Transformation of Salvianolic Acid B to Salvianolic Acid A in Aqueous Solution and the In Vitro Liver Protective Effect of the Main Products
Transformation of Salvianolic Acid B to Salvianolic Acid A in Aqueous Solution and the In Vitro Liver Protective Effect of the Main Products
复制标题
丹酚酸B在水溶液中向丹酚酸A的转化及主要产品的体外保肝作用
DOI：
10.1111/1750-3841.12415
复制
发表时间：
2014-04-01
影响因子：
3.9
通讯作者：
Li, Ji'an
中科院分区：
文献类型：
--
作者：
Kan, Shidong;Chen, Zhouzhou;Li, Ji'an
丹参酸A（Salvioleacid A，Sal A）是丹参中活性最高的化合物。由于其在原料中含量较低，许多研究报道了从丹参素B（Sal B）制备丹参素。然而，这种转变的过程仍然是未知的。我们的目标是找到从Sal B转化为Sal A的化学变化。结果表明，在热水溶液中，水杨醛B首先水解为紫草酸，后者再转化为水杨醛A。采用DPPH自由基清除法测定了Sal A、Sal B和LA的自由基清除能力，结果表明Sal A的自由基清除能力高于Sal B和LA。用四氯化碳诱导人肝细胞株WRL68的体外肝损伤。Sal A、Sal B和LA均表现出剂量依赖性的保肝作用，其中Sal A的保肝作用明显强于Sal B和LA。实际应用发现丹参素B发生化学变化生成丹参素A，丹参素B首先水解生成紫草酸，后者可迅速转化为丹参素A。这一发现有助于优化丹参素A的生产工艺，为丹参素A的工业化生产奠定基础。
Salvianolic acid A (Sal A) was considered to be the compound with highest activity in Salvia miltiorrhiza (danshen). Due to its low content in raw materials, many studies reported its preparation from salvianolic acid B (Sal B). However, the process of this transformation is still unknown. Our objective was to find the chemical change of the transformation from Sal B to Sal A. The results showed that Sal B was hydrolyzed to lithospermic acid (LA) first, and the latter was transformed into Sal A in thermal aqueous solution. The radical scavenging ability of Sal A, Sal B, and LA was tested through DPPH, and Sal A showed higher radical elimination ability compared to Sal B and LA. In vitro liver damage was induced by CCl4 in human hepatic WRL68 cell line. Sal A, Sal B, and LA showed liver protective ability in a dose-dependent manner, while Sal A possessed a much higher ability compared to Sal B and LA.Practical Application The chemical change of salvianolic acid B to salvianolic A was found. Salvianolic acid B was hydrolyzed to lithospermic acid first, and the latter could be transformed to salvianolic acid A quickly. This finding may be useful to the process optimization of salvianolic acid A and results in the industrial production of salvianolic acid A.