Preparation and Chemical Structural Modification of Asiatic Acid

Asiatic acid was prepared using asiaticoside as the raw material. The high-throughput screening model related to skin pain and itch receptors was applied to investigate the targets of the soothing effect of asiatic acid. Then, ester derivatives were synthesized, and their oil solubility and soothing effect were evaluated. Results showed that receptors associated with the soothing effect of asiatic acid included the endothelin receptor type A (EDNRA), histamine H1 receptor (HRH1), and transient receptor potential vanilloid-1 (TRPV1). Twelve derivatives were synthesized with asiatic acid as the parent compound. After the esterification of asiatic acid, its oil solubility was significantly improved. Among these derivatives, asiatica acid hexadecanol ester, asiatica acid octadecanol ester and asiatica acid decyl tetradecanol ester exhibited a significantly stronger inhibitory effect against EDNRA and TRPV1 compared to that of asiatic acid.