title: Antiproliferative activity of the Netherlands propolis and its active principles in cancer cell lines.
abstract: The MeOH extract of the Netherlands propolis showed promising antiproliferative activity toward highly liver-metastatic murine colon 26-L5 carcinoma with an EC(50) value of 3.5 microg/ml. Further, antiproliferative activity-guided purification of the MeOH extract led us to isolate four flavonoids (1-4), seven cinnamic acid derivatives (5-11) and two new glycerol derivatives (12, 13), whose structures were elucidated on the basis of spectral analysis. The isolated compounds were tested for their antiproliferative activity against murine colon 26-L5, murine B16-BL6 melanoma, human HT-1080 fibrosarcoma and human lung A549 adenocarcinoma cell lines. The benzyl (9), phenethyl (10) and cinnamyl caffeates (11) possessed potent antiproliferative activities with EC(50) values of 0.288, 1.76 and 0.114 microM, respectively, toward colon 26-L5 carcinoma. These caffeates were considered to be active constituents of the Netherlands propolis in their antiproliferative activity. The antioxidative activity of these caffeates may play an important role in their antiproliferative activities.
authors.affiliation: Department of Natural Products Chemistry, Institute of Natural Medicine, Toyama Medical and Pharmaceutical University, 2630-Sugitani, 930-0194, Toyama, Japan.
authors.forename: Arjun H
authors.initials: AH
authors.lastname: Banskota
authors.forename: Takema
authors.initials: T
authors.lastname: Nagaoka
authors.forename: Lucia Yoshie
authors.initials: LY
authors.lastname: Sumioka
authors.forename: Yasuhiro
authors.initials: Y
authors.lastname: Tezuka
authors.forename: Suresh
authors.initials: S
authors.lastname: Awale
authors.forename: Kiyoshi
authors.initials: K
authors.lastname: Midorikawa
authors.forename: Katsumichi
authors.initials: K
authors.lastname: Matsushige
authors.forename: Shigetoshi
authors.initials: S
authors.lastname: Kadota
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000302:isolation & purification* / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D016166:Free Radical Scavengers / Q000494:pharmacology*; D006801:Humans; D051379:Mice; D009426:Netherlands; D011429:Propolis / Q000737:chemistry* / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D016166:Free Radical Scavengers; D011429:Propolis