Key words: YPE-01 — Diarylheptanoid — 5-Lipoxygenase — Leukotriene — Ear edema
Springer Online Journal Archives 1860-2000
Abstract. Objective and Design: We investigated the anti-inflammatory effect of YPE-01, a novel diarylheptanoid derivative in vitro and in vivo.¶Material: In the in vitro study, rat basophilic leukemia (RBL-1) cells were used. For the in vivo study, ICR and ddY mice (male, 7 weeks old) were used.¶Treatment: In the in vitro study, the supernatant of RBL-1 cells lysate was incubated with 50 μM arachidonic acid (AA) and 0.01-100 μM test drugs for 15 min. RBL-1 cells were preincubated with 0.01–100 μM test drugs for 10 min before incubation with 0.5 μM calcium ionophore A23187 for 10 min. In the in vivo study, YPE-01 (0.1–3 mg/ear) was applied to the ear of mice at the same time as a 12-O-tetradecanoylphorbol 13-acetate (TPA) application or 1 h before an AA application.¶Methods: In the in vitro study, the amounts of 5-hydroxyeicosatetraenoic acid and leukotrienes were measured by high-performance liquid chromatography and an enzyme immunoassay, respectively. In the in vivo study, a circular tissue sample from the ear of the mice was weighed. Statistical analysis was done using Dunnett's test.¶Results: YPE-01 inhibited the 5-lipoxygenase activity (IC50, 0.28 μM) and the leukotriene B4 (IC50, 0.035 μM) and C4 (IC50, 0.046 μM) production by RBL-1 cells without any inhibition of cyclooxygenase activity in vitro. The topical application of YPE-01 significantly suppressed both the AA- and TPA-induced ear edemas in vivo.¶Conclusions: YPE-01 is a selective 5-lipoxygenase inhibitor with a suppressive effect against dermal inflammation.
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