Inhibition of TNF-α-mediated NF-κB Transcriptional Activity in HepG2 Cells by Dammarane-type Saponins from Panax ginseng Leaves

Abstract

Panax ginseng (PG) is a globally utilized medicinal herb. The medicinal effects of PG are primarily attributable to ginsenosides located in the root and leaf. The leaves of PG are known to be rich in various bioactive ginsenosides, and the therapeutic effects of ginseng extract and ginsenosides have been associated with immunomodulatory and anti-inflammatory activities. We examined the effect of PG leaf extract and the isolated ginsenosides, on nuclear factor (NF)-κB transcriptional activity and target gene expression by applying a luciferase assay and reverse transcription polymerase chain reaction in tumor necrosis factor (TNF)-α-treated hepatocarcinoma HepG2 cells. Air-dried PG leaf extract inhibited TNF-α-induced NF-κB transcription activity and NF-κB-dependent cyclooxygenase (COX)-2 and inducible nitric oxide synthase (iNOS) gene expression more efficiently than the steamed extract. Of the 10 ginsenosides isolated from PG leaves, Rd and Km most significantly inhibited activity in a dose-dependent manner, with IC50 values of 12.05±0.82 and 8.84±0.99 μM, respectively. Furthermore, the ginsenosides Rd and Km inhibited the TNF-α-induced expression levels of the COX-2 and iNOS gene in HepG2 cells. Air-dried leaf extracts and their chemical components, ginsenoside Rd and Km, are involved in the suppression of TNF-α-induced NF-κB activation and NF-κB-dependent iNOS and COX-2 gene expression. Consequently, air-dried leaf extract from PG, and the purified ginsenosides, have therapeutic potential as anti-inflammatory.

21-O-Angeloyltheasapogenol E3, a Novel Triterpenoid Saponin from the Seeds of Tea Plants, Inhibits Macrophage-Mediated Inflammatory Responses in a NF-κB-Dependent Manner

“…Transfections were performed using the PEI method in 12-well plates as previously outlined [26, 27]. Transfected cells were used at 48 h posttransfection for all experiments.…”

Ginsenoside-Re ameliorates ischemia and reperfusion injury in the heart: a hemodynamics approach

“…In the present study, TNF-α is measured using the basis of determining TNF-α related to tissue injury [28]. Samples taken from left ventricular tissues after reperfusion of 120 min were immediately stored at -70℃ at the end of experiment until assayed as previously described [29].…”

Identification and quantification of the anti-inflammatory constituents in Pian-Tze-Huang by liquid chromatography combined with quadrupole time-of-flight and triple quadrupole mass spectrometry

“…Among these compounds, ginsenoside Rb1 (22) (27), ginsenoside Rh2 (37), and ginsenoside Rh3 (38). There are reports for anti-inflammatory properties of notoginseng saponins, bile acids, taurine, and muscone [20][21][22][23][24][25][26] and hence, these components present in PZH are responsible for anti-inflammatory activity of PZH.…”