Search results for "Oxazole"
showing 10 items of 227 documents
Effects of excitatory amino acids and neuropeptide Y on the discharge activity of suprachiasmatic neurons in rat brain slices
1997
Effects of L-glutamate, AMPA, NMDA and NPY on the discharge activity of neurons located in the ventral subdivision of the suprachiasmatic nucleus were examined in submerged coronal slices of the rat hypothalamus. All substances were bath applied. Application of L-glutamate (14 neurons examined) induced an excitatory response in 8 suprachiasmatic neurons (+248.9 +/- 122.24%, mean +/- S.E.M.; P0.001). A biphasic response, i.e. an initial transient excitation (+54.3 +/- 8.21%; P0.001) succeeded by an inhibition (-66.2 +/- 9.31%; P0.001), was observed in 6 neurons. Application of AMPA (36 neurons examined) resulted in an excitation of 31 neurons (+209.2 +/- 58.58%; P0.0001). Application of NMDA…
Post-weaning xenohormone intake affects adult rat submandibular gland in a sex-dependent manner
2018
International audience; OBJECTIVES: We previously reported that maternal exposure to genistein, vinclozolin, ingested alone or in combination, affects submandibular salivary glands of rats' offspring's. Here, we investigated the responsiveness of submandibular gland when such xenohormone exposure occurs later in life. MATERIALS AND METHODS: Chemicals were given orally to male and female Wistar rats (1mg/kg body weight per day), from weaning to adulthood. Submandibular glands and plasma were collected at postnatal day 100 for histological and molecular analysis. RESULTS: Whereas no effect was observed in females, increases in granular convoluted tubules area coupled with a modification of sa…
Perinatal xenohormone exposure impacts sweet preference and submandibular development in male rats.
2013
Objective To determine the effect of perinatal exposure to low doses of genistein and/or vinclozolin on submandibular salivary gland (SSG) development in juvenile and adult male rats and to establish a link with sweet preference. Material and Methods Female rats received orally (1 mg kg−1 body weight/day) genistein and vinclozolin, alone or in combination, from the first gestational day up to weaning. Sweet preference was assessed at weaning and in adulthood in male offspring; submandibular glands were then collected to study the morphogenesis and mRNA expression of steroid receptors, growth factors and taste related proteins. Results Exposure to genistein and/or vinclozolin resulted in a h…
Epistaxis and systemic disease
2008
Abstract We report the case of a 77-year-old man who presented nasal obstruction sensation and epistaxis. Otorhinolaryngologic examination revealed occupation of the left nasal passage and the left maxillary sinus by an inflammatory tumour, the biopsy results of which were inconclusive. While diagnostic tests were being carried out, the patient presented a severe systemic condition consisting mainly of anemia, acute renal failure, and cavitated diffuse bilateral lung infiltrates. In the light of the results of anti-neutrophilic cytoplasmic antibodies and renal biopsy, Wegener's granulomatosis was diagnosed and treatment for the disease was instituted, with a favourable response. Finally, cl…
An Inverse Thermogelling Bioink Based on an ABA-Type Poly(2-oxazoline) Amphiphile
2021
Hydrogels are key components in several biomedical research areas such as drug delivery, tissue engineering, and biofabrication. Here, a novel ABA-type triblock copolymer comprising poly(2-methyl-2-oxazoline) as the hydrophilic A blocks and poly(2-phenethyl-2-oxazoline) as the aromatic and hydrophobic B block is introduced. Above the critical micelle concentration, the polymer self-assembles into small spherical polymer micelles with a hydrodynamic radius of approx 8-8.5 nm. Interestingly, this specific combination of hydrophilic and hydrophobic aromatic moieties leads to rapid thermoresponsive inverse gelation at polymer concentrations above a critical gelation concentration (20 wt %) into…
Preclinical Activity of New [1,2]Oxazolo[5,4-e]isoindole Derivatives in Diffuse Malignant Peritoneal Mesothelioma
2016
A series of 22 derivatives of the [1,2]oxazolo[5,4-e]isoindole system were synthesized through an efficient and versatile procedure that involves the annelation of the [1,2]oxazole moiety to the isoindole ring, producing derivatives with a wide substitution pattern. The structure-activity relationship indicates that the N-4-methoxybenzyl group appears crucial for potent activity. In addition, the presence of a 6-phenyl moiety is important and the best activity is reached with a 3,4,5-trimethoxy substituent. The most active compound, bearing both the structural features, was able to inhibit tumor cell proliferation at nanomolar concentrations when tested against the full NCI human tumor cell…
Modeling the mobility of glyphosate from two contrasting agricultural soils in laboratory column experiments
2019
Glyphosate (GLP) currently is one of the most widely used herbicides worldwide. The persistence of GLP and its major metabolite, aminomethylphosphonic acid (AMPA) in the environment has been described by other authors. This study was aimed at comparing the GLP and AMPA behavior in sandy and loamy sand soils after spiking with enhanced (445 µg g−1) concentrations of GLP in herbicide KLINIK® (Nufarm, Austria) and bioaugmentation followed by 40 days weathering and a consistent three-stage leaching in a laboratory column experiment. Soil samples were obtained from mineral topsoil (0–10 cm) within former agricultural lands where soil parent material was formed by glacigenic deposits. The total a…
Toxoplasmosis after hematopoietic stem cell transplantation.
2000
In immunocompromised individuals, toxoplasmosis mostly occurs as a reactivation of a latent infection, causing severe to life-threatening disease. Thus, recipients who are seropositive for Toxoplasma gondii before an allogeneic hematopoietic stem cell transplant (HCT) are at highest risk, although primary infections may also cause severe toxoplasmosis. The disease most often affects the central nervous system, but in HCT recipients other organs are involved in more than half of the cases. Because of the alteration of the immune response in these patients, serodiagnosis is not sufficiently reliable in the diagnosis of post-HCT toxoplasmosis, and direct detection of the causative agent is req…
Contrasting Effects of Environmental Concentrations of Sulfonamides on Microbial Heterotrophic Activities in Freshwater Sediments
2021
The sulfonamide antibiotics sulfamethoxazole (SMX) and sulfamethazine (SMZ) are regularly detected in surface sediments of contaminated hydrosystems, with maximum concentrations that can reach tens of μg kg–1 in stream and river sediments. Little is known about the resulting effects on the exposed benthic organisms. Here we investigated the functional response of stream sediment microbial communities exposed for 4 weeks to two levels of environmentally relevant concentrations of SMX and SMZ, tested individually. To this end, we developed a laboratory channel experiment where natural stream sediments were immersed in water contaminated with nominal environmental concentrations of 500 and 5,0…
Heterocyclic and Phenyl Double-Bond-Locked Combretastatin Analogues Possessing Potent Apoptosis-inducing activity in HL60 and in MDR Cell lines
2005
Two new series of combretastatin (CA-4) analogues have been prepared. The alkenyl motif of CA-4 was replaced either by a five-membered heterocyclic (isoxazoline or isoxazole) or by a six-membered ring (pyridine or benzene). The new compounds have been evaluated for their effects on tubulin assembly and for cytotoxic and apoptotic activities. Five compounds (18b, 20a, 21a, 34b, and 35b) demonstrated an attractive profile of cytotoxicity (IC501 microM) and apoptosis-inducing activity but poor antitubulin activity. The isoxazoline derivatives 18b, 20a, and 21a, demonstrated potent apoptotic activity different from that of natural CA-4. Their ability to block most cells in the G2 phase suggests…