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Jin X.,Jiangsu Provincial Academy | Jin X.,Nanjing University | Zhang Z.-H.,Jiangsu Provincial Academy | Chen L.-L.,Jiangsu Provincial Academy | And 4 more authors.
Chinese Traditional and Herbal Drugs | Year: 2011

Objective: To investigate the effect of non-ionic surfactant vitamin E tocopherol polyethylene glycol succinate 1000 (TPGS) on the intestinal absorption of baohuoside I across membrane transport of Caco-2 monolayer model. Methods: The membrane transport of Caco-2 monolayer model was carried out to examine the effects of TPGS on the intestinal absorption of baohuoside I. The baohuoside I was determined by UPLC and the apparent permeability coefficients (P app) were calculated. Results: P app values of membrane transport capacity from the apical (AP) to basolateral (BL) of baohuoside I were significantly increased (P<0.05) and its efflux ratios were markedly reduced (P<0.05) in the presence of the TPGS. The efflux of baohuoside I was 1.9788, 1.7798, and 1.6090, respectively, when the proportion of baohuoside I and TPGS was 1:1, 1:3, and 1:9. The ratio decreased 73%, 76%, and 78% by using baohuoside I only. Conclusion: TPGS could obviously promote the absorption of baohuoside I on Caco-2 monolayer model.

Feng L.,Jiangsu Provincial Academy | Chen Y.,Jiangsu Provincial Academy | Yuan L.,Jiangsu Provincial Academy | Liu X.,Jiangsu Provincial Academy | And 3 more authors.
Molecules | Year: 2013

Experiments were conducted to evaluate the induction of apoptosis and the immunomodulatory activities of alkaloids and triterpenes of Alstonia scholaris (Linn.) R. Br. leaves (ASL). Importantly, their possible synergistic properties were also explored in this study. Human lung adenocarcinoma cell line A549 and Lewis tumor-bearing C57BL/6 mice were used for the evaluation of their activities. A MTT assay was used to determine the proliferation inhibition in A549 cells. Annexin-V/PI double staining as well as flow cytometry was performed to detect apoptosis and cell cycle status. Enzyme-linked immunosorbent assay (ELISA) was conducted to determine the levels of inflammatory mediators interleukin-6 (IL-6) and tumor necrosis factor-α (TNF-α) in serum. Furthermore, western blot analysis was applied to evaluate the expressions of proteins associated with cell death. Alkaloids or triterpenes showed a high anti-proliferative activity in A549 cells, with IC50 values of 14.4 μg/mL and 9.3 μg/mL, respectively. The alkaloids and triterpenes combination could significantly inhibit tumor growth in tumor-bearing C57BL/6 mice, compared with alkaloids or triterpenes alone (7.5, 15, 30 g raw material/kg). The immune organs indexes including spleen index and thymus index were increased remarkably by the combination of alkaloids and triterpenes, whereas the levels of IL-6 and TNF-α were up-regulated significantly. Moreover, Annexin-V/PI double staining and flow cytometry showed that the combination of alkaloids and triterpenes (1, 2 and 3 mg raw material/kg) could induce apoptosis and cause S cell cycle arrest in A549 cells. Western blot analysis also showed that their combination (2 mg raw material/kg) significantly down-regulated Bcl-2 expression and pro-casp8 level, whereas it remarkably increased the level of cleaved caspase-8 leading to apoptosis in A549 cells. These observations provide preliminary evidence that both alkaloids and triterpenes possess immune regulation and induction apoptosis activities. Their combination has a stronger activity than that of either class alone. Our findings suggested that these components might be beneficial for the prevention and treatment of NSCLC through a significant synergy effect. © 2013 by the authors.

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