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异紫堇定

异紫堇定用途

Isocorydine 是从美德罗克线虫 Dicranostigma leptopodum (Maxim.) Fedde 中分离出来的。Isocorydine 与阿霉素 (DOX) 的结合具有消除肝细胞癌 (HCC) 的潜力。

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异紫堇定名称

[ CAS 号 ]:
475-67-2

[ 中文名 ]:
异紫堇定碱

[ 英文名 ]:
(+)-Isocorynoline

[中文别名 ]:

[英文别名 ]:

artabotrin
1,2,10-Trimethoxy-6aa-aporphin-11-ol
d-isocorydine
6aα-Aporphin-11-ol, 1,2,10-trimethoxy-
luteanin
isocorydine
iso-Corydine
LUTEANINE

异紫堇定生物活性

[ 描述 ]:

Isocorydine 是从美德罗克线虫 Dicranostigma leptopodum (Maxim.) Fedde 中分离出来的。Isocorydine 与阿霉素 (DOX) 的结合具有消除肝细胞癌 (HCC) 的潜力。

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 其他 >> 其他

[体外研究]

Isocorydine(0-400 ug/ml；48小时)显示ICD和DOX的IC50显着降低,Huh-7,Hep-G2,SNU-449和SNU-387的CI值分别为0.605,0.644,0.804和0.707。[1]。Isocorydine(0-400 ug/ml；48小时)可消除DOX诱导的间充质标志物上调和人HCC细胞系上皮标志物的下调[1]。细胞活力测定[1]细胞系：Huh-7,Hep-G2,SNU-387,SNU-449细胞浓度：0-400 ug/ml孵育时间：24小时结果：与HCC细胞相比,HCC细胞具有更高的细胞毒性单独使用ICD或DOX。蛋白质印迹分析[1]细胞系：Huh-7,Hep-G2,SNU-387,SNU-449细胞浓度：孵育时间：24小时结果：下调Claundin-1和E-钙粘蛋白的蛋白质水平。

[体内研究]

Isocorydine(腹腔注射；0.4 mg/kg；每2天2周)可延缓肿瘤生长,但多柔比星(DOX)或ICD联合治疗可显着抑制肿瘤生长[1]。动物模型：雌性裸鼠[1]剂量：0.4 mg/ml给药：每2天腹腔注射2周结果：异可啶和DOX联合治疗显示出根除HCC的潜力。

[参考文献]

[1]. Pan JX, et al. Isocorydine suppresses doxorubicin-induced epithelial-mesenchymal transition via inhibition of ERK signaling pathways in hepatocellular carcinoma. Am J Cancer Res. 2018 Jan 1;8(1):154-164. eCollection 2018.

异紫堇定物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
506.1±50.0 °C at 760 mmHg

[ 熔点 ]:
216-220ºC(lit.)

[ 分子式 ]:
C₂₀H₂₃NO₄

[ 分子量 ]:
341.401

[ 闪点 ]:
259.9±30.1 °C

[ 精确质量 ]:
341.162720

[ PSA ]:
51.16000

[ LogP ]:
3.09

[ 外观性状 ]:
粉末

[ 蒸汽压 ]:
0.0±1.4 mmHg at 25°C

[ 折射率 ]:
1.604

[ 储存条件 ]:
-20℃

异紫堇定MSDS

详细MSDS(安全技术说明书)

异紫堇定毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: CE1057950

CHEMICAL NAME :: 6a-alpha-Aporphin-11-ol, 1,2,10-trimethoxy-

CAS REGISTRY NUMBER :: 475-67-2

BEILSTEIN REFERENCE NO. :: 0094792

LAST UPDATED :: 199612

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C20-H23-N-O4

MOLECULAR WEIGHT :: 341.44

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 10900 ug/kg

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

REFERENCE :: AUPMAF Acta Universitatis Palackianae Olomucensis, Facultatis Medicae. (Statni Pedagogicke Nakladatelstvi, Ostrovni 30, 1 Nove Mesto, 113 01 Prague 1, Czechoslovakia) V.24- 1961- Volume(issue)/page/year: 61,213,1972

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 104 mg/kg

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

REFERENCE :: CTYAD8 Zhongcaoyao. Chinese Traditional and Herbal Medicine. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.11- 1980- Volume(issue)/page/year: 12,402,1981

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 52 mg/kg

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

REFERENCE :: FATOAO Farmakologiya i Toksikologiya (Moscow). For English translation, see PHTXA6 and RPTOAN. (V/O Mezhdunarodnaya Kniga, 113095 Moscow, USSR) V.2- 1939- Volume(issue)/page/year: 31,44,1968

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 56 mg/kg

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

REFERENCE :: CTYAD8 Zhongcaoyao. Chinese Traditional and Herbal Medicine. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.11- 1980- Volume(issue)/page/year: 12,402,1981

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异紫堇定安全信息

[ WGK德国 ]:
3

[ RTECS号 ]:
CE1057950