The aim of this study is to determine the location of MB2 in maxillary first molars in relation to the MB1 using the cone-beam computed tomography (CBCT) imaging. In this retrospective study, electronic health records' system was utilised to identify patients who acquired CBCT for the maxillary first molar as an imaging adjunct to their endodontic treatment. Data were evaluated, and statistical analysis was performed.
View Article and Find Full Text PDFThe fused quinazolinone derivative, RX-207, is chemically and functionally related to small molecule inhibitors of protein binding to glycosaminoglycans (SMIGs). Composed of a planar aromatic amine scaffold, it inhibits protein binding to glycosaminoglycans (GAGs). RX-207 reduced neutrophil migration in thioglycollate-induced peritonitis (37%), inhibited carrageenan-induced paw edema (32%) and cerulein-induced pancreatitis (28%), and increased animal survival in the mouse model of cecal ligation and puncture (CLP)-induced sepsis (60%).
View Article and Find Full Text PDFObjective: To determine the prevalence of primary aldosteronism (PA) in hypertensive patients presenting to the primary care clinic at The Mount Sinai Hospital, regardless of the degree of hypertension and to identify clinical criteria that should prompt screening for PA.
Methods: An aldosterone:renin ratio (ARR, cutoff ≥20, with plasma aldosterone concentration [PAC] ≥10 and suppressed renin) was used to prospectively screen 296 hypertensive patients (blood pressure [BP] ≥140/90) over the age of 18 from August 2012 through May 2013. Subjects who screened positive then underwent confirmatory oral salt load testing (OSLT).
Objective And Design: Elucidate the mechanism of action of the small molecule inhibitor of protein binding to glycosaminoglycans, RX-111 and assay its anti-inflammatory activity in animal models of inflammatory disease.
Materials: The glycosaminoglycan, heparin, was used in the mechanism of action study of RX-111. Human T lymphocytes and umbilical vein endothelial cells were used to assay the in vitro activity of RX-111.
Background: Small molecule inhibitors of biologically important protein-glycosaminoglycan (GAG) interactions have yet to be identified.
Methods: Compound libraries were screened in an assay of L-selectin-IgG binding to heparin (a species of heparan sulfate [HS-GAG]). Hits were validated, IC-50s established and direct binding of hits to HS-GAGs was investigated by incubating compounds alone with heparin.
Primary aldosteronism (PA) is the most common etiology of endocrine hypertension (HTN), and recent prevalence studies suggest that it may be under-diagnosed. Indications for screening have been expanded with recognition that many patients with PA do not have hypokalemia and that the disease may be familial. The aldosterone:renin ratio (ARR) is the preferred screening test for PA.
View Article and Find Full Text PDFSubstituted cinnamoyl chlorides, 11, were converted into (2-hydroxyethyl)-oxazolinium chlorides 14, N,N-bis-(2-chloroethyl)amides 16 and (2-chloroethyl)-oxazolinium chlorides 17. Although derivatives 14 which possess electron-donating substituents (Me or MeO) were more potent than those substituted by electron-withdrawing groups (NO(2), Cl or CF(3)), the difference in cytotoxic actin was not significant. Modification of the lipophilic character in a series of alkoxy-substituted derivatives 14 led to more active compounds, where 14t that possesses a 4-octyloxy-phenyl-substituent was the most potent and displayed cytotoxic activity in the microM range.
View Article and Find Full Text PDFTreatment of intestinal necrosis, caused by an acute mesenterial ischemia, represents the most complex field of surgery. Results of surgical treatment of 74 patients with various forms of mesenterial ischemia, complicated by intestinal infarction, were analyzed. Revascularization ought to be conducted if the ischemia may be eliminated.
View Article and Find Full Text PDFThe synthesis and biological activities of acidic, basic and neutral types of butyric acid (BA) prodrugs possessing increased aqueous solubility are described. The compounds are butyroyloxyalkyl derivatives of carboxylic acids, which possess functionalities suitable for aqueous solubilization. The anticancer activity of the prodrugs in vitro was evaluated by examining their effect on the growth of human colon, breast and pancreatic carcinoma cell lines, and their solubility in aqueous media was determined.
View Article and Find Full Text PDFJ Cancer Res Clin Oncol
December 2000
Unlabelled: Pivaloyloxymethyl butyrate (AN-9), a butyric acid (BA) prodrug, exhibited low toxicity and significant anticancer activity in vitro and in vivo. The purpose of this study was to elucidate the basis for AN-9 increased anticancer activity compared to BA, by studying the uptake of BA and AN-9 into the cells.
Methods: The uptake rate and level of [14C]-AN-9 and [14C]-BA, labeled on the carboxylic moiety of BA, into HL-60 and MEL leukemic cell lines was measured.
The bifunctionally reactive nucleoside and distant nucleoside analogs adenosine (Ado), S-[(adenine-9-yl)methoxyethyl]-L-cysteine (Na-salt) (cysA) and 9-vinyladenine (vA) in aqueous solutions assemble on complementary polyuridylic acid templates to form complex lyomesophases. The systems are investigated by polarizing microscopy, differential scanning calorimetry (DSC) and 1H- and 31P-nmr spectroscopies, assisted by molecular modeling studies. The results indicate the importance of biomesogenic (pre)ordering in nucleic acid native and artificial matrix reactions.
View Article and Find Full Text PDFNucleosides Nucleotides Nucleic Acids
July 2000
Amphiphilic complementary nucleobase derivatives, containing n-octadecyloxymethyl substituents at the N1 position of pyrimidine and N9 of purine, dissolved in chloroform form non-specific lyotropic mesophases, which were analyzed by optical polarizing microscopy. Molecular modeling studies visualize hypothetical horizontal and vertical nucleobase hydrogen-bonding and stacking arrangements, as well as aliphatic long-chain interstrand interaction.
View Article and Find Full Text PDFInt J Immunopharmacol
November 1999
In this study we investigated the effects of two guanine derivatives, 9-benzyl- (I) and 7-benzyl-8-bromoguanines (II) on the proliferation of human T-cell leukemia and T-cell lymphoma, normal human peripheral blood mononuclear cells (PBMC), and mouse Th1 (pGL10) and Th2 (D10.G4.1) clones.
View Article and Find Full Text PDFThe appropriate anesthesia for renal transplantation (RT) requires minimal toxicity for patient and transplant besides of sufficient pain relief and correction of vital functions. Since 1990 for this reason prolonged epidural anesthesia (PEA) was used for 42 RT. The catheterization of epidural space was performed on the spine level Th9-Th12.
View Article and Find Full Text PDFA series of new acycloguanosine O-alkoxyalkyl derivatives have been obtained by the reaction of 9-(2-hydroxyethoxymethyl)- and 8-bromo-9-(2-hydroxyethoxymethyl)-N2-acetylguanines with cyclic and acyclic alpha-vinyl ethers. 9-[2-(Alkoxyalkyl)oxyethoxymethyl]-N2-acetylguanines are better soluble in water and low-polar organic solvents as compared with acycloguanosine. The compounds have the pronounced antiviral activity against HSV-I in the experiments in vivo and can be applied as acycloguanosine prodrugs.
View Article and Find Full Text PDFNucleic Acids Res
October 1989
Conformational possibilities of a series of deoxyguanosine analogues possessing or lacking antiviral activity were evaluated using methods of the molecular mechanics. Comparison of the spatial structures of acyclic analogues with one another and with the spatial structures of deoxyguanosine demonstrates restricted conformational mobility for compounds devoid of activity. The level of sterically allowed superposition of functional groups from the acyclic moieties of analogues and the corresponding atomic centres of deoxyribose could serve as a criterion of activity.
View Article and Find Full Text PDFNucleic Acids Res
March 1976
A convenient method is suggested for synthesis of uracil-1-malonic acid diethyl ester by alkylating 2,4-bis(trimethylsilyl) uracil with bromo-malonic acid diethyl ester. This compound has been shown to hydrolyze with NaOH yielding either uracil or uracil-1-acetic acid, depending on reaction conditions. Similarly, thymine-1-malinic acid diethyl ester and 5-fluorouracil-1,3-dimalonic acid tetraethyl ester were obtained.
View Article and Find Full Text PDFPatients with dedifferentiated brain astrocytoma during an operation were injected intravenously 2-C14-fluorofur (3 muC/Kg). In different periods after the injection the level of radioactivity was determined in different sites of the tumor, brain tissue, as well as in blood plasma, cerebrospinal liquor and urine. Intracellular localization of the labeled substance in the tumor tissue was examined autohistoradiographically.
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