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倒千里光碱

倒千里光碱用途

Retrorsine 是一种天然存在的有毒吡咯利西啶生物碱。Retrorsine 可以与 DNA 结合,抑制肝细胞的增殖能力。

倒千里光碱名称

[ CAS 号 ]:
480-54-6

[ 中文名 ]:
倒千里光碱

[ 英文名 ]:
isatidine

[英文别名 ]:

(15Z)-12,18-Dihydroxysenecionan-11,16-dione
isatidine
b-Longilobine
12,18-dihydroxy-senecionane-11,16-dione
12,18-Dihydroxysenecionan-11,16-dione
β-Longilobine
cis-Retronecic acid ester of retronecine
Retrorsin
MFCD00013331

倒千里光碱生物活性

[ 描述 ]:

Retrorsine 是一种天然存在的有毒吡咯利西啶生物碱。Retrorsine 可以与 DNA 结合,抑制肝细胞的增殖能力。

[ 相关类别 ]:

研究领域 >> 其他

信号通路 >> 其他 >> 其他

[体外研究]

逆转录酶抑制剂(60-240μM；24小时)显著降低HSEC-CYP3A4细胞活力,消耗GSH,并增加吡咯-蛋白质加合物的形成[3]。细胞活力测定[3]细胞系：HSEC-CYP3A4细胞浓度：60μM、120μM、240μM孵育时间：24小时结果：细胞活力明显降低。

[体内研究]

逆转录酶抑制剂(30mg/kg；腹腔注射；两次)不仅通过S期或G2/M期阻滞,而且通过位于细胞周期G1/S转换之前的阻滞,损害PBL模型中的肝再生[1]。动物模型：雄性Wistar大鼠(180±20g),门脉分支结扎(PBL)模型[1]剂量：30mg/kg给药：腹腔注射,2次,间隔2周。结果：PBL后肝脏增重、蛋白质和DNA合成以及再生叶细胞周期相关蛋白的诱导明显受损。

[参考文献]

[1]. F J Cubero, et al. Hepatic proliferation in Gunn rats transplanted with hepatocytes: effect of retrorsine and tri-iodothyronine. Cell Prolif. 2005 Jun;38(3):137-46.

[2]. F J Cubero, et al. Hepatic proliferation in Gunn rats transplanted with hepatocytes: effect of retrorsine and tri-iodothyronine. Cell Prolif. 2005 Jun;38(3):137-46.

[3]. Yao Lu, et al. Establishment of a novel CYP3A4-transduced human hepatic sinusoidal endothelial cell model and its application in screening hepatotoxicity of pyrrolizidine alkaloids. J Environ Sci Health C Toxicol Carcinog. 2020;38(2):169-185.

倒千里光碱物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
583.2±50.0 °C at 760 mmHg

[ 熔点 ]:
208-211ºC(lit.)

[ 分子式 ]:
C₁₈H₂₅NO₆

[ 分子量 ]:
351.394

[ 闪点 ]:
306.5±30.1 °C

[ 精确质量 ]:
351.168182

[ PSA ]:
96.30000

[ LogP ]:
-0.14

[ 外观性状 ]:
白色至米白色固体

[ 蒸汽压 ]:
0.0±3.7 mmHg at 25°C

[ 折射率 ]:
1.590

[ 储存条件 ]:
20°C，惰性气体，干燥

倒千里光碱MSDS

详细MSDS(安全技术说明书)

倒千里光碱毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: VH7525000

CHEMICAL NAME :: Retrorsine

CAS REGISTRY NUMBER :: 480-54-6

LAST UPDATED :: 199512

DATA ITEMS CITED :: 22

MOLECULAR FORMULA :: C18-H25-N-O6

MOLECULAR WEIGHT :: 351.44

WISWESSER LINE NOTATION :: T55-12- 1A Q EN IOVY OVO BUTJ KU2 M1 NQ N1Q

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 :: 34 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 - rat

DOSE/DURATION :: 34 mg/kg

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - acute pulmonary edema Liver - other changes Nutritional and Gross Metabolic - weight loss or decreased weight gain

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 38 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 :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 35 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 :: 65 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 :: 59 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 :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 46 mg/kg

TOXIC EFFECTS :: Liver - hepatitis (hepatocellular necrosis), zonal Liver - other changes Blood - macrocytosis

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - species unspecified

DOSE/DURATION :: 33 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 :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 175 mg/kg/5D-I

TOXIC EFFECTS :: Liver - other changes Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 560 mg/kg/62W-I

TOXIC EFFECTS :: Tumorigenic - neoplastic by RTECS criteria Liver - tumors

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 150 mg/kg/22W-I

TOXIC EFFECTS :: Tumorigenic - equivocal tumorigenic agent by RTECS criteria Liver - tumors

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 68 mg/kg/43W-I

TOXIC EFFECTS :: Tumorigenic - equivocal tumorigenic agent by RTECS criteria Liver - tumors Kidney, Ureter, Bladder - Kidney tumors

TYPE OF TEST :: Sex chromosome loss and nondisjunction

MUTATION DATA

TYPE OF TEST :: Cytogenetic analysis

TEST SYSTEM :: Rodent - hamster Lung

DOSE/DURATION :: 3160 nmol/L

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 282,169,1992 *** REVIEWS *** IARC Cancer Review:Animal Limited Evidence IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 10,303,1976 IARC Cancer Review:Human No Adequate Data IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 10,303,1976 IARC Cancer Review:Group 3 IMSUDL IARC Monographs, Supplement. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) No.1- 1979- Volume(issue)/page/year: 7,56,1987 TOXICOLOGY REVIEW CTRRDO Cancer Treatment Reports. (Washington, DC) V.60-71, 1976-87. For publisher information, see JNCIEQ. Volume(issue)/page/year: 60,1171,1976

倒千里光碱安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H300

[ 警示性声明 ]:
P264-P301 + P310

[ 个人防护装备 ]:
Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T

[ 风险声明 (欧洲) ]:
25

[ 安全声明 (欧洲) ]:
S22;S45;S36/S37/S39

[ 危险品运输编码 ]:
UN 1544

[ RTECS号 ]:
VH7525000

[ 包装等级 ]:
II

[ 危险类别 ]:
6.1(a)

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倒千里光碱文献

Diversity of pyrrolizidine alkaloids in native and invasive Senecio pterophorus (Asteraceae): implications for toxicity.

Phytochemistry 108 , 137-46, (2014)

Changes in plant chemical defenses after invasion could have consequences on the invaded ecosystems by modifying the interactions between plants and herbivores and facilitating invasion success. Howev...

Involvement of organic cation transporter 1 and CYP3A4 in retrorsine-induced toxicity.

Toxicology 322 , 34-42, (2014)

Retrorsine (RTS) is a hepatotoxic pyrrolizidine alkaloid present in plants of the Senecio genus. The present study is aimed at clarifying the role of organic cation transporters (OCTs) in the liver di...

Are effects of common ragwort in the Ames test caused by pyrrolizidine alkaloids?

Mutat. Res. 778 , 1-10, (2015)

It has previously been demonstrated by others that acetone extracts of Senecio jacobaea (syn. Jacobaea vulgaris, common or tansy ragwort) test positive in the Salmonella/microsome mutagenicity test (A...

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