COPTISINE(P)
黄连碱(Coptisine)
CAS: 3486-66-6
化学式: C19H14NO4+
| 中文名 | 黄连碱 |
| 英文名 | Coptisine |
| 别名 | 黄连碱 黃蓮鹼 黄连碱(游离) 黄连碱(标准品) 黄连碱, 来源于黄连 COPTISINE 黄连碱 |
| 英文别名 | YHL II Coptisin Coptisine COPTISINE COPTISINE(P) Coptisine Sulfate Alkaloid A, fromCoptis groenlandica |
| CAS | 3486-66-6 |
| 化学式 | C19H14NO4+ |
| 分子量 | 320.32 |
| 密度 | g/cm3 |
| 熔点 | 212-217 °C |
| 沸点 | °Cat760mmHg |
| 闪点 | °C |
| 溶解度 | 极微溶微溶于水, 微溶于乙醇, 溶于碱 |
| 存储条件 | 2-8℃ |
| 外观 | 浅黄色针状结晶 (乙醇) |
| 物化性质 | 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 |
| MDL号 | MFCD03792689 |
| 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. |
| 参考资料 展开查看 | 1. 王永占 沈勇 史晓倩 韩玙 杨生超 梁艳丽 谢世清.HPLC法同时测定云黄连中四种生物碱的含量[J].中国药师 2013 16(07):947-949. 2. 尚婵 李孟璇 李海波 何亮伟 孟兆青 黄文哲 王振中 丁岗 杨中林 萧伟.LC-MS/MS同时测定痛安注射液中13个成分的含量[J].中国中药杂志 2017 42(10):1901-1907. 3. 李文芳 王晓明 潘桂湘 等. LC-MS/MS测定养血清脑颗粒中15个生物碱成分的含量[J]. 辽宁中医杂志 2017(10):134-136+229. 4. 柳鑫,杨艳芳,宋红萍,张小波,黄璐琦,吴和珍.基于MaxEnt和ArcGIS的黄连生长适宜性区划研究[J].中国中药杂志,2016,41(17):3186-3193. 5. 房康, 吴高荣, 王辉,等. 黄连解毒汤自沉淀化学成分及其抗PC12细胞损伤研究[J]. 中草药, 2017(18). 6. 曹一佳 曲玉霞 孙雨 等. UPLC-MS/MS法同时测定砂连和胃胶囊中10种化合物含量[J]. 国际药学研究杂志 2020 v.47(01):76-81. 7. 李听弦, 李蒙, 张志,等. 基于高效液相色谱指纹图谱及红外光谱评价黄连及其炮制品质量差异[J]. 中南药学, 2019, 017(004):556-560. 8. 皮文霞 朱鑫仙 方婷 等. HPLC同时测定"三热论"方各纯化部位中药根碱、表小檗碱、黄连碱、巴马汀和小檗碱的含量[J]. 中国实验方剂学杂志 2012 18(14):110-113. 9. 米佳, 贺文达, 梁心怡,等. 黄连肉桂药对指纹图谱的聚类分析及多指标的定量分析[J]. 时珍国医国药, 2019, 30(01):83-86. 10. 赵露, 江健梅, 孟琦,等. 白屈菜生育期内生物碱含量的变化规律[J]. 吉林农业大学学报, 2017(5):590-595. 11. 张潇, 张亚丽, 苗祥贞,等. 黄连不同炮制品及组分的抗肿瘤活性与6种生物碱含量相关性研究[J]. 中华中医药杂志, 2019, v.34(06):350-353. 12. 李听弦 李蒙 张志 等. 一测多评法测定不同味连饮片中6个生物碱类成分的含量[J]. 药物分析杂志 2018 038(007):1132-1138. 13. 王盼,储全根,轩云,蔡正银.抵当陷胸汤HPLC-MS指纹图谱研究[J].时珍国医国药,2020,31(12):2937-2940. 14. 纪万里,周泽华,王婷婷,安叡,梁琨,王新宏.基于UPLC-LTQ-Orbitrap-MS方法分析半夏泻心汤化学成分[J].药物分析杂志,2020,40(10):1736-1750. 15. 康念欣,袁炎炎,张潇,路颖慧,李晴霞,李飞,谭鹏.酒黄连HPLC特征图谱的建立及聚类分析和主成分分析[J].世界科学技术-中医药现代化,2020,22(08):2790-2798. 16. Zhu, Ling, et al. "Coptis chinensis inflorescence extract protection against ultraviolet-B-induced phototoxicity, and HPLC–MS analysis of its chemical composition." Food and chemical toxicology 50.7 (2012): 2584-2588.http://doi.org/10.1016/j.fct.2012.04.0 17. Yang, Yanfang, et al. "Determination of alkaloid contents in various tissues of Coptis chinensis Franch. by reversed phase-high performance liquid chromatography and ultraviolet spectrophotometry." Journal of chromatographic science 55.5 (2017): 556-563. h 18. Liang, Jie, et al. "Expression and functional activity of bitter taste receptors in primary renal tubular epithelial cells and M-1 cells." Molecular and cellular biochemistry 428.1-2 (2017): 193-202.http://doi.org/10.1007/s11010-016-2929-1 19. Ma, Bingxin, et al. "Coptis chinensis inflorescence ameliorates hyperglycaemia in 3T3-L1 preadipocyte and streptozotocin-induced diabetic mice." Journal of Functional Foods 21 (2016): 455-462.http://doi.org/10.1016/j.jff.2015.12.021 20. Yue, Xiao, et al. "Berberine activates bitter taste responses of enteroendocrine STC-1 cells." Molecular and cellular biochemistry 447.1 (2018): 21-32.http://doi.org/10.1007/s11010-018-3290-3 21. Chen, Meng, et al. "Comprehensive analysis of Huanglian Jiedu decoction: Revealing the presence of a self-assembled phytochemical complex in its naturally-occurring precipitate." Journal of Pharmaceutical and Biomedical Analysis 195 (2021): 113820.http:// 22. [IF=6.023] Ling Zhu et al."Coptis chinensis inflorescence extract protection against ultraviolet-B-induced phototoxicity, and HPLC–MS analysis of its chemical composition."Food Chem Toxicol. 2012 Jul;50:2584 23. [IF=4.759] Lvhuan Wang et al."Online screening of acetylcholinesterase inhibitors in natural products using monolith-based immobilized capillary enzyme reactors combined with liquid chromatography-mass spectrometry."J Chromatogr A. 2018 Aug;1563:135 24. [IF=3.935] Ka-Yan Kwok et al."Quality evaluation of commercial Huang-Lian-Jie-Du-Tang based on simultaneous determination of fourteen major chemical constituents using high performance liquid chromatography."J Pharmaceut Biomed. 2013 Nov;85:239 25. [IF=3.396] Liang Jie et al."Expression and functional activity of bitter taste receptors in primary renal tubular epithelial cells and M-1 cells."Mol Cell Biochem. 2017 Apr;428(1):193-202 26. [IF=3.197] Bingxin Ma et al."Coptis chinensis inflorescence ameliorates hyperglycaemia in 3T3-L1 preadipocyte and streptozotocin-induced diabetic mice."J Funct Foods. 2016 Mar;21:455 27. [IF=2.795] Yue Xiao et al."Berberine activates bitter taste responses of enteroendocrine STC-1 cells."Mol Cell Biochem. 2018 Oct;447(1):21-32 28. [IF=1.618] Li Jiang-Yan et al."Seasonal Variation of Alkaloid Contents and Anti-Inflammatory Activity of Rhizoma coptidis Based on Fingerprints Combined with Chemometrics Methods."J Chromatogr Sci. 2015 Aug;53(7):1131-1139 29. [IF=1.618] Yang Yanfang et al."Determination of Alkaloid Contents in Various Tissues of Coptis Chinensis Franch. by Reversed Phase-High Performance Liquid Chromatography and Ultraviolet Spectrophotometry."J Chromatogr Sci. 2017 May;55(5):556-563 30. [IF=6.4] Jing Zhao et al."Natural Nano-Drug Delivery System in Coptidis Rhizoma Extract with Modified Berberine Hydrochloride Pharmacokinetics."Int J Nanomed. 2021; 16: 6297–6311 31. [IF=6.023] Maiquan Li et al."Discovery of Keap1−Nrf2 small−molecule inhibitors from phytochemicals based on molecular docking."Food Chem Toxicol. 2019 Nov;133:110758 32. [IF=5.81] Zhao Jing et al."Intra-Herb Interactions: Primary Metabolites in Coptidis Rhizoma Extract Improved the Pharmacokinetics of Oral Berberine Hydrochloride in Mice."Front Pharmacol. 2021 Jun;0:1426 33. [IF=4.845] Xiaohong Zhang et al."Laboratory bioassay, greenhouse experiment and 3D-QSAR studies on berberine analogues: a search for new herbicides based on natural products."Pest Manag Sci. 2021 Apr;77(4):2054-2067 34. [IF=3.963] Zhong-min Zhao et al."Anti-phytopathogenic activity and the possible mechanisms of action of isoquinoline alkaloid sanguinarine."Pestic Biochem Phys. 2019 Sep;159:51 35. [IF=3.935] Yang Song et al."Pharmacokinetics, tissue distribution and plasma protein binding rate of palmatine following intragastric and intravenous administration in rats using liquid chromatography tandem mass spectrometry."J Pharmaceut Biomed. 2021 Sep;203:11422 36. [IF=3.935] Meng Chen et al."Comprehensive analysis of Huanglian Jiedu decoction: Revealing the presence of a self-assembled phytochemical complex in its naturally-occurring precipitate."J Pharmaceut Biomed. 2021 Feb;195:113820 37. [IF=3.463] Xiao-Meng Liu et al."Comparative transcriptome analysis provides novel insights into the molecular mechanism of berberine biosynthesis in Coptis chinensis."Sci Hortic-Amsterdam. 2022 Jan;291:110585 38. [IF=3.004] Kai Zhang et al."Untargeted metabolomics reveals the synergistic mechanisms of Yuanhu Zhitong oral liquid in the treatment of primary dysmenorrhea."J Chromatogr B. 2021 Feb;1165:122523 39. [IF=1.345] Ya-Li Zhang et al."Coptisine suppresses proliferation and inhibits metastasis in human pancreatic cancer PANC-1 cells."J Asian Nat Prod Res. 2020;22(5):452-463 |
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产品名: Coptisine黄连碱 去供应商网站查看 询盘CAS: 3486-66-6
产地: 北京
包装: 盒
规格: IC0530-5mg,5mg,IC0530-10mg,10mg
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库存: 现询
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产品描述: 产品覆盖：小分子化合物、分析对照品、染色试剂、生化试剂盒、细胞生物学、分子生物学、抗体、蛋白、多肽、ELISA试剂盒、微生物培养、化学合成、仪器耗材、CRO技术 更多
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产品名: 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 询盘CAS: 3486-66-6
产地: 上海
包装: 100mg；10mg；250mg；25mg；50mg
规格: 98%
价格: 电话、微信、QQ、邮件
库存: 现货
电话: 400-968-2212
手机: 18916960931
电子邮件: 3623107365@qq.com
QQ: 3623107365
微信: 18916960931
产品描述: 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,98%,Amole/阿摩尔
提供多种规格现货供应
产品名: Coptisine黄连碱 去供应商网站查看 询盘CAS: 3486-66-6
产地: 北京
包装: 盒
规格: IC0530-5mg,5mg,IC0530-10mg,10mg
价格: 电话、微信、QQ、邮件
库存: 现询
电话: 010-50973130
手机: 18101056239(微信同号)
电子邮件: 3193328036@qq.com
QQ: 3193328036
微信: 18101056239
产品描述: 产品覆盖：小分子化合物、分析对照品、染色试剂、生化试剂盒、细胞生物学、分子生物学、抗体、蛋白、多肽、ELISA试剂盒、微生物培养、化学合成、仪器耗材、CRO技术 更多
现货供应
产品名: 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 询盘CAS: 3486-66-6
产地: 上海
包装: 100mg；10mg；250mg；25mg；50mg
规格: 98%
价格: 电话、微信、QQ、邮件
库存: 现货
电话: 400-968-2212
手机: 18916960931
电子邮件: 3623107365@qq.com
QQ: 3623107365
微信: 18916960931
产品描述: 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,98%,Amole/阿摩尔
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