scholarly journals Synthesis of Novel Pyridopyridazin-3(2H)-one Derivatives and Evaluation of Their Cytotoxic Activity against MCF-7 Cells

2014 ◽  
Vol 2014 ◽  
pp. 1-7 ◽  
Author(s):  
Periasamy Selvakumar ◽  
Sathiah Thennarasu ◽  
Asit Baran Mandal
Keyword(s):  
Cell Proliferation ◽  
Cytotoxic Activity ◽  
Intramolecular Cyclization ◽  
Amide Proton ◽  
Breast Adenocarcinoma ◽  
Moderate Activity ◽  
Human Breast ◽  
Human Breast Adenocarcinoma ◽  
Derivatives Of ◽  
Mcf 7

A series of pyridopyridazin-3(2H)-one derivatives was synthesized in two facile steps. Mannich-type three-component condensation afforded the 2,6-diaryl piperidin-4-one derivatives, which underwent intramolecular cyclization in the presence of hydrazine or phenylhydrazine to yield the corresponding pyridopyridazin-3(2H)-one derivatives. All the derivatives of pyridopyridazin-3(2H)-one, except 3e and 3f, showed moderate activity against human breast adenocarcinoma (MCF-7) cells. The higher degree of inhibition of MCF-7 cell proliferation shown by 2a–2f indicates the significance of the amide proton in pyridopyridazin-3(2H)-one derivatives.

scholarly journals Polyisoprenylated Acylphloroglucinols from Garcinia nervosa

2018 ◽  
Vol 13 (3) ◽  
pp. 1934578X1801300 ◽  
Author(s):  
Alfarius Eko Nugroho ◽  
Hitomi Nakamura ◽  
Daisuke Inoue ◽  
Yusuke Hirasawa ◽  
Chin Piow Wong ◽  
...  
Keyword(s):  
Hepatocellular Carcinoma ◽  
Cytotoxic Activity ◽  
Spectroscopic Data ◽  
Human Lung ◽  
Carcinoma Cells ◽  
Breast Adenocarcinoma ◽  
Human Breast ◽  
Human Breast Adenocarcinoma ◽  
Human Hepatocellular Carcinoma Cells ◽  
Mcf 7

Two new polyisoprenylated acylphloroglucinols, 7- epi-isoxanthochymol and 7- epi-cycloxanthochymol (1 – 2), were isolated from the barks of Garcinia nervosa together with their 7-epimers isoxanthochymol (3) and cycloxanthochymol (4). Their structures were determined on the basis of NMR spectroscopic data. The cytotoxic activity of the isolated compounds against HL-60, MCF-7 (human breast adenocarcinoma), A549 (human lung adenocarcinoma) and HepG2 (human hepatocellular carcinoma) cells were evaluated, and all compounds showed cytotoxic activity against all cell lines.

scholarly journals Pit-1/GHF-1 and GH expression in the MCF-7 human breast adenocarcinoma cell line

2002 ◽  
Vol 173 (1) ◽  
pp. 161-167 ◽  
Author(s):  
C Gil-Puig ◽  
M Blanco ◽  
T Garcia-Caballero ◽  
C Segura ◽  
R Perez-Fernandez
Keyword(s):  
Cell Proliferation ◽  
Cell Line ◽  
Carcinoma Cell ◽  
Breast Adenocarcinoma ◽  
Human Breast ◽  
Rt Pcr ◽  
Adenocarcinoma Cell Line ◽  
Adenocarcinoma Cell ◽  
Human Breast Adenocarcinoma ◽  
Mcf 7

GH expression in mammary tumors has been related to the increase and spreading of cell proliferation. Using the MCF-7 human breast adenocarcinoma cell line, it has been demonstrated that autocrine GH-stimulated mammary carcinoma cell proliferation decreased the apoptosis rate and enhanced cell spreading. Surprisingly, no data are available about the presence of Pit-1 (the main pituitary regulator of GH) or GH expression in this cell line. Using RT-PCR, Western blot and immunohistochemistry, we have demonstrated the presence of both mRNA coding Pit-1 and GH as well as Pit-1 and GH protein in the MCF-7 cell line. These data could imply that Pit-1 may be an adequate target to inhibit breast cell proliferation.

scholarly journals Induction of Apoptosis by Gluconasturtiin-Isothiocyanate (GNST-ITC) in Human Hepatocarcinoma HepG2 Cells and Human Breast Adenocarcinoma MCF-7 Cells

Molecules ◽  
2020 ◽  
Vol 25 (5) ◽  
pp. 1240
Author(s):  
Asvinidevi Arumugam ◽  
Muhammad Din Ibrahim ◽  
Saie Brindha Kntayya ◽  
Nooraini Mohd Ain ◽  
Renato Iori ◽  
...  
Keyword(s):  
Cell Proliferation ◽  
Cell Death ◽  
Cell Lines ◽  
Chromatin Condensation ◽  
Time Dependent ◽  
Breast Adenocarcinoma ◽  
Dependent Manner ◽  
Human Breast ◽  
Human Breast Adenocarcinoma ◽  
Mcf 7

Gluconasturtiin, a glucosinolate present in watercress, is hydrolysed by myrosinase to form gluconasturtiin-isothiocyanate (GNST-ITC), which has potential chemopreventive effects; however, the underlying mechanisms of action have not been explored, mainly in human cell lines. The purpose of the study is to evaluate the cytotoxicity of GNST-ITC and to further assess its potential to induce apoptosis. GNST-ITC inhibited cell proliferation in both human hepatocarcinoma (HepG2) and human breast adenocarcinoma (MCF-7) cells with IC50 values of 7.83 µM and 5.02 µM, respectively. Morphological changes as a result of GNST-ITC-induced apoptosis showed chromatin condensation, nuclear fragmentation, and membrane blebbing. Additionally, Annexin V assay showed proportion of cells in early and late apoptosis upon exposure to GNST-ITC in a time-dependent manner. To delineate the mechanism of apoptosis, cell cycle arrest and expression of caspases were studied. GNST-ITC induced a time-dependent G2/M phase arrest, with reduction of 82% and 93% in HepG2 and MCF-7 cell lines, respectively. The same treatment also led to the subsequent expression of caspase-3/7 and -9 in both cells demonstrating mitochondrial-associated cell death. Collectively, these results reveal that GNST-ITC can inhibit cell proliferation and can induce cell death in HepG2 and MCF-7 cancer cells via apoptosis, highlighting its potential development as an anticancer agent.

scholarly journals Anti-proliferative Activity and Apoptotic Potential of Britannin, a Sesquiterpene Lactone from Inula aucheriana

2012 ◽  
Vol 7 (8) ◽  
pp. 1934578X1200700 ◽  
Author(s):  
Maryam Hamzeloo Moghadam ◽  
Homa Hajimehdipoor ◽  
Soodabeh Saeidnia ◽  
Azadeh Atoofi ◽  
Roxana Shahrestani ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Sesquiterpene Lactone ◽  
Cell Lines ◽  
Mtt Assay ◽  
Proliferative Activity ◽  
Terminal Deoxynucleotidyl Transferase ◽  
Breast Adenocarcinoma ◽  
Human Breast ◽  
Human Breast Adenocarcinoma ◽  
Mcf 7

Inula aucheriana n-hexane, CHCl3 and MeOH extracts were evaluated for their anti-proliferative activity against HepG-2, MCF-7, MDBK and A-549 cells. The CHCl3 extract exhibited cytotoxic activity to the above cell lines with IC50 values of 13.5, 23.4, 10.5, and 26.9 μg/mL, respectively. The sesquiterpene lactone britannin was isolated from the above extract. This was further evaluated in the MTT assay to demonstrate strong cytotoxicity to the mentioned cell lines (IC50: 2.2, 5.9, 5.4, and 3.5 μg/mL, respectively), and the apoptotic inducing properties of britannin were evaluated on human breast adenocarcinoma (MCF-7) cells through the terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL) assay.

scholarly journals CYTOTOXIC ACTIVITY OF A MEDICINAL MANGROVE PLANT CERIOPS DECANDRA (GRIFF.) DING HOU LEAVES ON HUMAN BREAST ADENOCARCINOMA CELL LINE MCF-7

2018 ◽  
Vol 11 (12) ◽  
pp. 296
Author(s):  
Sukasini S ◽  
Bhargav Iyer M
Keyword(s):  
Cytotoxic Activity ◽  
Brine Shrimp ◽  
Cytotoxic Effect ◽  
Morphological Changes ◽  
Breast Adenocarcinoma ◽  
Phytochemical Screening ◽  
Human Breast ◽  
Human Breast Adenocarcinoma ◽  
Induction Of Apoptosis ◽  
Mcf 7

Objective: Ceriops decandra (Griff.) Ding Hou (Rhizophoraceae) is an evergreen mangrove tree widely used in folklore medicine for the treatment of several diseases. Concerning the presence of anticancer molecule in C. decandra, the present investigation was carried out to study the preliminary phytochemical screening, in vitro cytotoxic effect, and apoptotic induction of methanol extract of C. decandra.Methods: The preliminary phytochemical investigations were done using standard methods. Cytotoxic activity was analyzed in terms of brine shrimp (Artemia salina Leach) lethality bioassay. MTT (3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide) assay was used to evaluate the cell viability and growth inhibition of MCF-7 (human breast adenocarcinoma) cells after treatment with different doses of C. decandra extract. Cell morphological changes induced by the extract were observed using phase contrast inverted microscope. Induction of apoptosis was determined by DNA fragmentation assay.Results: Phytochemical screening revealed the presence of various potent phytochemicals. In the brine shrimp lethality bioassay, the LC50 of the extract was found to be 12.5 μg/mL, implying a promising cytotoxic effect. The MTT assay results showed increased inhibitory activity at a concentration-dependent manner and altered the cell morphology after exposure with C. decandra extract which exhibited typical apoptotic morphological changes. Furthermore, the characteristic DNA ladder pattern of C. decandra treated cells in agarose gel electrophoresis confirms the induction of apoptosis.Conclusion: The research revealed the cytotoxic effect of C. decandra on MCF-7 cells through its nature of induction of apoptosis.

Cytotoxicity evaluation of indomethacin-loaded polymeric nanoparticles in a human breast adenocarcinoma cell model/ Avaliação da citotoxicicidade de nanopartículas poliméricas contendo indometacina em modelo celular de adenocarcinoma de mama humano

2021 ◽  
Vol 7 (7) ◽  
pp. 67004-67014
Author(s):  
Camila Franco ◽  
Manoela Lunkes Silva ◽  
Altevir Rossato Viana ◽  
Aline Ferreira Ourique ◽  
Luciana Maria Fontanari Krause
Keyword(s):  
Cell Model ◽  
Polymeric Nanoparticles ◽  
Cáncer De Mama ◽  
Breast Adenocarcinoma ◽  
Human Breast ◽  
Adenocarcinoma Cell ◽  
Human Breast Adenocarcinoma ◽  
Mcf 7

Novas pesquisas indicam que anti-inflamatórios podem ser aplicados como agentes anti-cancerígenos como indometacina para hepatocarcinoma humano, canceres de colon e estômago. Como sabe-se, indometacina possui efeitos adversos gastrointestinais, cardiovasculares e renais. Uma vez que cancer de mama tem alta incidência e não há estudo da indometacina carreada em nanopartículas para esta aplicação, este estudo envolve o desenvolvimento de nanocapsulas de poli-epsilon-caprolactona carregadas com indometacina para a redução de citotoxicidade como agente quimioprotetor para cancer de mama. O nanocarreador foi preparado por método de deposição interfacial e sua caracterização foi realizada por determinação de pH, diâmetro médio e índice de polidispersão por espalhamento dinâmico de luz, potencial zeta por mobilidade eletroforética, eficiência de encapsulação por método de cromatografia líquida de alta eficiência e seu ensaio de citotoxicidade com linhagem de células queratinócitos (HaCaT) e células de cancer de mama (MCF-7). As formulações branca (C-NC) e contendo indometacina (Ind-OH-NC) mostraram leve pH ácido, diâmetros em torno de 200 nm e PDI0,2 com potencial zeta em torno de -20 mV e eficiência de encapsulação de 99% (1 mg.mL-1), cujo coeficiente de distribuição indicou efeito de permeação e retenção (efeito EPR). Ambas formulações não foram citotóxicas às células HaCaT, provando serem seguras às células normais e Ind-OH-NC teve uma permeação concentração e tempo-dependente e teve eficácia em reduzir a viabilidade celular da linhagem MCF-7.

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