黄杨碱; 环维黄杨星D

黄杨碱; 环维黄杨星D用途

Cyclovirobuxine D (CVB-D) 是中药黄杨 Buxus microphylla 的主要活性成分。Cyclovirobuxine D 诱导自噬并减弱 Akt 和 mTOR 的磷酸化。Cyclovirobuxine D 通过抑制细胞周期进程和诱导线粒体介导的细胞凋亡 apoptosis 抑制癌细胞的增殖。Cyclovirobuxine D 治疗心肌梗死引起的心力衰竭,具有治疗心力衰竭的潜力。

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黄杨碱; 环维黄杨星D名称

[ CAS 号 ]:
860-79-7

[ 中文名 ]:
环维黄杨星 D

[ 英文名 ]:
Cyclovirobuxine

[中文别名 ]:

[英文别名 ]:

MFCD00468040
bebuxine
cyclovirobuxind
cyclovirobuxinum D
cyclobuxine D
cvb-d
Cyclovirobuxine-D
CYCLOVIROBUXINE

黄杨碱; 环维黄杨星D生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> PI3K/Akt/mTOR 信号通路 >> mTOR

信号通路 >> 细胞凋亡 >> 细胞凋亡

研究领域 >> 心血管疾病

信号通路 >> 自噬 >> 自噬

信号通路 >> PI3K/Akt/mTOR 信号通路 >> AKT

[体外研究]

Cyclovirobuxine D(0-240μM; 24-72小时)显示CVB-D处理后细胞活力的浓度和时间依赖性降低,用240μM处理后72小时,只有10％MGC-803细胞和20％MKN28细胞存活[2]。环维布辛D(0-120μM; 48小时)以浓度依赖性方式阻滞胃癌细胞在S期的细胞周期[2]。环维罗布辛D(0-120μM; 48小时)以浓度依赖性方式导致胃癌细胞凋亡,特别是早期凋亡。环维罗布辛D(0-120μM; 48小时)通过上调胃癌细胞中凋亡相关蛋白,切割的Caspase-3和Bax/Bcl-2的比率引起细胞凋亡[2]。细胞活力测定[2]细胞系：MGC-803和MKN28细胞浓度：0,30,60,120和240μM培养时间：24,48,72小时结果：胃癌细胞周期分析的细胞活力和集落形成能力降低[2]细胞系：MGC-803和MKN28细胞浓度：0,30,60和120μM培养时间：48小时结果：MGC-803和MKN28细胞的停滞细胞周期进程。细胞凋亡分析[2]细胞系：MGC-803和MKN28细胞浓度：0,30,60和120μM培养时间：48小时结果：诱导MGC-803和MKN28细胞凋亡。Western Blot分析[2]细胞系：MGC-803和MKN28细胞浓度：0,30,60和120μM培养时间：48小时结果：上调切割的Caspase-3和Bax,降低Bcl-2表达的表达。

[参考文献]

[1]. Lu J, et al. Cyclovirobuxine D induces autophagy-associated cell death via the Akt/mTOR pathway in MCF-7 human breast cancer cells. J Pharmacol Sci. 2014;125(1):74-82. Epub 2014 Apr 24.

[2]. Wu J, et al. Cyclovirobuxine D Inhibits Cell Proliferation and Induces Mitochondria-Mediated Apoptosis in Human Gastric Cancer Cells. Molecules. 2015 Nov 19;20(11):20659-68.

[3]. Yu B, et al. Beneficial effect of Cyclovirobuxine D on heart failure rats following myocardial infarction. Fitoterapia. 2011 Sep;82(6):868-77.

黄杨碱; 环维黄杨星D物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
495.7±10.0 °C at 760 mmHg

[ 分子式 ]:
C₂₆H₄₆N₂O

[ 分子量 ]:
402.656

[ 闪点 ]:
34.1±9.6 °C

[ 精确质量 ]:
402.361023

[ PSA ]:
44.29000

[ LogP ]:
4.86

[ 蒸汽压 ]:
0.0±2.9 mmHg at 25°C

[ 折射率 ]:
1.551

[ 储存条件 ]:
2-8C

黄杨碱; 环维黄杨星D毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: GZ0590030

CHEMICAL NAME :: 9,19-Cyclo-5-alpha,9-beta-pregnan-16-alpha-ol, 4,4,14-trimethyl-3-beta,20-alpha-bis (methylamino)-

CAS REGISTRY NUMBER :: 860-79-7

LAST UPDATED :: 199007

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C26-H46-N2-O

MOLECULAR WEIGHT :: 402.74

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 :: 293 mg/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: 3,101,1982

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 9200 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: 3,101,1982

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 8900 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: 3,101,1982