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鼠尾草酚

鼠尾草酚用途

Carnosol 是一种有效的核糖体S6激酶 (RSK2) 抑制剂,可用于治疗胃癌,其 IC50 值约为 5.5 μM。

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鼠尾草酚名称

[ CAS 号 ]:
5957-80-2

[ 中文名 ]:
鼠尾草酚

[ 英文名 ]:
Carnosol

[中文别名 ]:

鼠尾草苦内脂

[英文别名 ]:

Carnosol

鼠尾草酚生物活性

[ 描述 ]:

Carnosol 是一种有效的核糖体S6激酶 (RSK2) 抑制剂,可用于治疗胃癌,其 IC50 值约为 5.5 μM。

[ 相关类别 ]:

信号通路 >> MAPK/ERK信号通路 >> 核糖体S6激酶(RSK)

天然产物 >> 酚类

研究领域 >> 癌症

[ 靶点 ]

IC50: 5.5 μM (RSK2)[1].

[体外研究]

结果表明,鼠尾草酚对GES1细胞没有细胞毒作用,10μM鼠尾草酚强烈抑制RSK2活性,但对其他任何激酶影响不大。 Carnosol对RSK2自身磷酸化及其底物ATF1的磷酸化具有强烈的剂量依赖性抑制作用[1]。

[体内研究]

结果表明,相对于媒介物处理组,Carnosol显着降低胃肿瘤的体积和重量。另外,与载体治疗组相似,小鼠耐受用鼠尾草酚治疗而没有显着的体重减轻。 CREK(RSK2的直接下游蛋白)的磷酸化在狂犬病治疗组中被强烈抑制,但总CREB的表达相对不变[1]。

[动物实验]

小鼠[1]小鼠口服给药浓度为100 mg / kg的Carnosol或载体，每周5次，持续31天[1]。

[参考文献]

[1]. Wang L, et al. Carnosol suppresses patient-derived gastric tumor growth by targeting RSK2. Oncotarget. 2018 Feb 6;9(76):34200-34212.

[相关活性小分子]

2-[(3,5-二氟-4-羟基苯基)氨基]-7,8-二氢-5,7-二甲基-8-(3-甲基丁基)-6(5H)-蝶啶酮 | 1-[4-氨基-7-(3-羟基丙基)-5-(4-甲基苯基)-7H-吡咯并[2,3-d]嘧啶-6-基]-2-氯-乙酮 | 2-[[4-(5-乙基-4-嘧啶基)-1-哌嗪基]甲基]-6-(三氟甲基)-1H-苯并咪唑 | LY-2584702对甲苯磺酸盐 | BIX 02565 | 4-(4-氯苯基)-4-[4-(1H-吡唑-4-基)苯基]哌啶 | Pluripotin | 槲皮苷 | AD80 | LJI308 | 2,6-二氟-4-[4-[4-(4-甲基-1-哌嗪基)苯基]-3-吡啶基]苯酚 | AT13148

鼠尾草酚物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
524.8±50.0 °C at 760 mmHg

[ 分子式 ]:
C₂₀H₂₆O₄

[ 分子量 ]:
330.418

[ 闪点 ]:
187.0±23.6 °C

[ 精确质量 ]:
330.183105

[ PSA ]:
66.76000

[ LogP ]:
3.71

[ 外观性状 ]:
白色至米色固体

[ 蒸汽压 ]:
0.0±1.4 mmHg at 25°C

[ 折射率 ]:
1.607

[ 储存条件 ]:
−20°C

鼠尾草酚MSDS

详细MSDS(安全技术说明书)

鼠尾草酚安全信息

[ 危害码 (欧洲) ]:
F+

[ 安全声明 (欧洲) ]:
24/25

[ 危险品运输编码 ]:
NONH for all modes of transport

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鼠尾草酚文献

Calcium and α-tocopherol suppress cured-meat promotion of chemically induced colon carcinogenesis in rats and reduce associated biomarkers in human volunteers.

Am. J. Clin. Nutr. 98(5) , 1255-62, (2013)

Processed meat intake has been associated with increased colorectal cancer risk. We have shown that cured meat promotes carcinogen-induced preneoplastic lesions and increases specific biomarkers in th...

Degradation study of carnosic acid, carnosol, rosmarinic acid, and rosemary extract (Rosmarinus officinalis L.) assessed using HPLC.

J. Agric. Food Chem. 60(36) , 9305-14, (2012)

Rosemary, whose major caffeoyl-derived and diterpenoid ingredients are rosmarinic acid, carnosol, and carnosic acid, is an important source of natural antioxidants and is being recognized increasingly...

Relevance of carnosic acid, carnosol, and rosmarinic acid concentrations in the in vitro antioxidant and antimicrobial activities of Rosmarinus officinalis (L.) methanolic extracts.

J. Agric. Food Chem. 60(38) , 9603-8, (2012)

The importance of the diterpenic and rosmarinic acid content in the biological activities of rosemary extracts has been studied previously, but how the relationship between the concentration of these ...

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