scholarly journals New Amphiphilic Amino Acid Derivatives for Efficient DNA Transfection <i>in Vitro</i>

2017 ◽  
Vol 07 (02) ◽  
pp. 191-205 ◽  
Author(s):  
Lucía C. Peña ◽  
María F. Argarañá ◽  
María M. De Zan ◽  
Antonella Giorello ◽  
Sebastián Antuña ◽  
...  
Keyword(s):  
Amino Acid ◽  
Amino Acid Derivatives ◽  
Dna Transfection ◽  
Amphiphilic Amino Acid

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.

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

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.

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

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

Synthesis of thiosulphonate and amino acid derivatives of benzochinone and predicted screening of their biological activity

2021 ◽  
Vol 4 (2) ◽  
pp. 40-46
Author(s):  
N. Y. Monka ◽  
◽  
L. R. Zhurakhivska ◽  
M. S. Kurka ◽  
G. B. Shiуan ◽  
...  
Keyword(s):  
Biological Activity ◽  
Amino Acid ◽  
Experimental Studies ◽  
Physicochemical Characteristics ◽  
Biologically Active ◽  
Amino Acid Derivatives ◽  
Online Resource ◽  
Methods Of Synthesis ◽  
Pass Online

Quinoid derivatives are attractive not only as interesting synthons for synthesis, but also as potential biologically active substances, so it is important to modify the compounds of the quinone series with different pharmacoform fragments. In this work, the structural design of chlorine and bromanyl disulfur-containing fragments, namely thiosulfonate, and chloranyl – a fragment of 4- aminobutanoic acid. Methods of synthesis were developed and physicochemical characteristics of thiosulfonate and amino acid derivatives were studied: 2,5-bis (thiosulfonate) -3,6-halogen -1,4- benzoquinones and 2,5-bis (3-carboxypropylamino) -3,6 - dichlorobenzoquinone. The prospects for the design of chlorine and bromanyl thiosulfonate fragments and chloranyl fragment of 4- aminobutanoic acid are confirmed by the results of predicting the biological activity of 5 a, b, 6 a, b, 7 using the online resource PASS Online. In particular, the substance 6a obtained by us is promising in terms of research on Antiviral (Picornavirus). The obtained results of predicted cytotoxicity screening indicate the feasibility of conducting experimental studies by in vitro methods on anticancer activity against cancer cell lines of hematopoietic and lymphoid tissue, lungs, skin, ovaries, blood, breast, kidney, colon, brain.

scholarly journals Amino Acid Derivatives as Palmitoylethanolamide Prodrugs: Synthesis, In Vitro Metabolism and In Vivo Plasma Profile in Rats

PLoS ONE ◽  
2015 ◽  
Vol 10 (6) ◽  
pp. e0128699 ◽  
Author(s):  
Federica Vacondio ◽  
Michele Bassi ◽  
Claudia Silva ◽  
Riccardo Castelli ◽  
Caterina Carmi ◽  
...  
Keyword(s):  
Amino Acid ◽  
In Vitro Metabolism ◽  
Amino Acid Derivatives ◽  
Plasma Profile

scholarly journals Synthesis and Anti-Hepatocarcinoma Effect of Amino Acid Derivatives of Pyxinol and Ocotillol

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 780
Author(s):  
Ying Zhang ◽  
Hui Yu ◽  
Shuzheng Fu ◽  
Luying Tan ◽  
Junli Liu ◽  
...  
Keyword(s):  
Amino Acid ◽  
Human Cancer ◽  
Ultra Performance Liquid Chromatography ◽  
Amino Acid Derivatives ◽  
Flight Mass Spectrometry ◽  
Liver And Kidney ◽  
Derivatives Of ◽  
Cancer Activity

Aiming at seeking an effective anti-hepatocarcinoma drug with low toxicity, a total of 24 amino acid derivatives (20 new along with 4 known derivatives) of two active ocotillol-type sapogenins (pyxinol and ocotillol) were synthesized. Both in vitro and in vivo anti-hepatocarcinoma effects of derivatives were evaluated. At first, the HepG2 human cancer cell was employed to evaluate the anti-cancer activity. Most of the derivatives showed obvious enhanced activity compared with pyxinol or ocotillol. Among them, compound 2e displayed the most excellent activity with an IC50 value of 11.26 ± 0.43 µM. Next, H22 hepatoma-bearing mice were used to further evaluate the anti-liver cancer activity of compound 2e. It was revealed that the growth of H22 transplanted tumor was significantly inhibited when treated with compound 2e or compound 2e combined with cyclophosphamide (CTX) (p < 0.05, p < 0.01), and the inhibition rates of tumor growth were 35.32% and 55.30%, respectively. More importantly, compound 2e caused limited damage to liver and kidney in contrast with CTX causing significant toxicity. Finally, the latent mechanism of compound 2e was explored by serum and liver metabolomics based on ultra-performance liquid chromatography quadrupole time-of-flight mass spectrometry (UPLC-QTOF-MS) technology. A total of 21 potential metabolites involved in 8 pathways were identified. These results suggest that compound 2e is a promising agent for anti-hepato-carcinoma, and that it also could be used in combination with CTX to increase efficiency and to reduce toxicity.

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