Development of a Liver Carcinoma Biomarker Panel in 3D HepG2 Liver Spheroids Following Exposure to Ag and Tio2 Nanomaterials

: In this work, 1,2,4-triazine derivatives were synthesized and evaluated for anticancer activities. Series of 1,2,4-triazine derivatives (4a, b) were prepared via the reaction of N-benzoyl glycine (1) with aromatic aldehydes in presence of fused sodium acetate and acetic anhydride to give 1,3-oxazolinone derivatives (2a, b), followed by condensation with 1-(ethoxycarbonyl) hydrazine (3) in glacial acetic acid. Compounds (4a, b) then reacted with acetic anhydride, ethyl chloroacetate and 2,4-dinitrophenyl hydrazine yielded the corresponding to N-acetyl derivatives (5a, b), N-(ethoxycarbonyl) methyl derivative (6) and 1,2-disubstituted hydrazine (7), respectively. The structures of the 1,2,4-triazine derivatives were confirmed by IR, 1H, 13C NMR, MS and elemental analyses. Anticancer activity of some 1,2,4-triazine derivatives (4-7) have been investigated. The results revealed that compounds 4a (IC50= 2.7μM), 5a (IC50= 1.5μM), and 5b (IC50= 3.9μM) show promising inhibitory growth efficacy compared to a standard antitumor drug (IC50= 4.6μM). These three compounds can be considered as potential agents against human hepatocellular carcinoma cell lines (HepG-2).

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Synthesis of New α-Amino Phosphonates Containing 3-Amino-4(3H) Quinazolinone Moiety as Anticancer and Antimicrobial Agents: DFT, NBO, and Vibrational Studies

Current Organic Synthesis ◽

10.2174/1570179414666170703141629 ◽

2018 ◽

Vol 15 (2) ◽

pp. 286-296 ◽

Cited By ~ 4

Author(s):

Mohamed K. Awad ◽

Mahmoud F. Abdel-Aal ◽

Faten M. Atlam ◽

Hend A. Hekal

Keyword(s):

Biological Activity ◽

Cell Line ◽

Quantum Chemical ◽

Density Functional ◽

Carcinoma Cell ◽

Liver Carcinoma ◽

Anticancer Activities ◽

Functional Theory ◽

Ft Ir ◽

Good Agreement

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.

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Improved Method for Obtaining of Arctigenin from Arctium Lappa L. and its Antiproliferative Effect on Human Hepatocarcinoma HepG2 Cells

Current Bioactive Compounds ◽

10.2174/1573407214666181115124223 ◽

2020 ◽

Vol 16 (3) ◽

pp. 358-362

Author(s):

Renan S. Teixeira ◽

Paulo H.D. Carvalho ◽

Jair A.K. Aguiar ◽

Valquíria P. Medeiros ◽

Ademar A. Da Silva Filho ◽

...

Keyword(s):

Antitumor Activity ◽

Crude Extract ◽

Hepg2 Cells ◽

Liver Carcinoma ◽

Adhesion Assay ◽

Dependent Manner ◽

Concentration Dependent Manner ◽

Arctium Lappa ◽

Nih 3T3

Background: Arctigenin is a lignan found in Arctium lappa L. (Asteraceae) that displays anti-inflammatory activities. Previous studies showed that the crude extract of A. Lappa has antitumor activity in human liver carcinoma, lung and stomach cancer cells. The aim of this study was to obtain arctigenin from A. lappa L., as well as to evaluate its antiproliferative effects in cells of liver carcinoma (HepG2) and fibroblasts (NIH/3T3). Methods: Arctigenin was obtained from the hydrolysis of arctiin, which was isolated from the crude extract of A. lappa. The effects of arctigenin and arctiin on HepG2 cell viability and cell adhesion were analyzed by MTT method. Adhesion assay was also carried out to evaluate the antitumor activity. Results: Our results showed that the analytical process to obtain arctigenin was fast and easy. In vitro experiments showed that arctigenin (107-269 μM) decreased HepG2 cells viability and did not cause cytotoxicity on NIH/3T3 cells. Arctigenin (27-269 μM) demonstrated anti-adhesion in HepG2 cells in a concentration-dependent manner, when compared with control. Conclusion: These results suggest a promising pharmacological activity for arctigenin as an antiproliferative compound.

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Synthesis and photocatalytic properties of Sn–TiO2 nanomaterials

Journal of Advanced Dielectrics ◽

10.1142/s2010135x20600188 ◽

2020 ◽

Vol 10 (01n02) ◽

pp. 2060018

Author(s):

E. M. Bayan ◽

T. G. Lupeiko ◽

L. E. Pustovaya ◽

M. G. Volkova

Keyword(s):

Phase Transition ◽

Thermal Stability ◽

Sol Gel ◽

Rutile Phase ◽

Photocatalytic Properties ◽

Light Activation ◽

X Ray ◽

Tio2 Nanomaterials ◽

Visible Light Activation ◽

Thermal Stability Of

Sn-doped TiO2 nanomaterials were synthesized by sol–gel method. It was shown the phase compositions and phase transitions change with the introduction of different tin amounts (0.5–20[Formula: see text]mol.%). X-ray powder diffraction was used to study the effect of different tin amounts on the anatase–rutile phase transition. It was found that the introduction of ions increases the thermal stability of anatase modifications. The material’s photocatalytic activity was studied in reaction with a model pollutant (methylene blue) photodegradation under UV and visible light activation. The best photocatalytic properties were shown for material, which contains 5[Formula: see text]mol.% of Sn.

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