scholarly journals THE SYNTHESIS OF A NOVEL BIBENZOPYRAN RELIED ON ELECTROOXYDATION OF MALLOAPELTA B BY CYCLIC VOLTAMMETRY

2017 ◽  
Vol 24 (4) ◽  
pp. 387-392
Author(s):  
Phan Thi Binh ◽  
Bui Hai Ninh ◽  
Chau Van Minh ◽  
Nguyen Hoai Nam ◽  
Le Mai Huong ◽  
...  
Keyword(s):  
Hepatocellular Carcinoma ◽  
Cyclic Voltammetry ◽  
Cell Lines ◽  
Cancer Cell ◽  
Structure Determination ◽  
Supporting Electrolyte ◽  
Cancer Cell Lines ◽  
Spectral Measurements ◽  
Nmr Studies ◽  
Mass Spectral

A novel bibenzopyran named bimalloapelta (1) was synthesized relying on electrooxydation of malloapelta B by cyclic voltammetry in acetonitril adding LiClO4 0.1 M as supporting electrolyte. Its structure determination based on extensive NMR studies and ESI mass spectral measurements. The new compound showed significant cytotoxicity againsts two cancer cell lines as human hepatocellular carcinoma (Hep-2; IC50: 0.46 µg/m) and rhabdosarcoma (RD; IC50: 0.33 µg/m). These results were the same that of  malloapelta B  (Hep-2, IC50: 0.49 µg/ml and  KB, IC50: 0.54 µg/ml). 

Naphthoquinone-based hydrazone hybrids: synthesis and potent activity against cancer cell lines

2020 ◽  
Vol 16 ◽  
Author(s):  
Délis Galvão Guimarães ◽  
Arlan de Assis Gonsalves ◽  
Larissa Araújo Rolim ◽  
Edigênia Cavalcante Araújo ◽  
Victória Laysna dos Anjos Santos ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Biological Activities ◽  
Supporting Electrolyte ◽  
Cancer Cell Lines ◽  
Molecular Structures ◽  
Cytotoxic Activities ◽  
Electrochemical Studies ◽  
Ic50 Values

Background: Natural naphthoquinones have shown diversified biological activities including antibacterial, antifungal, antimalarial, and cytotoxic activities. However, they are also compounds with acute cytotoxicity, immunotoxicity, carcinogenesis, and cardio- and hepatotoxicity, then the modification at their redox center is an interesting strategy to overcome such harmful activity. Objective: In this study, four novel semisynthetic hydrazones, derived from the isomers α- and β-lapachones (α and β, respectively) and coupled with the drugs hydralazine (HDZ) and isoniazid (ACIL), were prepared, evaluated by electrochemical methods and assayed for anticancer activity. Method: The semisynthetic hydrazones were obtained and had their molecular structures established by NMR, IR, and MS. Anticancer activity was evaluated by cell viability determined by reduction of 3-(4,5-dimethyl-2-thiazol)-2,5-diphenyl-2H-tetrazolium bromide (MTT). The electrochemical studies, mainly cyclic voltammetry, were performed, in aprotic and protic media. Result: The study showed that the compounds 2, 3, and 4 were active against at least one of the cancer cell lines evaluated, being compounds 3 and 4 the most cytotoxic. Toward HL-60 cells, compound 3 was 20x more active than β-lapachone, and 3x more cytotoxic than doxorubicin. Furthermore, 3 showed an SI value of 39.62 for HL-60 cells. Compound 4 was active against all cancer cells tested, with IC50 values in the range 2.90–12.40 μM. Electrochemical studies revealed a profile typical of self-protonation and reductive cleavage, dependent on the supporting electrolyte. Conclusion: These results therefore indicate that compounds 3 and 4 are strong candidates as prototypes of new antineoplastic drugs.

scholarly journals Anti-Proliferative Effects of an Extra-Virgin Olive Oil Extract Enriched in Ligstroside Aglycone and Oleocanthal on Human Liver Cancer Cell Lines

Cancers ◽  
2019 ◽  
Vol 11 (11) ◽  
pp. 1640 ◽  
Author(s):  
De Stefanis ◽  
Scimè ◽  
Accomazzo ◽  
Catti ◽  
Occhipinti ◽  
...  
Keyword(s):  
Hepatocellular Carcinoma ◽  
Liver Cancer ◽  
Olive Oil ◽  
Cell Lines ◽  
Cancer Cell ◽  
Virgin Olive Oil ◽  
Cancer Cell Lines ◽  
Liver Cancer Cell ◽  
Antioxidant Power ◽  
Polyphenolic Extract

Oleocanthal and ligstroside aglycone are olive oil-derived polyphenols. The former interferes with tumor growth with minor or no cytotoxicity on non-tumorigenic primary cell lines. The information about the bioactivity of ligstroside aglycone are scanty, with the exception of a known antioxidant power. Hepatocellular carcinoma is a malignant tumor with high mortality rates. Systemic chemotherapy is only marginally effective and is frequently complicated by toxicity. Previous observations have shown that hepatocellular carcinoma cell lines become more sensitive to taxol when it is combined with Tumor Necrosis Factor α (TNFα). The present work aimed to assess the effects of a polyphenolic extract containing both oleocanthal and ligstroside aglycone on proliferation and/or death in three liver cancer cell lines (HepG2, Huh7 and Hep3B). The possibility to enhance such effect by the addition of TNFα was also investigated. Both cell proliferation and death were enhanced by the exposure to the polyphenolic extract. Such effect was associated with induction of autophagy and could be potentiated by TNFα. The presence of ligstroside aglycone in the extract lowered the oleocanthal concentration required for cytotoxicity. These results show for the first time that the effects of a polyphenol extract can be potentiated by TNFα and that modulation of autophagy likely account for these effects.

scholarly journals Synthesis of New Bicyclic Hydroxamic Acids with Cytotoxic Activity

2018 ◽  
Vol 61 (4) ◽  
Author(s):  
Iker S. Escalona-Torres ◽  
Francisco Yuste ◽  
Rubén Sánchez-Obregón
Keyword(s):  
Cytotoxic Activity ◽  
Nitro Group ◽  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Hydroxamic Acids ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
H Nmr ◽  
C Nmr

Six new bicyclic hydroxamic acids were synthesized through an uncommon nitro group rearrangement between β-nitrostyrenes and dimedone. The structures of all the new synthesized compounds were confirmed using a combination of FTIR, <sup>1</sup>H NMR, <sup>13</sup>C NMR and mass spectral data. Likewise, the cytotoxic activity of the obtained products was evaluated in six different cancer cell lines. Two compounds showed significant potency on two cancer cell lines with IC50 between 9.31±0.1 and 23.38±0.9 μM.

scholarly journals Analysis of Liver Cancer Cell Lines Identifies Agents With Likely Efficacy Against Hepatocellular Carcinoma and Markers of Response

2019 ◽  
Vol 157 (3) ◽  
pp. 760-776 ◽  
Author(s):  
Stefano Caruso ◽  
Anna-Line Calatayud ◽  
Jill Pilet ◽  
Tiziana La Bella ◽  
Samia Rekik ◽  
...  
Keyword(s):  
Hepatocellular Carcinoma ◽  
Liver Cancer ◽  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Liver Cancer Cell

scholarly journals The adipokine vaspin reduces apoptosis in human hepatocellular carcinoma (Hep-3B) cells, associated with lower levels of NO and superoxide anion

2019 ◽  
Vol 20 (1) ◽  
Author(s):  
Magdalena Skonieczna ◽  
Dorota Hudy ◽  
Tomasz Hejmo ◽  
Rafal J. Buldak ◽  
Małgorzata Adamiec ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Hepatocellular Carcinoma ◽  
Cell Lines ◽  
Cancer Cell ◽  
Superoxide Anion ◽  
Reactive Oxygen ◽  
Cancer Cell Lines ◽  
Protective Role ◽  
Apoptotic Pathway ◽  
Physiological Level

Abstract Background Among adipose-derived factors, adipocytokines play roles as hormones and signaling mediators for apoptotic pathway. Among of them, vaspin, regulates the metabolism of adipose tissue itself as an endocrine organ, and stimulates adipocytes to maturation, differentiation, etc. Damaged adipocytes, present in obesity and hepatocellular carcinoma (HCC) respond with over-production of inflammatory cytokines. Such pro-inflammatory stimulation remains under adipokine control. Pro-inflammatory pathways are connected to oxidative stress and apoptosis, reported as co-existing with an elevated level of some adipokines in cancer cell lines. However, some hormones, such as vaspin, reduce apoptosis, have anti-inflammatory and anti-oxidative roles in cancer cell lines. Methods Hep-3B cells were cytometrically evaluated under vaspin treatment for reactive oxygen species (ROS) and apoptosiss induction. The statistical significant changes to the untreated controls was calculated by T-tests (indicated at value p < 0.05). Results Here we studied the production of reactive oxygen and nitrogen species in cells of HCC line Hep-3B after vaspin treatment. A decreased level of nitric oxide and superoxide anion 24 h after vaspin addition at 5 ng/ml was correlated with restricted, to the physiological level, apoptosis. A protective role of vaspin was displayed as enhanced cell viability and proliferation, which could be a poor prognostic in liver cancer. Conclusions Apoptosis was suppressed after vaspin treatment, together with low levels of nitric oxide and superoxide anions.

scholarly journals Decreased IL‑37 expression in hepatocellular carcinoma tissues and liver cancer cell lines

2020 ◽  
Author(s):  
Peng Li ◽  
Hongsheng Guo ◽  
Kun Wu ◽  
Liudan Su ◽  
Kai Huang ◽  
...  
Keyword(s):  
Hepatocellular Carcinoma ◽  
Liver Cancer ◽  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Liver Cancer Cell

scholarly journals Oxovanadium(IV) Complexes with Nitrogen Donors: Synthesis, Characterisation, and Biological Activities

2013 ◽  
Vol 2013 ◽  
pp. 1-11 ◽  
Author(s):  
Gauri D. Bajju ◽  
Puja Sharma ◽  
Ashu Kapahi ◽  
Madhulika Bhagat ◽  
Sujata Kundan ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Human Cancer Cell ◽  
Nmr Studies ◽  
Human Cancer Cell Lines ◽  
Axial Ligands ◽  
Nitrogen Donors

Some oxovanadium(IV) complexes of SA/SSA and 5, 10, 15, and 20-meso-tetraphenylporphyrin (H2tpp) with unidentate and bidentate nitrogen donors have been synthesized and characterized by elemental analysis, conductivity measurements, magnetic susceptibility, UV-Vis, IR, mass spectroscopy, TGA/DTA, and 1H, 13C and 51V NMR studies to investigate the steric and electronic effects of axial ligands on the properties of porphyrins. On the basis of these studies, it has been investigated that the axial ligands bind to the sixth coordination site of the vanadium ion to form a relatively stable six-coordinate-porphyrin complex where as in the case of SA/SSA complexes the nitrogen donors bind to the equatorial position giving square pyramidal geometry. The in vitro cytotoxicity against human cancer cell lines and antimicrobial activities of the synthesized compounds have been done against various fungal and bacterial pathogens. The [VO(SA/SSA)L/L-L] complexes were found to possess higher antibacterial, antifungal activity and in vitro cytotoxicity against human cancer cell lines than VO(tpp)L complexes.

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