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单响尾蛇毒蛋白

单响尾蛇毒蛋白用途

Monocrotaline是从猪屎豆植物的种子提取的吡咯里西啶生物碱,用于在啮齿动物中诱导肺动脉高血压。

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单响尾蛇毒蛋白名称

[ CAS 号 ]:
315-22-0

[ 中文名 ]:
野百合碱

[ 英文名 ]:
Crotaline

[中文别名 ]:

[英文别名 ]:

Monocrotaline/crotaline
Monccrotalire
Bulbus Lilii
CROTALINE
Monocrotaline
MONOCRATALINE
MFCD00084656
A 6080
MONOCROTALIN
CROTALIN

单响尾蛇毒蛋白生物活性

[ 描述 ]:

Monocrotaline是从猪屎豆植物的种子提取的吡咯里西啶生物碱,用于在啮齿动物中诱导肺动脉高血压。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

天然产物 >> 其他

研究领域 >> 代谢疾病

[体外研究]

野百合碱(MCT)是一种11元大环吡咯里西啶生物碱(PA),来源于猪屎豆(Crotalaria spectabilis)植物的种子[1]。野甘露碱是一种天然配体,具有剂量依赖性细胞毒性,具有强大的抗肿瘤活性。野百合碱的体外细胞毒性证实为IC50为24.966μg/ mL,2 X IC50对HepG2细胞的遗传毒性[2]。

[体内研究]

MCT引起大鼠肺血管综合征,其特征为增殖性肺血管炎,肺动脉高压(PH)和肺心病[3]。在肺动脉高压(PAH)的临床前模型中,野百合碱动物模型提供了模拟人PAH几个关键方面的优势,包括血管重塑,平滑肌细胞增殖,内皮功能障碍,炎性细胞因子上调和右心室衰竭,需要单次注射药物[4]。通过注射野百合碱观察到与PH发展相关的多种途径的变化,包括活化的糖酵解,增加的增殖标记,肉毒碱稳态的破坏,炎症和纤维化生物标志物的增加以及谷胱甘肽生物合成的减少[5]。

[动物实验]

大鼠：在该研究中使用总共20只雄性Sprague Dawley大鼠（SD; 220-270g）（每组n = 10）。对照组接受野百合碱（MCT）的载体。肺动脉高压前期（PH）组单次注射MCT（60 mg / kg ip）诱导并在14天后处死[5]。

[参考文献]

[1]. Gomez-Arroyo JG, et al. The monocrotaline model of pulmonary hypertension in perspective. Am J Physiol Lung Cell Mol Physiol. 2012 Feb 15;302(4):L363-9.

[2]. Kusuma SS, et al. Antineoplastic activity of monocrotaline against hepatocellular carcinoma. Anticancer Agents Med Chem. 2014;14(9):1237-48.

[3]. Wilson DW, et, al. Mechanisms and pathology of monocrotaline pulmonary toxicity. Crit Rev Toxicol. 1992;22(5-6):307-25.

[4]. Nogueira-Ferreira R, et al. Exploring the monocrotaline animal model for the study of pulmonary arterial hypertension: A network approach. Pulm Pharmacol Ther. 2015 Dec;35:8-16.

[5]. Rafikova O,et al. Metabolic Changes Precede the Development of Pulmonary Hypertension in the Monocrotaline Exposed RatLung. PLoS One. 2016 Mar 3;11(3):e0150480.

[相关活性小分子]

单响尾蛇毒蛋白物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
537.3±50.0 °C at 760 mmHg

[ 熔点 ]:
204ºC (dec.)(lit.)

[ 分子式 ]:
C₁₆H₂₃NO₆

[ 分子量 ]:
325.357

[ 闪点 ]:
278.7±30.1 °C

[ 精确质量 ]:
325.152527

[ PSA ]:
96.30000

[ LogP ]:
-0.37

[ 外观性状 ]:
白色至淡黄褐色的粉末

[ 蒸汽压 ]:
0.0±3.2 mmHg at 25°C

[ 折射率 ]:
1.586

[ 储存条件 ]:
2~8°C

单响尾蛇毒蛋白MSDS

详细MSDS(安全技术说明书)

单响尾蛇毒蛋白毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: QB3140000

CHEMICAL NAME :: Monocrotaline

CAS REGISTRY NUMBER :: 315-22-0

BEILSTEIN REFERENCE NO. :: 0048732

LAST UPDATED :: 199612

DATA ITEMS CITED :: 44

MOLECULAR FORMULA :: C16-H23-N-O6

MOLECULAR WEIGHT :: 325.40

WISWESSER LINE NOTATION :: T55 AN CUTJ FQ D1OV1- ET5OVTJ C1 D1 EQ

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 :: 66 mg/kg

TOXIC EFFECTS :: Liver - hepatitis (hepatocellular necrosis), diffuse

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 130 mg/kg

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - other changes Liver - other changes

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 60 mg/kg

TOXIC EFFECTS :: 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 :: 92 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 :: Unreported

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 60 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 :: 259 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 :: 261 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 :: Unreported

SPECIES OBSERVED :: Mammal - species unspecified

DOSE/DURATION :: 60 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 :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 61600 ug/kg/28D-C

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - changes in lung weight Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - other oxidoreductases Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 18 mg/kg/10D-C

TOXIC EFFECTS :: Cardiac - changes in heart weight Lungs, Thorax, or Respiration - changes in lung weight Nutritional and Gross Metabolic - weight loss or decreased weight gain

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 75600 ug/kg/3W-C

TOXIC EFFECTS :: Vascular - BP elevation not characterized in autonomic section Lungs, Thorax, or Respiration - changes in lung weight Cardiac - changes in heart weight

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 288 mg/kg/48W-I

TOXIC EFFECTS :: Vascular - thrombosis distant from injection site Blood - hemorrhage Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1050 mg/kg/14D-I

TOXIC EFFECTS :: Liver - changes in liver weight Endocrine - changes in spleen weight Blood - changes in leukocyte (WBC) count

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 130 mg/kg/1Y-I

TOXIC EFFECTS :: Tumorigenic - Carcinogenic by RTECS criteria Lungs, Thorax, or Respiration - tumors Liver - tumors

TYPE OF TEST :: Specific locus test

TYPE OF TEST :: Sex chromosome loss and nondisjunction

TYPE OF TEST :: Heritable translocation test

TYPE OF TEST :: DNA damage

TYPE OF TEST :: Mutation test systems - not otherwise specified

TYPE OF TEST :: Mutation test systems - not otherwise specified

TYPE OF TEST :: Micronucleus test

TYPE OF TEST :: Micronucleus test

MUTATION DATA

TYPE OF TEST :: Cytogenetic analysis

TEST SYSTEM :: Mammal - species unspecified Leukocyte

DOSE/DURATION :: 25 umol/L

REFERENCE :: CYTBAI Cytobios. (Faculty Press, 88 Regent St., Cambridge, UK) V.1- 1969- Volume(issue)/page/year: 14,151,1975 *** REVIEWS *** IARC Cancer Review:Animal Sufficient 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: 10,291,1976 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: 10,291,1976 IARC Cancer Review:Group 2B 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 FEPRA7 Federation Proceedings, Federation of American Societies for Experimental Biology. (Bethesda, MD) V.1-46, 1942-87. Volume(issue)/page/year: 35,89,1976 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

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单响尾蛇毒蛋白安全信息

[ 符号 ]:

GHS06, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301-H351

[ 警示性声明 ]:
P281-P301 + P310

[ 个人防护装备 ]:
Eyeshields;Faceshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T: Toxic;

[ 风险声明 (欧洲) ]:
R25

[ 安全声明 (欧洲) ]:
36/37/39-45

[ 危险品运输编码 ]:
UN 1544 6.1/PG 3

[ WGK德国 ]:
3

[ RTECS号 ]:
QB3140000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
29399990

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单响尾蛇毒蛋白文献

The Japanese toxicogenomics project: application of toxicogenomics.

Mol. Nutr. Food. Res. 54 , 218-27, (2010)

Biotechnology advances have provided novel methods for the risk assessment of chemicals. The application of microarray technologies to toxicology, known as toxicogenomics, is becoming an accepted appr...

Developing structure-activity relationships for the prediction of hepatotoxicity.

Chem. Res. Toxicol. 23 , 1215-22, (2010)

Drug-induced liver injury is a major issue of concern and has led to the withdrawal of a significant number of marketed drugs. An understanding of structure-activity relationships (SARs) of chemicals ...

A predictive ligand-based Bayesian model for human drug-induced liver injury.

Drug Metab. Dispos. 38 , 2302-8, (2010)

Drug-induced liver injury (DILI) is one of the most important reasons for drug development failure at both preapproval and postapproval stages. There has been increased interest in developing predicti...

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