黄连碱

中文名称:

黄连碱

中文同义词:

硫酸黄连碱;黄连碱(标准品);黃蓮鹼;COPTISINE 黄连碱;黄连碱, 来源于黄连;黄连碱

英文名称:

COPTISINE

英文同义词:

COPTISINE;Coptisin;5,6-Dihydro-2,3:9,10-bis(methylenedioxy)dibenzo[a,g]quinolizinium;6,7-Dihydrobis[1,3]benzodioxolo[5,6-a:4,5-g]quinolizinium;Coptisine Sulfate;Coptisine, 98%, from Coptis chinensis Franch.;COPTISINE(P);Bis[1,3]benzodioxolo[5,6-a:4,5-g]quinolizinium,6,7-dihydro-

CAS号:

3486-66-6

分子式:

C19H14NO4+

分子量:

320.32

EINECS号:

相关类别:

中草药成分;对照品;植提标准品;中药对照品;标准品;分析标准品;植物提取物;Alkaloids;chemical reagent;pharmaceutical intermediate;phytochemical;reference standards from Chinese medicinal herbs (TCM).;standardized herbal extract;标准品 -中药标准品;化工原料

Mol文件:

3486-66-6.mol

熔点 

212-217 °C

生物活性

Coptisine 是从黄连中分离到的生物碱，是一种有效的非竞争性的 IDO 抑制剂，Ki 值为 5.8 μM，IC50 值为 6.3 μM。

靶点

IDO 6.3 μM (IC 50 ) IDO 5.8 μM (Ki)

IDO 6.3 μM (IC 50 )

IDO 5.8 μM (Ki)

体外研究

Coptisine is an efficient uncompetitive IDO inhibitor with a K i value of 5.8 μM and an IC 50 value of 6.3 μM. Coptisine (0.1-100 μM) inhibits the proliferation of A549, H460, H2170, MDA-MB-231 and HT-29 cells, with IC 50 s of 18.09, 29.50, 21.60, 20.15 and 26.60 µM, respectively. Coptisine (12.5, 25, 50 μM) upregulates the expression of pH2AX and p21, reduces expression of cyclin B1, cdc2, and cdc25C, and induces G2/M arrest and apoptosis of A549 cells in a concentration-dependent manner. Coptisine (12.5, 25, 50 μM) also induces mitochondrial dysfunction and activates caspases activities in A549 cells. Furthermore, Coptisine (50 μM) increases ROS levels in a time-dependent manner (0.5, 1, 2, 4, 12, and 24 h).

体内研究

Coptisine shows increased toxicity in mice in a concentration dependent manner, with LD 50 value of 880.18 mg/kg. Coptisine (154 mg/kg/day, 90 days) shows no toxicity on SD rats. Coptisine (23.35, 46.7, 70.05 mg/kg, p.o.) dose-dependently decreases the levels of TC, TG, and LDL-c and increases HDL-c content in serum of hamsters to different degree, slows down weight gain induced by the HFHC diet, and raises the level of cholesterol and TBA in feces dose-dependently in hamsters. Coptisine (70.05 mg/kg, p.o.) suppresses HMGCR protein expression level and induces the protein expression of SREBP-2, LDLR, and CYP7A1 involved in cholesterol metabolism.

化学性质 

极略微溶于水, 微溶于乙醇, 溶于碱。 来源于罂粟科植物白屈菜根

用途 

用于含量测定/鉴定/药理实验等。 药理药效:有抗微生物活性, 其抗卡尔酵母菌的效力比小檗碱、巴马汀及非洲防己碱都强；杀虫活性；诱导神经细胞分化；对胃粘膜有保护作用；抗癌作用；免疫系统的作用；平滑肌松弛作用；抗肾炎作用。