Inhibitory Mechanisms of Water Extract of Oplopanax elatus on Lipopolysaccharide-Induced Inflammatory Responses in RAW 264.7 Murine Macrophage Cells / 中国结合医学杂志

OBJECTIVE@#To study the anti-inflammatory action and cellular mechanism of Oplopanax elatus.@*METHODS@#A hot water extract of OE (WOE) was prepared and a major constituent, syringin, was successfully isolated. Its content in WOE was found to be 214.0 µg/g dried plant (w/w). Their anti-inflammatory activities were examined using RAW 264.7 macrophages and a mouse model of croton oil-induced ear edema.@*RESULTS@#In lipopolysaccharide (LPS)-treated RAW 264.7 cells, a mouse macrophage cell line, WOE was found to significantly and strongly inhibit cyclooxygenase-2 (COX-2)-induced prostaglandin E (PGE) production [half maximal inhibitory concentration (IC)=135.2 µg/mL] and inducible nitric oxide synthase (iNOS)-induced NO production (IC=242.9 µg/mL). In the same condition, WOE was revealed to inhibit NO production by down-regulating iNOS expression, mainly by interrupting mitogen activated protein kinases (MAPKs)/activator protein-1 (AP-1) pathway. The activation of all three major MAPKs, p38 MAPK, extracellular signal-regulated kinase (ERK), and c-Jun N-terminal kinase, was inhibited by WOE (50-300 µg/mL). On the other hand, WOE reduced PGE production by inhibiting COX-2 enzyme activity, but did not affect COX-2 expression levels. In addition, WOE inhibited the production of proinflammatory cytokines such as interleukin-6 and tumor necrosis factor-α. In croton oil-induced ear edema in mice, oral administration of WOE (50-300 mg/kg) dose-dependently inhibited edematic inflammation.@*CONCLUSION@#Water extract of OE exhibited multiple anti-inflammatory action mechanisms and may have potential for treating inflammatory disorders.

Anti-arthritic Effects of Oplopanax elatus in a Rat Model of Rheumatoid Arthritis (Adjuvant-induced Arthritis)

The stems of Oplopanax elatus (OE) have long been used to treat inflammatory disorders in herbal medicine, and in the previous investigation, OE was found to possess anti-inflammatory activity in lipopolysaccharide-treated macrophages, RAW 264.7 cell. OE reduces inducible nitric oxide (NO) synthase-induced NO production, and interferes with mitogen-activated protein kinase activation pathways. In the present study, the pharmacological action of the water extract of OE was examined to establish anti-arthritic action, using a rat model of adjuvant-induced arthritis (AIA). The water extract of OE administered orally inhibited AIA-induced arthritis at (100 – 300) mg/kg/day. The paw edema was significantly decreased, in combination with reduced production of pro-inflammatory cytokines. The action mechanism includes an inhibition of MAPKs/nuclear transcription factor-κB activation. These new findings strongly suggest that OE possesses anti-arthritic action, and may be used as a therapeutic agent in inflammation-related disorders, particularly in arthritic condition.

Phenolic glycosides from root of Oplopanax elatus / 中草药

Objective To investigate the hydrophilic constituents from the anti-colorectal cancer extract of Oplopanax elatus. Methods The compounds were isolated and purified using macroporous resin, silica gel, ODS gel and pre-HPLC, and their chemical structures were identified by spectral data and physicochemical properties. The extracts and compounds from O. elatus were screened for anti-proliferation on HCT-116 and HT-29 cancer cell lines. Results Eleven phenolic compounds had been purified and identified from the n-butanol fraction including six phenylpropanoid glycosides: (E)-sinapic acid-4-O-β-D-glucopyranoside (1), 3- hydroxyphenethyl alcohol-4-O-β-D-glucopyranoside (2), 3-methoxycinnamyl alcohol-4-O-β-D-glucopyranoside (3), homovanillyl alcohol-4-O-β-D-glucopyranoside (4), dihydrosyringin (5), and syringin (6); And five lignan glycosides: 3,3'-dimethoxy-4,9,9'- trihydroxy-4',7-epoxy-5',8-lignan-4,9-bis-O-β-D-glucopyranoside (7), (+)-5,5'-dimethoxylariciresinol 4'-O-β-D-glucopyranoside (8), (+)-isolariciresinol-9'-O-β-D-glucopyranoside (9), (+)-isolariciresinol-4-O-β-D-glucopyranoside (10), and (+)-5,5'-dimethoxylariciresinol- 9'-O-β-D-glucopyranoside (11). All the phenolic glycosides showed no significant effects on the proliferation of HCT-116 and HT-29 cancer cell lines with IC50 > 100 μmol/L. Conclusion Compounds 4, 6, 9, and 11 are isolated and purified from this herb for the first time, while compounds 1, 2, and 10 are firstly obtained from the genus Oplopanax.

Pharmacokinetic profiles of falcarindiol and oplopandiol in rats after oral administration of polyynes extract of Oplopanax elatus / 中国天然药物

Polyynes, such as facarindiol (FAD) and oplopandiol (OPD), are responsible for anticancer activities of Oplopanax elatus (O. elatus). A novel approach to pharmacokinetics determination of the two natural polyynes in rats was developed and validated using a liquid chromatography-electrospray ionization-mass spectrometry (LC-MS) method. Biosamples were prepared by liquid-liquid extraction using ethyl acetate/n-hexane (V : V = 9 : 1) and the analytes were eluted on an Agilent ZORBAX Eclipse Plus C18 threaded column (4.6 mm × 50 mm, 1.8 μm) with the mobile phase of acetonitrile-0.1% aqueous formic acid at a flow-rate of 0.5 mL·min(-1) within a total run time of 11 min. All analytes were simultaneously monitored in a single-quadrupole mass spectrometer in the selected ion monitoring (SIM) mode using electrospray source in positive mode. The method was demonstrated to be rapid, sensitive, and reliable, and it was successfully applied to the pharmacokinetic studies of the two polyynes in rat plasma after oral administration of polyynes extract of O. elatus.

Oplopanax elatus (Nakai) Nakai: chemistry, traditional use and pharmacology / 中国天然药物

Oplopanax elatus (Nakai) Nakai, a member of the ancient angiosperm plant family Araliaceae, is used for the treatment of different disorders in the medicine systems of China, Russia, and Korea, and was designated in Russia as a classical adaptogen. Despite extensive studies of classical adaptogens, there are comparatively few reports concerning the chemical composition and pharmacological effects of O. elatus in English. The plant is a potential source of saponins, flavonoids, anthraquinones, terpenes, and other active compounds. Experimental studies and clinical applications have indicated that O. elatus possesses a number of pharmacological activities, including adaptogenic, anti-convulsant, anti-diabetic, anti-fungal, anti-inflammatory, anti-oxidant, blood pressure modulating, and reproductive function effects. In this review, the chemistry, safety, and therapeutic potential of O. elatus are summarized and highlighted to encourage the further development of this plant.