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硫酸化可以增强体外和体内青蒿多糖的抗肿瘤活性。

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

机构信息

College of Life Science, Northwest Normal University, Lanzhou 730070, China; Bioactive Products Engineering Research Center for Gansu Distinctive Plants, Northwest Normal University, Lanzhou 730070, China.

College of Life Science, Northwest Normal University, Lanzhou 730070, China.

出版信息

Int J Biol Macromol. 2018 Feb;107(Pt A):502-511. doi: 10.1016/j.ijbiomac.2017.09.018. Epub 2017 Sep 8.

Abstract

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 IC 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.

摘要

在这项研究中,制备了一种硫酸化青蒿多糖(ASPs),并在肿瘤细胞和肝癌 22 荷瘤小鼠中评价了其抗肿瘤活性。体外实验结果表明,ASPs 对 HepG2 和 Hela 细胞的生长具有显著的抑制作用,其 IC 值分别为 172.03μg/mL 和 161.42μg/mL。此外,ASPs 在体外对小鼠成纤维细胞 L929 正常细胞没有直接的细胞毒性。经过 12 天的口服给药,ASPs 在 200mg/kg 剂量下显著抑制肿瘤生长(抑制率为 60.85%)。肿瘤组织形态学和细胞周期分析结果表明,ASPs 可将 H22 细胞阻滞在 S 期,并促进细胞凋亡。此外,免疫组化分析表明,ASPs 可使突变型 p53 蛋白表达呈剂量依赖性下调。因此,这些发现为硫酸化多糖作为一种有前途的癌症治疗药物的抗肿瘤特性提供了新的见解。

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