Metabolism of rhaponticin and chrysophanol 8-o-β-D-glucopyranoside from the rhizome of Rheum undulatum by human intestinal bacteria and their anti-allergic actions

Metabolism of rhaponticin and chrysophanol 8-o-β-D-glucopyranoside from the rhizome of Rheum undulatum by human intestinal bacteria and their anti-allergic actions
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DOI:
10.1248/bpb.23.830
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发表时间:
2000-07-01
影响因子:
2
通讯作者:
Han, MJ
Han, MJ
中科院分区:
医学4区
文献类型:
--
作者:
Kim, DH;Park, EK;Han, MJ

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从大黄根茎中分离得到的大黄素和大黄酚8-o-β-D-吡喃葡萄糖苷分别被人体肠道菌群代谢为大黄素和大黄酚。从人类粪便中分离的大多数肠道细菌都催化了这些代谢途径。在大黄素和大黄酚8-O-β-D-吡喃葡萄糖苷及其代谢物中,大黄素对透明质酸酶、肥大细胞释放组胺和被动皮肤过敏反应的抑制作用最强。Rhapontigenin的抑制活性强于市售抗过敏药物色甘酸二钠。这些结果表明,波纹刺参根茎中的大黄素是一种具有广泛抗过敏作用的前药。
Rhaponticin and chrysophanol 8-o-beta-D-glucopyranoside isolated from the rhizomes of Rheum undulatum (Family Polygonaceae) are metabolized to rhapontigenin and chrysophanol, respertively, by human intestinal microflora. Most intestinal bacteria isolated from human feces catalyzed these metabolic pathways. Among rhaponticin and chrysophanol 8-o-beta-D-glucopyranoside and their metabolites, rhapontigenin had the most potent inhibitory activity on a hyaluronidase, a histamine release from mast cell and passive cutaneous anaphylaxis (PCA) PCA reaction. The inhibitory activity of rhapontigenin was more potent than that of disodium cromoglycate, one of the commercial anti-allergic drugs. These results suggest that rhaponticin in the rhizomes of R. undulatum is a prodrug that has an extensive anti-allergic property.