Inhibitory Activity of Bioactive Phloroglucinols from the Rhizomes of Dryopteris crassirhizoma on Escherichia coli β-Glucuronidase: Kinetic Analysis and Molecular Docking Studies

ABSTRACT: Phloroglucinols-one of the major secondary metabolites in Dryopteris crassirhizoma-exhibit various pharmacological effects, such as antiviral, antioxidant, and antidiabetic activities. This study evaluated 30 phloroglucinols isolated from the rhizomes of D. crassirhizoma for their inhibitory activity on β-glucuronidase via in vitro assays. Among them, dimeric phloroglucinols 13-15 moderately inhibited β-glucuronidase, and trimeric phloroglucinols 26-28 showed strong inhibitory effects, with IC₅₀ values ranging from 5.6 to 8.0 μM. Enzyme kinetic analysis confirmed all six active compounds to be in a competitive mode of inhibition. Molecular docking simulations revealed the key binding interactions with the active site of

SUBMITTER: Phong NV 

PROVIDER: S-EPMC9610990 | biostudies-literature | 2022 Oct

REPOSITORIES: biostudies-literature