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Gelain, Arianna,Barlocco, Daniela,Kwon, Byong-Mog,Jeong, Tae-Sook,Im, Kyung-Ran,Legnani, Laura,Toma, Lucio WILEY-VCH Verlag 2006 Archiv der Pharmazie Vol.339 No.12
<P>A series of novel Acyl-CoA: cholesterol acyltransferase (ACAT) inhibitors 8a–f was synthesized; the substances were characterized by the presence of a 2,5-dimethylpyrazin-3-yl moiety at one end and a 3-heptylamino-5-phenylpyridazine system at the other one, linked through linear alkyl spacers of different length. The new derivatives were designed based on the hypothesis that the 3-amino-5-phenylpyridazine moiety could mimic the aryl substituted urea, which was present in a number of ACAT inhibitors previously described. The choice of the 2,5-dimethylpyrazin-3-yl substituent was supported by a preliminary investigation, which indicated that this moiety is the most powerful in conferring ACAT inhibitory properties to the new series. The pharmacological results proved the idea to be sound. Finally, compounds 9a–c, lacking the phenylpyridazine moiety were prepared and tested to further strengthen our hypothesis.</P>
Vitamin A Supplementation for Different Periods Alters Oxidative Parameters in Lungs of Rats
Matheus Augusto de Bittencourt Pasquali,Daniel Pens Gelain,Marcos Roberto de Oliveira,Guilherme Antônio Behr,Leonardo Lisbôa da Motta,Ricardo Fagundes da Rocha,Fábio Klamt,José Cláudio Fonseca Moreira 한국식품영양과학회 2009 Journal of medicinal food Vol.12 No.6
Lungs require an adequate supply of vitamin A (retinol) for normal embryonic development, postnatal maturation, and maintenance and repair during adult life. However, recent intervention studies revealed that supplementation with retinoids resulted in higher incidence of lung cancer, although the mechanisms underlying this effect are still unknown. Here, we studied the effect of vitamin A supplementation on oxidative stress parameters in lungs of Wistar rats. Vitamin A supplementation at either therapeutic (1,000 and 2,500IU/kg) or excessive (4,500 and 9,000IU/kg) doses for 3, 7, or 28 days induced lipid peroxidation, protein carbonylation, and oxidation of protein thiol groups, as well as change in catalase and superoxide dismutase activity. Together, these results suggest that vitamin A supplementation causes significant changes in redox balance, which are frequently associated with severe lung dysfunction.
Marcos G.S. Gouveia,Maria A. Xavier,Andre´ S. Barreto,Daniel P. Gelain,Joa˜o P.A. Santos,Adriano A.S. Arau´jo,Francilene A. Silva,Jullyana S. Quintans,Maria F. Agra,Analu´cia G.S. Cabral,Josean F. Tav 한국식품영양과학회 2011 Journal of medicinal food Vol.14 No.11
The antioxidant, antinociceptive, and anti-inflammatory activities of the ethanolic extract from leaves of Combretum duarteanum (EEC) were assessed in rodents through in vitro tests. The antioxidant activity was investigated by using thiobarbituric acid reactive species (TBARS), hydroxyl radical–scavenging, and scavenging activity of nitric oxide assays. The antinociceptive activity was investigated by using acetic acid–induced writhing, formalin, and hot-plate tests in mice. The anti-inflammatory activity was assessed in rats by using the carrageenan-induced hind-paw edema test and arachidonic acid–induced paw edema test. EEC possesses a strong antioxidant potential according to the TBARS, nitric oxide, and hydroxyl radical–scavenging assays; it also presented scavenger activity in all in vitro tests. After intraperitoneal injection, EEC (100, 200, and 400 mg/kg) significantly reduced the number of writhes (38.1%, 90.6%, and 97.8%, respectively) in a writhing test and the number of paw licks during phase 1 (30.5% and 69.5%, higher doses) and phase 2 (38.1%, 90.6%, and 97.8%, all doses) of a formalin test when compared with the control group. Naloxone (1.5 mg/kg, intraperitoneally) antagonized the antinociceptive action of EEC (400 mg/kg), and this finding suggests participation of the opioid system. Administration of 200 and 400 mg/kg (intraperitoneally) of EEC exhibited an anti-inflammatory activity in the carrageenin test, which was based on interference with prostaglandin synthesis. This finding was confirmed by the arachidonic acid test. Together, these results indicate that properties of EEC might be further explored in the search for newer tools to treat painful inflammatory conditions, including those related to pro-oxidant states.
Influence of Toxoplasma gondii Acute Infection on Cholinesterase Activities of Wistar Rats
Alexandre Alberto Tonin,Aleksandro Schafer da Silva,Maria Luiza Thorstenberg,Livia Gelain Castilhos,Raqueli Teresinha Franca,Daniela Bitencourt Rosa Leal,Marta Maria Medeiros Frescura,Fernanda Silveir 대한기생충학열대의학회 2013 The Korean Journal of Parasitology Vol.51 No.4
Meneghetti, Fiorella,Villa, Stefania,Masciocchi, Daniela,Barlocco, Daniela,Toma, Lucio,Han, Dong‐,Cho,Kwon, Byoung‐,Mog,Ogo, Naohisa,Asai, Akira,Legnani, Laura,Gelain, Arianna WILEY‐VCH Verlag 2015 EUROPEAN JOURNAL OF ORGANIC CHEMISTRY Vol.2015 No.22
<P><B>Abstract</B></P><P>Three new ureido‐pyridazinone derivatives, which are structurally related to the known STAT3 inhibitor <B>AVS‐0288</B>, were designed by taking into account the structure–activity relationships determined for several ureido‐oxadiazole derivatives previously studied by our group. Their synthesis was first attempted through suitable 5‐aminopyridazinone intermediates (<B>6a</B> and <B>6b</B>), which molecular structures were confirmed by means of X‐ray diffraction data on <B>6a</B>. Amine functionalization was unsuccessful, therefore, an alternative method was devised. Dual‐luciferase and AlphaScreen‐based assays were used to test their activity. The obtained data were rationalized on the basis of a modeling study, which focused our attention on the geometrical preferences of the ureido moiety. Computational results seem to indicate that both the 1,2,5‐oxadiazole ring and the extended <I>ZZ</I> arrangement are essential and probably act in a synergistic way to confer significant activity against STAT3.</P>
Mairim Russo Serafini,Rodrigo Correia Santos,Adriana Gibara Guimarães,João Paulo Almeida dos Santos,Alan Diego da Conceicão Santos,Izabel Almeida Alves,Daniel Pens Gelain,Paulo Cesar de Lima Nogueira 한국식품영양과학회 2011 Journal of medicinal food Vol.14 No.10
Herbal drugs have been used since ancient times to treat a wide range of diseases. Morinda citrifolia Linn (popularly known as “Noni”) has been used in folk medicine by Polynesians for over 2,000 years. It is reported to have a broad range of therapeutic effects, including effects against headache, fever, arthritis, gingivitis, respiratory disorders, infections, tuberculosis, and diabetes. The aim of this study was to investigate the antioxidant, anti-inflammatory, antinociceptive, and antibacterial properties of the aqueous extract from M. citrifolia leaves (AEMC). Antioxidant activity was observed against lipid peroxidation, nitric oxide, and hydroxyl radicals. The antinociceptive effect of AEMC was observed in the acetic acid–induced writhing test at the higher dose. Moreover, AEMC significantly reduced the leukocyte migration in doses of 200 and 400 mg/kg and showed mild antibacterial activity. Together, the results suggest that properties of M. citrifolia leaf extract should be explored further in order to achieve newer tools for managing painful and inflammation conditions, including those related to oxidant states.