Abstract
Purpose : To evaluate the anti-tumor activity and explore the possible mechanisms of action of paederosidic acid isolated from Paederia scandens (Lour.) Merrill. Methods : Paederosidic acid (PA) was isolated from P. scandens and identified by spectroscopic methods. The cytotoxic effects of PA in gastric cancer cell lines (MGC-803, BGC-823, and SGC-7901 cells) were assayed using 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT). Apoptosis of PA in SGC-7901 cells was evaluated by DAPI staining. To investigate the possible mechanisms of apoptosis, the effect of PA on C-caspase-3, C-caspase-9, Bcl-2 and Bax expressions in SGC-7901 cells were assayed by Western blot analysis. Results : PA exerted significant inhibitory effects on MGC-803, BGC-823, and SGC-7901 cells with 50 % inhibitory concentration (IC50) values of 42.2, 43.7, and 30.5 μM, respectively, and in a concentration-dependent manner. Subsequently, SGC-7901 cells were selected for further studies. After treatment with PA, obvious condensation of the nucleus was observed in fluorescence photomicrographs, which is a characteristic of apoptosis. In addition, caspase-3, caspase-9 proteins and Bax were significantly up-regulated (p < 0.05), whereas Bcl-2 was significantly down-regulated (p < 0.05) by PA in a concentration-dependent manner. Conclusion : PA has significant anti-tumor activity on SGC-7901 cells in vitro, and the possible mechanism of action may be related to PA-induced apoptosis via mitochondria-mediated apoptosis pathway. Keywords : Paederosidic acid, Paederia scandens, Anti-tumor activity, Apoptosis, Gastric cancer
Highlights
Gastric cancer (GC) is a common cancer worldwide, and it is the second leading cause of cancer mortality [1]
The SGC-7901 cell line was selected from three cell lines for further research due to paederosidic acid (PA) possess the best antiproliferative effect on SGC-7901 among the three tested cell lines
After treatment with PA, significant condensation of the nucleus was induced as shown in Figure 3, which meets the characteristics of apoptosis
Summary
Gastric cancer (GC) is a common cancer worldwide, and it is the second leading cause of cancer mortality [1]. Paederia scandens (Lour.) Merrill, known as “Ji Shi Teng” in Chinese, is a climbing plant belonging to the family Rubiaceae [8]. It is widely distributed in China, India, Vietnam, Japan, the Philippines, and the USA. All cell lines were cultured in RPMI-1640 medium with 10 % fetal bovine serum, 100 U/mL penicillin and 100 mg/mL streptomycin. All these cells were incubated in the presence of 5 % CO2 at 37 oC. Proteins were probed with corresponding primary monoclonal antibody respectively and with goat antirabbit/HRP subsequently, and detected by using the chemiluminescence peroxidase reagents. Results were analyzed by one-way analysis of variance (ANOVA) and p < 0.05 was considered significant
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