Inhibitory effects of 2,3,5,4′-tetrahydroxystilbene-2-O-β-d-glucoside on experimental inflammation and cyclooxygenase 2 activity

Abstract

The inhibitory effects of 2,3,5,4'-tetrahydroxystilbene-2-O-beta-d-glucoside (THSG), extracted from the roots of Polygonum multiflorum Thunb, on inflammatory activity in animal models and cyclooxygenase-2 (COX-2) activity in lipopolysaccharide (LPS)-induced mouse RAW264.7 macrophage cells were investigated. The carrageenin (CGN)-induced rat paw oedema model and dimethylbenzene-induced mouse ear oedema model were prepared; MTT assay, semi-quantitative RT-PCR, Western blot and ELISA were adopted. THSG 2.3, 4.6 and 9.2 mg kg(- 1) by oral administration inhibited mouse ear oedema and the percentage of inhibition of THSG 9.2 mg kg(- 1) is 87%. THSG 3.2, 6.4 and 12.8 mg kg(- 1) by oral administration dose-dependently inhibited rat paw oedema and the percentage of inhibition of THSG 12.8 mg kg(- 1) is 56% at 6 h. Indomethacin 13 and 9 mg kg(- 1) showed 90% and 57% inhibition in the same animal models, respectively. LPS 1 microg ml(- 1) significantly up-regulated prostaglandin E(2) (PGE(2)) production (inducing COX-2 activity) by 35% (exogenous arachidonic acid, AA), which was dose-dependently decreased by THSG 1, 10, and 100 micromol L(- 1) and the percentage of inhibition of THSG 10 micromol L(- 1) was 40%. NS-398 10 micromol L(- 1) decreased PGE(2) production by 42%. THSG 1, 10, 100 micromol L(- 1) was shown to markedly inhibit the LPS-induced COX-2 protein and mRNA expression in RAW264.7 cells (P < 0.05) but had no effect on COX-1 protein and mRNA (P>0.05). In summary, the data showed that THSG possessed an anti-inflammatory effect, which was perhaps related to the inhibition of COX-2 enzyme activity and expression in RAW264.7 macrophage cells.

Farnesyl protein transferase inhibitory components of Polygonum multiflorum

“…Although the activity of compound 1 and 2 is not strong, this is the first report on the inhibitory activity of anthraquinones on the FPTase. It is known that stilbene glycosides, including 2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucopyranoside have diverse biological activities such as anti-inflammatory (Zhang et al, 2006;Zhang et al, 2007), antioxidant (Ryu et al, 2002;Teguo et al, 1998), antileukemic (Mannila et al, 1993), and kinase inhibitory (Jayatilake et al, 1993) activities. However, it was not observed the inhibitory activity of 4 on FPTase.…”

Mechanism of 2,3,4',5-Tetrahydroxystilbene 2-O-β-<smlcap>D</smlcap>-Glucoside-Induced Upregulation of Glutamate Transporter 1 Protein Expression in Mouse Primary Astrocytes

“…2,3,4',5-tetrahydroxystilbene 2-O-β- D -glucoside (TSG), a monomer of stilbene from a traditional Chinese herbal medicine polygonummultiflorum [5], exhibits various pharmacological effects, such as anti-oxidation, free radical scavenging and anti-inflammation [6,7]. In the CNS, TSG has been reported to protect dopaminergic neurons against 1-methyl-4-phenylpyridinium (MPP + )-induced injuries [8] and reverse the Aβ 1-42 -induced down-regulation of N-methyl- D -aspartate 2B expression and impairment in learning and memory [9,10].…”

In Vitro Study of the Anti-Inflammatory Activity of Some Medicinal and Edible Plants Growing in Russia

“…In addition to resveratrol, Japanese knotweed extracts contain such compounds as quercetin and emodin, which have anti-inflammatory activities [32]. The antiinflammatory properties of certain other polygonaceous species have also been explored: P. stagninum and P. multiflorum have been investigated using animal models [33] and their cyclooxygenase-2 activity has been investigated in LPS-induced mouse RAW264.7 macrophage cells [34]. The water pepper and redshank plants of the Polygonaceae family tested in the present work are, as yet, less well studied.…”