Department of Life and Nanopharmaceutical Sciences, Kyung Hee University, Seoul, South Korea.
Immunopharmacol Immunotoxicol. 2010 Sep;32(3):357-63. doi: 10.3109/08923970903383889.
To investigate the antiallergic effect of the rhizome of Anemarrhena asphodeloides (AA, family Liliaceae), which was found to inhibit the mouse passive cutaneous anaphylaxis (PCA) reaction induced by the antigen-immunoglobulin E (IgE) complex in preliminary experiments, main steroidal saponins, timosaponins AIII, BIII, and D, were isolated and their inhibitory effects against PCA reaction and scratching behaviors investigated in mice. Oral administration of three main steroidal sapogenins blocked the PCA reaction and scratching behaviors, timosaponin AIII was the most potent. However, intraperitoneal administration of timosaponin AIII showed weak inhibition. To understand its metabolism and antiallergic mechanism, timosaponin AIII was anaerobically incubated with human intestinal microflora to afford a main metabolite, sarsasapogenin. Intraperitoneal administration of sarsasapogenin inhibited allergic reaction more potently than timosaponin AIII. In addition, sarsasapogenin more potently inhibited degranulation and IL-4 protein expression of RBL-2H3 cells induced by IgE-antigen complex than timosaponin AIII. On the basis of these findings, antiallergic effect of AA may be due to those of its steroidal constituents, and that of timosaponin AIII may be activated by using intestinal microflora.
为了研究知母根茎（AA，百合科）的抗过敏作用，我们在初步实验中发现它可以抑制抗原-免疫球蛋白 E（IgE）复合物诱导的小鼠被动皮肤过敏（PCA）反应。从知母根茎中分离出主要甾体皂苷、知母皂苷 AIII、BIII 和 D，并研究它们对 PCA 反应和小鼠搔抓行为的抑制作用。三种主要甾体皂苷的口服给药可阻断 PCA 反应和搔抓行为，知母皂苷 AIII 的抑制作用最强。然而，知母皂苷 AIII 的腹腔给药显示出较弱的抑制作用。为了了解其代谢和抗过敏机制，将知母皂苷 AIII 与人体肠道微生物群进行厌氧孵育，得到主要代谢产物菝葜皂苷元。菝葜皂苷元的腹腔给药比知母皂苷 AIII 更有效地抑制过敏反应。此外，菝葜皂苷元比知母皂苷 AIII 更有效地抑制 IgE-抗原复合物诱导的 RBL-2H3 细胞脱颗粒和 IL-4 蛋白表达。基于这些发现，知母的抗过敏作用可能归因于其甾体成分，而知母皂苷 AIII 的作用可能是通过肠道微生物群的作用而被激活的。
