Fingolimod interrupts the cross talk between estrogen metabolism and sphingolipid metabolism within prostate cancer cells

Allam, Rasha M.; Al‐Abd, Ahmed M.; Khedr, Alaa; Sharaf, Ola A.; Nofal, Salwa M.; Khalifa, Amani E.; Mosli, Hisham A.; Abdel-Naim, Ashraf B.

doi:10.1016/j.toxlet.2018.04.008

Cited by 178 publications

(111 citation statements)

References 50 publications

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“…To examine the in vitro anticancer activity of the two complexes, colorectal cancer cell line (HT-29) and MCF-7 breast adenocarcinoma were treated with different concentrations of p-SC4, p-SC6, oxaliplatin, p-SC4-oxaliplatin and p-SC6-oxaliplatin complexes. The cell viability of HT-29 cells was evaluated using SRB assay [52][53][54]. Briefly, aliquots of 100 µL cell suspension (5 × 10 3 cells) were seeded in 96-well plates and incubated in DMEM medium for 24 h at 37 • C and 7% CO 2 .…”

Section: Sulforhodamine B Colorimetric Assay (Srb)mentioning

confidence: 99%

Host-Guest Complexation of Oxaliplatin and Para-Sulfonatocalix[n]Arenes for Potential Use in Cancer Therapy

et al. 2020

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P-sulfonatocalix[n]arenes have demonstrated a great potential for encapsulation of therapeutic drugs via host-guest complexation to improve solubility, stability, and bioavailability of encapsulated drugs. In this work, guest-host complexes of a third-generation anticancer drug (oxaliplatin) and p-4-sulfocalix[n]arenes (n = 4 and 6; p-SC4 and p-SC6, respectively) were prepared and investigated, using 1H NMR, UV, Job’s plot analysis, and DFT calculations, for use as cancer therapeutics. The peak amplitude of the prepared host-guest complexes was linearly proportional to the concentration of oxaliplatin in the range of 1.0 × 10−5 M−1 to 2.1 × 10−4 M−1. The reaction stoichiometry between either p-SC4 or p-SC6 and oxaliplatin in the formed complexes was 1:1. The stability constants for the complexes were 5.07 × 104 M−1 and 6.3 × 104 M−1. These correspond to complexation free energy of −6.39 and −6.52 kcal/mol for p-SC4 and p-SC6, respectively. Complexation between oxaliplatin and p-SC4 or p-SC6 was found to involve hydrogen bonds. Both complexes exhibited enhanced biological and high cytotoxic activities against HT-29 colorectal cells and MCF-7 breast adenocarcinoma compared to free oxaliplatin, which warrants further investigation for cancer therapy.

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Section: Sulforhodamine B Colorimetric Assay (Srb)mentioning

confidence: 99%

Host-Guest Complexation of Oxaliplatin and Para-Sulfonatocalix[n]Arenes for Potential Use in Cancer Therapy

et al. 2020

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“…The Supplementary Material Figures S1-S36 contain the NMR charts for the synthesized compounds. In the present work, sulforhodamine B (SRB) colorimetric assay [29,30] was done to evaluate the cytotoxic activity of the synthesized 3-cyano pyridines 4a-4e, 5a-5e, and 6a-6e on three human cancer cell lines: prostate carcinoma (PC-3), breast cancer (MDA-MB-231) and hepatocellular carcinoma (HepG2) cell lines. 5-FU was used as a standard drug for comparison.…”

Section: Chemistrymentioning

confidence: 99%

Discovery of Novel 3-Cyanopyridines as Survivin Modulators and Apoptosis Inducers

et al. 2020

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The overexpression of survivin is usually accompanied by an increased resistance of cancer cells to chemotherapeutic agents in addition to cancer aggressiveness. Consequently, survivin is considered as an attractive target to develop new promising anticancer candidates. A series of novel 3-cyanopyridine derivatives was synthesized and assessed for their cytotoxic activity against three human cancer cell lines: prostate carcinoma (PC-3), breast cancer (MDA-MB-231) and hepatocellular carcinoma (HepG2). In addition, their activities were evaluated in comparison with a standard anticancer drug 5-FU. Compounds 5c and 5e both exhibited promising cytotoxicity against all the tested cell lines; especially, 5e showed better cytotoxic effect than the reference drug 5-FU. In order to evaluate the safety of these compounds, they were tested on the normal cell line WI-38, revealing their toxic selectivity toward cancer cells over normal ones. Further studies were performed in order to understand their mechanism of action; we examined the ability of our promising compounds 5c and 5e to induce cell cycle arrest. Both resulted in a notable induction of cell cycle arrest at the G2/M phase, along with an increase in the DNA content in the pre-G1 phase, giving us an indication of the incidence of apoptosis. 5c and 5e were further subjected to additional study using Annexin V-FITC assay in order to evaluate their ability to induce apoptosis. The results showed a marked increase in the early and late apoptotic cells, as well as an increase in the percentage of necrosis. Furthermore, Western blotting assay was accomplished using different concentrations of 5c and 5e. The results revealed a striking reduction in survivin expression through proteasome-dependent survivin degradation in addition to a decrease in the expression of some other inhibitor of apoptosis proteins (IAP) family proteins: Livin, XIAP, and C-IAP1 in a concentration-dependent manner. A docking study of 5c and 5e compounds in the dimerization site of survivin was also performed, showing agreement with the in vitro anti-survivin activity.

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“…Then, 150 mL of Tris (10 mM) was added to dissolve protein-bound SRB stain; the absorbance was measured at 540 nm using microplate reader. The percentage of cell viability was calculated by using the following formula: 26 Percentage viability ¼ A 540 nm of treated cells A 540 nm of untreated control cells Â 100…”

Section: Cytotoxicity Assaymentioning

confidence: 99%

Identification, isolation, structural characterization, in silico toxicity prediction and in vitro cytotoxicity assay of simeprevir acidic and oxidative degradation products

et al. 2020

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Fingolimod interrupts the cross talk between estrogen metabolism and sphingolipid metabolism within prostate cancer cells

Cited by 178 publications

References 50 publications

Host-Guest Complexation of Oxaliplatin and Para-Sulfonatocalix[n]Arenes for Potential Use in Cancer Therapy

Host-Guest Complexation of Oxaliplatin and Para-Sulfonatocalix[n]Arenes for Potential Use in Cancer Therapy

Discovery of Novel 3-Cyanopyridines as Survivin Modulators and Apoptosis Inducers

Identification, isolation, structural characterization, in silico toxicity prediction and in vitro cytotoxicity assay of simeprevir acidic and oxidative degradation products

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