Anti-allergy activities of Kuji amber extract and kujigamberol

作者：Maruyama Miku; Kobayashi Miki; Uchida Takeshi; Shimizu Eisaku; Higashio Hironori; Ohno Misa; Uesugi Shota; Kimura Ken ichi^*

来源：Fitoterapia, 2018, 127: 263-270.

DOI：10.1016/j.fitote.2018.02.033

• Kuji amber
• Saccharomyces cerevisiae
• RBL-2H3 cells
• ERK
• Rhinitis guinea pig model
• Kujigamberol (15,20-dinor-5,7,9-labdatrien-18-ol)

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 Delta erg3 Delta pdr1 Delta pdr3 Delta)] 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 mu g/ml and 29.1 mu M) and A23187 (IC50 = 19.6 mu g/ml and 24.9 mu M) without cytotoxicity, but not by stimulation of IgE + DNP-BSA (Ag) (IC50 > 50.0 mu g/ml and 50.0 mu M). However, both inhibited Ca2+-influx in RBL-2H3 cells by all three stimulations in a dose dependent manner. Leukotriene C-4 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 antiallergy agents.

• 出版日期2018-6