Effect of a hepatic activation system on the antiproliferative activity of hexamethylmelamine against human tumor cell lines

1985 ◽  
Vol 15 (1) ◽  
Author(s):  
KrysJ. Miller ◽  
ReneeM. McGovern ◽  
MatthewM. Ames
2012 ◽  
Vol 2012 ◽  
pp. 1-12 ◽  
Author(s):  
Lívia Câmara de Carvalho Galvão ◽  
Vivian Fernandes Furletti ◽  
Salete Meyre Fernandes Bersan ◽  
Marcos Guilherme da Cunha ◽  
Ana Lúcia Tasca Góis Ruiz ◽  
...  

This study aimed to evaluate the activity of essential oils (EOs) againstStreptococcus mutansbiofilm by chemically characterizing their fractions responsible for biological and antiproliferative activity. Twenty EO were obtained by hydrodistillation and submitted to the antimicrobial assay (minimum inhibitory (MIC) and bactericidal (MBC) concentrations) againstS. mutansUA159. Thin-layer chromatography and gas chromatography/mass spectrometry were used for phytochemical analyses. EOs were selected according to predetermined criteria and fractionated using dry column; the resulting fractions were assessed by MIC and MBC, selected as active fractions, and evaluated againstS. mutansbiofilm. Biofilms formed were examined using scanning electron microscopy. Selected EOs and their selected active fractions were evaluated for their antiproliferative activity against keratinocytes and seven human tumor cell lines. MIC and MBC values obtained for EO and their active fractions showed strong antimicrobial activity. Chemical analyses mainly showed the presence of terpenes. The selected active fractions inhibitedS. mutansbiofilm formation (P<0.05) did not affect glycolytic pH drop and were inactive against keratinocytes, normal cell line. In conclusion, EO showed activity at low concentrations, and their selected active fractions were also effective against biofilm formed byS. mutansand human tumor cell lines.


Planta Medica ◽  
2014 ◽  
Vol 80 (18) ◽  
pp. 1692-1697 ◽  
Author(s):  
Zsuzsanna Hajdú ◽  
Judit Hohmann ◽  
Peter Forgo ◽  
Imre Máthé ◽  
Judit Molnár ◽  
...  

2009 ◽  
Vol 64 (4) ◽  
pp. 257-263 ◽  
Author(s):  
Buk-Gu Heo ◽  
Sang-Uk Chon ◽  
Yun-Jum Park ◽  
Jong-Hyang Bae ◽  
Su-Min Park ◽  
...  

2008 ◽  
Vol 16 (2) ◽  
pp. 862-868 ◽  
Author(s):  
Julio Benites ◽  
Jaime A. Valderrama ◽  
Felipe Rivera ◽  
Leonel Rojo ◽  
Nair Campos ◽  
...  

2008 ◽  
Vol 46 (10) ◽  
pp. 3325-3332 ◽  
Author(s):  
F. Conforti ◽  
G. Ioele ◽  
G.A. Statti ◽  
M. Marrelli ◽  
G. Ragno ◽  
...  

1989 ◽  
Vol 1 (6) ◽  
pp. 359-365 ◽  
Author(s):  
Richard D. H. Whelan ◽  
Louise K. Hosking ◽  
Alan J. Townsend ◽  
Kenneth H. Cowan ◽  
Bridget T. Hill

2020 ◽  
Vol 17 (4) ◽  
pp. 512-517
Author(s):  
Ognyan Ivanov Petrov ◽  
Yordanka Borisova Ivanova ◽  
Mariana Stefanova Gerova ◽  
Georgi Tsvetanov Momekov

Background: Chemotherapy is one of the mainstays of cancer treatment, despite the serious side effects of the clinically available anticancer drugs. In recent years increasing attention has been directed towards novel agents with improved efficacy and selectivity. Compounds with chalcone backbone have been reported to possess various biological activities such as anticancer, antimicrobial, anti-inflammatory, analgesic, antioxidant, etc. It was reported that aminomethylation of hydroxy chalcones to the corresponding Mannich bases increased their cytotoxicity. In this context, our interest has been focused on the design and synthesis of the so-called multi-target molecules, containing two or more pharmacophore fragments. Methods: A series of Mannich bases were synthesized by the reaction between 6-[3-(3,4,5- trimethoxyphenyl)-2-propenoyl]-2(3Н)-benzoxazolone, formaldehyde, and a secondary amine. The structures of the compounds were confirmed by elemental analysis, IR and NMR spectra. The new Mannich bases were evaluated for their in vitro cytotoxicity against a panel of human tumor cell lines, including BV-173, SKW-3, K-562, HL-60, HD-MY-Z and MDA-MB-231. The effects of selected compounds on the cellular levels of glutathione (GSH) were determined. Results: The new compounds 4a-e exhibited concentration-dependent cytotoxic effects at micromolar concentrations in MTT-dye reduction assay against a panel of human tumor cell lines, similar to those of starting chalcone 3. The tested agents led to concentration - dependent depletion of cellular GSH levels, whereby the effects of the chalcone prototype 3 and its Mannich base-derivatives were comparable. Conclusion: The highest chemosensitivity to the tested compounds was observed in BV- 173followed by SKW-3 and HL-60 cell lines.


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