ABSTRACT
The stem and branch extract of Tripterygium wilfordii (Celastraceae) afforded seven new dihydroagarofuran sesquiterpene polyesters [tripterysines A-G (1-7)] and eight known ones (8-15). The chemical structures of these new compounds were established based on combinational analysis of HR-ESI-MS and NMR techniques. The absolute configurations of tripterysines A-C (1-3) and E-G (5-7) were determined by X-ray crystallographic analysis and circular dichroism spectra. All the compounds were screened for their inhibitory effect on inflammation through determining their inhibitory effect on nitric oxide production in LPS-induced RAW 264.7 cells and the secretion of inflammatory cytokines TNF-α and IL-6 in LPS-induced BV2 macrophages. Compound 9 exhibited significant inhibitory activity on NO production with an IC50 value of 8.77 μmol·L-1. Moreover, compound 7 showed the strongest inhibitory effect with the secretion of IL-6 at 27.36%.
Subject(s)
Tripterygium/chemistry , Esters/pharmacology , Interleukin-6 , Lipopolysaccharides/pharmacology , Plant Leaves/chemistry , Anti-Inflammatory Agents/chemistry , Nitric Oxide/analysis , Sesquiterpenes/chemistry , Molecular StructureABSTRACT
Objective To investigate the effects of human IL-18 gene combined with diterpenoid alkaloids in inhibiting the proliferation and inducing the apoptosis of tongue squamous carcinoma cells Tscca.Methods We constructed recombinant plasmid pEGFPN3-IL-18 and tranfected it into tongue squamous carcinoma cells Tscca.The transduction efficiency of the target cells was detected by fluorescent microscopy,cytotoxic effect of IL-18 gene with diterpenoid alkaloids on Tscca was detected by MTT assay,and apoptosis was detected by flow cytometry. Western blot was employed to examine the expression level of cellular signal-regulated kinase Akt/p-Akt.Results The tongue squamous cells Tscca which transfected pEGFPN3-IL-18 had significantly increased apoptosis compared with non-transfected cells (P<0 .05 ).Tongue carcinoma squamous cells cultured with diterpenoid alkaloids at the concentrations of 0 .2 ,0 .4 and 0 .6 mg/mL had significantly increased apoptosis in a dose-dependent manner (P<0.05).Human IL-18 gene combined with diterpenoid alkaloids for 48 hours inhibited significantly Tscca in a concentration-dependent manner compared with diterpenoid alkaloids alone (P<0 .05 ).The two in combination could also decrease the protein level of p-Akt dose-dependently.Conclusion The combination of pEGFPN3-IL-18 and diterpenoid alkaloids has a synergistic effect in inhibiting the growth of tongue squamous carcinoma cells Tscca.