title: Anti-inflammatory activity of 6-hydroxy-2,7-dimethoxy-1,4-henanthraquinone from tuberous roots of yam (Dioscorea batatas) through inhibition of prostaglandin D₂ and leukotriene C₄ production in mouse bone marrow-derived mast cells.
abstract: 6-Hydroxy-2,7-dimethoxy-1,4-phenanthraquinone (PAQ) isolated from the tuberous roots of Yam (Dioscorea batatas) inhibited cyclooxygenase-2 (COX-2) and cyclooxygenase-1 (COX-1) dependent prostaglandin D(2) (PGD(2)) generation in mouse bone marrow-derived mast cells in a concentration-dependent manner with IC(50) values of 0.08 μM and 0.27 μM, respectively. In the Western blotting with specific anti-COX-2 antibodies, the decrease of the quantity of PGD(2) was accompanied by a decrease in the COX-2 protein level. But PAQ did not affect COX-1 protein level. In addition, this compound inhibited 5-lipoxygenase (5-LOX) dependent production of leukotriene C(4) in a dose-dependent manner, with an IC(50) of 0.032 μM. These results demonstrate that PAQ has a dual COX-2/5-LOX inhibitory activity. This compound also inhibited the degranulation reaction in a dose-dependent manner with an IC(50) of 2.7 μM. Thus, these results suggest that PAQ may be useful in regulating mast cell-mediated inflammatory diseases.
authors: College of Pharmacy, Yeungnam University, Gyeongsan 712-749, Korea.
authors: Meihua
authors: M
authors: Jin
authors: Yue
authors: Y
authors: Lu
authors: Ju Hye
authors: JH
authors: Yang
authors: Tae Hyung
authors: TH
authors: Jo
authors: Young In
authors: YI
authors: Park
authors: Chong-Kil
authors: CK
authors: Lee
authors: Sang-Jo
authors: SJ
authors: Park
authors: Kun Ho
authors: KH
authors: Son
authors: Hyeun Wook
authors: HW
authors: Chang
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology*; D015153:Blotting, Western; D001854:Bone Marrow Cells / Q000166:cytology*; D002470:Cell Survival / Q000187:drug effects; D027742:Dioscorea / Q000737:chemistry*; D004305:Dose-Response Relationship, Drug; D004591:Electrophoresis, Polyacrylamide Gel; D020128:Inhibitory Concentration 50; D017997:Leukotriene C4 / Q000037:antagonists & inhibitors* / Q000096:biosynthesis; D008297:Male; D008407:Mast Cells / Q000187:drug effects* / Q000276:immunology; D051379:Mice; D008807:Mice, Inbred BALB C; D010616:Phenanthrenes / Q000494:pharmacology*; D035281:Plant Tubers / Q000737:chemistry; D015230:Prostaglandin D2 / Q000037:antagonists & inhibitors* / Q000096:biosynthesis; D011809:Quinones / Q000494:pharmacology*
chemical_list: C574031:6-hydroxy-2,7-dimethoxy-1,4-phenanthraquinone; D000894:Anti-Inflammatory Agents, Non-Steroidal; D010616:Phenanthrenes; D011809:Quinones; D017997:Leukotriene C4; D015230:Prostaglandin D2