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CAS No.: 6020-18-4

Coptisine chloride/盐酸黄连碱 Catalog No. CSN18353

Synonyms: Q-100696;NSC-119754;Coptisine (chloride)

Coptisine Chloride is a naturally occuring cytotoxic alkaloid found in Chinese goldthread which shows cytotoxic effect on heptoma and leukemic cells and is reported to block cell cycle progression.

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实验方案

技术信息

生物活性

描述Coptisine chloride is an alkaloid from Chinese goldthread, and acts as an efficient uncompetitive IDO inhibitor with a Ki value of 5.8 μM and an IC50 value of 6.3 μM^[1]. Coptisine (0.1-100 μM) inhibits the proliferation of A549, H460, H2170, MDA-MB-231 and HT-29 cells, with IC50s 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)^[2]. Coptisine shows increased toxicity in mice in a concentration dependent manner, with LD50 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 (high-fat and high-cholesterol diet) diet, and raises the level of cholesterol and TBA (total bile acid) in feces dose-dependently in hamsters. Coptisine (70.05 mg/kg, p.o.) suppresses HMGCR (3-hydroxy-3-methyl-glutaryl-CoA reductase) protein expression level and induces the protein expression of SREBP-2, LDLR(low-density lipoprotein receptor), and CYP7A1 (cholesterol 7α-hydroxylase) involved in cholesterol metabolism^[3].
参考文献

[1] Yu D, Tao BB, Yang YY, Du LS, Yang SS, He XJ, Zhu YW, Yan JK, Yang Q. The IDO inhibitor coptisine ameliorates cognitive impairment in a mouse model of Alzheimer's disease. J Alzheimers Dis. 2015;43(1):291-302.
[2] Rao PC, Begum S, Sahai M, Sriram DS. Coptisine-induced cell cycle arrest at G2/M phase and reactive oxygen species-dependent mitochondria-mediated apoptosis in non-small-cell lung cancer A549 cells. Tumour Biol. 2017 Mar;39(3):1010428317694565
[3] He K, Ye X, Wu H, Wang Y, Zou Z, Ning N, Hu Y, Chen B, Fang X, Li X. The safety and anti-hypercholesterolemic effect of coptisine in Syrian golden hamsters. Lipids. 2015 Feb;50(2):185-94

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8108 mL
- 14.0540 mL
- 28.1079 mL
- 5 mM
- 0.5622 mL
- 2.8108 mL
- 5.6216 mL
- 10 mM
- 0.2811 mL
- 1.4054 mL
- 2.8108 mL

技术信息

CAS号

6020-18-4

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H14ClNO4

运输

蓝冰

分子量

355.77

别名

Q-100696;NSC-119754;Coptisine (chloride);盐酸黄连碱

溶解度

DMSO	4.0 mg/mL (11.2 mM) warming
Water	insoluble

动物实验配方

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