Department of Natural Medicines, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
J Pharm Biomed Anal. 2013 Mar 5;75:64-73. doi: 10.1016/j.jpba.2012.11.024. Epub 2012 Nov 23.
The metabolites and pharmacokinetics of ganoderic acid C2 (GAC2), a bioactive triterpenoid in Ganoderma lucidum in rat plasma were investigated by high-performance liquid chromatography coupled with electrospray ionization tandem mass spectrometry (HPLC-ESI-MS/MS). Totally, ten minor phase I metabolites of GAC2 were characterized after oral administration of GAC2, on the basis of their mass fragmentation pathways or direct comparison with authentic compounds by high-performance liquid chromatography coupled with diode array detection and electrospray ion trap tandem mass spectrometry (HPLC-DAD-ESI-MS(n)), and liquid chromatography coupled with electrospray ionization hybrid ion trap and time-of-flight mass spectrometry (LC-ESI-IT-TOF/MS) methods. Moreover, a rapid and specific method for quantification of GAC2 in rat plasma after oral administration was developed by using a liquid-liquid extraction procedure and HPLC-ESI-MS/MS analysis. It is the first time to report the metabolites and pharmacokinetics of GAC2.
采用高效液相色谱-电喷雾串联质谱（HPLC-ESI-MS/MS）法研究了灵芝中生物活性三萜化合物灵芝酸 C2（GAC2）在大鼠血浆中的代谢物和药代动力学。口服 GAC2 后，基于其质量裂解途径或与高效液相色谱-二极管阵列检测-电喷雾离子阱串联质谱（HPLC-DAD-ESI-MS(n)）和液相色谱-电喷雾离子阱串联飞行时间质谱（LC-ESI-IT-TOF/MS）中鉴定的标准化合物的直接比较，鉴定了 GAC2 的十种微量 I 相代谢物。此外，还通过液-液萃取和 HPLC-ESI-MS/MS 分析，建立了大鼠口服 GAC2 后测定血浆中 GAC2 的快速、特异的定量方法。这是首次报道 GAC2 的代谢物和药代动力学。
