魚藤素

魚藤素

中文名称魚藤素
中文同义词魚藤素;藤素;AKT抑制剂(DEGUELIN);(-)-DEGUELIN;(-)-鱼藤素;(7AS,13AS)-9,10-二甲氧基-3,3-二甲基-13,13A-二氢-3H-吡喃并[2,3-C:6,5-F']二苯并吡喃--7(7AH)-酮
英文名称DEGUELIN
英文同义词(7as-cis)-oxy-;3h-bis(1)benzopyrano(3,4-b:6’,5’-e)pyran-7(7ah)-one,13,13a-dihydro-9,10-dimeth;(7AS,13AS)-13,13A-DIHYDRO-9,10-DIMETHOXY-3,3-DIMETHYL-3H-BIS[1]BENZOPYRANO[3,4-B:6',5'-E]PYRAN-7(7AH)-ONE;(-)-DEGUELIN;DEGUELIN;(7aS,13aS)-13,13a-Dihydro-9,10-dimethoxy-3,3-dimethyl-(3H)-bis[1]benzopyrano[3.4-b.6'.5'-e]pyran-7(7aH)-one;(7aS)-3,3-Dimethyl-9,10-dimethoxy-7,7aα,13,13aα-tetrahydro-3H-bis[1]benzopyrano[3,4-b:6',5'-e]pyran-7-one;3,3-Dimethyl-9,10-dimethoxy-7,7aα,13,13aα-tetrahydro-3H-bis[1]benzopyrano[3,4-b:6',5'-e]pyran-7-one
CAS号522-17-8
分子式C23H22O6
分子量394.42
EINECS号200-258-5
相关类别标准品;植物提取物;合成;细胞生物学试剂;精细化工;Miscellaneous Natural Products;Antitumour;黄酮;对照品;标准品 -中药标准品;标准品,对照品;原料药及中间体
Mol文件522-17-8.mol
结构式魚藤素 结构式

魚藤素 性质

熔点85-87 °C(lit.)
沸点560.1±50.0 °C(Predicted)
比旋光度D27 -97.2° (c = 0.2 in benzene)
密度1?+-.0.06 g/cm3(Predicted)
储存条件-20°C
溶解度二甲基亚砜:>10 mg/mL
形态固体
颜色白色至黄色
旋光性 (optical activity)[α]/D -70 to -80°, c = 0.2 in methanol
稳定性从购买之日起 2 年内保持稳定。 DMSO 或乙醇溶液可在 -20℃ 下保存长达 3 个月。

魚藤素 用途与合成方法

Deguelin 是一种天然存在的鱼藤酮类化合物,通过阻止多种途径 (如 PI3K-Akt,IKK-NF-κB 和 MAPK-mTOR-survivin 等) 充当化学预防剂。Deguelin 与 Hsp90 的结合导致许多致癌蛋白 (包括 MEK1/2,Akt,HIF1α,COX-2 和 NF-κB) 的表达降低。。

Akt

Deguelin (0-500 nM) in a dose and time dependent manner inhibits the growth of MDA-MB-231, MDA-MB-468, BT-549 and BT-20 cells. Deguelin at all concentrations fails to reduce cell numbers in the presence of 1 ng EGF but in the presence of EGF 20 ng reinstated deguelin mediated growth inhibition. Deguelin treated cells show reduced expression of Survivin as determined by western blot and immunofluorescence examinations. Deguelin inhibits p-ERK and its downstream target p-STAT-3 and c-Myc expression in a dose dependent manner. Deguelin down-regulates Akt signaling probably by disrupting its association with Hsp 90 in cultured HNSCC cells. Deguelin deguelin disrupts the association between Hsp 90 with survivin and Cdk4. Deguelin deguelin treatment increases cellular ceramide level through de novo synthase pathway to mediate HNSCC cell death and apoptosis. Deguelin inhibits the proliferation of MPC-11 cells in a concentration- and time-dependent manner and causes the apoptotic death of MPC-11 cells. Following exposure to deguelin, the phosphorylation of Akt is decreased. Deguelin-induced apoptosis is characterized by the upregulation of Bax, downregulation of Bcl-2 and activation of caspase-3.

Deguelin (2 or 4 mg/kg, i.p.) reduces the in vivo tumor growth of MDA-MB-231 cells transplanted subcutaneously in athymic mice. Deguelin (4 mg/kg, p.o.) treatment shows a great inhibition in tumor growth, which is demonstrated by reduced tumor size and improved mice survival and, indicating a significant anti-tumor ability by deguelin in vivo. In the colon cancer xenograft model, the volume of the tumor treated with deguelin is significantly lower than that of the control, and the apoptotic index for deguelin-treated mice is much higher.

安全信息

安全说明22-24/25
WGK Germany3
RTECS号DX1500000
海关编码29329990

MSDS信息

提供商 语言
英文
更新日期产品编号产品名称CAS号包装价格
2024/01/25HY-13425Deguelin1 mg246元
2024/01/25HY-13425魚藤素
Deguelin
522-17-85mg493元

魚藤素 上下游产品信息

"魚藤素"相关产品信息
鱼藤酮 榆树皮提取物 鱼腥草提取物 美洛昔康 抑制剂 吲哚美辛 吡罗昔康 S-布洛芬 锯叶棕提取物 魚藤素 6-甲氧基-2-(4-苯甲氧基)苯并噻吩 雌马酚
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