponding N(9)-ribosides. Finally, the pH stability of the two model compounds was assessed in acidic and neutral water solutions (pH 3-7) by high-performance liquid chromatography (HPLC).
- MeSH
- cytokininy chemie metabolismus MeSH
- fibroblasty účinky léků MeSH
- financování organizované MeSH
- furany chemická syntéza chemie toxicita MeSH
- kinetika MeSH
- koncentrace vodíkových iontů MeSH
- lidé MeSH
- nádorové buněčné linie MeSH
- puriny chemická syntéza chemie toxicita MeSH
- pyrany chemická syntéza chemie toxicita MeSH
- stabilita léku MeSH
- Check Tag
- lidé MeSH
- Klíčová slova
- Ochratoxin A,
- MeSH
- dioxiny škodlivé účinky toxicita MeSH
- dítě MeSH
- furany izolace a purifikace škodlivé účinky toxicita MeSH
- hodnocení stavu výživy MeSH
- kojenec MeSH
- kojení * MeSH
- lidé MeSH
- mateřské mléko * MeSH
- mykotoxiny izolace a purifikace škodlivé účinky toxicita MeSH
- ochratoxiny izolace a purifikace škodlivé účinky toxicita MeSH
- pesticidy izolace a purifikace škodlivé účinky toxicita MeSH
- rozpouštědla izolace a purifikace škodlivé účinky toxicita MeSH
- xenobiotika * izolace a purifikace metabolismus škodlivé účinky MeSH
- Check Tag
- dítě MeSH
- kojenec MeSH
- lidé MeSH
Retinoids are known to regulate important processes such as differentiation, development, and embryogenesis. Some effects, such as malformations in frogs or changes in metabolism of birds, could be related to disruption of the retinoid signaling pathway by exposure to organic contaminants. A new reporter gene assay has been established for evaluation of the modulation of retinoid signaling by individual chemicals or environmental samples. The bioassay is based on the pluripotent embryonic carcinoma cell line P19 stably transfected with the firefly luciferase gene under the control of a retinoic acid-responsive element (clone P19/ A15). The cell line was used to characterize the effects of individual chemicals and sediments extracts on retinoid signaling pathways. The extracts of sediments from the River Kymi, Finland, which contained polychlorinated dioxins and furans and polycyclic aromatic hydrocarbons (PAHs), significantly increased the potency of all-trans retinoic acid (ATRA), while no effect was observed with the extract of the sediment from reference locality. Considerable part of the effect was caused by the labile fraction of the sediment extracts. Also, several individual PAHs potentiated the effect of ATRA; on the other hand, 2,3,7,8-tetrachlorodibenzo-p-dioxin and several phthalates showed slightly inhibiting effect. These results suggest that PAHs could be able to modulate the retinoid signaling pathway and that they could be responsible for a part of the proretinoid activity observed in the sediment extracts. However, the effects of PAHs on the retinoic acid signaling pathways do not seem to be mediated directly by crosstalk with aryl hydrocarbon receptor.
- MeSH
- biotest metody MeSH
- dioxiny analýza toxicita MeSH
- embryonální karcinom patologie MeSH
- financování organizované MeSH
- furany analýza toxicita MeSH
- geologické sedimenty chemie MeSH
- hodnocení rizik MeSH
- kyseliny ftalové analýza toxicita MeSH
- látky znečišťující životní prostředí analýza toxicita MeSH
- luciferasy světlušek genetika MeSH
- nádorové buněčné linie MeSH
- polycyklické aromatické uhlovodíky analýza toxicita MeSH
- reportérové geny MeSH
- retinoidy genetika metabolismus MeSH
- signální transdukce MeSH
- tretinoin analýza toxicita MeSH
- zvířata MeSH
- Check Tag
- zvířata MeSH
- Geografické názvy
- Finsko MeSH
- MeSH
- antifungální látky farmakologie MeSH
- finanční podpora výzkumu jako téma MeSH
- flukonazol farmakologie MeSH
- furany farmakologie toxicita MeSH
- houby účinky léků ultrastruktura MeSH
- kvasinky účinky léků MeSH
- lidé MeSH
- myši MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- mužské pohlaví MeSH
- myši MeSH
- zvířata MeSH