毛果天芥菜碱

毛果天芥菜碱用途

拉索卡品是一种肝毒性吡咯利嗪生物碱(PA),在体内可引起致命的肝静脉闭塞性疾病。只有在其代谢转化为有毒中间体(包括脱氢罗拉西平和N-氧化物)后,罗拉西平才具有毒性[1]。

毛果天芥菜碱名称

[ CAS 号 ]:
303-34-4

[ 中文名 ]:
毛果天芥菜碱

[ 英文名 ]:
Lasiocarpine

[中文别名 ]:

毛果天芥菜鹼

[英文别名 ]:

Lasiocarpin

毛果天芥菜碱生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

[体外研究]

只有在其代谢转化为有毒中间体(称为脱氢罗拉西卡品[1])后,拉西卡品才具有毒性。脱氢罗拉西平和其他假定的二氢吡咯里西啶生物碱(吡咯酯)非常活泼,它们攻击DNA和蛋白质等亲核大分子,引发严重毒性,包括肝静脉阻塞性疾病和肿瘤[1]。拉西阿品在体外主要通过五种代谢途径进行代谢,即脱氢、酯键断裂和去甲基化[1]。

[参考文献]

[1]. Muluneh M Fashe, et al. Species-Specific Differences in the in Vitro Metabolism of Lasiocarpine. Chem Res Toxicol. 2015 Oct 19;28(10):2034-44.

毛果天芥菜碱物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
519.8±50.0 °C at 760 mmHg

[ 熔点 ]:
97ºC

[ 分子式 ]:
C₂₁H₃₃NO₇

[ 分子量 ]:
411.489

[ 闪点 ]:
268.1±30.1 °C

[ 精确质量 ]:
411.225708

[ PSA ]:
105.53000

[ LogP ]:
2.85

[ 外观性状 ]:
无色至米色结晶固体

[ 蒸汽压 ]:
0.0±3.1 mmHg at 25°C

[ 折射率 ]:
1.545

毛果天芥菜碱毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: OE7875000

CHEMICAL NAME :: Lasiocarpine

CAS REGISTRY NUMBER :: 303-34-4

LAST UPDATED :: 199803

DATA ITEMS CITED :: 32

MOLECULAR FORMULA :: C21-H33-N-O7

MOLECULAR WEIGHT :: 411.55

WISWESSER LINE NOTATION :: T55 AN CUTJ D1OVXQXQ1&1&Y1&O1 FOVY1&U2

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 :: 110 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 :: 78 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 - rat

DOSE/DURATION :: 88 mg/kg

TOXIC EFFECTS :: Liver - other changes

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

ROUTE OF EXPOSURE :: Parenteral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 80 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 :: 72 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 :: 85 mg/kg

TOXIC EFFECTS :: Liver - other changes

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 20 mg/kg

TOXIC EFFECTS :: Liver - other changes

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 50 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold 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 - hamster

DOSE/DURATION :: 67500 ug/kg

TOXIC EFFECTS :: Liver - other changes

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 255 mg/kg/2Y-C

TOXIC EFFECTS :: Tumorigenic - Carcinogenic by RTECS criteria Liver - tumors Liver - angiosarcoma

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 470 mg/kg/56W-I

TOXIC EFFECTS :: Tumorigenic - Carcinogenic by RTECS criteria Liver - tumors Skin and Appendages - tumors

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 546 mg/kg/2Y-C

TOXIC EFFECTS :: Tumorigenic - Carcinogenic by RTECS criteria Liver - tumors Liver - angiosarcoma

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1310 mg/kg/2Y-C

TOXIC EFFECTS :: Tumorigenic - Carcinogenic by RTECS criteria Liver - tumors Liver - angiosarcoma

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 760 mg/kg/48W-C

TOXIC EFFECTS :: Tumorigenic - Carcinogenic by RTECS criteria Liver - tumors Skin and Appendages - tumors

TYPE OF TEST :: Sex chromosome loss and nondisjunction

TYPE OF TEST :: Sex chromosome loss and nondisjunction

TYPE OF TEST :: Heritable translocation test

TYPE OF TEST :: DNA inhibition

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

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: 10,281,1976 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: 10,281,1976 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 CTRRDO Cancer Treatment Reports. (Washington, DC) V.60-71, 1976-87. For publisher information, see JNCIEQ. Volume(issue)/page/year: 60,1171,1976

毛果天芥菜碱安全信息

[ 危险品运输编码 ]:
UN 1544

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)