Objective To investigate the chemical constituents of the intestinal bacteria transformation products of total saponins from Platycodon grandiflorus and their anti-drug-induced liver injury activity. Methods The compounds were isolated and purified by column chromatography techniques including AB-8 macroporous resin, normal phase silica gel, Sephadex LH-20 gel chromatography, and semi-preparative high-performance liquid chromatography. Their structures were identified based on physicochemical properties, mass spectrometry and nuclear magnetic resonance spectral data. The anti-drug-induced liver injury activities of the isolated compounds were evaluated using an acetaminophen-induced AML12 cell hepatic injury model. Results A total of 16 compounds were isolated from the intestinal bacteria transformation products of total saponins from P. grandifloras and identified as 3-O-β-D-glucopyranosyloxy-2β,3β,16α,23-tetrahydroxyolean-12-en-28-oic acid-28-O-α-L-rhamnopyranosyl-(1→2)-α-L-arabinopyranoside (1), polygalacin D (2), 3-O-β-D-glucopyranosyl platycodigenin (3), platycodin D₃ (4), platycoside F (5), platycodin D (6), deapio-platycodin D (7), platycodonoid B (8), 3-O-β-D-glucopyranosyl polygalacic acid (9), leiyemudanoside A (10), linoleic acid (11), (6Z,9Z)-6,9-hexadecadienoic acid (12), glyceryl linoleate (13), (2S)-1-O-(9Z,12Z-octadecandienyl)-3-O-β-galactosyl glycerol (14), dibutyl phthalate (15), and triallyl isocyanurate (16). Anti-drug-induced liver injury activity study showed that compounds 1—3, 5—7, 9, and 14 significantly inhibited the levels of alanine aminotransferase and aspartate aminotransferase in acetaminophen-induced AML12 cell supernatants (P < 0.05,0.01). Conclusion A total of 16 compounds were successfully isolated and identified from the intestinal bacterial transformation products from total saponins of P. grandiflorus. Compound 1 is a new compound named des-apio-xylosyl polygalacin D. Compounds 1—3, 5—7, 9, and 14 exhibit significant anti-drug-induced liver injury activities, showing potential hepatoprotective effects.

total saponins of Platycodonis Radix  /  intestinal bacterial  /  transformation product  /  drug-induced liver injury  /  des-apio-xylosyl polygalacin D  /  polygalacin D  /  platycodin D₃