scholarly journals Terpenoid from Indonesian temu mangga (Curcuma mangga, Val) rhizomes and review of its anticancer towards MCF-7 breast cells

2021 ◽  
Author(s):  
Alicia N. A. Ganur ◽  
Dyah U. C. Rahayu ◽  
Hanhan Dianhar ◽  
Ichsan Irwanto ◽  
Purwantiningsih Sugita
Keyword(s):  
2013 ◽  
Vol 04 (07) ◽  
pp. 65-69 ◽  
Author(s):  
Silvana Aparecida Alves Corrêa de Noronha ◽  
Werica Bernardo ◽  
Alexandre Jesus Barros ◽  
Clovis Ryuichi Nakaie ◽  
Suma Imura Shimuta ◽  
...  

2019 ◽  
Vol 19 (4) ◽  
pp. 538-545 ◽  
Author(s):  
Maher A. El-hashash ◽  
Amira T. Ali ◽  
Rasha A. Hussein ◽  
Wael M. El-Sayed

Background: The genetic heterogeneity of tumor cells and the development of therapy-resistant cancer cells in addition to the high cost necessitate the continuous development of novel targeted therapies. Methods: In this regard, 14 novel benzoxazinone derivatives were synthesized and examined for anticancer activity against two human epithelial cancer cell lines; breast MCF-7 and liver HepG2 cells. 6,8-Dibromo-2- ethyl-4H-benzo[d][1,3]oxazin-4-one was subjected to react with nitrogen nucleophiles to afford quinazolinone derivatives and other related moieties (3-12). Benzoxazinone 2 responds to attack with oxygen nucleophile such as ethanol to give ethyl benzoate derivative 13. The reaction of benzoxazinone 2 with carbon electrophile such as benzaldehyde derivatives afforded benzoxazinone derivatives 14a and 14b.The structure of the prepared compounds was confirmed with spectroscopic tools including IR, 1H-NMR, and 13C-NMR. Results: Derivatives 3, 9, 12, 13, and 14b exhibited high antiproliferative activity and were selective against cancer cells showing no toxicity in normal fibroblasts. Derivative 3 with NH-CO group in quinazolinone ring was effective only against breast cells, while derivative 12 with NH-CO group in imidazole moiety was only effective against liver cells probably through arresting cell cycle and enabling repair mechanisms. The other derivatives (9, 13, and 14b) had broader antiproliferative activity against both cell lines. These derivatives enhance the expression of the p53 and caspases 9 and 3 to varying degrees in both cell lines. Derivative 14b caused the highest induction in the investigated genes and was the only derivative to inhibit the EGFR activity. Conclusions: The unique features about derivative 14b could be attributed to its high lipophilicity, high carbon content, or its extended conjugation through planar aromatic system. More investigations are required to identify the lead compound(s) in animal models.


2021 ◽  
Vol 22 (2) ◽  
pp. 862
Author(s):  
Noemi Monti ◽  
Maria Grazia Masiello ◽  
Sara Proietti ◽  
Angela Catizone ◽  
Giulia Ricci ◽  
...  

Metazoan living cells exposed to microgravity undergo dramatic changes in morphological and biological properties, which ultimately lead to apoptosis and phenotype reprogramming. However, apoptosis can occur at very different rates depending on the experimental model, and in some cases, cells seem to be paradoxically protected from programmed cell death during weightlessness. These controversial results can be explained by considering the notion that the behavior of adherent cells dramatically diverges in respect to that of detached cells, organized into organoids-like, floating structures. We investigated both normal (MCF10A) and cancerous (MCF-7) breast cells and found that appreciable apoptosis occurs only after 72 h in MCF-7 cells growing in organoid-like structures, in which major modifications of cytoskeleton components were observed. Indeed, preserving cell attachment to the substrate allows cells to upregulate distinct Akt- and ERK-dependent pathways in MCF-7 and MCF-10A cells, respectively. These findings show that survival strategies may differ between cell types but cannot provide sufficient protection against weightlessness-induced apoptosis alone if adhesion to the substrate is perturbed.


Molecules ◽  
2022 ◽  
Vol 27 (2) ◽  
pp. 447
Author(s):  
Christos Vassileiou ◽  
Stefania Kalantzi ◽  
Eleanna Vachlioti ◽  
Constantinos M. Athanassopoulos ◽  
Christos Koutsakis ◽  
...  

Polyamine toxins (PATs) are conjugates of polyamines (PAs) with lipophilic carboxylic acids, which have been recently shown to present antiproliferative activity. Ten analogs of the spider PATs Agel 416, HO-416b, and JSTX-3 and the wasp PAT PhTX-433 were synthesized with changes in the lipophilic head group and/or the PA chain, and their antiproliferative activity was evaluated on MCF-7 and MDA-MB-231 breast cancer cells, using Agel 416 and HO-416b as reference compounds. All five analogs of PhTX-433 were of very low activity on both cell lines, whereas the two analogs of JSTX-3 were highly active only on the MCF-7 cell line with IC50 values of 2.63–2.81 μΜ. Of the remaining three Agel 416 or HO-416b analogs, only the one with the spermidine chain was highly active on both cells with IC50 values of 3.15–12.6 μM. The two most potent compounds in this series, Agel 416 and HO-416b, with IC50 values of 0.09–3.98 μΜ for both cell lines, were found to have a very weak cytotoxic effect on the MCF-12A normal breast cells. The present study points out that the structure of both the head group and the PA chain determine the strength of the antiproliferative activity of PATs and their selectivity towards different cells.


Toxicology ◽  
2006 ◽  
Vol 226 (1) ◽  
pp. 56-57
Author(s):  
Valon Llabjani ◽  
Michael J. Walsh ◽  
Maneesh Singh ◽  
Pierre L. Martin-Hirsch ◽  
Francis L. Martin
Keyword(s):  

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