title: A Calluna vulgaris extract 5-lipoxygenase inhibitor shows potent antiproliferative effects on human leukemia HL-60 cells.
abstract: A water-Calluna vulgaris extract (water-CVE) was found to be a relatively specific arachidonate 5-lipoxygenase inhibitor and showed potent anti-proliferative effects on human leukemic HL60 cells. Water-CVE completely inhibited potato 5-lipoxygenase activity at 250 micrograms/ml, partially inhibited soybean 15-lipoxygenase at pH 7.4 and had no effect either on this 15-lipoxygenase at its optimal activity pH (pH 9) or on Lupinus albus 5-, 8-, 15-lipoxygenase. In culture, the proliferation and DNA synthesis of HL60 cells were decreased by water-CVE in a dose-dependent manner with an IC50 of 200 micrograms/ml at day 4. This effect of water-CVE is related to the starting density of HL60 cells. These results suggest that arachidonate 5-lipoxygenase metabolites and/or leukotrienes could play an essential role in cellular functions of leukemic cells and may explain the success of the use of Calluna vulgaris as tea and baths in folk medicine.
authors.affiliation: CNRS-URA 1485/C.J.F. INSERM 88-03, Faculté de Médecine, Université de Limoges, France.
authors.forename: A
authors.initials: A
authors.lastname: Najid
authors.forename: A
authors.initials: A
authors.lastname: Simon
authors.forename: C
authors.initials: C
authors.lastname: Delage
authors.forename: A J
authors.initials: AJ
authors.lastname: Chulia
authors.forename: M
authors.initials: M
authors.lastname: Rigaud
mesh_terms: D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology*; D016718:Arachidonic Acid / Q000097:blood; D002455:Cell Division / Q000187:drug effects; D006801:Humans; D007938:Leukemia / Q000188:drug therapy*; D008084:Lipoxygenase / Q000032:analysis; D016859:Lipoxygenase Inhibitors / Q000494:pharmacology*; D008264:Macrophages / Q000378:metabolism; D051379:Mice; D008807:Mice, Inbred BALB C; D013936:Thymidine / Q000378:metabolism; D014407:Tumor Cells, Cultured
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D016859:Lipoxygenase Inhibitors; D016718:Arachidonic Acid; D008084:Lipoxygenase; D013936:Thymidine