scholarly journals Fabrication, Characterization, and Functionalization of Single-Walled Carbon Nanotube Conjugated with Tamoxifen and Its Anticancer Potential against Human Breast Cancer Cells

2018 ◽  
Vol 2018 ◽  
pp. 1-13 ◽  
Author(s):  
Arshin Oskoueian ◽  
Khamirul Amin Matori ◽  
Saadi Bayat ◽  
Ehsan Oskoueian ◽  
Farhad Ostovan ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Polyethylene Glycol ◽  
Cancer Cells ◽  
Human Breast Cancer ◽  
Breast Cancer Cells ◽  
Hydroxyl Groups ◽  
Cytotoxic Action ◽  
Therapeutic Effects ◽  
Human Breast Cancer Cells ◽  
Human Breast

In this experiment, we aimed to fabricate SWCNT conjugated with tamoxifen and evaluated its anticancer potential against human breast cancer cells (MCF-7). The results showed that SWCNT was synthetized successfully using chemical vapor deposition (CVD) method. The results of Raman spectroscopy, SEM, and TEM analyses confirmed the synthesis of highly pure SWCNT. The functionalization of SWCNT was performed by oxidizing of SWCNT, attachment of polyethylene glycol (PEG) to oxidized SWCNT, and attachment of azelaic acid to the polyethylene glycol group. As a result, the SWCNT with free functional carboxylic acid and hydroxyl groups (SWCNT-PEG) was developed. The SWCNT-PEG was then conjugated with tamoxifen (SWCNT-PEG-TAM). The FT-IR together with NMR results confirmed the conjugation of tamoxifen to functionalized SWCNT (SWCNT-PEG-TAM). The cytotoxic concentrations (CC50) of SWCNT-PEG, tamoxifen, and SWCNT-PEG-TAM were >100, 12.67±2.69, and 5.49±1.34μg/ml, respectively. Linking tamoxifen to functionalized SWCNT enhanced the cytotoxic action of tamoxifen against breast cancer cells up to 2.3 times. The results of the morphological examination and caspase-3 activity confirmed the higher cytotoxic action of SWCNT-PEG-TAM as compared to free tamoxifen. The results obtained in this study indicated that this delivery system enhanced the therapeutic effects and anticancer potential of tamoxifen against human breast cancer cells.

scholarly journals Effect of sulphation on the oestrogen agonist activity of the phytoestrogens genistein and daidzein in MCF-7 human breast cancer cells

2008 ◽  
Vol 197 (3) ◽  
pp. 503-515 ◽  
Author(s):  
D Pugazhendhi ◽  
K A Watson ◽  
S Mills ◽  
N Botting ◽  
G S Pope ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cancer Cells ◽  
Human Breast Cancer ◽  
Breast Cancer Cells ◽  
The Body ◽  
Hydroxyl Groups ◽  
Agonist Activity ◽  
Human Breast Cancer Cells ◽  
Human Breast ◽  
Mcf 7

The phytoestrogens genistein, daidzein and the daidzein metabolite equol have been shown previously to possess oestrogen agonist activity. However, following consumption of soya diets, they are found in the body not only as aglycones but also as metabolites conjugated at their 4′- and 7-hydroxyl groups with sulphate. This paper describes the effects of monosulphation on the oestrogen agonist properties of these three phytoestrogens in MCF-7 human breast cancer cells in terms of their relative ability to compete with [3H]oestradiol for binding to oestrogen receptor (ER), to induce a stably transfected oestrogen-responsive reporter gene (ERE-CAT) and to stimulate cell growth. In no case did sulphation abolish activity. The 4′-sulphation of genistein reduced oestrogen agonist activity to a small extent in whole-cell assays but increased the relative binding affinity to ER. The 7-sulphation of genistein, and also of equol, reduced oestrogen agonist activity substantially in all assays. By contrast, the position of monosulphation of daidzein acted in an opposing manner on oestrogen agonist activity. Sulphation at the 4′-position of daidzein resulted in a modest reduction in oestrogen agonist activity but sulphation of daidzein at the 7-position resulted in an increase in oestrogen agonist activity. Molecular modelling and docking studies suggested that the inverse effects of sulphation could be explained by the binding of daidzein into the ligand-binding domain of the ER in the opposite orientation compared with genistein and equol. This is the first report of sulphation enhancing activity of an isoflavone and inverse effects of sulphation between individual phytoestrogens.

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