Synthesis, Characterisation and Cytotoxic Activity Evaluation of New Metalsalen Complexes Based on the 1,2-bicyclo[2.2.2]octane Bridge

Diaminobicyclo[2.2.2]octane was used as starting material for the preparation, in solution or in a ball-mill, of a salen ligand. Five metal salen complexes were prepared in high yield and their cytotoxic activities were evaluated against HCT116 cell lines. Original manganese salen complex displayed the highest activity with a potency 16 fold higher than the one of cisplatin, demonstrating the benefit of the bridging backbone, compared to other salen systems. An alternative preparation route for this complex by mechanochemistry was also performed.<br>

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Cytotoxic activity and anti-cancer potential of Ontario grown onion extracts against breast cancer cell lines

Functional Foods in Health and Disease ◽

10.31989/ffhd.v8i3.408 ◽

2018 ◽

Vol 8 (3) ◽

pp. 159 ◽

Cited By ~ 1

Author(s):

Meghan Fragis ◽

Abdulmonem I. Murayyan ◽

Suresh Neethirajan

Keyword(s):

Breast Cancer ◽

Cytotoxic Activity ◽

Cell Lines ◽

Cancer Cell ◽

Breast Cancer Cell ◽

Cancer Cell Lines ◽

Breast Cancer Cell Lines ◽

Cytotoxic Activities ◽

Cancer Line ◽

Mcf 7

Background: Breast cancer is the most commonly diagnosed cancer and the second leading cause of cancer deaths among Canadian women. Cancer management through changes in lifestyle, such as increased intake of foods rich in dietary flavonoids, have been shown to decrease the risk associated with breast, liver, colorectal, and upper-digestive cancers in epidemiologic studies. Onions are high in flavonoid content and one of the most common vegetables. Additionally, onions are used in most Canadian cuisines.Methods: We investigated the effect of five prominent Ontario grown onion (Stanley, Ruby Ring, LaSalle, Fortress, and Safrane) extracts on two subtypes of breast cancer cell lines: a triple negative breast cancer line MDA-MB-231 and an ER+ breast cancer line MCF-7.Results: These onion extracts elicited strong anti-proliferative, anti-migratory, and cytotoxic activities on both the cancer cell lines. Flavonoids present in these onion extracts induced apoptosis, cell cycle arrest in the G2/M phase, and a reduction in mitochondrial membrane potential at dose-dependent concentrations. Onion extracts were more effective against MDA-MB-231 compared to the MCF-7 cell line. Conclusion: In this study, we investigated the extracts synthesized from Ontario-grown onion varieties in inducing anti-migratory, cytostatic, and cytotoxic activities in two sub-types of human breast cancer cell lines. Anti-tumor activity of these extracts depends upon the varietal and can be formulated into nutraceuticals and functional foods for the wellbeing of cancer patients. Overall, the results suggest that onion extracts are a good source of flavonoids with anti-cancerous properties.Keywords: onion extracts; flavonoids; anti-proliferative; breast cancer; cytotoxic activity

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Design, Synthesis, In vitro Cytotoxic Activity Evaluation, and Study of Apoptosis Inducing Effect of New Styrylimidazo[1,2-a]Pyridines as Potent Anti-Breast Cancer Agents

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520618666180903100835 ◽

2019 ◽

Vol 19 (2) ◽

pp. 265-275 ◽

Cited By ~ 2

Author(s):

Faeze Khalili ◽

Sara Akrami ◽

Malihe Safavi ◽

Maryam Mohammadi-Khanaposhtani ◽

Mina Saeedi ◽

...

Keyword(s):

Breast Cancer ◽

Cytotoxic Activity ◽

High Yield ◽

Breast Cancer Cell Lines ◽

Pyridine Derivatives ◽

One Pot ◽

Standard Drug ◽

Three Component Reaction ◽

Anti Cancer

Background: This paper reports synthesis, cytotoxic activity, and apoptosis inducing effect of a novel series of styrylimidazo[1,2-a]pyridine derivatives. Objective: In this study, anti-cancer activity of novel styrylimidazo[1,2-a]pyridines was evaluated. Methods: Styrylimidazo[1,2-a]pyridine derivatives 4a-o were synthesized through a one-pot three-component reaction of 2-aminopyridines, cinnamaldehydes, and isocyanides in high yield. All synthesized compounds 4a-o were evaluated against breast cancer cell lines including MDA-MB-231, MCF-7, and T-47D using MTT assay. Apoptosis was evaluated by acridine orange/ethidium bromide staining, cell cycle analysis, and TUNEL assay as the mechanism of cell death. Results: Most of the synthesized compounds exhibited more potent cytotoxicity than standard drug, etoposide. Induction of apoptosis by the most cytotoxic compounds 4f, 4g, 4j, 4n, and 4m was confirmed through mentioned methods. Conclusion: In conclusion, these results confirmed the potency of styrylimidazo[1,2-a]pyridines for further drug discovery developments in the field of anti-cancer agents.

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In Vitro Cytotoxic Effects of Secondary Metabolites Present in Sarcopoterium Spinosum L.

Applied Sciences ◽

10.3390/app11115300 ◽

2021 ◽

Vol 11 (11) ◽

pp. 5300

Author(s):

Jozef Hudec ◽

Jan Mojzis ◽

Marta Habanova ◽

Jorge A. Saraiva ◽

Pavel Hradil ◽

...

Keyword(s):

Mammary Gland ◽

Ethyl Acetate ◽

Cytotoxic Activity ◽

Cell Lines ◽

Benzalkonium Chloride ◽

Ethanol Extract ◽

Cytotoxic Activities ◽

Sarcopoterium Spinosum ◽

Mcf 7

Sarcopoterium spinosum (L.) is a medicinal plant traditionally used for the treatment of various diseases including cancer in the Near- and Middle East. The fractions and constituents of the ethanol extract of S. spinosum were screened for in vitro cytotoxic activities on Jurkat (acute T-lymphoblastic leukemia), HeLa (cervical adenocarcinoma), MCF-7 (mammary gland adenocarcinoma), Caco-2 (human colorectal adenocarcinoma), and MDA-MB-231 (mammary gland adenocarcinoma) cell lines using the MTT (3-(dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. The ethanol extract was subsequently re-extracted with ethyl acetate and in its sub-fraction obtained by column chromatography three compounds (stachydrine, benzalkonium chloride and rutine) were the first time identified by nuclear magnetic resonance (NMR) analyses. The most active subfraction showed cytotoxic activity against HeLa, MCF-7, and Caco-2 cell lines. The three compounds mentioned, as standards of high-performance liquid chromatography (HPLC) quality, were studied individually and in combination. Cytotoxic activity observed might be due to the presence of benzalkonium chloride and rutin. Benzalkonium chloride showed the strongest growth suppression effect against HeLa cells (IC50 8.10−7 M) and MCF-7 cells (IC50 5.10−6 M). The mixture of stachydrine and benzalkonium chloride allowed a synergistic cytotoxic effect against all tested cancer and normal cells to be obtained. Anti-cancer activity of the plant extract of S. spinosum remains under-investigated, so this research describes how the three major compounds identified in the ethyl acetate extract can exert a significant dose dependent in vitro cytotoxicity.

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Synthesis, Cytotoxic Activity, Crystal Structure, DFT Studies and Molecular Docking of 3-Amino-1-(2,5-dichlorophenyl)-8-methoxy-1H-benzo[f]chromene-2-carbonitrile

Crystals ◽

10.3390/cryst11020184 ◽

2021 ◽

Vol 11 (2) ◽

pp. 184

Author(s):

Menna El Gaafary ◽

Tatiana Syrovets ◽

Hany M. Mohamed ◽

Ahmed A. Elhenawy ◽

Ahmed M. El-Agrody ◽

...

Keyword(s):

Cytotoxic Activity ◽

Cell Lines ◽

Cancer Cell ◽

Dna Methyltransferase ◽

Human Cancer ◽

Theoretical Calculations ◽

Cancer Cell Lines ◽

Molecular Structures ◽

Cytotoxic Activities ◽

X Ray

The target compound 3-amino-1-(2,5-d ichlorophenyl)-8-methoxy-1H-benzo[f]-chromene-2-carbonitrile (4) was synthesized via a reaction of 6-methoxynaphthalen-2-ol (1), 2,5-dichlorobenzaldehyde (2), and malononitrile (3) in ethanolic piperidine solution under microwave irradiation. The newly synthesized β-enaminonitrile was characterized by FT-IR, 1H NMR, 13C NMR, mass spectroscopy, elemental analysis and X-ray diffraction data. Its cytotoxic activity was evaluated against three different human cancer cell lines MDA-MB-231, A549, and MIA PaCa-2 in comparison to the positive controls etoposide and camptothecin employing the XTT cell viability assay. The analysis of the Hirshfeld surface was utilized to visualize the reliability of the crystal package. The obtained results confirmed that the tested molecule revealed promising cytotoxic activities against the three cancer cell lines. Furthermore, theoretical calculations (DFT) were carried out with the Becke3-Lee-Yang-parr (B3LYP) level using 6-311++G(d,p) basis. The optimization geometry for molecular structures was in agreement with the X-ray structure data. The HOMO-LUMO energy gap of the studied system was discussed. The intermolecular-interactions were studied through analysis of the topological-electron-density(r) using the QTAIM and NCI methods. The novel compound exhibited favorable ADMET properties and its molecular modeling analysis showed strong interaction with DNA methyltransferase 1.

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Cytotoxic Activity of Major Compounds from Phaleria macrocarpa (Scheff.) Boerl. Fruits

Jurnal Teknologi ◽

10.11113/jt.v64.2044 ◽

2013 ◽

Vol 64 (2) ◽

Author(s):

Siti Nur Atiqah Md Othman ◽

Norazah Basar ◽

Siti Pauliena Mohd Bohari

Keyword(s):

Cytotoxic Activity ◽

Cell Line ◽

Cell Lines ◽

Fibroblast Cell ◽

Mouse Embryonic Fibroblast ◽

Cytotoxic Activities ◽

Anticancer Properties ◽

Cervical Carcinoma Cell Line ◽

Cell Line Hela ◽

3T3 Cell Lines

P. macrocarpa is a well known Indonesian medicinal plant which is traditionally claimed to have anticancer properties. To date, there are numerous cytotoxic studies conducted on crude extracts of this plant. However, there are limited informations available regarding cytotoxic activity of the compounds isolated from this plant. Thus, this study investigated cytotoxic activity of two benzophenones derivatives identified as 2,6,4'-trihydroxy-4-methoxybenzophenone (1) and 6,4'-dihydroxy-4-methoxybenzophenone-2-O-β-D-glucopyranoside (2) isolated from the ethyl acetate extract. Cytotoxic activities of these compounds were performed against human cervical carcinoma cell line (HeLa) and mouse embryonic fibroblast cell line (3T3) using MTT assay. The result showed that benzophenone (1) exhibited low cytotoxic effect against HeLa and 3T3 cell lines with IC50 values of 132 µg/ml and 158 µg/ml, repectively while benzophenone (2) was non toxic against HeLa and 3T3 cell lines are because the IC50 is more than 250 µg/ml. These findings may sheds light on the actual properties of this plant.

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Synthesis and application of Co(salen) complexes containing proximal imidazolium ionic liquid cores

Canadian Journal of Chemistry ◽

10.1139/v11-106 ◽

2012 ◽

Vol 90 (1) ◽

pp. 60-70 ◽

Cited By ~ 15

Author(s):

Swapnil Sonar ◽

Kenson Ambrose ◽

Arthur D. Hendsbee ◽

Jason D. Masuda ◽

Robert D. Singer

Keyword(s):

Ionic Liquid ◽

Ionic Liquids ◽

Model Compound ◽

Veratryl Alcohol ◽

Oxidation Catalysts ◽

Imidazolium Ionic Liquid ◽

Lignin Model Compound ◽

Salen Complexes ◽

Lignin Model ◽

Salen Ligand

Ionic ligands derived from a salen ligand containing two proximal 1,3-disubstituted imidazolium ionic liquid cores form cobalt(III) complexes capable of selectively oxidizing veratryl alcohol, a lignin model compound, to veratraldehyde using air as the source of oxygen. These complexes are easy to prepare, inexpensive, water stable, and soluble in ionic liquids, making them viable candidates for use as oxidation catalysts.

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DIARRHEA OUTBREAK IN PERNAMBUCO, BRAZIL, ASSOCIATED WITH A HEAT-STABLE CYTOTOXIC ENTEROTOXIN PRODUCED BY Aeromonas caviae

Revista do Instituto de Medicina Tropical de São Paulo ◽

10.1590/s0036-46652015000400013 ◽

2015 ◽

Vol 57 (4) ◽

pp. 349-351

Author(s):

Ana Carolina Amaral LOPES ◽

Luciano Moura MARTINS ◽

Maria Silvia Viccari GATTI ◽

Cristhiane Moura FALAVINA DOS REIS ◽

Ernesto HOFER ◽

...

Keyword(s):

Cytotoxic Activity ◽

Virulence Factor ◽

Acute Diarrhea ◽

Cytotoxic Activities ◽

Fluid Accumulation ◽

Suckling Mice ◽

Heat Stable ◽

Aeromonas Caviae ◽

Culture Supernatants

SUMMARY In the present study enterotoxic and cytotoxic activities of twenty Aeromonas caviaestrains were examined. They originated from fecal specimens of patients with acute diarrhea during an outbreak in Brazil in 2004. Culture supernatants of fourteen strains (70%) caused fluid accumulation in rabbit ileal intestinal loops and in suckling mice assays, and also showed a cytotoxic activity in Vero and Caco-2 cells. The enterotoxic and cytotoxic factors were heat-stable after culture supernatants treatment at 100 ºC. The results revealed that A. caviaestrains produce a putative diarrheagenic virulence factor, a heat-stable cytotoxic enterotoxin that could be linked to the diarrhea outbreak that took place in Brazil.

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Salen ligand complexes as electrocatalysts for direct electrochemical reduction of gaseous carbon dioxide to value added products

RSC Advances ◽

10.1039/c4ra09818h ◽

2015 ◽

Vol 5 (5) ◽

pp. 3581-3589 ◽

Cited By ~ 12

Author(s):

Surya Singh ◽

Bedika Phukan ◽

Chandan Mukherjee ◽

Anil Verma

Keyword(s):

Carbon Dioxide ◽

Electrochemical Reduction ◽

Value Added ◽

Salen Complexes ◽

Gaseous Carbon Dioxide ◽

Salen Ligand ◽

Centrosymmetric Molecule ◽

Value Added Products

CO2, being a linear and centrosymmetric molecule, is very stable, and the electrochemical reduction of CO2 requires energy. However, the salen complexes are found to be very efficient to minimize overpotential as compared to their metal counterparts.

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Cytotoxic Activity of tropane alkaloides of Species of Erythroxylum

Mini-Reviews in Medicinal Chemistry ◽

10.2174/1389557521666210119123409 ◽

2021 ◽

Vol 21 ◽

Author(s):

José Fernando Araújo Neto ◽

Erika Maria de Oliveira Ribeiro ◽

Ademir Evangelista do Vale ◽

Jorge Maurício David ◽

Juceni Pereira de Lima David

Keyword(s):

Natural Products ◽

Cytotoxic Activity ◽

Screening Program ◽

Evaluation Studies ◽

Tropane Alkaloids ◽

Chemotherapeutic Agents ◽

In Vitro Tests ◽

Cytotoxic Activities ◽

Cytotoxic Potential

: Erythroxylaceae is a family composed of four genera being Erythroxylum the only one represented in the Neotropical region. Chemical studies indicate the presence of alkaloids, terpenes, flavonoids and phenolic compounds as main compounds. The incorporation of cytotoxic activity assays of natural products using cell cultures assists in the selection of potential chemotherapeutic agents. In this work we describe a revision of the cytotoxicity evaluation studies performed with extracts and/or pure substances obtained from Erythroxylum species through an integrative review. We have found studies that evaluated the cytotoxic activity of 21 species of Erythroxylum against 45 different cell lines, the analysis of the chemical composition of these species shows that the metabolites present in each species influence the cytotoxic potential of them, especially the presence of disubstituted tropane alkaloids species with the highest cytotoxic potential. MTT and Sulforrodamine B assays were the main in vitro tests used for the evaluation of the cytotoxic activities. From the total of species, less than 10% of the Erythroxylum species have already been evaluated for the cytotoxic activity, four of them showed high cytotoxic activity according to with the criteria of the NCI plant screening program. Thus, this genus represents a potential source of natural products with antitumor activity.

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