The Inhibitory Effect of Triterpenoid Glycosides Originating fromSanguisorba officinalison Tissue Factor Activity and the Production of TNF-α

Abstract

We examined the inhibitory effects of novel triterpene glycoside compounds [ziyu-glycoside II (ZY-II) and its methyl ester (ZYM-201)], which originated from the roots of sanguisorba officinalis L. (Rosaceae), on tissue factor (TF) activity and tumor necrosis factor (TNF)-alpha production. In in vitro TF activity tests, ZY-II but not ZYM-201 strongly blocked lung TF activity with an IC50 value of 0.46 microM. By contrast, only ZYM-201 dose-dependently inhibited in vivo TF activity with an ED50 value of 1.7 mg/kg, when orally administered. Furthermore, ZYM-201 diminished both in vitro and in vivo TNF-alpha production with IC50 or ED50 values of 69.4 microM and 87.4 mg/kg, respectively. Therefore, these results suggest either that ZYM-201 may be developed as a potent inhibitor of both TF- and TNF-alpha-mediated diseases such as atherosclerosis and septic shock, or it may be a lead compound to be derivatized for further improvement of its curative efficacy.

Inhibitory effect of Sanguisorba officinalis ethanol extract on NO and PGE2 production is mediated by suppression of NF-κB and AP-1 activation signaling cascade

“…Some components have been reported to have radical scavenging activity (Masaki et al, 1995). But it has not been possible to define the exact active principle responsible for the anti-inflammatory activity of So-EE, some of triterpenes or anti-oxidative components may be regarded as active principles (Masaki et al, 1995;Cho et al, 2006). Therefore, further experiments will be focused on identifying major compounds with Src and MAPK suppressive effects, contributing to inhibition of NF-B and AP-1 activation.…”

“…So far, saponin components such as triterpenes and their glycosides (e.g. ziyuglycoside I), gallic acid, and disaccharide (5-O-alpha-D-(3-C-hydroxymethyl)lyxofuranosyl-beta-D-(2-C-hydroxymethyl) arabino furanose) have been reported as major active principles that possess these in vitro and in vivo pharmacological effects (Park et al, 2004;Cho et al, 2006;Ban et al, 2008;Kim et al, 2008).…”

Antioxidant and immunomodulatory activities of polysaccharides from the roots of Sanguisorba officinalis

“…Its roots have haemostatic, analgesic, and astringent properties, and have been used in traditional Chinese medicine for the treatment of burns, scalds, inflammation and internal haemorrhage [17,18]. Several scientific investigations, involving extraction and pharmacological studies of terpenoids and triterpenoid glycosides from this herb, have been carried out that demonstrate significant antioxidant and neuroprotective activities [18][19][20][21][22]. However, there is very limited literature [23] on the polysaccharides from S. officinalis and their bioactivities.…”

Comprehensive characterization of the in vitro and in vivo metabolites of ziyuglycoside I in rat microsome, intestinal flora, excretion specimen and fresh tissues based on LC–Q-TOF/MS

“…An equal volume of 0.1% CMC-Na was administered to the control group. Feces and urine samples were collected from three rats at 0 to 24, 24 to 48, 48 to 72, and 72 to 7 …”

“…A variety of bioactive ingredients, including saponins, flavonoids, tannins, anthraquinones and steroids, were isolated from S. officinalis, and their pharmacological effects on anti-wrinkle, hemostatic and anti-inflammatory properties had been studied [3][4][5]. Saponin components such as triterpenes and their glycosides, gallic acid, and disaccharide have been confirmed as major active ingridients in S. officinalis L. [6][7][8]. Ziyuglycoside I (3-O-alpha-L-Arabinopyranosylpomolic acid beta-D-glucopyranosyl ester), one of the major saponins in S. officinalis with the highest content, was confirmed as an active ingredient with free radical scavenging activity and elastase inhibitory activity,etc [9,10].…”