Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound   Target Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound

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Query: EC:2.7.10.1 (ERK)
95,504 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Three decomposition products of Morazone (ingredient of the pharmaceutical preparation Rosimon-Neu) were observed following heat treatment in acid medium (hydrochloric or tartaric acid). These products were isolated by TLC and identified as bis-antipyryl-methane, phenmetrazine and 4-hydroxymethyl-antipyrine by mass spectrometry and IR-spectroscopy and 1H-nuclear magnetic resonance. Morazone and the metabolite phenmetrazine may be extracted from alkaline urine using chloroform, however acid hydrolysis (pH 1) of the urine before alkaline extraction will improve the sensitivity of detection of morazone by producing the metabolite phenmetrazine in addition to bis-antipyrylmethane. The metabolite 4-hydroxymethyl-antipyrine is barely detectable by TLC from alkaline extraction of urine.
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PMID:[Investigations of the decomposition and detection of morazone by thin-layer- and gas-liquid-chromatography]. 98 92

An account is given on the development of general anaesthesia at the university clinics of Heidelberg. During the last century mainly chloroform was employed for general anaesthesia. Important events were the first demonstration of Koller's local anaesthesia in the eye in 1884, the first intubation for anaesthesia in Heidelberg, performed by F. Kuhn of Kassel and the development by M. Neu of a rotameter apparatus for nitrous oxide/oxygen anaesthesia in 1910. From 1932 on the surgeon M. Kirschner advanced the methods of high pressure infiltration for regional anaesthesia and segmental hypobaric spinal anaesthesia. In 1951 K. H. Bauer requested R. Frey to set up an "anaesthesia squad" consisting of 2 physicians and 3 nurses to become the nucleus of today's Institute of Anaesthesiology, with O. H. Just as its first professor and chairman.
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PMID:[The history of anesthesia at the Heidelberg University]. 352 5

The logarithm of the 1-octanol-water partition coefficient value (log Poct) was compared with those from CHCl3-water (log PCL) and di-n-butyl ether-water (log PE) for (di)azines substituted singly by nonhydrogen-bonding and hydrogen-accepting substituents (2-substituted pyrazines, 2-substituted pyrimidines, 5-substituted pyrimidines, and 2-substituted pyridines). The difference between log Poct and log PCL for diazines was primarily governed by the number of hydrogen-bonding sites in the substituent. For 2-substituted pyridines, the difference in the hydrogen-bonding association of the ring N-atom with octanol from that with CHCl3 was also significant. In the relationship between log Poct and log PE, the hydrogen-bonding solvations of the ring N-atom(s), as well as the hydrogen-accepting substituent with octanol, should be taken into account because the butyl ether acts as a nonhydrogen-bonding solvent.
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PMID:Hydrophobicity parameter of diazines. III: Relationship of partition coefficients of monosubstituted diazines and pyridines in different partitioning systems. 844 28

This study examined the effect of acute cadmium on stress-related gene expression and free radical production in wild-type and metallothionein-I/II-null (MT-null) mice. Atlas Toxicology arrays showed that acute cadmium (40 micromol/kg as CdCl(2), ip for 3 h) markedly increased the expression of genes encoding heat-shock proteins, heme oxygenase-1, and genes in response to DNA damage/repair. The expression of genes encoding cytochrome P450 enzymes, UDP-glucuronosyltransferases, Mn-superoxide dismutase, and catalase was suppressed by cadmium. MT-null mice were more sensitive than wild-type mice to cadmium-induced, stress-related gene expression, in accord with greater activation of transcription factor AP-1 and phosphorylated JNK and ERK. To evaluate free radical production, mice were simultaneously given the spin trap agent, N-tert-butyl-alpha-phenylnitrone (PBN, 250 mg in DMSO/kg, ip) with cadmium, and livers were removed 30 min later for PBN-trapped radical extraction with chloroform:methanol (2:1), and detected with electron spin resonance (ESR). Cadmium treatment caused detectable ESR signals for PBN adducts as well as lipid peroxidation in the liver similarly in both wild-type and MT-null mice. Thus, the mechanism of acute cadmium toxicity involves multiple facets including oxidative damage and aberrant gene expression, and absence of MT exacerbates Cd-induced aberrant gene expression.
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PMID:Acute cadmium exposure induces stress-related gene expression in wild-type and metallothionein-I/II-null mice. 1195 53

Segmented poly(ether-ester-amide)s (PEEAs) derived from poly(epsilon-caprolactone) oligomers, sebacoyl chloride, hydrophilic diamide-diamines based on short sequences of ethylenoxy groups and containing amino acids, were used to produce matrix systems intended for the delivery of metronidazole in the periodontal pocket. PEEAs are soluble in chloroform and insoluble in water and show M(n) values in the range 8.5-18.6 kDa. The melting temperatures (53-59 degrees C) are close to that of poly(epsilon-caprolactone) (PCL) with a similar M(n). The water absorption of PEEAs is improved if compared with that of pure PCL and depends on both the length of oxyethylene sequences and the amino acid number, as well as on copolymer composition. Loaded-films containing 20% (w/w) of metronidazole were prepared by compression-molding. The release rate was diffusive in the first stage, whereas also other mechanisms, probably polymer degradation, contributed to the slower second phase. The rate of medium penetration within the film depended on PEEA hydrophilicity and crystallinity and was the main determinant governing the drug release rate. The opportunity to control effectively drug release rates by modulating the composition, and in turn the properties, of PEEAs is an attracting feature for their use in a number of drug delivery systems.
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PMID:New segmented copolymers containing poly(epsilon-caprolactone) and etheramide segments for the controlled release of bioactive compounds. 1236 52

Brain insulin receptor and ERK I/II are suggested to play a role in memory formation. We designed a series of experiments to explore if Asiasari radix (AR) extracts could display memory enhancing actions possibly via the activation of insulin receptor and ERK I/II in mice and rats. Methanol extract of AR had significantly increased survival time in the NaNO(2) intoxication assay in mice. Methanol extract of Asiasari radix (fraction 1) and its subfractions, chloroform-soluble fraction (fraction 2) and chloroform-insoluble, methanol-soluble fraction (fraction 4) were further tested for memory formation. In eight-arm radial maze experiments, both reference memory errors and working memory errors were significantly decreased in mice by fractions 1, 2 and 4. In addition, these fractions were also effective in promoting memory in the passive avoidance test in mice and rats. To gain insight into the mechanism of memory enhancing effects by Asiasari radix extracts, the activities of hippocampal insulin receptors and ERK I/II were tested in mice and rats. Fraction 1 significantly stimulated tyrosine phosphorylation of the insulin receptor, whereas ERK I/II were stimulated by fractions 1, 2 and 4. These fractions also inhibited cholinesterase activities in rats. These results suggest that Asiasari radix extracts may exert memory enhancing effects via activation of insulin receptor and ERK I/II as well as decreasing cholinesterase activity.
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PMID:Memory enhancing actions of Asiasari radix extracts via activation of insulin receptor and extracellular signal regulated kinase (ERK) I/II in rat hippocampus. 1274 37

The biodegradability of poly(epsilon-caprolactone) (PCL) was studied in blends and composites of modified and granular starch. Four types of PCL-starch compositions were prepared: (i) PCL-granular starch blends; (ii) hydrophobic coating of starch particles by n-butylisocyanate (C(4) starch) and octadecyltrichlorosilane (C(18) starch), followed by melt blending with PCL; (iii) PCL-starch blends compatibilized by PCL-g-dextran grafted copolymer (PGD); and (iv) PCL-grafted starch particles (PGS) as obtained by in situ ring-opening polymerization of caprolactone (CL) initiated directly from hydroxyl functions at the granular starch surface. Biodegradability of these materials was measured by monitoring the percentage of weight loss in composting and the rate of fungal colonization when samples were used as a sole carbon source for fungus (A. niger). Intrinsic viscosity [eta] of host PCL chains was measured after extraction of composted samples in boiled chloroform. SEM was used to study the surface morphology after compost incubation of the samples. The inherent biodegradability of host polymer was enhanced with surface compatibilization during composting for longer incubation. It was observed that the weight loss during composting increased with the decrease in interfacial tension between filler and polymer. In general, it was concluded that inherent biodegradability does not depend very significantly on the concentration of starch in the polyester matrix, but on the compatibilization efficiency. The effect of the PCL fraction in the graft copolymer, when used as compatibilizer, was also studied on the biodegradability of the host polymer.
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PMID:Biodegradation of poly(epsilon-caprolactone)/starch blends and composites in composting and culture environments: the effect of compatibilization on the inherent biodegradability of the host polymer. 1289 43

Poly(epsilon-caprolactone) (PCL) was dissolved in four solvent systems, chloroform, tetrahydrofuran, acetone and ethyl acetate, and cast onto glass Petri dishes. The surface properties of the resulting films were investigated. The extent to which their properties were determined by the solvent used in each case was quantified in terms of contact angle, surface morphology, attenuated total reflection-Fourier transform infrared spectroscopy (ATR-FTIR), and the adhesion and proliferation of fibroblasts by direct contact. The surface of the PCL film in contact with glass was denoted the SG surface, and the other, which was exposed to the gas phase, a mixture of air and residual solvent vapour, was denoted the SA surface. In the case of hydrophobic solvent systems, the advancing contact angle of the SG surface was always lower than that of the SA surface. With hydrophilic solvent systems, on the other hand, the advancing contact angle of the SG film surface was higher when the contact angle of the Petri dish was higher than that of the gaseous mixture of the air and solvent vapour, otherwise it was lower or equal to that of the surface on which it was cast. The surface morphology was dictated by the solubility of PCL in the respective solvent systems: high dissolution solvents such as chloroform and tetrahydrofuran produced films that comprised PCL aggregates, the particles being larger in the case of chloroform, whereas the less efficient solvents (acetone and ethyl acetate) resulted in a filamentous structure. The ATR-FTIR results confirmed that the chemistry of the SA surfaces differed according to the solvent system used. Preliminary cell culture experiments carried out with the PCL films established that murine (L929) fibroblasts grew well on all surfaces regardless of the solvent used, although the rates of adhesion and proliferation were not as great as on tissue culture plastic controls. Of all the surfaces examined in this study, the cells favoured the SG aspect of ethyl acetate cast PCL films, the surface of which had the finest pore size and relatively low contact angle.
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PMID:Surface properties and biocompatibility of solvent-cast poly[-caprolactone] films. 1512 May 20

Effects of chain-end structure and residual metal compounds on thermal degradation of poly(epsilon-caprolactone) (PCL) were investigated by means of thermogravimetric and pyrolysis-gas chromatograph mass spectrometric analyses. Four types of PCL samples with different chain-end structures (alpha-carboxylic acid-omega-hydroxyl-PCL, alpha-dodecyl ester-omega-hydroxyl-PCL, alpha-carboxylic acid-omega-acetyl-PCL, and alpha-dodecyl ester-omega-acetyl-PCL) were prepared by ring-opening polymerization of epsilon-caprolactone in the presence of zinc-based catalyst and by subsequent acetylation reaction of polymers with acetic anhydride. PCL samples with different zinc contents were obtained by washing with acetic acid in chloroform solution of polymer. Thermal degradation behaviors of these PCL samples with different chain-end structures were examined under both isothermal and nonisothermal conditions. From both the isothermal and nonisothermal experiments, the thermal degradation of PCL samples containing high amounts of residual zinc compounds from synthesis process revealed the selective unzipping depolymerization step below 300 degrees C producing epsilon-caprolactone exclusively. In contrast, zinc-free PCL samples were stable at temperatures below 300 degrees C, and the thermal degradation occurred only at temperatures above 300 degrees C regardless of the chain-end structure. From (1)H NMR analysis of the residual molecules after isothermal degradation of zinc-free PCL, it was confirmed that the omega-chain-end of residual molecules was 5-hexenoic acid unit. However, the cyclic monomer and oligomers were detected as the volatile products of zinc-free PCL samples. These results suggest that the dominant reaction of thermal degradation for PCL above 300 degrees C is a competition between the random chain scission via cis elimination reaction and the cyclic rupture via intramolecular transesterification of PCL molecules.
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PMID:Effects of residual zinc compounds and chain-end structure on thermal degradation of poly(epsilon-caprolactone). 1524 68

The novel Roussin red-salt ester (PPIX-RSE) with a pendant porphyrin chromophore was prepared and investigated as a precursor for the photochemical generation of nitric oxide. PPIX-RSE has the general formula Fe(2)(NO)(4)[(mu-S,mu-S')P] (where (S,S')P is the bis(2-thiolatoethyl) diester of protoporphyrin IX. The photoexcitation of PPIX-RSE with 436- or 546-nm light in an aerated chloroform solution led to the photodecomposition of the cluster with the respective quantum yields (5.2 +/- 0.7) x 10(-4) and (2.5 +/- 0.5 x 10(-4)) and the concomitant release of NO. PPIX-RSE is a significantly more effective NO generator at longer wavelength excitation than are other Fe(2)(mu-SR)(2)(NO)(4) esters for which R is a simple alkyl group such as CH(3)CH(2)- because of the much higher absorptivity of the pendant PPIX chromophore at these wavelengths and a modestly higher quantum yield. Fluorescence intensity and lifetime data indicate that the photoexcited porphyrin of PPIX-RSE is largely quenched by the energy transfer to the Fe(2)S(2)(NO)(4) cluster's core. However, a small fraction of this emission is not quenched, and it is proposed that PPIX-RSE may exist in solution as two conformers.
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PMID:Synthesis and photochemical properties of a novel iron-sulfur-nitrosyl cluster derivatized with the pendant chromophore protoporphyrin IX. 1533 5


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