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土木香内酯

土木香内酯用途

Alantolactone 是 STAT3 的选择性抑制剂,并具有抗肿瘤活性。

土木香内酯名称

[ CAS 号 ]:
546-43-0

[ 中文名 ]:
土木香内酯

[ 英文名 ]:
Alantolactone

[中文别名 ]:

[英文别名 ]:

8b-Hydroxy-4aH-eudesm-5-en-12-oic Acid g-Lactone
Inula camphor
ALLANTOLACTONE
MFCD00046915
Helenin
HELENINE
ALANTOLACTONE
Elecampane camphor
ALANTOLACETONE
Eupatal

土木香内酯生物活性

[ 描述 ]:

Alantolactone 是 STAT3 的选择性抑制剂,并具有抗肿瘤活性。

[ 相关类别 ]:

天然产物 >> 萜类化合物和糖苷

研究领域 >> 癌症

[ 靶点 ]

STAT3

[体外研究]

Alantolactone以剂量依赖性方式诱导HepG2细胞凋亡。发现这种Alantolactone诱导的细胞凋亡与GSH耗竭,STAT3激活抑制,ROS产生,线粒体跨膜电位耗散,Bax/Bcl-2比值增加和caspase-3激活有关[1]。 Alantolactone降低STAT3易位至细胞核,其DNA结合和STAT3靶基因表达。 Alantolactone显着抑制STAT3活化,对MAPKs和NF-κB转录具有边际效应;然而,这种作用并不是通过抑制STAT3上游激酶来实现的[2]。

[体内研究]

发现与对照小鼠相比,Alantolactone处理的小鼠的平均肿瘤体积约低2.17倍。然而,在实验期间给予Alantolactone不影响总体重,表明没有明显的毒性。另外,与对照小鼠相比,在Alantolactone处理的小鼠中平均肿瘤重量显着更低。此外,Alantolactone的使用导致肿瘤组织中p-STAT3和cyclin D1表达的显着降低[2]。

[细胞实验]

将细胞培养24小时，然后在96孔板中进行药物处理。用Alantolactone（0,10,20,30,40,50和60μM）处理细胞12小时，并通过MTT测定法测量细胞活力[1]。

[动物实验]

小鼠[2]使用6周龄的雌性无胸腺BALB / c裸鼠。将MDA-MB-231细胞（5×10 6个细胞/200μL）皮下注射到小鼠的右侧腹中。注射细胞10天后，将小鼠随机分成治疗组和对照组（n = 5）。每2天给动物施用Alantolactone（2.5mg / kg体重，悬浮于DMSO 0.1％v / v，100μL腹膜内注射），而对照动物用等体积的盐水处理[2]。

[参考文献]

[1]. Khan M, et al. Alantolactone induces apoptosis in HepG2 cells through GSH depletion, inhibition of STAT3 activation, and mitochondrial dysfunction. Biomed Res Int. 2013;2013:719858.

[2]. Chun J, et al. Alantolactone selectively suppresses STAT3 activation and exhibits potent anticancer activity in MDA-MB-231 cells. Cancer Lett. 2015 Feb 1;357(1):393-403.

[相关活性小分子]

土木香内酯物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
275.0±0.0 °C at 760 mmHg

[ 熔点 ]:
78-79ºC

[ 分子式 ]:
C₁₅H₂₀O₂

[ 分子量 ]:
232.318

[ 闪点 ]:
111.5±18.2 °C

[ 精确质量 ]:
232.146332

[ PSA ]:
26.30000

[ LogP ]:
3.69

[ 外观性状 ]:
结晶粉末

[ 蒸汽压 ]:
0.0±0.5 mmHg at 25°C

[ 折射率 ]:
1.534

[ 储存条件 ]:
?20°C

土木香内酯MSDS

详细MSDS(安全技术说明书)

土木香内酯安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H317

[ 警示性声明 ]:
P280

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
26-36

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

[ 海关编码 ]:
2932209090

土木香内酯海关

[ 海关编码 ]: 2932209090

[ 中文概述 ]:
2932209090. 其他内酯. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2932209090. other lactones. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

土木香内酯文献

Pharmacokinetics, tissue distribution and excretion of isoalantolactone and alantolactone in rats after oral administration of Radix Inulae extract.

Molecules 20 , 7719-36, (2015)

Radix Inulae is endemic to China and has been used in traditional medicine to treat upper body pain, emesis and diarrhoea, and to eliminate parasites. Here, an UPLC-MS/MS method was developed and appl...

A fluorescence high throughput screening method for the detection of reactive electrophiles as potential skin sensitizers.

Toxicol. Appl. Pharmacol. 289 , 177-84, (2015)

Skin sensitization is an important toxicological end-point in the risk assessment of chemical allergens. Because of the complexity of the biological mechanisms associated with skin sensitization, inte...

Anti-allergic effects of sesquiterpene lactones from the root of Aucklandia lappa Decne.

Mol. Med. Report. 12 , 7789-95, (2015)

Aucklandia lappa Decne, a well-known traditional herbal medicine, is used for the treatment of asthma, rheumatism, coughs, tuberculosis and numerous other diseases. The present study evaluated the inh...

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