The reports show that rutin has good potentials as an anticancer agent; however, rutin has poor bioavailability due to its low aqueous solubility. The present study was aimed at preparing and evaluating physicochemical properties as well as the anticancer activities of rutin nanocrystals (RNs). RNs were prepared via the ultrasonication method. The prepared nanocrystals then were physicochemically characterized by the conventional techniques. The cytotoxic effect of RNs and free rutin on the HN5 head and neck squamous carcinoma cell line was assessed. The HGF1-PI1 cells as normal oral cells were treated by RNs. Cells were also exposed to rutin and RNs to determine their effects on the expression of caspase-8, caspase-9, Bcl-2, and Bax genes. The prepared RNs have a mean particle size of  nm and quasispherical morphology. Rutin displayed no significant cytotoxic effect on HN5 cells to 2000 μM. However, RNs displayed a cytotoxic effect with IC50 of 30.51 μM and 27.34 μM in 24 and 48 h incubation times, respectively ( ). RNs had cytotoxic effect 100 times more than rutin on HN5 cells. There was no significant cytotoxic effect on HGF1-PI1 treated by RNs in 24 and 48 h. The expression of Bcl-2 mRNA was significantly decreased in attendance of RNs compared to the control group ( ). The increase in Bax/Bcl-2 ratio was revealed within IC50 of RNs in 24 h. Our results confirm that the anticancer effect of RNs is significantly more than that of rutin. The activation of the mitochondria-dependent apoptotic pathway of RNs occurred via modulation of Bcl-2 and Bax expression. These results suggest that RNs may be useful in the development of a cancer therapy protocol.

/pdf/preparation-characterization-and-evaluation-of-rutin-1tn57l0z76.pdf

Preparation, Characterization, and Evaluation of Rutin Nanocrystals as an Anticancer Agent against Head and Neck Squamous Cell Carcinoma Cell Line

Curcumin is an active ingredient isolated from Curcuma longa. It has several pharmacological effects, including anticancer, anti-inflammatory, and antioxidant effects. Due to its low bioavailability, chemical structure instability, and easy oxidation, the application of curcumin has been limited. In this study, to overcome these limitations, curcumin-loaded mesoporous silica nanoparticles (Cur-MSN) were prepared, and the anticancerous effect of Cur-MSNs on head and neck cancer cells, HN5, was investigated. Transmission electron microscopy (TEM) revealed rod-shaped mesoporous nanoparticles with average particle size smaller than 100 nm. Higher cytotoxicity of Cur-MSNs was seen in treated cancer cells compared with free curcumin. The expression of Bcl-2 was significantly reduced in the presence of Cur-MSNs compared to the control (untreated HN5 cells) (p < 0.05). A 3.43-fold increase in the Bax/Bcl-2 ratio was seen in Cur-MSNs treated HN5 cells at the IC50. Cur-MSNs increased intracellular reactive oxygen species (ROS) production. Based on these novel results, we suggest that Cur-MSNs offer efficacy for cancer treatment and future studies should further characterize their properties in various experimental cancer models.

/pdf/effect-of-curcumin-loaded-mesoporous-silica-nanoparticles-on-1rfoyb2x.pdf

Effect of Curcumin-Loaded Mesoporous Silica Nanoparticles on the Head and Neck Cancer Cell Line, HN5

Statement of the Problem: Evidence shows thiabendazole has the potential to inhibit angiogenesis in melanoma and fibrosarcoma; however, its effect on oral squamous cell carcinoma has not been previously studied. Purpose: This study sought to assess the cytotoxic effects of thiabendazole on HN5 head and neck squamous carcinoma cell line. Materials and Method: HN5 cell lines were exposed to different concentrations of thiabendazole (prepared from 99% pure powder) for 24, 48 and 72 hours. Cell viability was assessed by the methyl thiazol tetrazolium assay, and IC50 of thiabendazole was calculated. Cells were also exposed to different concentrations of thiabendazole for 48 hours to determine its effect on expression and transcription of vascular endothelial growth factor gene. Expression of vascular endothelial growth factor mRNA was assessed by real-time polymerase chain reaction. The vascular endothelial growth factor release was assessed by the enzyme-linked immunosorbent assay test. Results: In all concentrations of thiabendazole except for 200 and 550μM, cell viability was significantly different at different time points ( p < 0.05). At 48 and 72 hours, cell viability at all concentrations of thiabendazole (100-650μM) significantly decreased compared to the control group (zero concentration). In addition, cell viability significantly decreased with an increase in thiabendazole concentration. At 48 hours, expression of vascular endothelial growth factor mRNA was significantly lower in presence of 500μM thiabendazole compared to the control group ( p < 0.001) and release of vascular endothelial growth factor was inhibited in a dose-dependent manner. Conclusion: Thiabendazole inhibited the proliferation of HN5 cells in a dose-dependent and time-dependent manner. It also inhibited the expression of vascular endothelial growth factor gene.  Keywords ● Carcinoma  ● Squamous Cell  ● Vascular Endothelial Growth Factor  ● Angiogenesis Inhibitors  ● Thiabendazole

Cytotoxic Effect of Thiabendazole on Hn5 Head and Neck Squamous Cell Carcinoma Cell Line.

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Cytotoxic Effect of Thiabendazole on Hn5 Head and Neck Squamous Cell Carcinoma Cell Line.