Contribution of the glycidic moieties to the haemolytic and adjuvant activity of platycodigenin-type saponins from the root of Platycodon grandiflorum
Contribution of the glycidic moieties to the haemolytic and adjuvant activity of platycodigenin-type saponins from the root of Platycodon grandiflorum
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缩水甘油部分对桔梗根皂苷溶血和佐剂活性的贡献
DOI：
10.1016/j.vaccine.2008.04.023
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发表时间：
2008-06-25
期刊：
影响因子：
5.5
通讯作者：
Li, Duo
中科院分区：
文献类型：
--
作者：
Xie, Yong;Ye, Yi-Ping;Li, Duo
桔梗皂苷D（platycodin D，PD 3）和桔梗皂苷E（platycoside E，PE）是从桔梗（Platycodon grandiflorum）根中分离得到的3种桔梗皂苷配基。所有共享platycodigenin骨架和相同的糖侧链连接到C-28的糖苷配基，唯一的区别彼此的糖基单元的数量连接到C-3。为了评估缩水甘油酸链对生物活性的潜在贡献并阐明Platycocligenin型皂苷的结构-活性关系，评价了这三种皂苷的溶血活性和对小鼠抗卵蛋白（OVA）的细胞和体液免疫应答的佐剂潜力。3种皂苷的溶血活性大小顺序为PD > PD 3> PE（P< 0.001）。PD和PD 3能显著增强卵白蛋白免疫小鼠脾细胞的增殖反应（P< 0.001）。对OVA刺激的脾细胞增殖的促进作用顺序为PD > PD 3> PE（P< 0.05，P< 0.01或P< 0.001）。PD和PD 3可显著提高OVA免疫小鼠血清中OVA特异性IgG、IgG 1、IgG 2a和IgG 2b抗体水平。而PE仅能显著促进OVA免疫小鼠血清中特异性IgG 2a和IgG 2b抗体的产生。PD对抗体应答的辅助作用显著高于PD 3和PE（P < 0.05，P < 0.01或P< 0.001）。同时，PD还显著增强ConA诱导的小鼠脾细胞中细胞因子11-2、IFN-γ、11-4、IL-10和转录因子T-bet、加塔-3的mRNA表达（P< 0.05，P < 0.01，或P< 0.001）。这些结果表明，桔梗皂苷元C-3位糖基上的糖基数目影响桔梗皂苷元的溶血和佐剂活性，PD具有免疫佐剂活性，并通过调节Th 1/Th 2细胞因子和转录因子的基因表达，同时诱导Th 1和Th 2免疫应答。(c)2008爱思唯尔有限公司保留所有权利。
Platycodin D (PD), platycodin D3 (PD3), and platycoside E (PE) were the platycocligenin-type saponins isolated from the root ofPlatycodon grandiflorum. All shared a platycodigenin skeleton and the same sugar side chains attached to C-28 of the aglycone, only differ from one another by the number ofglycosyl units in sugar moieties attached to C-3. To assess the potential contribution of the glycidic chains to the biological activities and elucidate the structure-activity relationships of the platycocligenin-type saponins, these three saponins were evaluated for their haemolytic activities and adjuvant potentials on the cellular and humoral immune responses of mice against ovalburnin (OVA). Among three saponins, the ranking of the haemolytic activity was PD > PD3 > PE (P< 0.001). PD and PD3 could significantly enhance mitogen and OVA-induced splenocyte proliferation in the OVA-immunized mice (P< 0.001). The order of increasing OVA-stimulated splenocyte proliferation was PD > PD3 > PE (P< 0.05, P< 0.01, or P< 0.001). The sera OVA-specific IgG, lgG1, lgG2a and lgG2b antibody levels in the OVA-immunized mice were significantly enhanced by PD and PD3. However, PE only significantly promoted the production ofthe sera OVA-specific IgG2a and lgG2b antibody in the OVA-immunized mice. Adjuvant potentials of PD on antibody responses were higher than those of PD3 and PE (P < 0.05, P < 0.01, or P< 0.001). Meanwhile, PD also significantly enhanced the mRNA expression ofcytokines 11-2, IFN-y, 11-4, and IL-10 and transcription factors T-bet and GATA-3 in mice splenocyte induced by Con A (P< 0.05, P < 0.01, or P< 0.001). These results suggested that the number of sugar residues in the glycidic chains attached to C-3 ofaglycone could affect the haemolytic and adjuvant activities ofplatycocligenin-type saponins, and that PD had immunological adjuvant activity, and simultaneously elicited a Thl and Th2 immune response by regulating gene expression of Th1/Th2 cytokines and transcription factors. (c) 2008 Elsevier Ltd. All rights reserved.