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Methyl Ester (methyl + ester)
Kinds of Methyl Ester Terms modified by Methyl Ester Selected AbstractsPhotoreaction Between Benzoylthiophenes and N -BOC-Tryptophan Methyl Ester,PHOTOCHEMISTRY & PHOTOBIOLOGY, Issue 1 2006Julia Pérez-Prieto ABSTRACT Drug-induced photoallergy requires as the first step formation of covalent drug-protein photoadducts. One of the key amino acids involved in this process is tryptophan (Trp). In this context, several diaryl ketones, including 2-benzoylthiophene (BT), [2-(5-benzoyl-5-thienyl)]-2-methylpropanoic methyl ester (TPA methyl ester) and 4-(2-thienylcarbonyl)phenyl]-2-methylpropanoic methyl ester (SUP methyl ester) have been irradiated in the presence of N -BOC-(L)-tryptophan methyl ester. Laser flash photolysis has allowed to detect three neutral radicals (ketyl, indolyl and skatolyl radicals) resulting from formal hydrogen-atom abstraction. This correlates well with the isolation of homodimers, as well as with cross-coupling products, in the preparative irradiation. The main cross-coupling products were in all cases lactones arising from the reaction of the Trp-derived skatolyl radicals with the corresponding ketyl radicals. These lactones were obtained as the (4R) stereoisomers with remarkable diasteroselectivity. No coupling products through the phenyl p -position of BT or TPA methyl ester were found. By contrast, ketone homodimers and cross-coupling products arising from reaction through the thienyl 5-position were obtained when using BT and SUP methyl ester; this is very interesting, because stable LAT-derived products are difficult to isolate. [source] Total Synthesis of Spirastrellolide,F Methyl Ester,Part,1: Strategic Considerations and Revised Approach to the Southern Hemisphere,ANGEWANDTE CHEMIE, Issue 52 2009Gregory Um eine optimale Konvergenz bei der vorgesehenen Totalsynthese von Spirastrellolid,F zu gewährleisten, wurde der die südliche Hemisphäre repräsentierende Baustein mit einer freien Carbonsäure und einem Enoltriflat-Terminus hergestellt (siehe Bild). Dieses ungewöhnliche Muster ermöglicht den Aufbau des 38-gliedrigen makrocyclischen Kerns der Zielstruktur und minimiert die Zahl von Schutzgruppenmanipulationen gegen Ende der Syntheseroute. [source] Total Synthesis of Spirastrellolide,F Methyl Ester,Part,2: Macrocyclization and Completion of the Synthesis,ANGEWANDTE CHEMIE, Issue 52 2009Stefan Benson Dipl.-Chem. Wunder der See: Die kompakte und hoch konvergente Totalsynthese des Methylesters des marinen Makrolids Spirastrellolid,F (siehe Bild) wurde abgeschlossen. Dabei wurden die nördlichen und südlichen ,Hemisphären" in nur zwei Stufen ohne zwischengeschaltete Schutzgruppenmanipulationen zusammengefügt (Suzuki-Kupplung, Yamaguchi-Lactonisierung). [source] ChemInform Abstract: Synthesis of (.+-.)-(E)-2,6-Dimethyl-6-hydroxy-2,7-octadienoic Acid (III), Its Methyl Ester (V) and (.+-.)-(E)-2,6-Dimethyl-octa-2,7-diene-1,6-diol (VI) over Solid Support Using Microwave.CHEMINFORM, Issue 28 2009Ashima Singh Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] Cyclopropanation of Betulonic Acid and Its Methyl Ester with Dichlorocarbene Generated under Phase Transfer Catalysis Conditions.CHEMINFORM, Issue 37 2006N. G. Komissarova Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source] An Efficient Synthesis of Tricyclic Compounds, (.+-.),-(4a,,8a,,10a,) -1,2,3,4,4a,6,7,8,8a,9,10,10a-Dodecahydro-1,1,4a-trimethyl-2-oxophenanth rene-8a-carboxylic Acid, Its Methyl Ester, and (.+-.)-(4a,,8a,,10a,) -3,4,4a,6,7,8,8a,9,10,10a-Decahydro-8a-hydroxymethyl-1,1,4a-trimethylphe nanthren-2(1H)-one.CHEMINFORM, Issue 15 2006Tadashi Honda Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source] N -(4-Nitrophenylsulfonyl)- and N -(Fluorenylmethoxycarbonyl)- N -ethyl Amino Acid Methyl Esters , A Practical ApproachEUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Issue 22 2010Emilia Lucia Belsito Abstract An efficient one-pot preparation of N -ethyl- N -4-nitrophenylsulfonyl (nosyl) amino acid methyl esters was accomplished by a simple N -ethylation reaction by using triethyloxonium tetrafluoroborate in the presence of N,N -diisopropylethylamine. The N -ethylated amino acid methyl esters are obtained with total retention of stereochemistry at the original chiral centers. To further broaden the scope of this methodology, the N -ethylated nosyl-protected compounds are easily converted in the more practical fluorenylmethyloxycarbonyl (Fmoc)-protected derivatives. The cleavage of methyl ester by using a mild and neutral method enables the preparation of N -ethyl amino acids that are building blocks suitable for introduction into a peptide chain. The methodology works well with both nosyl- and Fmoc-based solution-phase peptide synthesis. [source] A Novel Direct Conversion of Primary Amides to Their Corresponding Methyl EstersEUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Issue 6 2007Liang-Chun Li Abstract A novel method was used to directly convert aliphatic and aromatic primary amides into their corresponding methyl esters in high yields (up to 99,%) under mild reaction conditions. Possible mechanisms were studied at the B3LYP/6-31++G(d,p) level of theory. Formation of the ester proceeded through a rearrangement of the ,OMe and ,NH2 groups in the RC(O)NHS(O)OMe intermediate in a H+ -catalyzed six-membered ring transition state structure. (© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2007) [source] ChemInform Abstract: Practical and Robust Method for Stereoselective Preparations of Ketene Silyl (Thio)acetal Derivatives and NaOH-Catalyzed Cross-Claisen Condensation Between Ketene Silyl Acetals and Methyl Esters.CHEMINFORM, Issue 44 2009Kenta Takai Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] ChemInform Abstract: New Synthesis of Methyl 5-Aryl or Heteroaryl Pyrrole-2-carboxylates by a Tandem Sonogashira Coupling/5-endo-dig-Cyclization from ,-Iododehydroamino Acid Methyl Esters and Terminal Alkynes.CHEMINFORM, Issue 12 2009Maria-Joao R. P. Queiroz Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] NaOH-Catalyzed Crossed Claisen Condensation Between Ketene Silyl Acetals and Methyl Esters.CHEMINFORM, Issue 45 2005Akira Iida Abstract For Abstract see ChemInform Abstract in Full Text. [source] A Novel Synthesis, Including Asymmetric Synthesis of ,-Quaternary ,-Amino Acid Methyl Esters from Ketones via Sulfinyloxiranes.CHEMINFORM, Issue 32 2005Tsuyoshi Satoh Abstract For Abstract see ChemInform Abstract in Full Text. [source] Improved Preparation and Structural Investigation of 4-Aryl-4-oxo-2-hydroxy-2-butenoic Acids and Methyl Esters.CHEMINFORM, Issue 47 2004Cedric Maurin Abstract For Abstract see ChemInform Abstract in Full Text. [source] A Novel Synthesis of Cyclic ,-Amino Aldehydes, Amino Alcohols, and ,-Amino Acid Methyl Esters from Cyclic Ketones Through Sulfinylaziridines.CHEMINFORM, Issue 34 2004Hiroyuki Ota Abstract For Abstract see ChemInform Abstract in Full Text. [source] A Versatile Synthesis of 6-Oxo-1,4,5,6-tetrahydro-pyrazine-2-carboxylic Acid Methyl Esters via MCR Chemistry.CHEMINFORM, Issue 21 2004Katrin Illgen Abstract For Abstract see ChemInform Abstract in Full Text. [source] ChemInform Abstract: Design, Synthesis, Photochemical Properties and Cytotoxic Activities of Water-Soluble Caged L-Leucyl-L-leucine Methyl Esters that Control Apoptosis of Immune Cells.CHEMINFORM, Issue 20 2002Hironori Mizuta Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] ChemInform Abstract: Synthesis of Substituted Hexa-3,5-dienoic Acid Methyl Esters from Conjugated Dienones.CHEMINFORM, Issue 43 2001Rishan Lang Nongkhlaw Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] Volatile Methyl Esters of Medium Chain Length from the Bacterium Chitinophaga Fx7914CHEMISTRY & BIODIVERSITY, Issue 9 2010Thorben Nawrath Abstract The analysis of the volatiles released by the novel bacterial isolate Chitinophaga Fx7914 revealed the presence of ca. 200 compounds including different methyl esters. These esters comprise monomethyl- and dimethyl-branched, saturated, and unsaturated fatty acid methyl esters that have not been described as bacterial volatiles before. More than 30 esters of medium C-chain length were identified, which belong to five main classes, methyl (S)-2-methylalkanoates (class A), methyl (S)-2,(,,1)-dimethylalkanoates (class B), methyl 2,(,,2)-dimethylalkanoates (class C), methyl (E)-2-methylalk-2-enoates (class D), and methyl (E)-2,(,,1)-dimethylalk-2-enoates (class E). The structures of the compounds were verified by GC/MS analysis and synthesis of the target compounds as methyl (S)-2-methyloctanoate (28), methyl (S)-2,7-dimethyloctanoate ((S)- 43), methyl 2,6-dimethyloctanoate (49), methyl (E)-2-methylnon-2-enoate (20a), and methyl (E)-2,7-dimethyloct-2-enoate (41a). Furthermore, the natural saturated 2-methyl-branched methyl esters showed (S)-configuration as confirmed by GC/MS experiments using chiral phases. Additionally, the biosynthetic pathway leading to the methyl esters was investigated by feeding experiments with labeled precursors. The Me group at C(2) is introduced by propanoate incorporation, while the methyl ester is formed from the respective carboxylic acid by a methyltransferase using S -adenosylmethionine (SAM). [source] Tritiation of CEP-1347 at high specific activity using several methodsJOURNAL OF LABELLED COMPOUNDS AND RADIOPHARMACEUTICALS, Issue 5 2005Judith A. Egan Abstract [Thiomethylenes- 3H] CEP-1347 (5) was synthesized by the tritiation of diformyl precursor 3 with NaB3H4 followed by treatment with ethanethiol. [Methyl ester- 3H] CEP-1347 (7) was prepared at even higher specific activity by the alkylation of precursor 6 with C3H3I. Copyright © 2005 John Wiley & Sons, Ltd. [source] Micro-reactor for transesterification of plant seed oilsEUROPEAN JOURNAL OF LIPID SCIENCE AND TECHNOLOGY, Issue 5 2009Phattaraporn Kaewkool Abstract The fatty acid compositions of vegetable or other plant seed oils are generally determined by gas chromatography (GC). Methyl esters (the most volatile derivatives) are the preferred derivatives for GC analysis. Esters of higher alcohols are good for the separation of volatile and positional isomers. All the esters of the C1,C8 alcohols of vegetable oils were silmilarly prepared by passing the reaction mixture containing the desired alcohol, oil and tetrahydrofuran through the micro-reactor (a 3-mL dispossible syringe packed with 0.5,g of NaOH powder). The reaction products were acidified with acetic acid and the mixture was analyzed by high-performance size exclusion chromatography and GC. Transesterification was quantitative for primary alcohols, but an appreciable amount of free fatty acids was formed for secondary alcohols. Coriander seed oil was quantitatively esterified with 2-ethyl 1-hexanol with the micro-reactor in less than 1,min. Oleic and petroselinic acid 2-ethyl 1-hexyl esters are baseline separated on an Rtx-2330 capillary column (30,m×0.25,mm, 0.25,µm film thickness). [source] Methyl esters of N -(dicyclohexyl)acetyl-piperidine-4-(benzylidene-4-carboxylic acids) as drugs and prodrugs: A new strategy for dual inhibition of 5,-reductase type 1 and type 2JOURNAL OF PHARMACEUTICAL SCIENCES, Issue 3 2005Martina Streiber Abstract Steroid 5,-reductase (5,R) inhibitory potency of three N -(dicyclohexyl)acetyl-piperidine-4-(benzylidene-4-carboxylic acids) and their corresponding methyl esters was monitored for type 2 isoenzyme in a benign prostatic hyperplasia cell free preparation and for type 1 isoenzyme in DU145 cells and in a cell free assay. The hydrolytic stability of the esters and their bioconversion to the corresponding acids was assessed in aqueous buffered solution (pH 7.4) and in selected biological media having measurable esterase activities. The carboxylic acids 1, 2, and 3 with high type 2 inhibitory potencies displayed only little type 1 inhibition. The esters 1a, 2a, and 3a, originally designed as prodrugs to enhance cell permeation, proved to be potent type 1 inhibitors and are therefore acting as drugs themselves. They are stable in buffered salt solution (pH 7.4), Caco-2 cells, and human plasma, whereas all esters are cleaved into the corresponding acids in benign prostatic hyperplasia tissue homogenate. Methyl esters, applied as hydrolytically stable precursor drugs to facilitate cell permeation, will yield the corresponding carboxylic acids as type 2 inhibitors after hydrolysis in the target organ. The esters themselves,stable in human plasma and Caco-2 cells,are acting as potent drugs toward 5,R type 1. Thus, dual inhibition of 5,R type 1 and type 2 can be achieved by applying a single parent compound. © 2004 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 94:473,480, 2005 [source] Lipid analysis of the sex pheromone gland of the moth Heliothis virescensARCHIVES OF INSECT BIOCHEMISTRY AND PHYSIOLOGY (ELECTRONIC), Issue 2 2005S.P. Foster Abstract The sex pheromone gland of female Heliothis virescens was analyzed for fatty acid and lipid content. Base methanolysis of the gland showed a large amount of methyl (Z)-11-hexadecenoate (Z11-16:Acyl), the fatty acyl analog of the major pheromone component, (Z)-11-hexadecenal, as well as a small amount of methyl (Z)-11-octadecenoate. Methyl esters of various common fatty acids were also observed. HPTLC analysis of the glandular lipids revealed large quantities of triacylglycerols (TGs), and lesser amounts of 1,2-diacylglycerols (1,2-DGs), 2- monoacylglycerols (2-MGs), phosphatidyl ethanolamines, and phosphatidyl cholines. The greatest amount of Z11-16:Acyl in these lipids was in the TGs, with lesser amounts in the two phospholipid classes and only trace amounts in the other neutral lipids. The glands of females at various ages and photoperiodic times were extracted, fractionated into neutral and polar fractions by silica SPE, and fatty acid titers in these fractions determined. All fatty acids, but notably Z11-16:Acyl, showed significant total and neutral lipid fraction peaks at mid scotophase for 2-day-old females; a less dramatic, but significant, Z11-16:Acyl peak in the polar fraction was also observed. However, only a relatively small proportion (<50%) of this acid was recovered from the silica at all times. This "non-recoverable" Z11-16:Acyl showed a dramatic and significant peak at mid scotophase for 2-day females, corresponding roughly with maximal pheromone titer. All other acids in the gland were recovered in high proportions, and their respective "non-recoverable" titers were not different at any of the times analyzed. Based on previous work, this non-recoverable Z11-16:Acyl is likely the CoA ester. Therefore, it appears that the pheromone gland of H. virescens maintains pools of Z11-16:Acyl in both CoA ester and TG forms, which are available for biosynthesis of pheromone. These pools are greatest during maximal pheromone production when the biosynthetic enzymes, possibly the fatty acid reductase, are unable to utilize rapidly enough the quantities of Z11-16:Acyl biosynthesized. Arch. Insect Biochem. Physiol. 59:80,90, 2005. © 2005 Wiley-Liss, Inc. [source] Nitric oxide bioavailability modulates the dynamics of microvascular oxygen exchange during recovery from contractionsACTA PHYSIOLOGICA, Issue 2 2010D. M. Hirai Abstract Aim:, Lowered microvascular PO2 (PO2mv) during the exercise off-transient likely impairs muscle metabolic recovery and limits the capacity to perform repetitive tasks. The current investigation explored the impact of altered nitric oxide (NO) bioavailability on PO2mv during recovery from contractions in healthy skeletal muscle. We hypothesized that increased NO bioavailability (sodium nitroprusside: SNP) would enhance PO2mv and speed its recovery kinetics while decreased NO bioavailability (l -nitro arginine methyl ester: l -NAME) would reduce PO2mv and slow its recovery kinetics. Methods:,PO2mv was measured by phosphorescence quenching during transitions (rest,1 Hz twitch-contractions for 3 min,recovery) in the spinotrapezius muscle of Sprague,Dawley rats under SNP (300 ,m), Krebs-Henseleit (Control) and l -NAME (1.5 mm) superfusion conditions. Results:, Relative to recovery in Control, SNP resulted in greater overall microvascular oxygenation as assessed by the area under the PO2mv curve (PO2 AREA; Control: 3471 ± 292 mmHg s; SNP: 4307 ± 282 mmHg s; P < 0.05) and faster off-kinetics as evidenced by the mean response time (MRToff; Control: 60.2 ± 6.9 s; SNP: 34.8 ± 5.7 s; P < 0.05), whereas l -NAME produced lower PO2 AREA (2339 ± 444 mmHg s; P < 0.05) and slower MRToff (86.6 ± 14.5 s; P < 0.05). Conclusion:, NO bioavailability plays a key role in determining the matching of O2 delivery-to-O2 uptake and thus the upstream O2 pressure driving capillary-myocyte O2 flux (i.e. PO2mv) following cessation of contractions in healthy skeletal muscle. Additionally, these data support a mechanistic link between reduced NO bioavailability and prolonged muscle metabolic recovery commonly observed in ageing and diseased populations. [source] Systemic nitric oxide clamping in normal humans guided by total peripheral resistanceACTA PHYSIOLOGICA, Issue 2 2010J. A. Simonsen Abstract Aim:, We wanted to stabilize the availability of nitric oxide (NO) at levels compatible with normal systemic haemodynamics to provide a model for studies of complex regulations in the absence of changes in NO levels. Methods:, Normal volunteers (23,28 years) were infused i.v. with the nitric oxide synthase (NOS) inhibitor NG -nitro- l -arginine methyl ester (l -NAME) at 0.5 mg kg,1 h,1. One hour later, the NO donor sodium nitroprusside (SNP) was co-infused in doses eliminating the haemodynamic effects of l -NAME. Haemodynamic measurements included blood pressure (MABP) and cardiac output (CO) by impedance cardiography. Results:,l -NAME increased MABP and total peripheral resistance (TPR, 1.02 ± 0.05 to 1.36 ± 0.07 mmHg s mL,1, mean ± SEM, P < 0.001). With SNP, TPR fell to a stable value slightly below control (0.92 ± 0.05 mmHg s mL,1, P < 0.05). CO decreased with l -NAME (5.8 ± 0.3 to 4.7 ± 0.3 L min,1, P < 0.01) and returned to control when SNP was added (6.0 ± 0.3 L min,1). A decrease in plasma noradrenaline (42%, P < 0.01) during l -NAME administration was completely reversed by SNP. Plasma renin activity decreased during l -NAME administration and returned towards normal after addition of SNP. In contrast, plasma aldosterone was increased by l -NAME and remained elevated. Conclusions:, Concomitant NOS inhibition and NO donor administration can be adjusted to maintain TPR at control level for hours. This approach may be useful in protocols in which stabilization of the peripheral supply of NO is required. However, the dissociation between renin and aldosterone secretion needs further investigation. [source] B2 kinin receptors mediate the Indian red scorpion venom-induced augmentation of visceral reflexes via the nitric oxide cyclic guanosine monophosphate pathwayACTA PHYSIOLOGICA, Issue 4 2009S. Kanoo Abstract Aim:, This study was performed to delineate the kinin (receptor)-dependent pathways in the Indian red scorpion (Mesobuthus tamulus; MBT) venom-induced pulmonary oedema as well as the augmentation of cardio-pulmonary reflexes evoked by phenyldiguanide (PDG). Methods:, In urethane-anaesthetized adult rats, the effect of venom on the PDG reflex responses (blood pressure, heart rate and respiration rate) and the pulmonary water content was ascertained using various antagonists(des- Arg, B1 receptor antagonist; Hoe 140, B2 receptor antagonist; N, -nitro- l -arginine methyl ester (l -NAME), nitric oxide (NO) synthase inhibitor; methylene blue, soluble guanylate cyclase inhibitor; and glibenclamide, K+ATP channel blocker). The effect of phosphodiesterase V inhibitor (sildenafil citrate) on the reflex response and the pulmonary water content was also examined and compared with venom-induced responses. Results:, Intravenous injection of PDG (10 ,g kg,1) evoked apnoea, bradycardia and hypotension lasting >60 s. Exposure to MBT venom (100 ,g kg,1) for 30 min augmented the PDG reflex responses by two times and increased the pulmonary water content, significantly. Hoe 140 blocked the venom-induced responses (augmentation of PDG reflex and increased pulmonary water content) whereas des-Arg did not. l -NAME, methylene blue or glibenclamide also blocked the venom-induced responses. Furthermore, sildenafil citrate (that increases cGMP levels) produced augmentation of PDG reflex response and increased the pulmonary water content as seen with venom. Conclusion:, The results indicate that venom-induced responses involve B2 kinin receptors via the NO-dependent guanylate cyclase-cGMP pathway involving K+ATP channels. [source] Role of neuronal nitric oxide synthase in response to hypertonic saline loading in ratsACTA PHYSIOLOGICA, Issue 4 2004R. Wangensteen Abstract Aims:, This study analyses the influence of neuronal nitric oxide synthase (nNOS) blockade with 7-nitroindazole (7NI) on the haemodynamic and renal response to a hypertonic saline load (HSL). We also evaluated the effects of non-specific NOS inhibitor N, -nitro- l -arginine methyl ester (l -NAME). Methods:, The following groups were used: controls, rats treated with 7NI at 0.5 or 5 mg kg,1, and rats treated with l -NAME at 0.5 or 5 mg kg,1. A further five groups received an isotonic saline load (ISL). Results:, Mean arterial pressure (MAP) was significantly increased in control rats after HSL. MAP was further increased in both 7NI-treated groups, and the l -NAME groups showed marked dose-related pressor responses. During ISL, MAP was only significantly increased in the group treated with 5 mg kg,1 of l -NAME. The pressure,natriuresis relationship during the experimental period after the HSL was reduced in the 7NI group treated with 5 mg kg,1 and severely attenuated in both l -NAME groups. The increase in plasma sodium was significantly greater after the HSL in both 7NI groups and both l -NAME groups compared with controls. Conclusions:, The present results suggest that nNOS and other NOS isozymes play a counter-regulatory role in the pressor response to HSL. Moreover, the blockade of nNOS with the higher dose of 7NI produces a blunted pressure,natriuresis relationship in response to the HSL. Finally, it is concluded that nNOS participates in the homeostatic cardiovascular and renal response to hypertonic saline loading by attenuating the blood pressure increase and hypernatremia, and facilitating natriuresis. [source] Thaliporphine protects ischemic and ischemic-reperfused rat hearts via an NO-dependent mechanismDRUG DEVELOPMENT RESEARCH, Issue 3 2001Li-Man Hung Abstract In ischemia or ischemia-reperfusion (I/R), nitric oxide (NO) can potentially exert several beneficial effects. Thaliporphine, a natural alkaloid with Ca2+ channel-activating and Na+/K+ channel-blocking activities, increased NO levels and exerted cardioprotective action in ischemic or I/R rats. The role of NO in the cardioprotective actions of thaliporphine was assessed. The severity of rhythm disturbances and mortality in anesthetized rats with either coronary artery occlusion for 30 min, or 5 min followed by 30-min reperfusion, were monitored and compared in thaliporphine- vs. placebo-treated groups. Thaliporphine treatment significantly increased NO and decreased lactate dehydrogenase (LDH) levels in the blood during the end period of ischemia or I/R. These changes in NO and LDH levels by thaliporphine were associated with a reduction in the incidence and duration of ventricular tachycardia (VT) and ventricular fibrillation (VF) during ischemic or I/R period. The mortality of animals was also completely prevented by 1 × 10,8 moles/kg of thaliporphine. In animals subjected to 4 h of left coronary artery occlusion, 1 × 10,7 moles/kg of thaliporphine dramatic reduced cardiac infarct zone from 46 ± 6% to 7.1 ± 1.9%. Inhibition of NO synthesis with 3.7 × 10,6 moles/kg of N, -nitro-L-arginine methyl ester (L-NAME) abolished the beneficial effects of thaliporphine during 30 min or 4 h myocardial ischemia. However, the antiarrhythmic activity and mortality reduction efficacy of thaliporphine during reperfusion after 5 min of ischemia was only partially antagonized by L-NAME. These results showed that thaliporphine efficiently exerted the cardioprotections either in acute or prolonged coronary artery occlusion or occlusion-reperfusion situations. The fact that thaliporphine induced cardioprotective effects were abrogated by L-NAME indicates that NO is an important mediator for the cardioprotective effects of thaliporphine in acute or prolonged ischemia, whereas antioxidant activities may contribute to the protection of I/R injury. Drug Dev. Res. 52:446,453, 2001. © 2001 Wiley-Liss, Inc. [source] Simple method for determination of cocaine and main metabolites in urine by CE coupled to MSELECTROPHORESIS, Issue 12 2009José Luiz da Costa Abstract In this work, a simple method for the simultaneous determination of cocaine (COC) and five COC metabolites (benzoylecgonine, cocaethylene (CET), anhydroecgonine, anhydroecgonine methyl ester and ecgonine methyl ester) in human urine using CE coupled to MS via electrospray ionization (CE-ESI-MS) was developed and validated. Formic acid at 1,mol/L concentration was used as electrolyte whereas formic acid at 0.05,mol/L concentration in 1:1 methanol:water composed the coaxial sheath liquid at the ESI nozzle. The developed method presented good linearity in the dynamic range from 250,ng/mL to 5000,ng/mL (coefficient of determination greater than 0.98 for all compounds). LODs (signal-to-noise ratio of 3) were 100,ng/mL for COC and CET and 250,ng/mL for the other studied metabolites whereas LOQ's (signal-to-noise ratio of 10) were 250,ng/mL for COC and CET and 500,ng/mL for all other compounds. Intra-day precision and recovery tests estimated at three different concentration levels (500, 1500 and 5000,ng/mL) provided RSD lower than 10% (except anhydroecgonine, 18% RSD) and recoveries from 83,109% for all analytes. The method was successfully applied to real cases. For the positive urine samples, the presence of COC and its metabolites was further confirmed by MS/MS experiments. [source] Electroenzymatic Synthesis of Chiral SulfoxidesENGINEERING IN LIFE SCIENCES (ELECTRONIC), Issue 2 2006C. Kohlmann Abstract Chloroperoxidase (CPO) from Caldariomyces fumago (E.C.,1.11.1.10) is able to enantioselectively oxidize various sulfides to the corresponding (R)-enantiomer of the sulfoxides. For these oxidations the enzyme requires an oxidant. Most commonly, tert -butyl hydroperoxide (TBHP) and hydrogen peroxide are used. As it is known that these oxidants inactivate the enzyme, the enzymatic reaction was combined with the electrochemical in situ generation of hydrogen peroxide. As substrates for this combination of an enzymatic and an electrochemical reaction methyl p-tolyl sulfide, 1-methoxy-4-(methylthio)benzene and N-MOC- L -methionine methyl ester were used to carry out batch experiments. [source] Bacterial community structure and function in a metal-working fluidENVIRONMENTAL MICROBIOLOGY, Issue 6 2003Christopher J. Van Der Gast Summary The diversity of bacterial populations colonizing spatially and temporally separated samples of the same metal-working fluid (MWF) formulation was investigated. Analyses were performed with a view to improve strategies for bioaugmentation of waste MWF in bioreactor systems and prevention of in-use MWF biodeterioration in engineering workshops. Significantly, complementary phenotypic, genotypic and in situ methods revealed that the bacterial communities in operationally exhausted MWFs had low diversity and were similar in species composition from different locations and uses. Of the 179 bacterial isolates studied, only 11 genera and 15 species were identified using fatty acid methyl ester (FAME) analysis, with culture independent analyses by 16S rDNA denaturing gradient gel electrophoresis (DGGE) and fluorescent in situ hybridization being congruent with these FAME data. In order to gain some insight into functional role of detected populations, we correlated the MWF chemical composition and potential pollution load with bacterial abundance and community composition detected within samples. [source] |