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. 2009 Aug;29(8):2993-6.

Selective cytotoxic activities of two novel synthetic drugs on human breast carcinoma MCF-7 cells

Ramesh B Badisa  1 , Selina F Darling-Reed, Patrick Joseph, John S Cooperwood, Lekan M Latinwo, Carl B Goodman
Affiliations

Selective cytotoxic activities of two novel synthetic drugs on human breast carcinoma MCF-7 cells

Ramesh B Badisa et al. Anticancer Res. 2009 Aug.

Abstract

Background: Breast cancer is the second leading cause of cancer deaths in US women. We evaluated two novel compounds, piperidinyl-diethylstilbestrol (DES) and pyrrolidinyl-diethylstilbestrol (DES) for cytotoxicity against brine shrimp larvae, MCF-7 and rat normal liver cells.

Materials and methods: In vivo cytotoxicity was evaluated against shrimp larvae for 24 h, while in vitro cell toxicity was evaluated by dye binding crystal-violet method after 48 h. The role of these compounds on different phases of the cell cycle was assessed by flow cytometry.

Results: In shrimp assay, piperidinyl-DES and pyrrolidinyl-DES were potent with 50% effective dose (ED(50)) values of 7.9+/-0.38 and 15.6+/-1.3 microM, respectively. In MCF-7 and normal liver cells, the 50% lethal concentration (LC(50)) values were 19.7+/-0.95, 17.6+/-0.4 microM and 35.1 and >50 microM, respectively. Cell cycle analyses indicated that MCF-7 cells were arrested at the G(0)/G(1) stage with these compounds.

Conclusion: The results indicate that pyrrolidinyl-DES possesses highly selective, potent anticancer activity.

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Figures

Figure 1
Figure 1
Effect of piperidinyl-DES on MCF-7 cell cycle. The cells at a starting density of 0.18×106/ml per dish in complete medium containing 10% regular FBS were treated with 0, 5, 10 or 15 μM of the compound for 48 h. Cells were harvested and stained by propidium iodide staining solution for 1 h in the dark and analyzed by flow cytometry. Data are represented as mean±SEM (n=3, *p<0.01; highly significant in comparison to control; one-way ANOVA, Bonferronic multiple comparison test).
Figure 2
Figure 2
Effect of pyrrolidinyl-DES on MCF-7 cell cycle. The cells at a starting density of 0.18×106/ml per dish in complete medium containing 10% regular FBS were treated with 0, 5, 10 or 15 μM of the compound for 48 h. Cells were harvested and stained by propidium iodide staining solution for 1 h in the dark and analyzed by flow cytometry. Data are represented as mean±SEM (n=3, *p<0.01; highly significant in comparison to control; one-way ANOVA, Bonferronic multiple comparison test).
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References

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    1. Badisa RB, Badisa VLD, Watson DM, Pilarinou E, Walker EH. Cytotoxic activities of Snow Lotus filtrates against human cancer cell lines, and origin of active factors. Pharmaceut Biol. 2004;42(2):117–124.
    1. Badisa RB, Tzakou O, Couladis M, Pilarinou E. Cytotoxic activities of Salvia plants of Labiatae family. Pharmaceut Biol. 2004;42(8):640–645.

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