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心菊内酯

心菊内酯用途

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。

心菊内酯名称

[ CAS 号 ]:
6754-13-8

[ 中文名 ]:
心菊内酯

[ 英文名 ]:
Helenalin

[英文别名 ]:

dl-Mexicanin I
Helenalin A
HELENALIN
PF 56

心菊内酯生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

研究领域 >> 炎症/免疫

[体外研究]

Helenalin(10μM；20-120分钟)可在80分钟后完全抑制NF-κB的DNA结合[1]。Helenalin是一种抗炎、抗癌的植物化学物质,是周期性Skp2积累的有效抑制剂,是介导SCF E3连接酶泛素化和S期两种CKIs降解的F-box蛋白[3]。Western Blot分析[1]细胞株：Jurkat T细胞浓度：10μM孵育时间：20-120分钟结果：80分钟后引起NF-κB-DNA结合完全抑制。

[体内研究]

Helenalin(25 mg/kg；i.p.；6至12小时)给未成熟雄性ICR小鼠造成肝脏谷胱甘肽水平迅速下降[2]。动物模型：未成熟雄性ICR小鼠[2]剂量：25mg/kg给药：i.p.；6～12h结果：导致肝脏谷胱甘肽水平迅速下降。

[参考文献]

[1]. Merrill JC, et al. Role of glutathione in the toxicity of the sesquiterpene lactones hymenoxon and helenalin. J Toxicol Environ Health. 1988;23(2):159-69.

[2]. Lyss G, et al. The anti-inflammatory sesquiterpene lactone helenalin inhibits the transcription factor NF-kappaB by directly targeting p65. J Biol Chem. 1998 Dec 11;273(50):33508-16.

[3]. Fernandes KM, et al. Helenalin-mediated post-transcriptional regulation of p21(Cip1) inhibits 3T3-L1 preadipocyteproliferation. J Cell Biochem. 2008 Oct 15;105(3):913-21.

心菊内酯物理化学性质

[ 密度 ]:
1.25g/cm3

[ 沸点 ]:
473ºC at 760 mmHg

[ 熔点 ]:
167-168ºC

[ 分子式 ]:
C₁₅H₁₈O₄

[ 分子量 ]:
262.30100

[ 闪点 ]:
179.9ºC

[ 精确质量 ]:
262.12100

[ PSA ]:
63.60000

[ LogP ]:
1.24630

[ 外观性状 ]:
固体

[ 折射率 ]:
1.565

[ 储存条件 ]:
2-8°C，密封，干燥

心菊内酯毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: BD9630000

CHEMICAL NAME :: Ambrosa-2,11(13)-dien-12-oic acid, 6-alpha,8-beta-dihydroxy-4-oxo-, 12,8-lactone

CAS REGISTRY NUMBER :: 6754-13-8

BEILSTEIN REFERENCE NO. :: 0028081

LAST UPDATED :: 199712

DATA ITEMS CITED :: 12

MOLECULAR FORMULA :: C15-H18-O4

MOLECULAR WEIGHT :: 262.33

WISWESSER LINE NOTATION :: T C575 DYVO MV KUTJ A1 BQ DU1 I1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 125 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 150 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 10 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - food intake (animal) Gastrointestinal - peritonitis

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 90 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - hamster

DOSE/DURATION :: 85 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - domestic

DOSE/DURATION :: 100 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 45 mg/kg/3D-I

TOXIC EFFECTS :: Liver - changes in liver weight Endocrine - changes in spleen weight Endocrine - changes in thymus weight

TYPE OF TEST :: DNA inhibition

MUTATION DATA

TYPE OF TEST :: Cytogenetic analysis

TEST SYSTEM :: Rodent - hamster Ovary

DOSE/DURATION :: 780 ppb

REFERENCE :: BSECBU Biochemical Systematics and Ecology. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.2- 1974- Volume(issue)/page/year: 13,365,1985

心菊内酯安全信息

[ 危险品运输编码 ]:
UN 2811

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)