Du Ting, Zeng Min, Chen Li, Cao Zheng, Cai Hua, Yang Guangde
School of Pharmacy, Xi'an Jiaotong University, No. 76 Yanta West road, Xi'an, 710061, China.
Department of Pharmacy, Affiliated Taihe Hospital of Xi'an Jiaotong University Health science center, 32 South Renmin Road, Shiyan, Hubei, 442000, China.
Rapid Commun Mass Spectrom. 2018 Mar 23. doi: 10.1002/rcm.8114.
Xiao Chai Hu Tang (XCHT, Sho-saiko-to in Japanese) is a well-known medicine formula used in Asia for centuries. However, the quality control and the absorption of XCHT components are the major remaining concerns.. The study was to develop a sensitive and robust method to characterize the chemical components in XCHT and evaluate their absorptions.
An ultra-high pressure liquid chromatography coupled with electrospray ionization quadrupole time-of-flight mass spectrometry (UHPLC-ESI-QTOF MS/MS) was used to identify the compounds in XCHT. The Caco-2 cell culture model was employed to determine the absorption of the identified components.
The results showed that 109 compounds were identified including organic acids, flavonoids, saikosaponins, ginsenosides, licoricesaponins and gingerols. The absorption study showed that among those identified, 33 compounds have decent absorption permerbilities ranging from 1.46 ± 0.24×10 to 3.10±0.61×10 cm/sec. These compounds were classified as classes II and IV in the biopharmaceutical classification system (BCS).
These identified compounds could be used to characterize quality of XCHT and those absorbed compounds with decent permreabiliteis are the potential active components in XCHT. Future pharmacodynamics studies should focus on these absorbed compounds.
小柴胡汤（XCHT，日语为Sho-saiko-to）是亚洲数百年来使用的著名药方。然而，小柴胡汤成分的质量控制和吸收仍是主要的遗留问题。本研究旨在开发一种灵敏且稳健的方法来表征小柴胡汤中的化学成分并评估其吸收情况。
采用超高压液相色谱-电喷雾电离四极杆飞行时间质谱联用技术（UHPLC-ESI-QTOF MS/MS）鉴定小柴胡汤中的化合物。利用Caco-2细胞培养模型测定已鉴定成分的吸收情况。
结果表明，共鉴定出109种化合物，包括有机酸、黄酮类、柴胡皂苷、人参皂苷、甘草皂苷和姜辣素。吸收研究表明，在这些已鉴定的化合物中，有33种化合物具有良好的吸收渗透率，范围为1.46±0.24×10至3.10±0.61×10厘米/秒。这些化合物在生物药剂学分类系统（BCS）中被归类为II类和IV类。
这些已鉴定的化合物可用于表征小柴胡汤的质量，那些具有良好渗透率的吸收化合物是小柴胡汤潜在的活性成分。未来的药效学研究应关注这些吸收化合物。
