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大黄酸 8-O-β-D-吡喃葡萄糖苷对大黄中番泻苷 A 致泻作用的影响。

The influence of rhein 8-O-β-D-glucopyranoside on the purgative action of sennoside A from rhubarb in mice.

机构信息

Faculty of Pharmacy and Pharmaceutical Sciences, Fukuyama University, 1 Sanzo, Gakuen-cho, Fukuyama, Hiroshima 729–0292, Japan.

出版信息

Biol Pharm Bull. 2012;35(12):2204-8. doi: 10.1248/bpb.b12-00632.

Abstract

Rhubarb is one of the most well-known herbal medicines that constitute daiokanzoto (DKT), which is clinically effective for constipation. Sennoside A is transformed into an active metabolite, rheinanthrone, by intestinal bacteria. Sennoside A in rhubarb showed significantly accelerated metabolic activity in intestinal bacteria in comparison with sennoside A alone. In this study, we investigated the influence of rhubarb constituents on the metabolism and purgative activity of sennoside A. The 20% MeOH-eluted fraction separated by MCI-gel CHP-20P column chromatography from the water extract of rhubarb showed sennoside A metabolic activity similar to that of rhubarb extract. The 20% MeOH elute was further purified and rhein 8-O-β-D-glucopyranoside (RG) was isolated. The metabolic activity of sennoside A was significantly accelerated by increasing the level of RG. Moreover, rhein, emodin and aloe-emodin also accelerated sennoside A metabolism. The purgative activity of sennoside A was significantly accelerated when RG or rhein was concomitantly given with sennoside A in a dose-dependent manner. These results suggest that anthraquinones contribute to the purgative action of sennoside A in rhubarb. Therefore, it is assumed that the influence of anthraquinones on the fate of rheinanthrone transformed from sennoside A may promote the purgative action of sennoside A.

摘要

大黄是构成大承气汤(DKT)的最著名草药之一,在临床上对便秘有效。番泻苷 A 通过肠道细菌转化为活性代谢物大黄蒽酮。与单独的番泻苷 A 相比,大黄中的番泻苷 A 在肠道细菌中表现出明显加速的代谢活性。在这项研究中,我们研究了大黄成分对番泻苷 A 代谢和泻下活性的影响。大黄水提物经 MCI-凝胶 CHP-20P 柱层析以 20%甲醇洗脱部分显示出与大黄提取物相似的番泻苷 A 代谢活性。20%甲醇洗脱部分进一步纯化,分离得到大黄苷 8-O-β-D-吡喃葡萄糖苷(RG)。RG 水平的增加显著加速了番泻苷 A 的代谢。此外,大黄酸、大黄素和芦荟大黄素也加速了番泻苷 A 的代谢。当 RG 或大黄酸与番泻苷 A 同时给予时,番泻苷 A 的泻下活性显著加速,呈剂量依赖性。这些结果表明蒽醌类化合物有助于大黄中番泻苷 A 的泻下作用。因此,可以假设蒽醌类化合物对番泻苷 A 转化而来的大黄蒽酮命运的影响可能促进了番泻苷 A 的泻下作用。

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