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首页> 外文期刊>Natural product communications >Inhibition of mast cell degranulation by saponins from Gleditsia sinensis- structure-activity relationships
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Inhibition of mast cell degranulation by saponins from Gleditsia sinensis- structure-activity relationships

机译：皂角皂苷对肥大细胞脱粒的抑制作用-构效关系

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摘要

The objective of the present study was to investigate the effects of saponins from the anomalous fruits of Gleditsia sinensis on mast cell degranulation triggered by compound 48/80 and to determine possible structure-activity relationships. Among the eleven saponins tested, four effectively inhibited β-hexosaminidase release from rat peritoneal mast cells. Studies of structure-activity relationships indicated that saponins with an aglycone of echinocystic acid instead of oleanolic acid were more effective. A sugar chain at C-3 was essential for the inhibitory effects, and a single sugar chain was the most effective. The length and structures of the oligosaccharide chain at C-28 were also critical for the activity of the compounds, and introduction of monoterpene units to the oligosaccharide chain substantially decreased the activity. To gain insight into the mechanisms responsible for preventing mast cell degranulation, the effects of saponins on intracellular cAMP were examined. After preincubation with mast cells for different times, the four active saponins significantly increased the intracellular cAMP content. These findings suggested that the four saponins might be the active constituents of the anomalous fruits of G. sinensis for antiallergic activities, and they prevented mast cell degranulation probably by elevating intracellular cAMP levels.
机译：本研究的目的是研究皂角异常果实中的皂苷对化合物48/80触发的肥大细胞脱粒的影响，并确定可能的构效关系。在测试的11种皂苷中，有4种有效抑制了大鼠腹膜肥大细胞中的β-己糖胺酶释放。结构-活性关系的研究表明，皂苷配以棘孢囊酸而不是齐墩果酸的糖苷配基更有效。 C-3处的糖链对于抑制作用至关重要，而一条糖链最有效。 C-28处的寡糖链的长度和结构对于化合物的活性也很关键，并且将单萜单元引入寡糖链实质上降低了活性。为了深入了解防止肥大细胞脱粒的机制，我们研究了皂苷对细胞内cAMP的作用。与肥大细胞预温育不同时间后，四种活性皂苷显着增加了细胞内cAMP含量。这些发现表明这四种皂苷可能是中华绒螯蟹异常果实抗过敏活性的活性成分，并且它们可能通过升高细胞内cAMP水平来防止肥大细胞脱粒。

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