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Víctor Manuel Muñoz-Pérez,Eduardo Fernández-Martínez,Héctor Ponce-Monter,Mario I. Ortiz 대한약리학회 2017 The Korean Journal of Physiology & Pharmacology Vol.21 No.4
The aim of this study was to evaluate the relaxant and anti-inflammatory effects of two thalidomide analogs as phosphodiesterase-4 (PDE-4) inhibitors in pregnant rat uterus. Uteri from Wistar female rats were isolated at 19 day of pregnancy. Uterine samples were used in functional studies to evaluate the inhibitory effects of the thalidomide analogs, methyl 3-(4-nitrophthalimido)-3-(3,4- dimethoxyphenyl)-propanoate (4NO2PDPMe) and methyl 3-(4-aminophthalimido)- 3-(3,4-dimethoxyphenyl)-propanoate (4APDPMe), on prostaglandin-F2α (PGF2α)- induced phasic, K+-induced tonic, and Ca2+-induced contractions. Accumulation of cAMP was quantified in uterine homogenates by ELISA. Anti-inflammatory effect was assessed by using ELISA for determination of the pro-inflammatory cytokines tumor necrosis factor-α (TNFα) and interleukin (IL)-1β, and anti-inflammatory IL-10, from uterine explants stimulated with lipopolysaccharide (LPS). Nifedipine, forskolin and rolipram were used as positive controls where required. Both thalidomide analogs induced a significant inhibition of the uterine contractions induced by the pharmaco- and electro-mechanic stimuli. Nifedipine and forskolin were more potent than the analogs to inhibit the uterine contractility, but these were more potent than rolipram, and 4APDPMe was equieffective to nifedipine. Thalidomide analogs increased uterine cAMP-levels in a concentration-dependent manner. The LPS-induced TNFα and IL-1β uterine secretion was diminished in a concentrationdependent fashion by both analogs, whereas IL-10 secretion was increased significantly. The thalidomide analogs induced utero-relaxant and anti-inflammatory effects, which were associated with the increased cAMP levels as PDE-4 inhibitors in the pregnant rat uterus. Such properties place these thalidomide analogs as potentially safe and effective tocolytic agents in a field that urgently needs improved pharmacological treatments, as in cases of preterm labor.
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Antonio Montes,Chandrasekar Chinnarasu,Clara Pereyra,Lourdes Casas,María Teresa Fernández-Ponce,Casimiro Mantell,Sangma Pattabhi,Enrique Martínez de la Ossa 한국화학공학회 2016 Korean Journal of Chemical Engineering Vol.33 No.2
Various extracts from olive leaves have been precipitated by a supercritical antisolvent (SAS) process to evaluate the possibility of producing polyphenol fine particles with controlled size and size distribution. Olive leaves were initially extracted with subcritical fluids using mixtures of CO2+ethanol at 10% and 50%, by pressurized liquid extraction (PLE) with water, ethanol and a hydroalcoholic mixture (50 : 50) (v/v), and also by conventional ethanol extraction (CE). PLE gave the extract with the highest yield and the best antioxidant activity. SAS precipitation was unsuccessful for the extracts obtained with pressurized water and with the hydroalcoholic mixture (50 : 50) (v/v). The SAS precipitates with the smallest particle sizes were produced from extracts obtained with subcritical fluids. The SAS precipitates obtained after the conventional ethanol extraction of olive leaves showed the best antioxidant activity.
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