Structure-function relationship of the saponins from the roots of Platycodon grandiflorum for hemolytic and adjuvant activity

Structure-function relationship of the saponins from the roots of Platycodon grandiflorum for hemolytic and adjuvant activity
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桔梗根皂苷溶血活性和佐剂活性的结构-功能关系

DOI:
10.1016/j.intimp.2011.08.018
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发表时间:
2011-12-01
影响因子:
5.6
通讯作者:
Zhou, Jiyong
Zhou, Jiyong
中科院分区:
医学2区
文献类型:
--
作者:
Sun, Hongxiang;Chen, Liqing;Zhou, Jiyong

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比较了桔梗皂苷D(PD)、D2(PD2)、D3(PD3)、桔梗皂苷A(PA)、E(PE)、脱脂糖苷E(DPE)和聚半乳糖素D2(PGD)的溶血活性和对新城疫重组禽流感疫苗(RL-H5)免疫应答的佐剂作用。7个化合物的溶血活性大小顺序为:Pd>Pd2≫PA>Pd3≫PE>DPE。PD、PD2、PA和PGD不仅能显著促进刀豆蛋白A(ConA)、脂多糖(LPS)和抗原诱导的小鼠脾细胞增殖,而且能显著增强RL-H5免疫小鼠的NK细胞活性。PD和PD2可提高免疫小鼠的特异性抗体效价,而PA和PGD仅能诱导免疫小鼠产生抗体应答。然而,没有观察到其他三种皂苷的佐剂活性。结果表明,C-3上的糖链、苷元C-28位的缩水甘油部分以及苷元影响其生物活性。有趣的是,通过反相高效液相分析,它们的溶血和佐剂活性随着保留时间的延长而增加。保留时间可用于初步评价皂苷与相同苷元的基本辅助性。(C)2011爱思唯尔B.V.保留所有权利。
To assess the contribution of the aglycone and sugar chain to the biological activity of saponins from Platycodon grandiflorum, seven structurally consecutive saponins, platycodin D (PD), D2 (PD2), D3 (PD3), platycoside A (PA), E (PE), deapioplatycoside E (DPE), and polygalacin D2 (PGD) were compared for their hemolytic activities and adjuvant potentials on the immune responses to Newcastle disease virus-based recombinant avian influenza vaccine (rL-H5) in mice. Among seven compounds, the order of the hemolytic activity was PGD approximate to PD>PD2>PA>PD3>PE>DPE. PD, PD2, PA, and PGD significantly not only promoted concanavalin A (Con A)-, lipopolysaccharide (LPS)- and antigen-induced splenocyte proliferation, but enhanced the NK cell activity in mice immunized with rL-H5. PD and PD2 increased the antigen specific IgG, IgG1, IgG2a, and IgG2b antibody titers, while PA and PGD only induce the IgG and IgG1 antibody responses in the immunized mice. However, the other three saponins were not observed for adjuvant activity. The results suggested that the sugar chains attached to C-3, the glycidic moiety at C-28 of aglycone, as well as aglycone affect their biological activities. Interestingly, their hemolytic and adjuvant activities increased with the retention time by reverse phase HPLC analysis. The retention time may be useful for primary estimation of fundamental adjuvanticity of saponin with the same aglycone. (C) 2011 Elsevier B.V. All rights reserved.