The Ursolic Acid-Rich Extract of <i>Dracocephalum heterophyllum</i> Benth. with Potent Antidiabetic and Cytotoxic Activities

Abstract

Pentacyclic triterpenoids are one of the main functional components in Dracocephalum heterophyllum. In this study the optimal process, the fairly simple and accessible extraction and purification of triterpenoids of D. heterophyllum, was developed by a remaceration method. Remaceration is characterized by minimal loss of biologically active compounds on diffusion, which contributes to the largest depletion of raw materials. The triterpenoid yield was 2.4% under optimal conditions which was enhanced to 98.03% after purification. The triterpenoid profiles and their anticancer and antidiabetic activities were further analyzed. GC-MS analysis of triterpenoidal extract of D. heterophyllum resulted ursolic acid (71.9%) and oleanolic acid (18.1%) as the major components. Additionally, total purified triterpenoid contents of D. heterophyllum and its main components were shown to possess significant cytotoxic activity against three human breast cancer cell lines (SK-Br-3, T47D, and MCF-7). The purification of triterpenoids influenced their biological activity. The antidiabetic effect, as measured by inhibition of protein-tyrosine phosphatase (PTP-1B), of the purified fraction of triterpenoids of D. heterophyllum increased by five-fold against the enzyme. The results provide important guidance for the industrial application of D. heterophyllum confirming the prospect of developing plant extracts into effective drugs and health foods for human applications.

Keywords

• <i>Dracocephalum heterophyllum</i>
• purification
• triterpenoids
• ursolic acid
• PTP-1B
• cytotoxicity