Identification, Prokaryote Expression of Medaka gdnfa/b and Their Biological Activity in a Spermatogonial Cell Line

2017 ◽  
Vol 26 (3) ◽  
pp. 197-205 ◽  
Author(s):  
Jing Wei ◽  
Linyan Liu ◽  
Zhenhua Fan ◽  
Yunhan Hong ◽  
Yang Zhao ◽  
...  
2018 ◽  
Vol 15 (2) ◽  
pp. 286-296 ◽  
Author(s):  
Mohamed K. Awad ◽  
Mahmoud F. Abdel-Aal ◽  
Faten M. Atlam ◽  
Hend A. Hekal

Aim and Objective: Synthesis of new .-aminophosphonates containing quinazoline moiety through Kabachnik-Fields reaction in the presence of copper triflate catalyst [32], followed by studying their antimicrobial activities and in vitro anticancer activities against liver carcinoma cell line (HepG2) with the hope that new anticancer agents could be developed. Also, the quantum chemical calculations are performed using density functional theory (DFT) to study the effect of the changes of molecular and electronic structures on the biological activity of the investigated compounds. Materials and Method: The structures of the synthesized compounds are confirmed by FT-IR, 1H NMR, 13C NMR, 31P NMR and MS spectral data. The synthesized compounds show significant antimicrobial and also remarkable cytotoxicity anticancer activities against liver carcinoma cell line (HepG2). Density functional theory (DFT) was performed to study the effect of the molecular and electronic structure changes on the biological activity. Results: It was found that the electronic structure of the substituents affects on the reaction yield. The electron withdrawing substituent, NO2 group 3b, on the aromatic aldehydes gave a good yield more than the electron donating substituent, OH group 3c. The electron deficient on the carbon atom of the aldehydic group may increase the interaction of the Lewis acid (Cu(OTf)2) and the Lewis base (imine nitrogen), and accordingly, facilitate the formation of imine easily, which is attacked by the nucleophilic phosphite species to give the α- aminophosphonates. Conclusion: The newly synthesized compounds exhibit a remarkable inhibition of the growth of Grampositive, Gram-negative bacteria and fungi at low concentrations. The cytotoxicity of the synthesized compounds showed a significant cytotoxicity against the liver cancer cell line (HepG 2). Also, it was shown from the quantum chemical calculations that the electron-withdrawing substituent increases the biological activity of the α-aminophosphonates more than the electron donating group which was in a good agreement with the experimental results. Also, a good agreement between the experimental FT-IR and the calculated one was found.


RSC Advances ◽  
2017 ◽  
Vol 7 (9) ◽  
pp. 5282-5296 ◽  
Author(s):  
Marija S. Jeremić ◽  
Hubert Wadepohl ◽  
Vesna V. Kojić ◽  
Dimitar S. Jakimov ◽  
Ratomir Jelić ◽  
...  

Two new Rh(iii)–ed3a complexes [Rh(ed3a)(OH2)]·H2O and Na[Rh(ed3a)Cl]·H2O have shown good antitumor activity, especially against HeLa cell line.


2017 ◽  
Vol 126 (1B) ◽  
pp. 127
Author(s):  
Duong Quoc Hoan

The acetohydrazides <strong>A5 </strong>containing an isoxazole ring and<strong> B5</strong> containing an indazole ring were synthesized from the corresponding acetohydrazide derivatives with acetic anhydride in about 80% high yield. Also, two acetohydrazones <strong>B6</strong> and <strong>B7</strong> were driven from acetohydrazide <strong>B4</strong> by condensation reaction. Bioactivity testes showed that none of them were active against on bacteria except acetohydrazones  <strong>B7</strong> showing moderate reactivity against KB cancer cell line at <em>IC<sub>50</sub></em> = 57 mg/L.


2018 ◽  
Vol 13 (1) ◽  
pp. 1934578X1801300 ◽  
Author(s):  
Chin-Soon Phan ◽  
Takashi Kamada ◽  
Takahiro Ishii ◽  
Toshiyuki Hamada ◽  
Charles Santhanaraju Vairappan

A new guaiane-type sesquiterpenoid, 10β- O-methyl-1αH,5αH-guaia-6-en-4β-ol (1) along with two known compounds, 10- O -methyl alismoxide (2) and alismoxide (3) were isolated from a population of Bornean soft coral Xenia stellifera. The structure of this metabolite was elucidated based on spectroscopic data such as NMR and HRESIMS. These compounds were evaluated for their biological activity against adult T-cell leukemia cell line.


Nutrients ◽  
2020 ◽  
Vol 12 (1) ◽  
pp. 154 ◽  
Author(s):  
Agata Jabłońska-Trypuć ◽  
Urszula Wydro ◽  
Elżbieta Wołejko ◽  
Grzegorz Świderski ◽  
Włodzimierz Lewandowski

Cichoric acid (CA) belongs to the group of polyphenols, which occurs in a variety of plant species and it is characterized by anticancer, antibacterial, and antiviral properties. Selected polyphenols have the ability to combine with metal ions to form chelate complexes that reveal greater biological activity than free compounds. In order to study possible antimicrobial and anticancer effect of CA and its complexes with copper(II)/zinc(II)/nickel(II)/cobalt(II) we decided to conduct cytotoxicity tests to estimate the most effective concentrations of tested compounds. The results of the presented study demonstrated, for the first time, that the treatment with newly synthesized CA-metal complexes has anticancer and antimicrobial effects, which were examined in seven different cell lines: MCF-7, MDA-MB-231, and ZR-75-1 breast cancer cell lines, A375 melanoma cell line, DLD-1 cell line, LN-229 cell line, FN cell line; five bacterial strains: Escherichia coli, Pseudomonas aeruginosa, Staphylococcus epidermidis, Proteus vulgaris, Lactobacillus rhamnosus, yeast Sacchcaromyces boulardii, and pathogenic yeast-like fungi Candida albicans. The presented study indicates that CA-metal complexes could be considered as a potential supplementary tool in anticancer therapy, however, because of their possible toxic activity on fibroblasts, they should be used with caution. Some of the tested complexes have also preservative properties and positive influence on normal non-pathogenic microorganisms, which was demonstrated in selected microbial strains, therefore they may serve as food preservatives of natural origin with cytoprotective properties.


2002 ◽  
Vol 282 (5) ◽  
pp. G766-G775 ◽  
Author(s):  
Vinzenz Stepan ◽  
Kentaro Sugano ◽  
Tadataka Yamada ◽  
Jung Park ◽  
Chris J. Dickinson

Gastrin requires extensive posttranslational processing for full biological activity. It is presumed that progastrin is cleaved at pairs of basic amino acids by a prohormone convertase to form a glycine-extended intermediate (G-Gly) that serves as a substrate for peptidyl-glycine α-amidating monooxygenase (PAM), resulting in COOH-terminally amidated gastrin. To confirm the nature of progastrin processing in a primary cell line, we performed [35S]methionine-labeled pulse-chase biosynthetic experiments in canine antral G cells. Radiolabeled progastrin reached a peak earlier than observed for G-Gly or amidated gastrin. G-Gly radioactivity accumulated in G cells and preceded the appearance of radioactivity in amidated gastrin. The conversion of G-Gly to amidated gastrin was enhanced by the PAM cofactor ascorbic acid. To determine whether one member of the prohormone convertase family (PC2) was responsible for progastrin cleavage, G cells were incubated with PC2 antisense oligonucleotide probes. Cells treated with antisense probes had reduced PC2 expression, an accumulation of radiolabeled progastrin, and a delay in the formation of amidated gastrin. Progastrin in antral G cells is cleaved via PC2 to form G-Gly that is converted to amidated gastrin via the actions of PAM.


Biomolecules ◽  
2020 ◽  
Vol 10 (6) ◽  
pp. 818 ◽  
Author(s):  
Ramona Fecker ◽  
Valentina Buda ◽  
Ersilia Alexa ◽  
Stefana Avram ◽  
Ioana Zinuca Pavel ◽  
...  

Oenothera biennis L. (OB), also commonly known as evening primrose, belongs to the Onagraceae family and has the best studied biological activity of all the members in the family. In therapy, the most frequently used type of extracts are from the aerial part, which are the fatty oils obtained from the seeds and have a wide range of medicinal properties. The aim of this study was to evaluate the phytochemical composition and biological activity of OB hydroalcoholic extract and to provide directions for the antimicrobial effect, antiproliferative and pro-apoptotic potential against A375 melanoma cell line, and anti-angiogenic and anti-inflammatory capacity. The main polyphenols and flavonoids identified were gallic acid, caffeic acid, epicatechin, coumaric acid, ferulic acid, rutin and rosmarinic acid. The total phenolic content was 631.496 µgGAE/mL of extract and the antioxidant activity was 7258.67 μmolTrolox/g of extract. The tested extract had a mild bacteriostatic effect on the tested bacterial strains. It was bactericidal only against Candida spp. and S. aureus. In the set of experimental conditions, the OB extract only manifested significant antiproliferative and pro-apoptotic activity against the A375 human melanoma cell line at the highest tested concentration, namely 60 μg/mL. The migration potential of A375 cells was hampered by the OB extract in a concentration-dependent manner. Furthermore, at the highest tested concentration, the OB extract altered the mitochondrial function in vitro, while reducing the angiogenic reaction, hindering compact tumor formation in the chorioallantoic membrane assay. Moreover, the OB extract elicited an anti-inflammatory effect on the experimental animal model of ear inflammation.


2012 ◽  
Vol 7 (11) ◽  
pp. 1934578X1200701
Author(s):  
Daniel Załuski ◽  
Helena D. Smolarz ◽  
Urszula Gawlik-Dziki

The content of phenols (TPC), and the antioxidative, antileukemic and anti-MMPs properties of Eleutherococcus spp. cultivated in Poland are reported. The highest TPC was found in the spring leaves (20.3 – 37.2 mg/g). The spring leaves and roots of E. divaricatus had the strongest anti-DPPH activity (EC50 1.2 and 1.2 mg/mL), whereas the greatest ability of iron (II) chelating was shown by autumn leaves of E. setchuensis (EC50 0.3 mg/mL), and the ethanolic extract of E. gracilistylus roots showed the strongest lipid antiperoxidation activity (EC50 0.7 mg/mL). The highest number of apoptotic cells was observed in the Jurkat 45 cell line after treatment with the ethanolic extract of E. sessiliflorus roots (27%). Only the chloroform extracts of roots of E. gracilistylus and E. divaricatus showed the inhibitory activity against MMPs. Most of the studied species have a significant biological activity that is probably due to the presence of phenols. To the best of our knowledge, neither detailed phytochemical nor biological studies have been performed for most of the investigated species.


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