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千里光宁

千里光宁用途

Senecionine是一种从 Senecio vulgaris 中分离出来的吡咯里西啶生物碱。 Senecionine对动物和人类有毒。

千里光宁名称

[ CAS 号 ]:
130-01-8

[ 中文名 ]:
千里光宁

[ 英文名 ]:
Senecionine

[中文别名 ]:

[英文别名 ]:

aureine
Senecionine
MFCD00221720
(15Z)-12-Hydroxysenecionan-11,16-dione
Integerrimine

千里光宁生物活性

[ 描述 ]:

Senecionine是一种从 Senecio vulgaris 中分离出来的吡咯里西啶生物碱。 Senecionine对动物和人类有毒。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 代谢疾病

[体外研究]

吡咯里西啶生物碱(PAs)被认为是植物来源的化合物中肝毒性最强的一种,并且存在于世界上约3％的开花植物中。大多数保护区通过食用植物和受PA污染的产品(如牛奶,蜂蜜,草药茶和药物)对牲畜和人类都有相当大的健康危害[1]。

[体内研究]

在静脉内给药和口服给予Senecionine和Adonifoline后,观察到药代动力学的显着差异,其中Senecionine和Adonifoline被快速吸收,生物利用度较低,并迅速代谢为PA的N-氧化物和羟基化产物或其N-氧化物[1] ]。 Senecionine不能刺激环氧化物酶,它会降低谷胱甘肽-s-转移酶,氨基比林脱甲基酶和AHH的活性[2]。从第12天或之后开始,每周两次注射第三种成分,即senecionine,导致7只大鼠中的3只早产,而所有窝中的幼仔在出生后不久死产或死亡[3]。

[动物实验]

将体重为155-175g的大鼠[1]瑞士白化大鼠与40mg或80mg / kg体重的日剂量的seneciphylline和senecionine一起温育3天。对照动物仅接受生理盐水。在最后一次给药后24小时杀死动物。取出肝脏，称重，然后在1.15％KCl，0.02HEPES（pH7.4）中均化[1]。

[参考文献]

[1]. Wang C, et al. The comparative pharmacokinetics of two pyrrolizidine alkaloids, senecionine and adonifoline, and their main metabolites in rats after intravenous and oral administration by UPLC/ESIMS. Anal Bioanal Chem. 2011 Jul;401(1):275-87.

[2]. Kakrani HK, et al. Effect of seneciphylline and senecionine on hepatic drug metabolizing enzymes in rats. J Ethnopharmacol. 1984 Dec;12(3):271-8.

[3]. Tu ZB, et al. Identification of senecionine and senecionine N-oxide as antifertility constituents in Senecio vulgaris. J Pharm Sci. 1988 May;77(5):461-3.

[相关活性小分子]

千里光宁物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
563.7±50.0 °C at 760 mmHg

[ 熔点 ]:
236ºC(lit.)

[ 分子式 ]:
C₁₈H₂₅NO₅

[ 分子量 ]:
335.395

[ 闪点 ]:
294.7±30.1 °C

[ 精确质量 ]:
335.173279

[ PSA ]:
76.07000

[ LogP ]:
0.88

[ 蒸汽压 ]:
0.0±3.5 mmHg at 25°C

[ 折射率 ]:
1.570

[ 储存条件 ]:
通风低温干燥,与库房食品原料分开存放

千里光宁MSDS

详细MSDS(安全技术说明书)

千里光宁毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: VT5710000

CHEMICAL NAME :: Senecionan-11,16-dione, 12-hydroxy-

CAS REGISTRY NUMBER :: 130-01-8

LAST UPDATED :: 199612

DATA ITEMS CITED :: 12

MOLECULAR FORMULA :: C18-H25-N-O5

MOLECULAR WEIGHT :: 335.44

WISWESSER LINE NOTATION :: T55-12- 1A Q EN IOVY OVO BUTJ KU2 M NQ N

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 :: 85 mg/kg

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

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 33 mg/kg

TOXIC EFFECTS :: Liver - other changes

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 41200 ug/kg

TOXIC EFFECTS :: Liver - other changes

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

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 40 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 :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 64 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory stimulation

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - hamster

DOSE/DURATION :: 61 mg/kg

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - acute pulmonary edema Liver - hepatitis (hepatocellular necrosis), diffuse Blood - lymphoma, including Hodgkin's disease

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 140 mg/kg

SEX/DURATION :: female 4-10 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

TYPE OF TEST :: Sex chromosome loss and nondisjunction

MUTATION DATA

TEST SYSTEM :: Rodent - mouse

DOSE/DURATION :: 90 mg/kg

REFERENCE :: TOXID9 Toxicologist. (Soc. of Toxicology, Inc., 475 Wolf Ledge Parkway, Akron, OH 44311) V.1- 1981- Volume(issue)/page/year: 1,42,1981 *** REVIEWS *** TOXICOLOGY REVIEW ZKKOBW Zeitschrift fuer Krebsforschung und Klinische Onkologie. (Berlin, Fed. Rep. Ger.) V.76-92, 1971-78. For publisher information, see JCROD7. Volume(issue)/page/year: 78,99,1972

千里光宁安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301

[ 警示性声明 ]:
P301 + P310

[ 危害码 (欧洲) ]:
T

[ 风险声明 (欧洲) ]:
R25

[ 安全声明 (欧洲) ]:
45

[ 危险品运输编码 ]:
UN 2811 6.1/PG 3

[ WGK德国 ]:
3

[ RTECS号 ]:
VT5710000

[ 包装等级 ]:
II

[ 危险类别 ]:
6.1(a)

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千里光宁文献

UPLC-MS/MS method for determination of selected pyrrolizidine alkaloids in feed.

Food Chem. 170 , 265-70, (2014)

Alkaloids known as secondary metabolites are grouped by typical structural characteristics into large families such as pyrrolizidine alkaloids (PAs) comprising more than 350 individual heterocyclic co...

Modeling K(m) values using electrotopological state: substrates for cytochrome P450 3A4-mediated metabolism.

Bioorg. Med. Chem. Lett. 15 , 4076-84, (2005)

In order to determine K(m) values of substrates for CYP3A4-mediated metabolism, an in silico model has been developed in the present work. Using electrotopological state (E-state) indices, together wi...

A competitive enzyme immunoassay for the pyrrolizidine alkaloids of the senecionine type.

Planta Med. 62(3) , 267-71, (1996)

We developed an immunoassay with antibodies against retrorsine to detect the closely related senecionine, the main alkaloid in various Asteraceae. Sensitivity is about 23 pg (68 fmol) for senecionine....

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