scholarly journals Middle Molecular Weight Heparinyl Amino Acid Derivatives (MHADs) Function as Indirect Radical Scavengers <i>in Vitro</i>

2016 ◽  
Vol 07 (03) ◽  
pp. 117-123
Author(s):  
Seiichi Takeda ◽  
Takao Toda ◽  
Kazuki Nakamura
Keyword(s):  
Molecular Weight ◽  
Amino Acid ◽  
Amino Acid Derivatives ◽  
Radical Scavengers

scholarly journals Studies on antimetastatic effects of middle molecular weight heparinyl amino acid derivatives using in vitro chemo-invasion assay and in vivo experimental metastatic assay.

1996 ◽  
Vol 71 ◽  
pp. 295
Author(s):  
Kazuki NAKAMURA ◽  
Shuichi TANAKA ◽  
Seiichi TAKEDA ◽  
Kenzo KAWAI ◽  
Chiaki SHIMADA ◽  
...  
Keyword(s):  
Molecular Weight ◽  
Amino Acid ◽  
Amino Acid Derivatives ◽  
Invasion Assay

scholarly journals In vitro anticancer potentiality and molecular modelling study of novel amino acid derivatives based on N1,N3-bis-(1-hydrazinyl-1-oxopropan-2-yl) isophthalamide

2019 ◽  
Vol 34 (1) ◽  
pp. 1247-1258 ◽  
Author(s):  
Asmaa F. Kassem ◽  
Gaber O. Moustafa ◽  
Eman S. Nossier ◽  
Hemat S. Khalaf ◽  
Marwa M. Mounier ◽  
...  
Keyword(s):  
Amino Acid ◽  
Molecular Modelling ◽  
Amino Acid Derivatives ◽  
Modelling Study

scholarly journals Novel Amino Acid Derivatives of Quinolines as Potential Antibacterial and Fluorophore Agents

2020 ◽  
Vol 88 (4) ◽  
pp. 57
Author(s):  
Oussama Moussaoui ◽  
Rajendra Bhadane ◽  
Riham Sghyar ◽  
El Mestafa El Hadrami ◽  
Soukaina El Amrani ◽  
...  
Keyword(s):  
Amino Acid ◽  
Methyl Esters ◽  
Amino Acid Derivatives ◽  
Bacterial Strains ◽  
Fluorescent Properties ◽  
Topoisomerase Iv ◽  
Microdilution Method ◽  
Hydrolysis Of ◽  
Derivatives Of

A new series of amino acid derivatives of quinolines was synthesized through the hydrolysis of amino acid methyl esters of quinoline carboxamides with alkali hydroxide. The compounds were purified on silica gel by column chromatography and further characterized by TLC, NMR and ESI-TOF mass spectrometry. All compounds were screened for in vitro antimicrobial activity against different bacterial strains using the microdilution method. Most of the synthesized amino acid-quinolines show more potent or equipotent inhibitory action against the tested bacteria than their correspond esters. In addition, many of them exhibit fluorescent properties and could possibly be utilized as fluorophores. Molecular docking and simulation studies of the compounds at putative bacterial target enzymes suggest that the antimicrobial potency of these synthesized analogues could be due to enzyme inhibition via their favorable binding at the fluoroquinolone binding site at the GyrA subunit of DNA gyrase and/or the ParC subunit of topoisomerase-IV.

A Favorable, Narrow, δh Hansen-Parameter Domain for Gelation of Low-Molecular-Weight Amino Acid Derivatives

2011 ◽  
Vol 17 (48) ◽  
pp. 13603-13612 ◽  
Author(s):  
Pasquale Curcio ◽  
Florent Allix ◽  
Guillaume Pickaert ◽  
Brigitte Jamart-Grégoire
Keyword(s):  
Molecular Weight ◽  
Amino Acid ◽  
Amino Acid Derivatives ◽  
Low Molecular Weight ◽  
Parameter Domain

In vitro studies on the inhibition of colon cancer by amino acid derivatives of bromothiazole

2017 ◽  
Vol 27 (15) ◽  
pp. 3507-3510 ◽  
Author(s):  
Nuno Vale ◽  
Ana Correia-Branco ◽  
Bárbara Patrício ◽  
Diana Duarte ◽  
Fátima Martel
Keyword(s):  
Colon Cancer ◽  
Amino Acid ◽  
In Vitro Studies ◽  
Amino Acid Derivatives ◽  
Derivatives Of

Trans-tegumental absorption of L-alanine and L-leucine by a monogenean, Diclidophora merlangi

Parasitology ◽  
1978 ◽  
Vol 76 (1) ◽  
pp. 29-37 ◽  
Author(s):  
D. W. Halton
Keyword(s):  
Amino Acids ◽  
Molecular Weight ◽  
Amino Acid ◽  
Sea Water ◽  
Low Molecular Weight ◽  
Acid Uptake ◽  
Neutral Amino Acids ◽  
Freeze Dried ◽  
Significant Difference

SummaryAn in vitro investigation has been made of the relative roles of the gut and tegument in the absorption of the neutral amino acids L-alanine and L-leucine by a marine fish-gill parasite, Diclidophora merlangi. The use of ligatures to preclude oral ingestion of trace-labelled medium has proved inadequate, invariably damaging the tegument, as revealed by stereoscan electron microscopy, and resulting in artifactual levels of absorption. Three alternative procedures have given consistently reliable data on the route of entry of low molecular weight substrates. (1) Ultrastructural examination of worms previously incubated in electron-dense cationic tracers has shown that, in vitro, there is no oral intake of sea water. (2) The suspending of worms in trace-labelled medium with the mouth out of the medium and comparing amino acid uptake with that of worms totally immersed in medium has revealed no statistically significant difference in the absorption levels. (3) Application of section (freeze-dried) auto-radiography to detect diffusible isotope has demonstrated directly transtegumental absorption of a neutral amino acid. It is concluded from these experiments that Diclidophora has a tegumental transport system for absorbing certain neutral amino acids, and whilst, clearly, the worm is sanguinivorous and digests blood in a well-developed gut, it may also be capable of supplementing this diet with low molecular weight organic nutrient absorbed directly from sea water via the tegument.

scholarly journals Molecular cloning and sequence of a cholesterol-repressible enzyme related to prenyltransferase in the isoprene biosynthetic pathway.

1987 ◽  
Vol 7 (9) ◽  
pp. 3138-3146 ◽  
Author(s):  
C F Clarke ◽  
R D Tanaka ◽  
K Svenson ◽  
M Wamsley ◽  
A M Fogelman ◽  
...  
Keyword(s):  
Molecular Weight ◽  
Amino Acid ◽  
Molecular Cloning ◽  
In Vitro Transcription ◽  
In Vitro Translation ◽  
Mrna Levels ◽  
Hmg Coa Reductase ◽  
Transcription System ◽  
Coa Reductase

Differential hybridization and molecular cloning have been used to isolate CR39, a cDNA which hybridizes to a 1.2-kilobase (kb) mRNA in rat liver. The level of CR39 mRNA was increased seven- to ninefold over normal levels by dietary cholestyramine and mevinolin and decreased about fourfold compared with normal levels by cholesterol feeding or administration of mevalonate. Similar changes in the mRNA levels of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase and HMG-CoA synthase were observed under the various conditions. In vitro translation of either CR39 hybrid selected RNA or 1.2-kb CR39 RNA generated by an SP6 in vitro transcription system produced a polypeptide of 39,000 daltons. As deduced from the nucleotide sequence of a full-length CR39 cDNA, the rat CR39 polypeptide contained 344 amino acids and had a molecular weight of 39,615. The predicted amino acid composition and submit molecular weight of the rat CR39 were very similar to those of prenyltransferases isolated from chicken, pig, and human. The sequence of amino acid residues 173 through 203 in the rat CR39 polypeptide showed that 17 out of 30 matched an active-site peptide of avian liver prenyltransferase. Thus, alterations in the rate of cholesterogenesis resulted in the coordinate regulation of three mRNAs encoding HMG-CoA reductase, HMG-CoA synthase, and CR39, the latter being tentatively identified as prenyltransferase.

scholarly journals Circular-dichroic studies on the conformational behaviour of troponin and tropomyosin from bovine cardiac muscle

1978 ◽  
Vol 175 (1) ◽  
pp. 137-147 ◽  
Author(s):  
T I Lin ◽  
J Y Cassim
Keyword(s):  
Molecular Weight ◽  
Biological Activity ◽  
Amino Acid ◽  
Conformational Changes ◽  
Cardiac Troponin ◽  
Surface Charges ◽  
Troponin Complex ◽  
Induced Changes ◽  
Circular Dichroic

Bovine cardiac troponin is similar to rabbit skeletal troponin with respect to secondary structure, amino acid composition and molecular weight of the subunits, but differs slightly with respect to biological activity and surface charges of the subunits. Previous circular-dichroic studies of the subunits and recombination of subunits have indicated significant Ca2+-induced delocalized conformational changes. Present studies of the native troponin complex are not in accord with such changes. Furthermore the formation of the troponin-tropomyosin complex in vitro results in no delocalized conformational changes, nor does it sensitize troponin to Ca2+-induced changes. It is suggested that the troponin complex cannot be dissociated into subunits without significant and irreversible conformational perturbation.

scholarly journals Research in vivo the qualities of potential antitumor amino-acid derivatives of glycosides of indolocarbazol

2017 ◽  
Vol 16 (4) ◽  
pp. 85-92 ◽  
Author(s):  
I. S. Golubeva ◽  
N. P. Yavorskaya ◽  
O. V. Goryunova
Keyword(s):  
Amino Acid ◽  
Antitumor Activity ◽  
Optimal Dose ◽  
Amino Acid Derivatives ◽  
Tumor Growth Inhibition ◽  
Active Metabolites ◽  
Derivatives Of ◽  
Potential Antitumor

Background. The addition of active metabolites (in particular, amino acids) to the molecule affects the physicochemical and prodrug properties of derivatives of indolocarbazoles. Using computed chemoinformatics, probability antitumor activity of amino-acid derivatives of glycosides of indolocarbazol (AADGI) is predicted with low probability of their cytotoxic activity in vitro. Based on these data, a study of these compounds in vivo is conducted. Objective: the assessment of AADGI as potential antitumor medications. Materials and methods. Research antitumor activity of AADGI was done using murine tumor models - cervical cancer CC-5. Investigated compounds were injected to mice СВА abdominally 5-times daily with interval of 24 h. Observation of animals were continued till their death. Antitumor effect of compounds was assessed by criteria of tumor growth inhibition and increase in life expectancy of mice comparing to control animals. Results. The optimal dose for these series of compounds was titrated and this dose is 100 mg/kg. Antitumor activity of AADGI was assessed on CC-5. Conclusions. Based on data received we suggest an extended study in vivo of antitumor qualities of selected 5 leader AADGI.

Synthesis and in vitro cytotoxicity evaluation of baicalein amino acid derivatives

2014 ◽  
Vol 11 (3) ◽  
pp. 284-288 ◽  
Author(s):  
Lei LI ◽  
Wen-Yuan LIU ◽  
Feng FENG ◽  
Chun-Yong WU ◽  
Ning XIE
Keyword(s):  
Amino Acid ◽  
In Vitro Cytotoxicity ◽  
Amino Acid Derivatives
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