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Anti-allergy activities of Kuji amber extract and kujigamberol

2018; Elsevier BV; Volume: 127; Linguagem: Inglês

10.1016/j.fitote.2018.02.033

1873-6971

Miku Maruyama, Miki Kobayashi, Takeshi Uchida, Eisaku Shimizu, H. Higashio, Misa Ohno, Shota Uesugi, Ken‐ichi Kimura,

Neurobiology and Insect Physiology Research

Amber is fossilized tree resin and several biologically active compounds were isolated from ambers using the growth-restoring activity of the mutant yeast [Saccharomyces cerevisiae (zds1∆ erg3∆ pdr1∆ pdr3∆)] involving Ca2+-signal transduction. The aim of this study is to investigate the anti-allergic effect of both the methanol extract of Kuji amber (MEKA) and its main biologically active constituent, kujigamberol (15,20-dinor-5,7,9-labdatrien-18-ol) having activity against the mutant yeast. Both MEKA and kujigamberol inhibited the degranulation of RBL-2H3 cells by stimulation of thapsigargin (Tg) (IC50 = 15.0 μg/ml and 29.1 μM) and A23187 (IC50 = 19.6 μg/ml and 24.9 μM) without cytotoxicity, but not by stimulation of IgE + DNP-BSA (Ag) (IC50 > 50.0 μg/ml and 50.0 μM). However, both inhibited Ca2+-influx in RBL-2H3 cells by all three stimulations in a dose dependent manner. Leukotriene C4 production in RBL-2H3 cells stimulated by A23187 was also inhibited by both through the inhibition of ERK1/2 phosphorylation. In an ovalbumin-induced rhinitis model of guinea pigs, nasal administration of MEKA and kujigamberol inhibited nasal blockade in a dose-dependent manner and the effect was about 5 times potent than that of a steroid clinical drug, mometasone furoate. The growth-restoring activity of MEKA and kujigamberol against the mutant yeast is involved in the anti-allergic activities against cells and animals, and both are expected to be candidates for the development of new anti-allergy agents.