Search results for "IPR"
showing 10 items of 1515 documents
Activity–Bioavailability balance in Oral Drug Development for a Selected Group of 6‐Fluoroquinolones
2002
Abstract A nomogram is proposed to select the best candidate in drug development studies with quinolones and is intended to substitute other possible models. The nomogram is referred to as an activity–bioavailability balance (ABB) because it includes the following two criteria: ABB= 1 / gm MIC ( drug candidate ) 1 /gm MIC ( ciprofloxacin ) · F calc \( drug candidate \) F calc ( ciproflaxacin ) . The in vitro activity of a group of 4′ N ‐alkyl‐ciprofloxacin derivatives was determined together with that of ciprofloxacin, initially against some reference strains and subsequently against 159 clinical isolates of eight selected species. The inverse of the geometric mean of the lowest concentrati…
A comparative study of the application of the method of least-squares in the potentiometric determination of protonation constants.
1982
Methods of simple and multiple linear regression applied to the potentiometric determination of protonation constants of diprotic and triprotic acids are studied critically. The best way of fitting the data, according to the order of magnitude of the constants, is established. The conclusions are checked by calculating the protonation constants of succinic and citric acids.
Synthesis and Crystal Structure of Ln3(OH)(CrO4)4 · 3.5H2O (Ln = Pr, Nd) and Ln2(OH)2(CrO4)2 (Ln = Tb, Gd): Thermal Behavior and Infrared Spectra of …
1993
Abstract Crystal structures of Ln 2 (OH) 2 (CrO 4 ) 2 ( Ln = Gd, Tb) and Ln 3 (OH)(CrO 4 ) 4 · 3.5H 2 O ( Ln = Pr, Nd) were determined by a conventional single-crystal X-ray diffraction technique. Crystals of Ln 2 (OH) 2 (CrO 4 ) 2 ( Ln = Gd, Tb) are monoclinic, space group P 2 1 / c (no. 14) with lattice parameters a = 8.2454(4) A, b = 11.3834(5) A, C = 12.1420(8) A, and β = 136,590(5)°, Z = 4, D x = 4.92 mg · m -3 for Gd 2 (OH) 2 (CrO 4 ) 2 and a = 8.214(1) A, b = 11.348(1) A, c = 12.094(2) A, and β = 136.59(1)°, Z = 4, D x = 5.01 Mg · m -3 for Tb 2 (OH) 2 (CrO 4 ) 2 . Crystals of Ln 3 (OH)(CrO 4 )) 4 · 3.5H 2 O ( Ln = Pr, Nd) are monoclinic, space group C 2/ c (No. 15) with lattice param…
Lipid Nanocarriers-Loaded Nanocomposite as a Suitable Platform to Release Antibacterial and Antioxidant Agents for Immediate Dental Implant Placement…
2021
Immediate implant placement is a single-stage restorative approach for missing teeth widely used to overcome the ridge remodeling process occurring after dental extractions. The success of this procedure relies on opportune osseointegration in the surrounding tissues. To support this process, a multifunctional nanocomposite, to be applied in the fresh post-extraction socket, was here designed, prepared, and characterized. This formulation consists of quercetin (QRC)-loaded nanostructured lipid carriers (NLCs) entrapped in a chitosan-based solid matrix containing ciprofloxacin (CPX). QRC-NLCs were prepared by homogenization followed by high-frequency sonication, and thereafter this dispersio…
Boronic Acids of Pharmaceutical Importance Affect the Growth and Photosynthetic Apparatus of Cyanobacteria in a Dose-Dependent Manner
2020
The dynamic increase in the commercial application of antimicrobial derivatives of boronic acids, and potential impact of their presence in aquatic systems, supports the necessity to study the toxicity of these substances towards microorganisms of crucial meaning in the environment. One example of the mentioned derivatives is tavaborole (5-fluoro-substituted benzoxaborole), a pharmaceutical agent with antifungal activity. Cyanobacteria were used as model organisms, which are photoautotrophic prokaryotes, as representative aquatic bacteria and photoautotrophs associated with the plant kingdom. To the best of our knowledge, we investigated this issue for the first time. In order to recognize …
The molecular architecture of the thylakoid membrane from various classes of eukaryotic algae
1990
There is convincing consensus that the photosynthetic apparatus is of prokaryotic origin. The wide variety of algal plastids is mostly assumed to be the result of different endocytological events. Chloroplasts surrounded by two membranes as in rhodophytes and chlorophytes were considered as the association of a prokaryotic symbiont and a eukaryotic host, whereas algae having a chloroplast surrounded with more than two membranes can be delineated from an endocytological event of two eukaryotes (see S. Gibbs in this volume). Since chlorophyll b was neither combined with chlorophyll c nor with phycobiliproteins it was proposed that all present day chloroplasts can be integrated in three lines.…
The Bile Acid Receptor GPBAR-1 (TGR5) Modulates Integrity of Intestinal Barrier and Immune Response to Experimental Colitis
2011
Background GP-BAR1, a member G protein coupled receptor superfamily, is a cell surface bile acid-activated receptor highly expressed in the ileum and colon. In monocytes, ligation of GP-BAR1 by secondary bile acids results in a cAMP-dependent attenuation of cytokine generation. Aims To investigate the role GP-BAR1 in regulating intestinal homeostasis and inflammation-driven immune dysfunction in rodent models of colitis. Methods Colitis was induced in wild type and GP-BAR1−/− mice by DSS and TNBS administration. Potential GP-BAR1 agonists were identified by in silico screening and computational docking studies. Results GP-BAR1−/− mice develop an abnormal morphology of colonic mucous cells a…
p53-Mediated downregulation of H ferritin promoter transcriptional efficiency via NF-Y.
2008
The tumor suppressor protein p53 triggers many of the cellular responses to DNA damage by regulating the transcription of a series of downstream target genes. p53 acts on the promoter of the target genes by interacting with the trimeric transcription factor NF-Y. H ferritin promoter activity is tightly dependent on a multiprotein complex called Bbf; on this complex NF-Y plays a major role. The aim of this work was to study the modulation of H ferritin expression levels by p53. CAT reporter assays indicate that: (i) p53 overexpression strongly downregulates the transcriptional efficiency driven by an H ferritin promoter construct containing only the NF-Y recognition sequence and that the phe…
The inner nuclear membrane protein Src1 associates with subtelomeric genes and alters their regulated gene expression
2008
Inner nuclear membrane proteins containing a LEM (LAP2, emerin, and MAN1) domain participate in different processes, including chromatin organization, gene expression, and nuclear envelope biogenesis. In this study, we identify a robust genetic interaction between transcription export (TREX) factors and yeast Src1, an integral inner nuclear membrane protein that is homologous to vertebrate LEM2. DNA macroarray analysis revealed that the expression of the phosphate-regulated genes PHO11, PHO12, and PHO84 is up-regulated in src1Δ cells. Notably, these PHO genes are located in subtelomeric regions of chromatin and exhibit a perinuclear location in vivo. Src1 spans the nuclear membrane twice an…
Evaluation of 10 pesticide residues in oranges and tangerines from Valencia (Spain)
2006
Abstract One hundred and sixteen orange and tangerine samples from an agricultural cooperative of the Valencian Community (Spain) were analyzed for bitertanol, carbendazim, hexythiazox, imazalil, imidacloprid, methidathion, methiocarb, pyriproxyfen, thiabendazole, and trichlorfon by liquid chromatography–mass spectrometry (LC–MS) after a conventional multiresidue extraction procedure. Of 52 samples that contained pesticide residues, carbendazim was detected in 27 (51.9%) in the concentration range of 0.02–0.04 mg kg−1, hexythiazox in 22 (42.3%) in the concentration range of 0.02–0.05 mg kg−1, imazalil in 8 (15.0%) in the concentration range of 0.02–1.2 mg kg−1, imidacloprid in 5 (9.6%) in a…