Chen Jian, Wu Hong, Dai Miao-Miao, Li Hui, Chen Jin-Yun, Hu Shun-Li
College of Pharmacy, Anhui University of Chinese Medicine, Key Laboratory of Modernized Chinese Medicine in Anhui Province, Hefei, Anhui, China.
College of Pharmacy, Anhui University of Chinese Medicine, Key Laboratory of Modernized Chinese Medicine in Anhui Province, Hefei, Anhui, China.
Fitoterapia. 2014 Sep;97:111-21. doi: 10.1016/j.fitote.2014.05.023. Epub 2014 Jun 6.
Geniposide (GE), also called Jasminoidin, is the major active ingredient of Gardenia jasminoides Ellis (GJ) fruit, which has long been used in traditional Chinese medicine (TCM). Growing evidences suggested that GE has a great potentiality for treating rheumatoid arthritis (RA). However, GE is rapidly metabolized, and we know little about its availability or metabolites in tissues. To elucidate the distribution of GE and its metabolites in tissues, three groups of adjuvant arthritis (AA) rats were given GE (33, 66 and 120 mg/kg) from days 18 to 24, and the biotransformation of GE in plasma, liver, spleen, synovium, urine and mesenteric lymph node (MLN) of rats was investigated by a novel approach named Information-Dependent Acquisition (IDA)-Mediated LC-MS/MS method. As a result, GE and its four major metabolites were detected as follows: GE, G1, G2 in plasma; GE, G2 in MLNs; only GE in liver and synovium; GE, G2, G3 and G4 in spleen; and GE, G1, G2 and G4 in urine. In total four metabolites (G1-G4) involved in the in vivo metabolism processes were identified. The results of this work have demonstrated the IDA-Mediated LC-MS/MS could screen rapidly and reliably the characterization of metabolites from iridoid compounds.
栀子苷（GE），又称京尼平苷，是栀子果实的主要活性成分，长期应用于传统中药。越来越多的证据表明，栀子苷在治疗类风湿性关节炎（RA）方面具有巨大潜力。然而，栀子苷代谢迅速，我们对其在组织中的可用性或代谢产物了解甚少。为了阐明栀子苷及其代谢产物在组织中的分布，在第18至24天给三组佐剂性关节炎（AA）大鼠给予栀子苷（33、66和120mg/kg），并通过一种名为信息依赖采集（IDA）介导的液相色谱-串联质谱法研究大鼠血浆、肝脏、脾脏、滑膜、尿液和肠系膜淋巴结（MLN）中栀子苷的生物转化。结果，检测到栀子苷及其四种主要代谢产物如下：血浆中有栀子苷、G1、G2；肠系膜淋巴结中有栀子苷、G2；肝脏和滑膜中只有栀子苷；脾脏中有栀子苷、G2、G3和G4；尿液中有栀子苷、G1、G2和G4。总共鉴定出四种参与体内代谢过程的代谢产物（G1-G4）。这项工作的结果表明，IDA介导的液相色谱-串联质谱法可以快速、可靠地筛选环烯醚萜类化合物代谢产物的特征。
