Radix bupleuri is a medical herba in traditional Chinese medicine which is widelyused as a key ingredient in many Chinese multiherb remedies. Most of thepharmacological action research of Radix bupleuri is focused on SSa and SSd whichare considered to be the main two active components of Radix bupleuri. However thiskind of understanding, which is based on the perspective of natural products effectiveingredients of Radix bupleuri, can not reflect traditional Chinese medicine (TCM)properties. Decoction is not only the main dosage forms of Chinese traditionalmedicine but also the carrier of TCM active substance. Only when the decoction ofRadix bupleuri is regarded as the main research objective can the Chinese medicineproperties of Radix bpleuri be clearly known. Only in this way can the theory researchprovides more information on how to use Radix bupleuri more reasonably.Bupleurum saponin a and d are a pair of isomer, of which the structure differencelies in configurations of OH on the C-16. The structure of the two components are notstable, and in the preparation process of Radix bupleuri decoction, the oxygen etherring between C-13and C-28is prone to crack generating secondary saikosaponin. Sofar too much attention has been paid to the SSa and SSd, and the secondarysaikosaponins attaract too little attention. Based on this, the structure transformationprocess of SSa and SSd are to be studied, and at the same time the preliminaryresearch on the toxicity of SSb2, the main secondary-saikosaponin in Radix bupleuridecoction is also to be studied.Objectives: Exploring the structure conversion process of SSa and SSd and apreliminary study on the toxicity of SSb2.Methods:Saikosaponins in aqueous samples was enriched by macroporous resin technology. Saikosaponins content in the samples was determined by the method of highperformance liquid chromatography (HPLC).The technology of Chromatographic separation and spectrum structureidentification were employed to study the structure of the saikosaponin in the structureconversion process.The toxicity of SSb2was evaluated by the alanine aminotransferase (ALT)activity, aspartate amino transferase (AST) energy, the content of total protein (TP),the albumin (propagated) content, the content of globulin (GLB), the glucose (GLU)content, the content of urea nitrogen (BUN), the CREB content, the total cholesterol,the triglyceride levels in rat blood serum as well as the system autopsy.Results:The structure transformation path from saikosaponin to secondary-saikosaponinwas optimized. Hydroxyl-saikosaponin mediates the structure transformation ofsaikosaponin. And the preparation methods of OH-SSa has been studied.The stability of the SSa was greater than the saikosaponin SSd.SSa and SSb2, which is structure transformed from saikosaponin d, was mainlyfound in decoction of Radix buupleuri, which provides clue for the establishment ofmore reasonable quality control system of Radix buupleuri.In the toxicity study of SSb2. At the dose of20and40mg/kg, in four consecutiveweeks, no the mice dead, SSb2has the toxicity on liver, in high dose group the contentof globulin in serum elvated, and the content of serum glucose reduced by SSb2, andSSb2can also cause pancreas hyperplasia in mice.Conclusions: SSa and SSb2are supposed to be the effective substance for Radixbupleuri decoction, the in-depth study on which will help to reveal the effectivematerial basis of Radix bupleuri,especially the SSb2. And this study set foundationfort the toxicity of SSb2. And because SSd can’t be detected in the decoction of Radixbupleuri, there is no possibility that SSd is the effective component of radix bupleuri inview of Chinese medicine, which does not deny the further pharmacological study onSSd as an natural ingredient. |