Department of Chemistry, Wuhan University, Wuhan 430072, People's Republic of China.
J Agric Food Chem. 2009 Nov 25;57(22):10565-72. doi: 10.1021/jf902597w.
Two water-soluble derivatives, sulfated and carboxymethylated Ganoderma lucidem polysaccharides, coded as S-GL and CM-GL, were prepared using derivatization of water-insoluble polysaccharides (GL-IV-I) extracted from the fruit body of G. lucidem . The degree of substitution (DS) of S-GL and CM-GL was 0.94 and 1.09, respectively. The weight-average molecular mass (Mw) of GL-IV-I, S-GL, and CM-GL was determined with light scattering to be 13.3x10(4), 10.1x10(4), and 6.3x10(4), respectively. S-GL and CM-GL inhibited the in vitro proliferation of Sarcoma 180 (S-180) tumor cells in a dose-dependent manner, with an IC50 value of 26 and 38 microg/mL, respectively. They also inhibited the growth of S-180 solid tumors implanted in BALB/c mice, with low toxicity to the animals. Flow cytometric studies revealed that treatment of S-GL and CM-GL with S-180 tumor cells could mediate the cell-cycle arrest in the G2/M phase. The expression of Bax increased, and the expression of Bcl-2 decreased dramatically, as shown by immuno-histochemical staining of S-180 tumor tissue excised from the animals. The sulfated and carboxmethylated groups in the polysaccharides played an important part in enhancing their antitumor activities, leading to the potential to be developed into antitumor drugs.
两种水溶性衍生物，硫酸化和羧甲基化灵芝多糖，分别编码为 S-GL 和 CM-GL，是通过对从灵芝子实体中提取的不溶性多糖（GL-IV-I）进行衍生化制备的。S-GL 和 CM-GL 的取代度分别为 0.94 和 1.09。GL-IV-I、S-GL 和 CM-GL 的重均分子量（Mw）分别用光散射法测定为 13.3x10(4)、10.1x10(4)和 6.3x10(4)。S-GL 和 CM-GL 呈剂量依赖性抑制肉瘤 180（S-180）肿瘤细胞的体外增殖，IC50 值分别为 26 和 38 μg/mL。它们还抑制了 BALB/c 小鼠体内 S-180 实体瘤的生长，对动物的毒性较低。流式细胞术研究表明，S-GL 和 CM-GL 处理 S-180 肿瘤细胞可介导细胞周期停滞在 G2/M 期。免疫组织化学染色显示，S-180 肿瘤组织中 Bax 的表达增加，Bcl-2 的表达明显下降。多糖中的硫酸化和羧甲基化基团在增强其抗肿瘤活性方面发挥了重要作用，有望开发成为抗肿瘤药物。
