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Damnacanthal

CAS No. : 477-84-9

MCE 站：Damnacanthal

产品活性：Damnacanthal 是从 Morinda citrifolia 的根中分离出来的蒽醌。Damnacanthal 是一种强效选择性的 p56^lck 酪氨酸激酶活性的抑制剂。天然的 Damnacanthal 抑制 p56^lck 的自磷酸化和外源底物的磷酸化，IC₅₀ 分别为 46 nM 和 220 nM。Damnacanthal 是一种具有抗癌活性的有效凋亡诱导剂。Damnacanthal 在小鼠中也具有镇痛，抗炎作用，并且对白色念珠菌具有抗真菌活性。

研究领域：Protein Tyrosine Kinase/RTK  |  Apoptosis  |  Anti-infection

作用靶点：Src  |  Apoptosis  |  Fungal

In Vitro: Damnacanthal has > 100-fold selectivity for p56^lck over the serine/threonine kinases, protein kinase A and protein kinase C, and > 40-fold selectivity for p56^lck over four receptor tyrosine kinases. Damnacanthal also demonstrates modest (7-20-fold), but highly statistically significant, selectivity for p56^lck over the homologous enzymes p60^src and p59^fyn.
Damnacanthal (0.1-100 μM; 1-4 days; HCT-116 and SW480 cells) treatment results in a significant reduction of cell proliferation in a concentration- and time-dependent manner.
Damnacanthal (1-50 μM; 72 hours; HCT-116 cells) treatment results in a significant enrichment in the number of cells in the S/G1 and G2/G1 phases at concentration of 50 μM.
Damnacanthal (10 μM; 24 hours; HCT-116 cells) treatment significantly increases caspase 3/7 activity. Damnacanthal-induced apoptosis.
Damnacanthal (0.1-10 μM; 24 hours; HCT-116 cells) treatment induces NAG-1 expression in HCT-116 cells. Cyclin D1 expression is reduced at 10 μM of Damnacanthal, whereas p21 and p53 does not alter their expression. PARP cleavage is seen at 10 μM Damnacanthal treatment only in HCT-116 cells, where NAG-1 is induced.
Damnacanthal treatment for 2 weeks shows significant decreasing colony number in HCT-116 cells in a concentration-dependent manner. Damnacanthal-treated cells show a dramatic inhibition of clonogenic capacity. Damnacanthal-treated (1-50 μM; 48 hours) cells significantly inhibits the migration of HCT-116 cells in a concentration-dependent manner.

In Vivo: Damnacanthal (10-100 mg/kg; oral administration; for 10-300 minutes; male ddY mice) treatment exhibits a significant antinociceptive effect in a dose-dependent manner in the formalin test. Administration of damnacanthal (100 mg/kg) shows significant inhibition of histamine-induced paw edema.

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