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1.
We evaluated VER effect on RNA synthesis of quiescent and angiotensin II (AII)- stimulated cultured rat aortic vascular smooth muscle cells (VSMC). In a dose-dependent manner, VER decreased [3H]uridine uptake by quiescent VSMCs (ED50 7 x 10(-6)M), an effect that was shared by other calcium antagonists, but to a variable degree. VER caused a significant effect within 3 hours and attained a maximal effect at 7 hours. In addition VER caused a 22 +/- 2% decrease in [3H]uridine uptake by VSMCs stimulated with 10% fetal bovine serum, while it completely abolished [3H]uridine uptake by VSMCs induced by AII. We conclude that VER decreases basal and inhibits AII-induced increase in mRNA synthesis of VSMCs. These data may explain in part how VER causes a decrease in vascular resistance and alters the vasoconstrictor effect of AII. 相似文献
2.
3.
The decomposition of the amidinohydrazone-type insecticide Hydramethylnon (HMN) by soil fungi has been investigated. A simple spectrophotometric method was developed for the estimation of HMN in soil and fungal culture media. HMN was found to be degraded in soil with a half life of 14 to 25 days.Degradation of HMN by the lignolytic fungus,Phanerochaete chrysosporium yielded two major breakdown products;p-(trifluoromethyl)-cinnamic acid (TFCA) andp-(trifluoromethyl)-benzoic acid (TFBA). TFCA was converted to TFBA which was subsequently metabolised via themeta-fission pathway. Fluoride release from HMN could not be detected.Abbreviations BzDAc
benzene, dioxane, acetic acid (60: 36: 4)
- DCM
dichloroethane
- DNPH
2,4-dinitro-phenylhydrazine
- HMN
Hydramethylnon
- TDAc
toluene, dioxane, acetic acid (90: 30: 1)
- TFCA
p-(trifluoromethyl)-cinnamic acid
- TFBA
p-(trifluoromethyl)-benzoic acid
- TFP
1,5-bis(trifluoro-p-tolyl)-1,4-pentadien-3-one
- VA
veratryl alcohol 相似文献
4.
John Leo Abernethy Charles M. Lovett Anton Haddad Jeff D. Felberg 《Bioorganic chemistry》1982,11(3):251-261
Acylated crude papain has been shown to exert stereoselective behavior toward racemic hydrazides devoid of an amino acid residue, namely, (RS)-mandelic and (RS)-atrolactic hydrazides. These hydrazides functioned as nucleophiles to yield N1,N2-diacylhydrazines. Several achiral acylating agents for the enzyme were chosen, including Z-glycine, BOC-glycine, AOC-glycine, and hippuric acid. With the exception of hippuric acid as the acylating agent, the reaction product, in every instance for these achiral hydrazides, consisted of an excess of the (+)-N1,N2-diacylhydrazine. The relative rates of product formation for the mandelic hydrazides were considerably greater than for corresponding reactions with racemic atrolactic hydrazide. When chiral Z-l-alanine was employed to acylate crude papain, the stereoselective action was most pronounced, with the formation of a mixture of diastereoisomers consisting of 73% N1-(Z-l-alanyl)-N2-[(R)-mandelyl]hydrazine. The relative reactivities for the electrophiles was Z-l-alanine ? Z-glycine ? hippuric acid ? AOC-glycine > BOC-glycine. The hydrazides of (R)-, (S)-mandelic, and (RS)-atrolactic acids were prepared by conversion of the corresponding acids to their esters by means of a catalytic dehydrating agent and subsequent treatment with a methanolic solution of hydrazine. 相似文献
5.
John Leo Abernethy Gary F. Kuzmin Charles M. Lovett Jr. William A. Wilson 《Bioorganic chemistry》1980,9(4):440-449
Hydrazides of five N-acylamino acids have been used alone as substrates for papain catalysis to yield N1,N2-diacylhydrazines. With the exception of N-(benzyloxycarbonyl)(Z)-
-alanine hydrazide, they were very effective as both acylating agents of the enzyme and nucleophiles in attacking the enzyme-substrate intermediate. Although Z-
-alanine hydrazide was a minimal acylating agent, it was a satisfactory nucleophile. The most favorable reaction involved Z-
-alanine hydrazide in producing N1,N2-bis(Z-
-alanyl)hydrazine. When Z-
-alanine hydrazide was the substrate, this same chiral diacylhydrazine was formed along with meso N1-(Z-
-alanyl)-N2-(Z-
-alanyl)hydrazine. For the acylation step, the enzyme displayed powerful, essentially stereospecific, bias toward the
enantiomer. Once the thioester intermediate was formed, little preference was detected for attack by the enantiomers as nucleophiles. The most direct procedure for synthesis of substrates was conversion of Z-amino acids to their esters by means of dry HCl in an absolute alcohol. Treatment with hydrazine produced the hydrazides in excellent yield. 相似文献
6.
Graeme D. Coles D. J. Abernethy Mary C. Christey A. J. Conner B. K. Sinclair 《Plant Molecular Biology Reporter》1991,9(1):13-20
Hairy roots, incited byAgrobacterium rhizogenes, form a useful system for analysing the expression and phenotypic effects of foreign genes in plant root tissue. Image analysis
offers a non-invasive method of describing their growth in culture. Images of pea (coarse) andBrassica (fine) hairy roots were captured, processed and analysed without difficulty using a commercially available image analysis
system. The value of this method in monitoring intermediate changes in growth pattern was illustrated by following the changes
in five putatively chlorsulfuron-resistantBrassicc hairy-root lines cultured with and without a selective level of chlorsulfuron. Areas of hairy-root research where this technique
will be particularly useful are discussed. 相似文献
7.
8.
John Leo Abernethy Charles M. Lovett Gary F. Kuzmin John D. Kuhlberg William A. Wilson 《Bioorganic chemistry》1981,10(2):189-199
Restriction of hydrazides of N-blocked amino acids mainly to electrophilic action, in acylating crude papain, has been achieved by means of a large amount of aniline, with formation of insoluble anilides of N-acylamino acids. Similarly, nucleophilic behavior, on the part of a hydrazide, has been promoted by introducing a large proportion of an N-acylamino acid to produce an insoluble N1,N2-diacylhydrazine. Achiral, chiral and racemic hydrazides and their corresponding N-acylamino acids were utilized in the study. Among the more informative combinations of reactants were Z-dl-alanine hydrazide with aniline and then with Z-glycine. A stereospecific response in the former situation produced Z-l-alanine anilide. In the latter case, a stereoselective interaction produced Z-Gly-NHNH-lAla-Z more rapidly than Z-Gly-NHNH-d-Ala-Z. The final incubation period yielded an optically pure D product. Differences in stereochemical control have been delineated in terms of different spatial aspects for interactions at the S and S′ subsites of sulfhydryl proteolytic enzymes. A racemic reactant encountered firm stereospecificity as an electrophile at the S subsite but only modest stereoselectivity as a nucleophile at the S′ subsite. The ready availability of crude papain allows an effective procedure for the synthesis of substantial quantities of diacylhydrazines. 相似文献
9.
Suzanne M. Marselis Katharine Abernethy Alfonso Alonso John Armston Timothy R. Baker Jean‐Francois Bastin Jan Bogaert Doreen S. Boyd Pascal Boeckx David F. R. P. Burslem Robin Chazdon David B. Clark David Coomes Laura Duncanson Steven Hancock Ross Hill Chris Hopkinson Elizabeth Kearsley James R. Kellner David Kenfack Nicolas Labrire Simon L. Lewis David Minor Herv Memiaghe Abel Monteagudo Reuben Nilus Michael O'Brien Oliver L. Phillips John Poulsen Hao Tang Hans Verbeeck Ralph Dubayah 《Global Ecology and Biogeography》2020,29(10):1799-1816
10.
Contradictory statements about the non-steroidal anti-inflammatory drugs from the European Medicines Agency and the United States Food and Drug Administration have raised questions about whether regulatory decisions are evidence-based. For the selective COX-2 inhibitors, there are clear contraindications and warnings in Europe, but only a vaguely worded Black Box warning in the United States. All the non-selective agents are given an almost "clean bill of health" in Europe, while all of them are judged to have a similar risk-benefit ratio as celecoxib in the United States. The regulatory agencies have failed to recognize the clinical trial evidence that the risk of cardiovascular events varies substantially among the non-selective agents, with diclofenac carrying the highest risk of harm. 相似文献