密执毒素

密执毒素用途

Mezerein是一种PKC激活剂,具有抗白血病特性。Mezerein抑制表达PKCα(IC50=1190 nM)、PKCβ1(IC50=908 nM)和PKCδ(IC50=141 nM)的酵母的生长,但不抑制表达PKC的酵母的生长[1][2]。

密执毒素名称

[ CAS 号 ]:
34807-41-5

[ 中文名 ]:
密执毒素

[ 英文名 ]:
2,4-Pentadienoic acid,5-phenyl-,(2S,3aR,3bS,3cS,4aR,5S,5aS,8aR,8bR,9R,10R,10aS)-3a,3b,3c,4a,5,5a,8a,9,10,10a-decahydro-5,5a-dihydroxy-4a-(hydroxymethyl)-7,9-dimethyl-10a-(1-methylethenyl)-6-oxo-2-phen

[英文别名 ]:

meserein
MFCD00135953

密执毒素生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 表观遗传学 >> PKC

研究领域 >> 癌症

信号通路 >> TGF-beta/Smad 信号通路 >> PKC

[体外研究]

梅泽林是从瑞香中分离出来的一种抗白血病成分[2]。Mezerein(50 ng/mL；72小时)能有效抑制致瘤小鼠巨噬细胞系M5076细胞增殖[3]。细胞增殖试验[3]细胞系：M5076细胞浓度：50ng/mL培养时间：72小时结果：抑制细胞增殖(大于90%)。

[体内研究]

Mezerein对小鼠P-388淋巴细胞白血病具有抗白血病活性。Mezerein(50μg/kg)对小鼠的P-388和L-1210白血病具有显著的抑制活性[2]。

[参考文献]

[1]. L Saraiva, et al. Differential activation by daphnetoxin and mezerein of PKC-isotypes alpha, beta I, delta and zeta. Planta Med. 2001 Dec;67(9):787-90.

[2]. S M Kupchan,et al.Mezerein: antileukemic principle isolated from Daphne mezereum L. Science. 1975 Feb 21;187(4177):652-3.

[3]. N T Goode, et al. Protein kinase C-induced stimulation or inhibition of cellular proliferation in a murine macrophage tumor cell line. Cancer Res. 1990 Mar 15;50(6):1828-33.

密执毒素物理化学性质

[ 密度 ]:
1.43 g/cm3

[ 熔点 ]:
258-262ºC

[ 分子式 ]:
C₃₈H₃₈O₁₀

[ 分子量 ]:
654.70200

[ 精确质量 ]:
654.24600

[ PSA ]:
144.28000

[ LogP ]:
3.12420

[ 外观性状 ]:
白色固体

[ 折射率 ]:
1.68

[ 储存条件 ]:
-20°C，密封，干燥

密执毒素MSDS

详细MSDS(安全技术说明书)

密执毒素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: HB5425500

CHEMICAL NAME :: Daphnetoxin, 12-((1-oxo-5-phenyl-2,4-pentadienyl)oxy)-, (12-beta(E,E))-

CAS REGISTRY NUMBER :: 34807-41-5

LAST UPDATED :: 199612

DATA ITEMS CITED :: 9

MOLECULAR FORMULA :: C38-H38-O10

MOLECULAR WEIGHT :: 654.76

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Administration onto the skin

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 3560 ug/kg/20W-I

TOXIC EFFECTS :: Tumorigenic - neoplastic by RTECS criteria Skin and Appendages - primary irritation (after topical exposure) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - other Enzymes

TYPE OF TEST :: TD - Toxic dose (other than lowest)

ROUTE OF EXPOSURE :: Administration onto the skin

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 18 mg/kg/20W-I

TOXIC EFFECTS :: Tumorigenic - neoplastic by RTECS criteria Skin and Appendages - primary irritation (after topical exposure) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - other Enzymes

TYPE OF TEST :: Unscheduled DNA synthesis

MUTATION DATA

TEST SYSTEM :: Rodent - mouse

DOSE/DURATION :: 340 nmol/kg

REFERENCE :: CNREA8 Cancer Research. (Public Ledger Building, Suit 816, 6th & Chestnut Sts., Philadelphia, PA 19106) V.1- 1941- Volume(issue)/page/year: 43,4126,1983 *** REVIEWS *** TOXICOLOGY REVIEW BLFSBY Basic Life Sciences. (Plenum Pub. Corp., 223 Spring St., New York, NY 10003) V.1- 1973- Volume(issue)/page/year: 24,253,1983

密执毒素安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H317

[ 警示性声明 ]:
P280

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Faceshields;Gloves

[ 危害码 (欧洲) ]:
Xi: Irritant;

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
S22;S24/25

[ 危险品运输编码 ]:
UN 2811

[ RTECS号 ]:
HB5425500

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

密执毒素文献

Models of acute inflammation in the ear.

Methods Mol. Biol. 225 , 129-37, (2003)

Gateway synthesis of daphnane congeners and their protein kinase C affinities and cell-growth activities.

Nature Chemistry 3(8) , 615-9, (2011)

The daphnane diterpene orthoesters constitute a structurally fascinating family of natural products that exhibit a remarkable range of potent biological activities. Although partial activity informati...

Analysis of daphnane orthoesters in poisonous Australian pimelea species by liquid chromatography-tandem mass spectrometry.

J. Agric. Food Chem. 58(12) , 7482-7, (2010)

Cattle grazing in arid rangelands of Australia suffer periodic extensive and serious poisoning by the plant species Pimelea trichostachya, P. simplex, and P. elongata. Pimelea poisoning (also known as...

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