Bioactivity Evaluation of Pinocembrin Derivatives From Penthorum chinense Pursh Stems

Abstract

The extract of Penthorum chinense Pursh (PCP), a well-known Miao herb medicine, has been used as a key component for a Chinese patented drug to treat several kinds of liver-related diseases. In this work, 3 pinocembrin derivatives, S1, S2, and S3, were isolated from PCP stems and identified with high-performance liquid chromatography and electrospray ionization mass spectrometer. The molecular masses of S1, S2, and S3 were identical to Pinocembrin-7-O-[4″,6″-hexahydroxydiphenoyl (HHDP)]-β-D-glucose, Pinocembrin-7-O-[3″-O-galloyl-4″,6″-(s)-HHDP)-β-D-glucose, and Thonningianin A, respectively. Their free radical scavenging capability was evaluated with the 2,2-diphenyl-1-picrylhydrazyl assay. The half-maximal effective concentrations of S1, S2, and S3 were 26.75, 9.06, and 5.50 μg/mL, respectively. In vitro AML-12 assays demonstrated that S1 (5-20 μg/mL), S2 (10-40 μg/mL), and S3 (10-40 μg/mL) not only protected cells from H2O2-induced oxidation and alcohol-induced cell damages, but also reduced oleic acid (OA)-induced triglyceride accumulations in a dose-dependent manner. However, the 3 compounds potently exhibited similar cytotoxicity effect at high concentrations. The half-maximal inhibitory concentrations of S1, S2, and S3 to AML-12 cells were 74.19, 85.86, and 80.43 μg/mL. In addition, the 3 compounds also showed antibacterial activity on Escherichia coli, Staphylococcus aureus, Enterococcus faecalis, Lactobacillus rhamnosus, and Bacillus subtilis.