Improving anticancer activities of Oplopanax horridus root bark extract by removing water‐soluble components

Abstract

Oplopanax horridus is used as a folk medicine by natives in the Northern Pacific coast of North America. This experiment studied the anti-proliferative effects of the extract of O. horridus root bark and its fractions chromatographed from Dianion HP20 resin column with water, 30, 50, 70 and 100% ethanol on human breast cancer MCF-7 cells and non-small cell lung cancer (NSCLC) cells. The role of O. horridus in the cell cycle and apoptosis of MCF-7 cells was also investigated. The results showed that the 70% and 100% ethanol fractions demonstrated more potent antiproliferative effects than the total extract on both cell lines. The anti-proliferative effects may result from the enrichment of active constituents detected by the HPLC. The IC 50 of the total extract, 50, 70, and 100% ethanol fractions for anti-proliferation on MCF-7 cells were 248.4, 123.1, 44.0, and 31.5 μg/mL, respectively, and on NSCLC cells were 125.3, 271.1, 17.6, and 23.2 μg/mL, respectively. On the other hand, the water and 30% ethanol fractions significantly promoted cell proliferation on MCF-7 cells at concentrations > 100 μg/mL, suggesting that the hydrophilic fractions should be removed from the extract when used for cancer chemoprevention in order to achieve desirable activities. The effects of the total extract on cell cycle and apoptosis were similar to that of the 100% ethanol fraction because of the similarity of their chemical composition. At higher concentrations, the apoptotic effects of the 70% ethanol fraction are more significant. Data from this study suggested that the 70% and 100% ethanol fractions are active anti-proliferative fractions and that induction of apoptosis is the mechanism involved in the antiproliferative effect observed.

Anticancer Activities of Polyynes from the Root Bark of Oplopanax horridus and Their Acetylated Derivatives

“…Acetylated polyynes OHR-1~OHR- 16 were synthesized from OH-1~OH-6 with acetic anhydride in ethyl acetate with sodium carbonate added to the stirring mixtures. After quenching the reactions, the reaction mixture was cooled to room temperature and evaporated to remove the organic solvents.…”

“…Anti-proliferative tests of the six isolated polyynes OH-1~OH-6 and their derivatives OHR-1~OHR- 16 were conducted on four cancer cell lines and a normal human hepatic cell line. As shown in Table 1, the 22 compounds exhibited different extents of anti-proliferative activity on the cancer cell lines with various IC50 values.…”

“…Recent studies have revealed that four purified polyynes from O. horridus showed potential anticancer activities [16][17][18]. All these polyynes possess hydroxy groups in their structures, and two of them, which occured naturally in acetylated form had weaker anti-proliferation effects.…”

Recovery of Oplopanax horridus (Sm.) Miq., an Important Ethnobotanical Resource, after Clearcut Logging in Northwestern British Columbia

“…The active ingredients contained in the inner bark of devil's club have been found to inhibit the growth of certain bacteria and fungi that cause a variety of illnesses, e.g., tuberculosis and fungal pneumonia (Kobaisy et al 1997, McCutcheon et al 1994. More recent studies suggest that devil's club extracts may be effective in preventing the further growth of several types of human cancer cells and have benefits as a tonic and for the treatment of arthritis, rheumatism, and perhaps adult-onset diabetes (Li et al 2010, Tai et al 2006, J. Tai pers. comm.…”

“…There is ongoing research with respect to the medicinal efficacy of devil's club. Physiologically relevant constituents include calcium oxalate crystals (which can cause a burning sensation in the mouth but can be broken down by cooking) and at least 18 complex secondary compounds, primarily terpenoids (Sun et al 2010). The active ingredients contained in the inner bark of devil's club have been found to inhibit the growth of certain bacteria and fungi that cause a variety of illnesses, e.g., tuberculosis and fungal pneumonia (Kobaisy et al 1997, McCutcheon et al 1994.…”