31 research outputs found
Factors Predisposing to Early Childhood Caries (ECC) in Children of Pre-School Age in the City of Zagreb, Croatia
The aim of this study was to investigate factors predisposing to early childhood caries
(ECC) in pre-school children in the city of Zagreb, Croatia. The investigation was
carried out on the sample of 145 children (77 boys and 68 girls) aged between 2 and 5
years, including clinical examination of dental status and survey on the habits among
the parents. The overall prevalence of ECC was 30%: in girls it was 25%, and in boys
48%. The study on the risk factors was designed as a classic case-control study. The
mean value of dmfs index among the cases amounted to 8.6, in comparison to 5.2 in the
control group (p<0.05). Bottle-feeding did not represent a significant risk, but night
consumption of sweet beverages after first 24 months and the lack of introduction of
teeth-brushing habit after first 24 months did (p<0.001 for both predictors). The study
revealed the importance of early introduction of teeth-brushing and giving up the nightly
consumption of sweet beverages in prevention of ECC
Development of fluorinated indanone-based derivatives for the imaging of monoamine oxidase B via positron emission tomography
Ziel/Aim The monoamine oxidase B (MAO B) isoenzyme is known to be
involved in the oxidative deamination of biogenic amines. While the use of
MAO B inhibitors is already well-established for the treatment of Parkinson’s
disease, recent reports suggest its involvement in certain types of brain
tumors.1 We herein aim at the synthesis and preclinical evaluation of fluorinated indanone-based derivatives targeting MAO B in the brain via positron
emission tomography (PET).
Methodik/Methods A small series of fluorinated indanone derivatives
was obtained via the O-alkylation or esterification starting with the
commercially available 6-hydroxy-2,3-dihydro-1H-inden-1-one in one or
two steps. Binding affinities towards the human MAO isoenzymes were
estimated in vitro by radioligand displacement. HL126 was selected for
radiofluorination via its corresponding boronic acid pinacol ester. In
vitro autoradiography of [18F]HL126 was performed in mice brain slices.
In vivo evaluation of [18F]HL126 in CD-1 mice was carried out and
metabolism studies were performed in plasma and brain samples via
radio-HPLC.
Ergebnisse/Results The fluorinated indanone derivatives were synthesized
in yields ranging from 65-89 %. The fluorophenyl ether derivative, HL126,
was further selected for radiofluorination based on its high binding affinity
towards MAO B (Ki = 6.9 ± 5.3 nM). [18F]HL126 was obtained by an alcohol-enhanced copper-mediated approach via the corresponding boronic
acid pinacol ester precursor with radiochemical yields of about 11 ± 3 %,
high radiochemical purities (≥99 %) and molar activities in the range of 20
GBq/mmol. In vitro autoradiography showed a specific blockade with
selective MAO-A/B inhibitors. PET/MRI analyses revealed that [18F]HL126
readily enters the brain. Some radiometabolites do cross the blood-brain
barrier.
Schlussfolgerungen/Conclusions Although metabolism studies with [18F]
HL126 revealed the presence of radiometabolites in the brain, the high binding affinity towards MAO B and the pronounced selectivity in in vitro autoradiography studies encourage further derivatization of indanone-based
scaffolds for targeting MAO B
Kemijski sastav, antioksidativno djelovanje, inhibicija elastaze i protuupalno djelovanje eteričnog ulja biljke Illicium anisatum
The essential oil of air-dried Illicium anisatum obtained by hydrodistillation was analyzed by gas chromatography–mass spectrometry (GC–MS). Fifty-two components were identified in the essential oil and the main component was eucalyptol (21.8 %). The antioxidant and anti-elastase activities of the essential oil were also investigated; the essential oil exhibited moderate DPPH scavenging and anti-elastase activities. To clarify the mechanism of the anti-inflammatory activities of I. anisatum essential oil (IAE), we evaluated whether it could modulate the production of nitric oxide (NO) and prostaglandin E2 (PGE2) by activated macrophages. The results indicate that IAE is an effective inhibitor of LPS-induced NO and PGE2 production in RAW 264.7 cells. These inhibitory activities were accompanied by dose-dependent decreases in the expression of iNOS and COX-2 proteins and iNOS and COX-2 mRNA. In order to determine whether IAE can be safely applied to human skin, the cytotoxic effects of IAE were determined by colorimetric MTT assays in human dermal fibroblast and keratinocyte HaCaT cells. IAE exhibited low cytotoxicity at 100 μg mL1. Based on these results, we suggest that IAE may be considered an anti-aging and anti-inflammatory candidate for cosmetic materials, but additional in vitro and in vivo tests have to be performed to prove its safety and efficacy.Eterično ulje biljke Illicium anisatum dobiveno destilacijom vodenom parom analizirano je plinskom kromatografijom-spektrometrijom masa (GC-MS). Identificirane su pedeset i dvije komponente eteričnog ulja, a glavna komponenta je eukaliptol (21,8 %). Ispitivanje antioksidativnog djelovanja te djelovanja na elastazu ukazuju na umjerenu sposobnost hvatanja DPPH radikala i inhibicije elastaze. Kako bi se objasnio mehanizam protuupalnog djelovanja eteričnog ulja I. anisatum (IAE), ispitan je učinak na moduliranje produkcije dušikovog(II) oksida (NO) i prostaglandina E2 (PGE2) iz aktiviranih makrofaga. Rezultati ukazuju da je IAE učinkovit inhibitor LPS-inducirane produkcije NO i PGE2 u RAW 264.7 stanicama. Inhibitorno djelovanje popraćeno je smanjenjem ekspresije iNOS i COX-2 proteina i iNOS i COX-2 mRNA. Kako bi se odredilo može li se IAE sigurno primijeniti na ljudsku kožu, citotoksični učinci IAE određeni su kolorimetrijskim MTT testom u humanim dermalnim fibroblastima i keratinocitima HaCaT. IAE je pokazao nisku citotoksičnost pri koncentraciji 100 μg mL-1. Temeljem ovih rezultata IAE se može smatrati potencijalnim sredstvom protiv starenja i protuupalnim sredstvom u kozmetičkim pripravcima. Međutim, dodatni in vitro i in vivo testovi nužni su za potvrdu njegove sigurnosti i učinkovitosti