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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.

The inhibitory effects of isoliensinine (IL), a bisbenzylisoquinoline alkaloid extracted from the seed embryo of the traditional chinese medicinal herb Nelumbo nucifera Gaertn, on the proliferation of porcine coronary arterial smooth muscle cells (CASMCs) induced by angiotensin II(Ang II) and its mechanisms of action were investigated. Counting cultured cell number, MTT assay, immunohistochemical method and Western blot were adopted. Ang II 0.1 micromol l (-1) significantly evoked CASMC proliferation by 42%, which could be dose-dependently inhibited by IL 0.01-3 micromol l (-1) and the percentage of inhibition of IL 0.1 micromol l (-1) was 25%. Irbesartan (Irb) 0.1 micromol l (-1) inhibited CASMC proliferation by 22%. IL or Irb 0.1 micromol l (-1) decreased Ang II-induced overexpression of Platelet-derived growth factor (PDGF)-beta and basic fibroblast growth factor (bFGF), respectively. Both of them also declined c-fos, c-myc and hsp70 overexpression, respectively. At the same concentration, the inhibitory effects of IL on PDGF-beta were even stronger than those of Irb (P < 0.05). In summary, the data showed that IL possesses an anti-proliferative effect, which is related to the decrease of the overexpression of growth factors PDGF-beta, bFGF, proto-oncogene c-fos, c-myc and hsp70.