Department of Life and Nanopharmaceutical Sciences, Kyung Hee University, 1, Hoegi, Dongdaemun-Ku, Seoul 130-701, Republic of Korea.
J Chromatogr B Analyt Technol Biomed Life Sci. 2010 Jul 1;878(21):1875-80. doi: 10.1016/j.jchromb.2010.05.003. Epub 2010 May 9.
A high-performance liquid chromatography tandem mass spectrometry (HPLC-MS/MS) method employing electrospray ionization (ESI) has been developed for simultaneous determination of lancemaside A (3-O-beta-D-glucuronopyranosyl-3beta, 16alpha-dihydroxyolean-12-en-28-oic acid 28-O-beta-D-xylopyranosyl(1-->3)-beta-D-xylopyranosyl-(1-->4)-alpha-L-rhamnopyranosyl-(1-->2)-alpha-L-arabinopyranosyl ester) and its metabolites in mouse plasma. When lancemaside A (60 mg/kg) was orally administered to mice, echinocystic acid was detected in the blood. T(max) and C(max) of the echinocystic acid were 6.5+/-1.9 h and 56.7+/-29.1 ppb. Orally administered lancemaside A was metabolized to lancemaside X (3beta, 16alpha-dihydroxyolean-12-en-28-oic acid 28-O-beta-D-xylopyranosyl(1-->3)-beta-D-xylopyranosyl-(1-->4)-alpha-L-rhamnopyranosyl-(1-->2)-alpha-L-arabinopyranosyl ester) by intestinal microflora in mice, which was metabolized to echinocystic acid by intestinal microflora and/or intestinal tissues. Human intestinal microflora also metabolized lancemaside A to echinocystic acid via lancemaside X. These results suggest that the metabolism by intestinal microflora may play an important role in pharmacological effects of orally administered lancemaside A.
建立了一种采用电喷雾电离（ESI）的高效液相色谱串联质谱（HPLC-MS/MS）方法，用于同时测定血浆中的龙舌兰糖苷 A（3-O-β-D-吡喃葡萄糖醛酸基-3β，16α-二羟基齐墩果-12-烯-28-酸 28-O-β-D-吡喃木糖基（1'→3）-β-D-吡喃木糖基（1'→4）-α-L-鼠李吡喃糖基（1'→2）-α-L-阿拉伯吡喃糖苷酯）及其代谢物。当龙舌兰糖苷 A（60mg/kg）口服给予小鼠时，在血液中检测到了羽扇豆酸。羽扇豆酸的 Tmax 和 Cmax 分别为 6.5±1.9h 和 56.7±29.1ppb。口服给予的龙舌兰糖苷 A 被肠道微生物群代谢为龙舌兰糖苷 X（3β，16α-二羟基齐墩果-12-烯-28-酸 28-O-β-D-吡喃木糖基（1'→3）-β-D-吡喃木糖基（1'→4）-α-L-鼠李吡喃糖基（1'→2）-α-L-阿拉伯吡喃糖苷酯），然后被肠道微生物群和/或肠道组织代谢为羽扇豆酸。人体肠道微生物群也通过龙舌兰糖苷 X 将龙舌兰糖苷 A 代谢为羽扇豆酸。这些结果表明，肠道微生物群的代谢可能在龙舌兰糖苷 A 的口服给药的药理学作用中发挥重要作用。
