魚藤素
中文名称 | 魚藤素 |
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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;(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;黄酮;对照品;Miscellaneous Natural Products;Antitumour;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 性质
熔点 | 85-87 °C(lit.) |
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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。 |
Akt
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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 |
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WGK Germany | 3 |
RTECS号 | DX1500000 |
海关编码 | 29329990 |
提供商 | 语言 |
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英文
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