3-Chlorogentisyl alcohol is a potent E. coli β-glucuronidase inhibitor with an IC 50 value of 0.74 μM, an K i value of 0.58 μM. 3-Chlorogentisyl alcohol shows antiproliferative activity. 3-Chlorogentisyl alcohol has the potential for the research of anti-cancer and anti-inflammatory therapies.