| In vitro: |
| Int J Pharm. 2012 Sep 15;434(1-2):453-9. | | Reformulation of etoposide with solubility-enhancing rubusoside.[Pubmed: 22698860] | Etoposide (ETO), a widely used anti-cancer drug, is constrained by its low aqueous solubility and by side effects from both the drug and its solubilizing excipients. In this study, a recently discovered natural solubilizer Rubusoside (RUB) was used to achieve the solubilization of ETO.
METHODS AND RESULTS:
Dynamic light scattering and freeze-fracture transmission electron microscopy studies showed that ETO and Rubusoside formed ETO-Rubusoside nanoparticles (～6 nm in diameter). The powder of ETO-Rubusoside nanoparticles was completely reconstitutable in water and remained stable in this solution at 25 and 37°C for at least 24h. Under other physiologic conditions, ETO solution was clear and free of precipitation at 25°C, but underwent various structural transformations. In PBS and simulated intestinal fluid, Rubusoside-solubilized ETO underwent epimerization and equilibrated to cis-ETO. In simulated gastric fluid, Rubusoside-solubilized ETO degraded to 4'-demethylepipodophyllotoxin-beta-d-glucoside and 4'-demethylepipodophyllotoxin. Higher temperatures favored epimerization or degradation. Furthermore, a side-by-side comparison with DMSO-solubilized ETO confirmed that the RUB-solubilized ETO showed no significant differences in cytotoxicity in colon, breast and prostate cancer cell lines.
CONCLUSIONS:
Rubusoside effectively solubilized and stabilized etoposide, which sets the stage for further toxicology, bioavailability, and efficacy investigations. | | Chinese Journal of Ethnomedicine & Ethnopharmacy, 2015, 24(24):16-8. | | Protective Effects of Rubusoside on the Ultrastructure and Cyt C Translocation Expression of the Palmitic Acid- induced INS- 1 Cells.[Reference: WebLink] | To investigate the protective mechanism of Rubusoside treating on the palmitic acid- induced INS- 1 cells.
METHODS AND RESULTS:
MTT assay was used to detect the cell viability rate of control group,palmitic acid group and different concentrations of Rubusoside group.
Transmission electron microscope( TEM) was used to observe the ultrastructur of every group and the immune electron microscopy was used to detect cytochrome C translocationexpression. As evidenced by MTT assay,the cell viability significantly was enhanced by different concentrations Rubusoside pretreatment. TEM revealed degenerative changes in the ultramicroscopic structure of palmitic acid- induced INS- 1 cells whereas various concentrationpretreatment with Rubusoside could significantly attenuated the deterioration of the damage. Immune electron microscopy showed that different concentrations Rubusoside could prevent the cytochrome C releasing from mitochondria to cytoplasm with palmitic acid induced.
CONCLUSIONS:
Rubusoside can improve the survival rate of palmitic acid- induced INS- 1 cells and inhibit the occurrence of apoptosis.
It is suggested that the mechanism may be associated with the inhibition of the oxidative stress induced by palmitic acid and prevent the cytochrome C releasing from mitochondrial to cytoplasm,which can activate caspase cascade and a downstream signaling to apopotosis. |
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