hematoxylin

Hematoxylin (Natural Black 1) 是一种天然存在的类黄酮化合物，衍生自木柴树Haematoxylon campechianum。它是一种组织学上的核染色剂，也是一种有效的Aβ42原纤维形成的抑制剂，IC50=1.6 µM。

Hematein 抑制Akt/PKB Ser129磷酸化，Wnt/TCF 途径，并增加癌症细胞的凋亡。Hematein 是苏木精的氧化产物，也是变构酪蛋白激酶II 抑制剂（IC50:0.74μM）。

DW532 is one of simplified analogues of hematoxylin that has shown broad-spectrum inhibition on tyrosine kinases and in vitro anti-cancer activities. DW532 inhibited EGFR and VEGFR2 in vitro kinase activity (the IC50 values were 4.9 and 5.5 μmol/L, respectively), and suppressed their downstream signaling. DW532 dose-dependently inhibited tubulin polymerization via direct binding to tubulin, thus disrupting the mitotic spindle assembly and leading to abnormal cell division. In a panel of human cancer cells, DW532 (1 and 10 μmol/L) induced G2/M phase arrest and cell apoptosis, which subsequently resulted in cytotoxicity. Knockdown of BubR1 or Mps1, the two core proteins of the spindle assembly checkpoint dramatically decreased DW532-induced cell cycle arrest in MDA-MB-468 cells. Moreover, treatment with DW532 potently and dose-dependently suppressed angiogenesis in vitro and in vivo. ( Acta Pharmacol Sin. 2014 Jul;35(7):916-28.)