Cytotoxic and COX-2 inhibitory constituents from the aerial parts ofAralia cordata

Abstract

Three diterpenes (1, 8, and 9), three triterpenes (3, 4, and 7), one saponin (11), four sterols (2, 5, 6, and 12), and one cerebroside (10) were isolated from the EtOH extract of the aerial parts of Aralia cordata by repeated silica gel column chromatography. Their chemical structures were identified by comparing their physicochemical and spectral data with those published in literatures. All isolated compounds were evaluated for their cytotoxicity against L1210, K562, and LLC tumor cell lines using MTT assay. Of which, 3beta,5alpha-dihydroxy-6beta-methoxyergosta-7,22-diene (6) showed a potent cytotoxicity against all cell lines with IC50 values of 11.7, 11.9, and 15.1 microM, respectively, while compounds 1, 5, and 11 showed a moderate or weak cytotoxicity. These isolates were also examined for their inhibitory activity against COX-1 and COX-2. Although most compounds, except for 2, 10, and 12, showed a strong inhibitory activity against COX-1, they exhibited a moderate or weak inhibitory activity against COX-2.

Anti-inflammatory effect of oleanoic acid 28-O--D-glycopyranosyl ester isolated from Aralia cordata in activated HMC-1 cells

“…Column chromatography was performed by using silica gel (Kieselgel 70 to 230 mesh and 230 to 400 mesh, Merck), and thin layer chromatography (TLC) was performed on pre-coated silica gel 60 F254 (0.25 mm, Merck). The structure of this compound was confirmed by comparison of spectral data with those reported in the literature (Figure 1) (Lee et al, 2006).…”

“…Although, NF-κB activation is regulated by MAPKs through multiple mechanisms, accumulating evidence indicates that NF-κB activation is modulated by MAPKs that induce sitespecific phosphorylation of an inhibitory protein called IκB (Kim et al, 1997). Activation of NF-κB is dependent on the degradation of IκB, an endogenous inhibitor that binds to NF-κB in the cytoplasm (Lee et al, 2006). In these studies, OA was shown to decrease the degradation and phosphorylation of IκB and nuclear translocation of NF-κB (p65) in PMA plus A23187-stimulated mast cells.…”

“…OA was isolated from the dried aerial parts of A. cordata as described previously (Lee et al, 2006). Briefly, the dried aerial parts of A. cordata (4 kg) were extracted three times with ethanol under reflux for 3 days, filtered and concentrated to yield an ethanol extract (300 g).…”

“…It has a strong scent typical of an aromatic medicinal plant, and its roots are used for the treatment of rheumatism, toothache, lumbago, and fever remedy (Perry, 1980). A. cordata was shown to inhibit cytotoxicity and COX-2 activity (Lee et al, 2006). In biological studies, a few essential oils and diterpenes isolated from the roots have been shown to have anti-inflammatory and analgesic effects (Han et al, 1983;Okuyama et al, 1991).…”

Aralia cordata Protects Against Amyloid β Protein (25–35)–Induced Neurotoxicity in Cultured Neurons and Has Antidementia Activities in Mice

“…Diterpenes have been elucidated as analgesic and anti-inflammatory agents of this plant root (18,19). In addition to diterpenes, polyacetylenes, a lipid glycerol, and sterols having cyclooxygenase (COX) inhibitory activity have been isolated from the root (20); and diterpenes, triterpenes, and a saponin have been isolated as COX-1 and COX-2 inhibitors from the aerial part of this plant (21). Since reactive oxygen species (ROS) and inflammation are part of the complex series of pathophysiological events that contribute to neurodegenerative diseases such as AD and stroke (22,23), free radical scavengers and anti-inflammatory agents have attracted considerable attention as potential neuroprotective agents.…”