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- CAS号:
- 3486-66-6
- 英文名:
- COPTISINE
- 英文别名:
- Coptisin;COPTISINE;COPTISINE(P);Coptisine Sulfate;2-Benzenedioic acid;COPTISINE USP/EP/BP;Coptisine, 98%, from Coptis chinensis Franch.;6,7-Dihydrobis[1,3]benzodioxolo[5,6-a:4',5'-g]quinolizinium;Bis[1,3]benzodioxolo[5,6-a:4',5'-g]quinolizinium,6,7-dihydro-;5,6-Dihydro-2,3:9,10-bis(methylenedioxy)dibenzo[a,g]quinolizinium
- 中文名:
- 黄连碱
- 中文别名:
- 黄连碱;黃蓮鹼;黄连碱(游离);黄连碱/HPLC;黄连碱(标准品);黄连碱(对照品);黄连碱, 来源于黄连;COPTISINE 黄连碱;标准品对照品】COPTISINE;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
- CBNumber:
- CB7246829
- 分子式:
- C19H14NO4+
- 分子量:
- 320.32
- MOL File:
- 3486-66-6.mol
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黄连碱性质、用途与生产工艺
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。
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IDO
6.3 μM (IC
50
)
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IDO
5.8 μM (Ki)
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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.
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。
黄连碱
上下游产品信息
上游原料
下游产品