Wang Ru-Feng, Li Juan, Hu Hai-Jun, Li Jia, Yang Ying-Bo, Yang Li, Wang Zheng-Tao
The MOE Key Laboratory for Standardization of Chinese Medicines and the SATCM Key Laboratory for New Resources and Quality Evaluation of Chinese Medicines, Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai, China.
Department of Pharmacognosy, China Pharmaceutical University, Nanjing, China.
J Ginseng Res. 2018 Jul;42(3):270-276. doi: 10.1016/j.jgr.2016.08.009. Epub 2016 Aug 26.
Notoginsenoside Ft1 is a promising potential candidate for cardiovascular and cancer disease therapy owing to its positive pharmacological activities. However, the yield of Ft1 is ultralow utilizing reported methods. Herein, an acid hydrolyzing strategy was implemented in the acquirement of rare notoginsenoside Ft1.
Chemical profiles were identified by ultraperformance liquid chromatography coupled with quadruple-time-of-flight and electrospray ionization mass spectrometry (UPLC-Q/TOF-ESI-MS). The acid hydrolyzing dynamic changes of chemical compositions and the possible transformation pathways of saponins were monitored by ultrahigh-performance LC coupled with tandem MS (UHPLC-MS/MS).
Notoginsenoside Ft1 was epimerized from notoginsenoside ST4, which was generated through cleaving the carbohydrate side chains at C-20 of notoginsenosides Fa and Fc, and vina-ginsenoside R7, and further converted to other compounds via hydroxylation at C-25 or hydrolysis of the carbohydrate side chains at C-3 under the acid conditions. High temperature contributed to the hydroxylation reaction at C-25 and 25% acetic acid concentration was conducive to the preparation of notoginsenoside Ft1. C-20 epimers of notoginsenoside Ft1 and ST4 were successfully separated utilizing solvent method of acetic acid solution. The theoretical preparation yield rate of notoginsenoside Ft1 was about 1.8%, which would be beneficial to further study on its bioactivities and clinical application.
三七皂苷Ft1因其积极的药理活性，是心血管疾病和癌症治疗中一个有前景的潜在候选药物。然而，利用已报道的方法，Ft1的产量极低。在此，一种酸水解策略被用于获取稀有的三七皂苷Ft1。
通过超高效液相色谱与四极杆飞行时间和电喷雾电离质谱联用（UPLC-Q/TOF-ESI-MS）来鉴定化学图谱。通过超高效液相色谱与串联质谱联用（UHPLC-MS/MS）监测化学成分的酸水解动态变化以及皂苷可能的转化途径。
三七皂苷Ft1是由三七皂苷ST4差向异构化而来，三七皂苷ST4是通过切断三七皂苷Fa和Fc、人参皂苷R7在C-20位的糖侧链产生的，并且在酸性条件下通过C-25位的羟基化或C-3位糖侧链的水解进一步转化为其他化合物。高温有助于C-25位的羟基化反应，25%的醋酸浓度有利于三七皂苷Ft1的制备。利用醋酸溶液的溶剂法成功分离了三七皂苷Ft1和ST4的C-20差向异构体。三七皂苷Ft1的理论制备产率约为1.8%，这将有利于对其生物活性和临床应用的进一步研究。
