DAMNACANTHAL CAS#: 477-84-9

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DAMNACANTHAL

生物活性靶点体外研究体内研究 用途与合成方法 MSDS DAMNACANTHAL价格(试剂级) 上下游产品信息

中文名称	DAMNACANTHAL
中文同义词	3-羟基-1-甲氧基-2-蒽醌甲醛;丹宁卡;丹拿堪索;丹宁卡【3-羟基-1-甲氧基-2-蒽醌甲醛】
英文名称	DAMNACANTHAL
英文同义词	DAMNACANTHAL;DAMNACANTAL;1-Methoxy-2-formyl-3-hydroxy-9,10-anthraquinone;1-Methoxy-3-hydroxy-9,10-dioxo-9,10-dihydroanthracene-2-carbaldehyde;3-HYDROXY-1-METHOXYANTHRAQUINONE-2-ALDEHYDE;9,10-Dihydroxy-3-hydroxy-1-methoxy-9,10-dioxo-2-anthracenecarboxaldehyde;1-Methoxy-3-hydroxy-9,10-dioxoanthracene-2-carbaldehyde;9,10-Dihydro-3-hydroxy-1-methoxy-9,10-dioxo-2-anthracenecarbaldehyde
CAS号	477-84-9
分子式	C16H10O5
分子量	282.25
EINECS号
相关类别	标准品;植物提取物;标准品 -对照药材;其它天然产物
Mol文件	477-84-9.mol
结构式

DAMNACANTHAL 性质

DAMNACANTHAL 用途与合成方法

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 Cycle Analysis

Apoptosis Analysis

Western Blot Analysis

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.

安全信息

MSDS信息

DAMNACANTHAL 价格(试剂级)

DAMNACANTHAL 上下游产品信息