中文名称:

心菊内酯

中文同义词:

心菊内酯;锦鸡菊素;海伦纳林

英文名称:

HELENALIN

英文同义词:

(3as-(3aalpha,4alpha,4abeta,7aalpha,8alpha,9aalpha))-ethyl-3-methylene;HELENALIN(SH);HELENALIN;6alpha,8beta-dihydroxy-4-oxoambrosa-2,11(13)-dien-12-oicacid12,8-lactone;a-dimethyl-3-methyleneazuleno[6,5-b]-furan-2,5-dione;ambrosa-2,11(13)-dien-12-oicacid,6-alpha,8-beta-dihydroxy-4-oxo-,12,8-lacton;ambrosa-2,11(13)-dien-12-oicacid,6alpha,8beta-dihydroxy-4-oxo-,12,8-lactone;azuleno(6,5-b)furan-2,5-dione,3,3a,4,4a,7a,8,9,9a-octahydro-4-hydroxy-4a,8-dim

CAS号:

6754-13-8

分子式:

C15H18O4

分子量:

262.3

EINECS号:

相关类别:

分析试剂标准品;标准品;中药对照品;Miscellaneous Natural Products

Mol文件:

6754-13-8.mol

熔点 

167-168°

比旋光度 

D25 -102.8° (c = 3.64 in 95% ethanol)

沸点 

325.55°C (rough estimate)

密度 

1.0772 (rough estimate)

折射率 

1.4300 (estimate)

酸度系数(pKa)

13.29±0.60(Predicted)

形态

White to off-white solid.

生物活性

Helenalin 是一种抗炎的倍半萜内酯。Helenalin 通过直接靶向 p65 选择性抑制转录因子 NF-κB。Helenalin 具有烷基化活性，以 NF-κB 的 p65 亚基中的半胱氨酸巯基为靶点，从而抑制其 DNA 结合。

体外研究

Helenalin (10 μM; 20-120 minutes) causes complete inhibition of NF-κB DNA binding after 80 minutes. The anti-inflammatory, anti-carcinogenic phytochemical, Helenalin is a potent inhibitor of periodic Skp2 accumulation, an F-box protein mediating SCF E3 ligase ubiquitylation and degradation of both CKIs during S phase progression. Western Blot Analysis Cell Line: Jurkat T cells Concentration: 10 μM Incubation Time: 20-120 minutes Result: Caused complete inhibition of NF-κB DNA binding after 80 minutes.

Cell Line:

Jurkat T cells

Concentration:

10 μM

Incubation Time:

20-120 minutes

Result:

Caused complete inhibition of NF-κB DNA binding after 80 minutes.

体内研究

Helenalin (25 mg/kg; i.p.; 6 to 12 hours) administers to immature male ICR mice caused a rapid decrease in hepatic glutathione levels. Animal Model: Immature male ICR mice Dosage: 25 mg/kg Administration: i.p.; 6 to 12 hours Result: Caused a rapid decrease in hepatic glutathione levels.

Animal Model:

Immature male ICR mice

Dosage:

25 mg/kg

Administration:

i.p.; 6 to 12 hours

Result:

Caused a rapid decrease in hepatic glutathione levels.

危险品运输编号 

2811

HazardClass 

6.1(b)

PackingGroup 

III

毒性

LD50 in mice, rats (mg/kg): 150, 125 orally (Witzel)