Bioactive constituents from the roots of Panax japonicus var. major and development of a LC-MS/MS method for distinguishing between natural and artifactual compounds.

Two new saponins, panajaponol (1) and pseudoginsenoside RT1 butyl ester (2), together with 35 known compounds (3-37), were isolated from the roots of Panax japonicus var. major. The structures of 1 and 2 were elucidated on the basis of spectroscopic analysis and chemical methods. Furthermore, a LC-MS/MS method was developed for confirming 2, 3, and 8 as natural compounds containing a butyl ester group. This method should be useful for distinguishing between minor natural and artifactual compounds in Panax species. Moreover, compounds 3, 6, 8, 9, 11, 13, and 15 exhibited strong inhibition of superoxide anion generation and elastase release by human neutrophils in response to formyl-l-methionyl-l-leucyl-l-phenylalanine/cytochalasin B (fMLP/CB), with IC(50) values ranging from 0.78 to 43.6 µM. In addition, 1 showed greater than 2- to 3-fold selective cytotoxic activity against KB and DU145 cancer cell lines.

Anti-inflammatory, anticholinesterase and antioxidative constituents from the roots and the leaves of Salvia nipponica Miq. var. formosana.

Reactive oxygen species and granule proteases produced by neutrophils contribute to the pathogenesis of inflammatory diseases. The extracts of the roots and the leaves of Salvia nipponica var. formosana were showed potent inhibitory effects on superoxide anion production in fMLP/CB-activated human neutrophils as well as other anti-inflammatory effects, and led to the isolation of 25 compounds. Among them, compounds 8, 12, 13, 14, 15, 17 and 20 were exhibited more potent inhibitory effect on superoxide anion generation and elastase release by human neutrophils in response to fMLP/CB. Moreover, those isolated compounds also showed significant anticholinesterase and antioxidative activities. To the best of our knowledge, this is the first report of phytochemical and biological activity study on S. nipponica var. formosana.

Potent alpha-glucosidase inhibitors from the roots of Panax japonicus C. A. Meyer var. major.

Bioassay-guided fractionation of the CHCl(3) soluble portion of the roots of Panax japonicus C. A. Meyer var. major afforded an active fraction with inhibitory activity against baker's yeast alpha-glucosidase with an IC(50) value 1.02 mg/mL. Furthermore, the active fraction isolated contained three previously unreported polyacetylenes, designated panaxjapynes A-C, together with 11 other compounds, including four polyacetylenes, five phenolic compounds, a sesquiterpenoid, and a sterol glucoside. The structures of the compounds were elucidated by spectroscopic and chemical methods. Compared with the control acarbose (IC(50) 677.97 microM), six compounds were shown to be more potent alpha-glucosidase inhibitors with IC(50) values in the range 22.21-217.68 microM.