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黄芪多糖的硫酸化修饰、表征及抗肿瘤活性。

Sulfated modification, characterization and antitumor activities of Radix hedysari polysaccharide.

机构信息

School of Basic Medical Science, Lanzhou University, Lanzhou 730000, China.

出版信息

Int J Biol Macromol. 2012 Nov;51(4):471-6. doi: 10.1016/j.ijbiomac.2012.06.004. Epub 2012 Jun 15.

Abstract

Sulfated modification of a polysaccharide obtained from Radix hedysari (RHP) was studied. Four sulfated derivatives (RHPS) with variable degrees of substitution (DS) were obtained by the chlorosulfonic acid method with ionic liquids (ILs) as solvent and 4-dimethylaminopyridine (DMAP) as catalyst. The structures of RHPS were characterized by FT-IR spectra and ¹³C NMR spectra, and the results indicated that the sulfated groups were modified mainly at the C-6 position and C-2 position. Four kinds of RHPS showed different DS ranging from 0.63 to 1.45, and different weight-average molecular mass (Mw) ranging from 60.8 to 71.1 kDa with a little degradation. Compared with RHP, all of RHPS exhibited obvious antitumor activity on A549 cells and BGC-823 cells in vitro. However, they had no obvious influence on HEK293 cells, which indicated that they had low toxicity to normal cells. Flow cytometric studies indicated that the treatment of RHPS against A549 cells and BGC-823 cells could mediate the cell-cycle arrest in the G1 phase.

摘要

对从狼牙刺(RHP)中获得的多糖进行了硫酸酯化修饰研究。采用离子液体(ILs)作为溶剂,4-二甲氨基吡啶(DMAP)作为催化剂,用氯磺酸法得到了 4 种取代度(DS)不同的硫酸酯化衍生物(RHPS)。RHPS 的结构通过傅里叶变换红外光谱(FT-IR)和 ¹³C NMR 光谱进行了表征,结果表明硫酸基主要修饰在 C-6 位和 C-2 位。4 种 RHPS 的 DS 从 0.63 到 1.45 不等,重均分子量(Mw)从 60.8 到 71.1 kDa 不等,略有降解。与 RHP 相比,所有 RHPS 均在体外对 A549 细胞和 BGC-823 细胞表现出明显的抗肿瘤活性。然而,它们对 HEK293 细胞没有明显影响,这表明它们对正常细胞的毒性较低。流式细胞术研究表明,RHPS 对 A549 细胞和 BGC-823 细胞的作用可以介导细胞周期停滞在 G1 期。

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