Synthesis, in vitro cytotoxicity activity against the human cervix carcinoma cell line and in silico computational predictions of new 4-arylamino-3-nitrocoumarin analogues

2020 ◽  
Vol 1200 ◽  
pp. 127047 ◽  
Author(s):  
Ahmed H. Halawa ◽  
Essam M. Eliwa ◽  
Ahmed A. Hassan ◽  
Hesham S. Nassar ◽  
R.A. El-Eisawy ◽  
...  
1993 ◽  
Vol 289 (2) ◽  
pp. 357-361 ◽  
Author(s):  
G Werner-Felmayer ◽  
E R Werner ◽  
D Fuchs ◽  
A Hausen ◽  
B Mayer ◽  
...  

We show here that the human cervix carcinoma cell line ME-180 expresses a constitutive nitric oxide (NO) synthase, as demonstrated by formation of [3H]citrulline and nitrite. The enzyme is dependent on tetrahydrobiopterin, NADPH, flavins and Ca2+/calmodulin. Enzyme activity is located in the cytosol rather than in the membrane fraction and can be inhibited by NG-monomethyl-L-arginine (NMMA). An antiserum to NO synthase purified from porcine cerebellum inhibited the enzyme activity. ME-180 cells released NO, as was shown by stimulation of guanylate cyclase (EC 4.6.1.2) in RFL-6 detector cells; this release was stimulated 8-fold by the Ca2+ ionophore A23187 and 2-fold by increasing the intracellular tetrahydrobiopterin levels with cytokines. This is the first characterization of a Ca2+/calmodulin-dependent NO synthase activity in human epithelial-type tumour cells.


2019 ◽  
Vol 74 (5-6) ◽  
pp. 131-137 ◽  
Author(s):  
Abdelaaty Hamed ◽  
Mohamed Ismail ◽  
Mohammad M. El-Metwally ◽  
Marcel Frese ◽  
Tarek M.A. Ibrahim ◽  
...  

Abstract As a continuation of our earlier research concerning the investigation of microbial bioactive secondary metabolites from the terrestrial Penicillium sp.KH Link 1809 isolate KHMM, the fungus was re-cultivated on a large scale to explore its bioactive compounds intensively. Fifteen compounds, including seven alkaloids (1–7), one sesquiterpene (8), an acetylenic system (9), two sterols, and sphengolipid, were identified. Their structures were established on the bases of extensive one- and two-dimensional nuclear magnetic resonance and mass measurements, and by comparison with literature data. The antimicrobial activity of the fungal extract and the corresponding compounds were studied using a panel of pathogenic microorganisms, and their in vitro cytotoxicity against the human cervix carcinoma cell line (KB-3-1) was reported as well. The molecular docking of the isolated compounds showed promising affinities for the alkaloidal compounds 4–6 towards α, β tubulins.


2015 ◽  
Vol 25 (2) ◽  
pp. 303-309 ◽  
Author(s):  
Marília R. Simão ◽  
Luiza J. Carneiro ◽  
Raquel A. dos Santos ◽  
Jairo K. Bastos ◽  
Rodrigo C. S. Veneziani ◽  
...  

2018 ◽  
Vol 2018 ◽  
pp. 1-10 ◽  
Author(s):  
Mohamed Shaaban ◽  
Mahmoud Ali ◽  
Michel Feussi Tala ◽  
Abdelaaty Hamed ◽  
Amal Zaki Hassan

This study deals with the ecology, phytochemistry, and biological activity investigation of Euphorbia retusa, belonging to Euphorbiaceae family, obtained from Egypt. Ecologically, Euphorbia retusa secretes white sap inhibiting the growth of the other species, so Euphorbia retusa is forming complete patches. Phytochemical study of the plant was visualized intensively based on its extraction with a protic organic solvent, working up and purifying its entire bioactive compounds using a series of different chromatographic techniques. A broad range of diverse compounds were isolated, namely, 1-hexacosanol (1), 3β-hydroxy-24-methylene-9,19-cyclolanostane; 24-methylenecycloartanol (2), 3β-hydroxy-9,19-cyclolanostane; cyclolaudanol (3), 3β,24S-Ergost-5-en-ol (4), and methyllinoleate. Additionally, GC-MS analysis of the unpolar fractions detected the existence of n-dodecane, methyllaurate, 6,10,14-trimethyl-pentadecan-2-one (5), 6,10-dimethyl-undecan-2-one (6), 2-methyl-hexadecanal (7), methylpalmitate, methyl-9,12,15-octadecatrienoate (8), and n-heneicosane (9). A full assignment for compounds 2 and 3 using 1 and 2 DNMR was carried out herein for the first time. The antimicrobial activity of the strain extract and obtained compounds was studied using a panel of pathogenic bacterial strains. The in vitro cytotoxicity of the compounds as well as the crude extract was studied against the human cervix carcinoma cell line (KB-3-1).


2020 ◽  
Vol 10 (6) ◽  
pp. 145-148
Author(s):  
Brajesh Kumar ◽  
Abhishek Suman

5-carbethoxy-2-thiouracil (eitotH2) reacts with CuX (X= Cl, Br, I) halides to give the formula [CuX(eitotH)2]2 dinuclear complexes, while the formula [CuX(PPh3)2(eitotH)2] mononuclear mixed ligand complexes result when reaction is carried out in the presence of two equivalent of triphenylphosphine (PPh3). The new copper (I) complexes were studied against two tumor cell lines, A549 (human pulmonary carcinoma cell line) and HeLa (human epithelial carcinoma cell line) and one regular immortalized cell line, MRC5 (human fetal lung fibroblast). In comparison to the phosphine free ones that hindered cell proliferation only at relatively high concentration, the mixed ligand complexes with triphenylphosphine were found to be extremely cytotoxic. Keywords: Copper (I), 5-carbethoxy-2-thiouracil (eitotH2), Triphenylphosphine, in vitro cytotoxicity, carcinoma cell lines


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