DAMNACANTHAL

生物活性靶点体外研究体内研究 DAMNACANTHAL 试剂级价格

DAMNACANTHAL

CAS号:477-84-9
英文名:DAMNACANTHAL
中文名:DAMNACANTHAL
CBNumber:CB0681393
分子式:C16H10O5
分子量:282.25
MOL File:477-84-9.mol

DAMNACANTHAL化学性质

熔点 :218～219℃
沸点 :531.9±50.0 °C(Predicted)
密度 :1.461±0.06 g/cm3(Predicted)
储存条件 :-20°C
溶解度 :Soluble in DMSO (up to 7 mg/ml)
酸度系数(pKa) :5.26±0.20(Predicted)
形态 :Pale orange solid.
颜色 :Yellow
稳定性 :Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.

DAMNACANTHAL性质、用途与生产工艺

生物活性 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 p56lck 酪氨酸激酶活性的抑制剂。天然的 Damnacanthal 抑制 p56lck 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。
靶点

IC50: 46 nM (p56 ^lck autophosphorylation) and 220 nM (phosphorylation of exogenous substrates by p56 ^lck );
Apoptosis;
Candida albicans

体外研究

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.

Cell Proliferation Assay

Cell Line:	HCT-116 and SW480 cells
Concentration:	0.1 μM, 1 μM, 10 μM, 100 μM
Incubation Time:	1, 2, and 4 days
Result:	Resulted in a significant reduction of cell proliferation in a concentration- and time-dependent manner.

Cell Cycle Analysis

Cell Line:	HCT-116 cells
Concentration:	1 μM, 10 μM and 50 μM
Incubation Time:	72 hours
Result:	Resulted in a significant enrichment in the number of cells in the S/G1 and G2/G1 phases at concentration of 50 μM.

Apoptosis Analysis

Cell Line:	HCT-116 cells
Concentration:	10 μM
Incubation Time:	24 hours
Result:	Significantly increased caspase 3/7 activity.

Western Blot Analysis

Cell Line:	HCT-116 cells
Concentration:	0.1 μM, 1 μM and 10 μM
Incubation Time:	24 hours
Result:	NAG-1 was induced in HCT-116 cells in a dose- and time-dependent manner. Cyclin D1 expression was reduced at 10 μM.

体内研究

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.

Animal Model:	Male ddY mice (5-6 weeks) injected with formalin or Histamine
Dosage:	10 mg/kg, 30 mg/kg and 100 mg/kg
Administration:	Oral administration; for 10 minutes, 30 minutes, 60 minutes or 300 minutes
Result:	Significantly reduced the growth of human lung tumor without acute toxicity.