Hydrophobic constituents and their potential anticancer activities from Devil's Club (Oplopanax horridus Miq.)

Abstract

Ethnopharmacological relevance-Devil's Club Oplopanax horridus (Sm.) Miq. is a widely used folk medicine in the Pacific Northwest such as Alaska and British Columbia for treating a variety of ailments including arthritis, cold, fever, infections, diabetes and cancer.Aim of the study-To investigate hydrophobic constituents and their potential anticancer activity from Devil's Club O. horridus. Materials and methods-The root bark of O. horridus (Sm.) Miq was isolated by chromatographic techniques. Structures of isolated compounds were identified by spectroscopic methods and comparison with published data. The anti-proliferation of isolated hydrophobic constituents in human breast cancer MCF-7 cells, human colon cancer SW-480 and HCT-116 cells were tested. The potential mechanism of anti-proliferation was also investigated using cell cycle and apoptosis assays.Results and discussion-Six compounds were isolated and structurally identified as 9,17-octadecadiene-12,14-diyne-1,11,16-triol, 1-acetate (1), oplopandiol acetate (2), falcarindiol (3), oplopandiol (4), trans-nerolidol (5) and t-cadinol (6). These compounds showed potential anticancer activities on human breast cancer and colon cancer cells, of which compound 3 possesses the strongest activity. Further cell cycle and apoptosis test by flow cytometry showed the polyacetylenes 1-4 induced HCT-116 cell arresting in G2/M phase and inhibited proliferation by the induction of apoptosis at both earlier and later stage.Conclusion-These results provide promising baseline information for the potential use of O. horridus as well as some of the isolated compounds in the treatment of cancer.

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

“…Previous work had reported that OH-1~4 exhibited potential anticancer acitives on human breast cancer and colon cancers through cell arrest in G2/M phase and induction of appoptosis at both earlier and later stages [17]. In this study, the potential mechanisms of the four new compounds OHR-1, -2, -3 and -5 with the strongest anti-proliferative activity among the series of acylated polyynes were investigated.…”

“…However, as the two acetylated polyynes had 18 carbon atoms in the main skeleton chain (C18 polyynes) while the others had 17 carbon atoms as the main structural chain (C17-polyynes). It seems that they could not be compared diretly together to reach that conclusion [17].…”

“…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.…”

“…Some of these compounds had displayed anti-proliferation activity against certain cancer cell lines [17,19]. Among the polyynes, (3S,8S)-falcarindiol had been obtained separately from (3R, 8S)-falcarindiol, which was also reported to have anticancer activities [20].…”

Pyranocoumarins from Root Extracts of Peucedanum praeruptorum Dunn with Multidrug Resistance Reversal and Anti-Inflammatory Activities

“…The 15 known compounds were identified as (+)-praeruptorin A (2) [20,21], (+)-praeruptorin B (3) [20,21], (+)-praeruptorin E (4) [20][21][22], selinidin (5) [23], cis-3′,4′-diisovalerylkhellactone (6) [19,24], pteryxin (7) [6], suksdorfin (8) [25,26], Pd-Ib (9) [27,28], qianhucoumarin D (10) [20,21], (+)-samidin (11) [25,[29][30][31], laserpitin (12) [32], (9R,10R)-9-acetoxy-8,8-dimethyl-9,10-dihydro-2H,8H-benzo [1,2-b:3,4-b′]dipyran-2-one-10-yl-ester (13) [33], bergapten (14) [34,35], xanthotoxin (15) [36], and falcalindiol (16) [37][38][39][40].…”