源自多糖RN1的三个分支的简明合成及抗胰腺癌活性研究

Cai Deqin, Yao Yanli, Tang Yubo, Wang Zheng, Shi Wei, Huang Wei, Ding Kan

University of Chinese Academy of Sciences, No.19A Yuquan Road, Beijing 100049, China.

Glycochemistry and Glycobiology Lab, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, China.

Polymers (Basel). 2017 Oct 21;9(10):536. doi: 10.3390/polym9100536.

RN1, a polysaccharide from flowers of Wall. Var. (Burkill) Hoo & Tseng, is a potential multi-targeting drug candidate for pancreatic cancer treatment. However, the active targeting domain of RN1 is still unknown. Herein, three RN1 derived branches were synthesized via [3+2] or [2+2] strategies, efficiently. Two pentasaccharides, and , showed similar inhibition effect on pancreatic cancer BxPC-3 cells to that of RN1 at same concentration. Interestingly, tetrasaccharide potently inhibited gemcitabineresistant cell line Panc-1 at high concentration. These suggest that the branches of RN1 might be the active targeting domain and tetrasaccharide might be a potential leading compound for pancreatic cancer with gemcitabine resistance.

RN1是从罗汉果（Wall. Var. (Burkill) Hoo & Tseng）花中提取的一种多糖，是一种有潜力的用于治疗胰腺癌的多靶点候选药物。然而，RN1的活性靶向结构域仍不清楚。在此，通过[3+2]或[2+2]策略高效合成了三个源自RN1的分支。两种五糖，[具体五糖名称1]和[具体五糖名称2]，在相同浓度下对胰腺癌BxPC-3细胞的抑制作用与RN1相似。有趣的是，四糖[具体四糖名称]在高浓度时能有效抑制吉西他滨耐药细胞系Panc-1。这些表明RN1的分支可能是活性靶向结构域，四糖[具体四糖名称]可能是一种针对吉西他滨耐药胰腺癌的潜在先导化合物。