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槐定碱

槐定碱用途

Sophoridine 是一种从豆科植物槐豆斜生植物的叶子中分离出来的喹喔啉生物碱。Sophoridine 诱导细胞凋亡 (apoptosis)。Sophoridine 有可能成为胰腺癌的有效,选择性和耐受性良好的候选药物。

槐定碱名称

[ CAS 号 ]:
6882-68-4

[ 中文名 ]:
槐定碱

[ 英文名 ]:
Sophoridine

[英文别名 ]:

Allomatrine
(5β)-Matridin-15-one
Bio-0637
5-Epidihydrosophocarpine
Dihydro-5-episophocarpine
sophoridine
matridin-15-one

槐定碱生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 细胞凋亡

研究领域 >> 癌症

[体外研究]

槐角苷(0-500μM；48小时)对人胰腺癌,胃癌,肝癌,结肠癌,胆囊癌和前列腺癌细胞的生长具有显着的抑制作用,IC50值约为20μM至200μM[1]。Sophoridine(0-20μM；48小时)使Miapaca-2细胞中S期细胞群从26.23%(对照)增加到38.67%,PANC-1细胞从29.56%(对照)增加到39.16%,约为1.5倍和分别增加1.3倍[1]。槐角苷(0-20μM；48小时)显着增加bad和bax水平,并降低bcl-2和bcl-xl水平,而bax/bcl-2比率显着增加[1]。细胞活力测定[1]细胞系：正常细胞：IOSE144,HL-7702和LO2,BEAS-2B,GES-1,HEK 293 T,HPDE,FHC,人癌细胞：PANC-1,Mapaca-1,hepG2,SGC-7901,CBC-SD,SGC-996,PC-3,MKN-45,MGC-803,Hela和HCT116细胞浓度：0,3.9,7.8,15.5,31,62.5,125,250,500μM孵育时间：48小时结果：对癌细胞表现出最有效的细胞毒性。细胞周期分析[1]细胞系：PANC-1细胞；Miapca-2细胞浓度：20μM孵育时间：48小时结果：导致S期累积群体。蛋白质印迹分析[1]细胞系：PANC-1细胞；Miapca-2细胞浓度：20μM孵育时间：48小时结果：诱导内源性凋亡途径的激活。

[体内研究]

槐角苷(腹腔注射；20或40 mg/kg；21天)可抑制异种移植胰腺肿瘤的生长[1]。动物模型：BALB/c纯合(nu/nu)裸鼠[1]剂量：20或40mg/kg给药：腹膜内注射；20或40mg/kg；21天结果：异种移植胰腺肿瘤质量减少。

[参考文献]

[1]. Xu Z, et al. Sophoridine induces apoptosis and S phase arrest via ROS-dependent JNK and ERK activation in human pancreatic cancer cells. J Exp Clin Cancer Res. 2017 Sep 11;36(1):124.

槐定碱物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
396.7±31.0 °C at 760 mmHg

[ 熔点 ]:
109 °C

[ 分子式 ]:
C₁₅H₂₄N₂O

[ 分子量 ]:
248.364

[ 闪点 ]:
172.7±17.2 °C

[ 精确质量 ]:
248.188858

[ PSA ]:
23.55000

[ LogP ]:
1.44

[ 外观性状 ]:
固体;White to Light yellow powder to crystal

[ 蒸汽压 ]:
0.0±0.9 mmHg at 25°C

[ 折射率 ]:
1.581

[ 储存条件 ]:
0-10°C;避免加热

槐定碱毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: WG1250000

CHEMICAL NAME :: Sophoridine

CAS REGISTRY NUMBER :: 6882-68-4

LAST UPDATED :: 199412

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C15-H24-N2-O

MOLECULAR WEIGHT :: 248.41

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 243 mg/kg

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

REFERENCE :: ZYZAEU Zhongguo Yaoxue Zazhi. Chinese Pharmacuetical Journal. (China International Book Trading Corp., POB 2820, Beijing, Peop. China) V.24- 1989- Volume(issue)/page/year: 27,201,1992

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 64300 ug/kg

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

REFERENCE :: CYLPDN Zhongguo Yaoli Xuebao. Acta Pharmacologica Sinica. Chinese Journal of Pharmacology. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.1- 1980- Volume(issue)/page/year: 8,153,1987

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 46800 ug/kg

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

REFERENCE :: YFZADL Yaowu Fenxi Zazhi. Journal of Pharmaceutical Analysis. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.1- 1981- Volume(issue)/page/year: 6,96,1986 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 350 mg/kg/35D-I

TOXIC EFFECTS :: Blood - changes in leukocyte (WBC) count

REFERENCE :: CYLPDN Zhongguo Yaoli Xuebao. Acta Pharmacologica Sinica. Chinese Journal of Pharmacology. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.1- 1980- Volume(issue)/page/year: 8,153,1987

槐定碱安全信息

[ 危害码 (欧洲) ]:
Xi

[ 安全声明 (欧洲) ]:
24/25

槐定碱