Department of Traditional Chinese Medicine, The College of Life Sciences, Northwest University, Xi'an, Shaanxi, PR China.
J Sep Sci. 2012 Jul;35(13):1619-26. doi: 10.1002/jssc.201200131.
Ergosta-4,6,8(14),22-tetraen-3-one (ergone) has been proved to have novel antitumor effects on HepG2 cells. The aim of this study was to investigate the pharmacokinetics, tissue distribution, and biliary excretion of ergone in rats following a single oral administration (5, 10, and 20 mg/kg). The levels of ergone in plasma, tissues, and bile were measured by ultra performance liquid chromatography coupled with electrospray and atmospheric pressure chemical ionization (ESCi)-quadrupole time-of-flight mass spectrometry with novel mass spectrometry(Elevated Energy) (MS(E)) data collection technique method. The results show ergone was distributed and eliminated from rat plasma and in non-linear pharmacokinetics from a dose range of 5-20 mg/kg. The ergone was found to distribute widely in the internal organs, with tissue concentrations in order of lungs, spleen, liver, intestine, kidneys, heart, stomach, parorchis, teasticles, and brain. At 12 h after dosing, the tissue concentrations in the organs were markedly decreased. The lungs, spleen, and liver were the dominant organs with high tissue concentrations that might be the primary sites for metabolism and elimination of ergone. Total recoveries of ergone within 24 h in bile were 34.14%.
麦角甾-4,6,8(14),22-四烯-3-酮(麦角甾酮)已被证明对 HepG2 细胞具有新颖的抗肿瘤作用。本研究旨在研究大鼠单次口服(5、10 和 20mg/kg)后麦角甾酮的药代动力学、组织分布和胆汁排泄。采用超高效液相色谱-电喷雾和大气压化学电离-四极杆飞行时间质谱联用(ESI-Q-TOF MS)结合新型质谱(高能)(MS(E)) 数据采集技术,测定血浆、组织和胆汁中麦角甾酮的浓度。结果表明,麦角甾酮在大鼠血浆中的分布和消除呈非线性,在 5-20mg/kg 剂量范围内呈非线性药代动力学。麦角甾酮广泛分布于内部器官,组织浓度依次为肺、脾、肝、肠、肾、心、胃、胆囊、睾丸和脑。给药 12 小时后,各器官组织浓度明显下降。肺、脾和肝是高组织浓度的主要器官,可能是麦角甾酮代谢和消除的主要部位。24 小时内胆汁中麦角甾酮的总回收率为 34.14%。