Faculty of Pharmacy, Kinki University, 3-4-1 Kowakae, Higashiosaka, Osaka, 577-8502, Japan.
J Nat Med. 2013 Jul;67(3):643-6. doi: 10.1007/s11418-012-0699-y. Epub 2012 Aug 18.
The anti-degranulating activity of flavonoids present in Citrus fruits was comprehensively evaluated. Among these, hesperetin and naringenin, respectively aglycones of hesperidin and narirutin, showed significant activity. The targets of hesperetin and naringenin were found: hesperetin inhibited phosphorylation of Syk and Akt, while naringenin suppressed the expression of Lyn and inhibited the phosphorylation of Akt. These results suggest that hesperetin and naringenin inhibit degranulation by suppression of pathway signals and reduce the symptoms of allergy by inhibiting phosphorylation of Akt, which leads to the suppression of cytokines. In addition, hesperetin showed inhibitory activity against the degranulation induced by calcium ionophores, indicating that hesperetin exerts its inhibitory activity by stabilizing the membrane structure.
全面评估了柑橘类水果中类黄酮的抗脱颗粒活性。其中，橙皮素和柚皮素分别是橙皮苷和柚皮苷的苷元，表现出显著的活性。发现橙皮素和柚皮素的作用靶点：橙皮素抑制 Syk 和 Akt 的磷酸化，而柚皮素抑制 Lyn 的表达并抑制 Akt 的磷酸化。这些结果表明，橙皮素和柚皮素通过抑制信号通路来抑制脱颗粒，并通过抑制 Akt 的磷酸化来减轻过敏症状，从而抑制细胞因子的产生。此外，橙皮素对钙离子载体诱导的脱颗粒具有抑制活性，表明橙皮素通过稳定膜结构发挥其抑制活性。
