Anthocyanins, but not anthocyanidins, from bilberry (Vaccinium myrtillus L.) alleviate pruritus via inhibition of mast cell degranulation.

We have previously reported that bilberry anthocyanins exhibit an anti-pruritic effect in a mouse model of allergic contact dermatitis. It has been reported that anthocyanins are particularly sensitive to thermal treatment and are easily hydrolyzed to anthocyanidins when exposed to high temperatures. The objective of this study was to compare the anti-pruritic effect of anthocyanin-rich quality-controlled bilberry extract and anthocyanidin-rich degraded extract using a mouse model of allergic contact dermatitis. BALB/c mice with allergic contact dermatitis induced by 4 weeks of repeated application of 2,4,6-trinitro-1-chlorobenzene (TNCB) were administered Bilberon-25 orally for 4 weeks after sensitization with TNCB. The effect of Bilberon-25 on pruritus was evaluated by measurement of scratching behavior. RBL-2H3 mast cells were used to investigate the effect of Bilberon-25 on degranulation in 48/80-stimulated mast cells. Compared with nonheated Bilberon-25, the proportion of anthocyanins in heated Bilberon-25 decreased, and the proportion of anthocyanidins was increased in heated-time dependent manner. Treatment with non-heated Bilberon-25 significantly attenuated the TNCB-induced increase in scratching behavior, whereas treatment with 2 h-heated Bilberon-25 did not. Moreover, 300 μg/mL nonheated Bilberon-25 showed significant inhibition of degranulation in RBL-2H3 mast cells, whereas 2 h-heated Bilberon-25 had no effect at any concentration studied. It is assumed that the inhibitory effect of bilberry anthocyanins on pruritus might be mediated, at least in part, by its inhibitory effect on mast cell degranulation. In conclusion, the anthocyanin-rich but not anthocyanidin-rich bilberry extract may be a useful dietary supplement for skin diseases involving pruritic symptoms, such as chronic allergic contact dermatitis, atopic dermatitis, and rhinitis.