黄连碱
中文名称 | 黄连碱 |
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中文同义词 | 黄连碱(标准品);黃蓮鹼;COPTISINE 黄连碱;黄连碱;黄连碱, 来源于黄连;黄连碱(游离);6,7-二氢-[1,3]二氧戊环并[4',5':7,8]异喹啉并[3,2-A][1,3]二氧戊环并[4,5-G]异喹啉-5-鎓;黄连碱(对照品) |
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(P);Bis[1,3]benzodioxolo[5,6-a:4',5'-g]quinolizinium,6,7-dihydro-;Coptisine, 98%, from Coptis chinensis Franch. |
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;标准品 -中药标准品;Alkaloids;chemical reagent;pharmaceutical intermediate;phytochemical;reference standards from Chinese medicinal herbs (TCM).;standardized herbal extract;化工原料 |
Mol文件 | 3486-66-6.mol |
结构式 |
黄连碱 性质
熔点 | 212-217 °C |
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储存条件 | Store at 2-8°C |
溶解度 | 溶于氯仿、二氯甲烷、乙酸乙酯、DMSO、丙酮等。 |
形态 | 粉末 |
IDO 6.3 μM (IC 50 ) |
IDO 5.8 μM (Ki) |
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).
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.
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。
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-N0430A | Coptisine Sulfate | 1 mg | 304元 | |
2024/08/19 | HY-N0430A | 黄连碱 Coptisine Sulfate | 3486-66-6 | 5mg | 600元 |