Sulfation can enhance antitumor activities of Artemisia sphaerocephala polysaccharide in vitro and vivo.

In this study, a sulfated Artemisia sphaerocephala polysaccharide (ASPs) was prepared and its antitumor activity was evaluated in tumor cells and Hepatoma 22 (H22) tumor-bearing mice. In vitro experiments, ASPs significantly inhibited the growth of HepG2 and Hela cells with the IC50 values of 172.03 and 161.42μg/mL, respectively. Moreover, no direct cytotoxicity against mouse fibroblast L929 normal cells was observed in vitro. After oral administration for 12days, the tumor growth was significantly suppressed by ASPs at the doses of 200mg/kg (inhibition rate of 60.85%). Results of tumor histological morphology and cell cycle analysis showed that ASPs could arrest H22 cells at S phase and promote cell apoptosis. Additionally, immunohistochemical analysis demonstrated that ASPs caused the down-regulation of mutant p53 protein expression in a dose-dependent manner. Therefore, these findings proposed new insight into antitumor properties of sulfated polysaccharide as a promising agent in cancer treatment.