Batatasin I, a naturally occurring phenanthrene derivative, isolated from tuberous roots of Dioscorea batatas suppresses eicosanoids generation and degranulation in bone marrow derived-mast cells

Abstract

To find anti-inflammatory compounds from the tuberous roots of Dioscorea batatas, we isolated 6-hydroxy-2,4,7-trimethoxyphenanthrene (batatasin I) from the dichloromethane (CH 2Cl 2) fraction of this plant. Batatasin I inhibited both the generation of prostaglandin D 2 (PGD 2), leukotriene C 4 (LTC 4) and degranulation reaction in mouse bone marrow-derived mast cells (BMMCs). This compound inhibited cyclooxygenase-2 (COX-2) dependent PGD 2 generation in a dose dependent manner, with IC 50 values of 1.78 μM. Western blotting probed with specific anti-COX-2 antibodies showed that the decrease in the quantity of the PGD 2 generation was accompanied by a decrease in the COX-2 protein level. In addition, this compound also inhibited the production of 5-lipoxygenase (5-LOX) dependent LTC 4 in a dose dependent manner (IC 50, 1.56 μM). Batatasin I also inhibited the mast cell degranulation reaction (IC 50, 6.7 μM) in BMMCs. This result indicates that batatasin I could be developed as an anti-inflammatory agent through further investigation. © 2011 Pharmaceutical Society of Japan.