Laboratory of Life Sciences, Faculty of Pharmacy, Yasuda Women's University, Hiroshima, Japan.
Planta Med. 2011 Feb;77(3):252-6. doi: 10.1055/s-0030-1250221. Epub 2010 Sep 2.
Pretreatment with parthenolide for 60 min inhibited the antigen-induced degranulation of RBL-2H3 mast cells; the IC(50) value being 4.5 ± 0.4 µM. The inhibition was not due to suppression of the phosphatidylinositol 3-kinase pathway because the antigen-induced phosphorylation of Akt was not inhibited by parthenolide. The antigen-induced increase in intracellular calcium levels was prevented by parthenolide, suggesting that parthenolide inhibited the antigen-induced degranulation by suppressing an increase in intracellular calcium levels. In support of this, parthenolide was found to prevent ionomycin-induced degranulation by inhibiting an increase in intracellular calcium levels. Therefore, parthenolide inhibits the degranulation of mast cells by preventing an increase in intracellular calcium levels.
预先用小白菊内酯处理 60 分钟可抑制 RBL-2H3 肥大细胞的抗原诱导脱粒；IC50 值为 4.5±0.4µM。这种抑制不是由于抑制磷脂酰肌醇 3-激酶途径所致，因为小白菊内酯并不抑制抗原诱导的 Akt 磷酸化。小白菊内酯可防止抗原诱导的细胞内钙离子水平升高，表明小白菊内酯通过抑制细胞内钙离子水平升高来抑制抗原诱导的脱粒。支持这一点的是，小白菊内酯通过抑制细胞内钙离子水平升高来防止离子霉素诱导的脱粒。因此，小白菊内酯通过防止细胞内钙离子水平升高来抑制肥大细胞的脱粒。
