Acacia Honey Component Has Therapeutic Effects on Many Cancers

Sulfonation Disposition of Acacetin: In Vitro and In Vivo

J Agric Food Chem. 2017 May 25

Acacetin, an important component of acacia honey, exerts extensive therapeutic effects on many cancers. However, sulfonation disposition of acacetin has rarely been reported. Therefore, this study aims to investigate the sulfonation disposition of acacetin systematically. Results showed that acacetin-7-sulfate was the main metabolite mediated primarily by sulfotransferases (SULT) 1A1.

Dog liver S9 presented the highest formation rate of acacetin-7-sulfate. Compared with that in wild-type Friend Virus B (FVB) mice, plasma exposure of acacetin-7-sulfate decreased significantly in multiple drug resistance protein 1 knockout (Mrp1-/-) mice, while increased evidently in breast cancer resistance protein knockout (Bcrp-/-) mice. In Caco-2 monolayers, efflux and clearance of acacetin-7-sulfate reduced distinctly by the BCRP inhibitor Ko143 in apical side and by the MRP1 inhibitor MK571 in basolateral side.

In conclusion, acacetin sulfonation was mediated mostly by SULT1A1. Acacetin-7-sulfate was transported mainly by BCRP and MRP1. Hence, SULT1A1, BCRP and MRP1 were responsible for acacetin-7-sulfate exposure in vivo.