中文名 | 荷叶碱 |
英文名 | Nuciferine |
别名 | 荷叶碱 荷叶黄铜 G)喹啉 天然荷叶提取物 荷叶碱(液相2) 荷叶碱, 来源于荷叶 2-二甲氧基-6-甲基-5 NUCIFERINE 荷叶碱 7-四氢-4H-二苯并(DE 1,2-二甲氧基-6-甲基-5,6,6a,7-四氢-4H-二苯并[de,g]喹啉 |
英文别名 | 6a Nuciferin Nuciferine (-)-nucipherine (r)-1,2-dimethoxyaporphine Lotus Leaf Extract Nuciferin satis indigotica fort Extract 1,2-dimethoxy-6a-beta-aporphin 1,2-Dimethoxy-6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline (6aR)-1,2-dimethoxy-6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline 4H-Dibenzo[de,g]quinoline,5,6,6a,7-tetrahydro-1,2-diMethoxy-6-Methyl-, (6aR)- Nuciferine 1,2-Dimethoxy-6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline |
CAS | 475-83-2 |
化学式 | C19H21NO2 |
分子量 | 295.38 |
InChI | InChI=1/C19H21NO2/c1-20-9-8-13-11-16(21-2)19(22-3)18-14-7-5-4-6-12(14)10-15(20)17(13)18/h4-7,11,15H,8-10H2,1-3H3 |
密度 | 1.1156 (rough estimate) |
熔点 | 165.5°C |
沸点 | 437.06°C (rough estimate) |
比旋光度 | (c, 1 in EtOH)-164 |
闪点 | 151.9°C |
蒸汽压 | 1.27E-07mmHg at 25°C |
溶解度 | 易溶于苯、乙醚、氯仿、卤代烷烃等极性较低的有机溶剂,在丙酮、乙醇等亲水性有机溶剂中也有较好的溶解度,而在水中溶解度较小或几乎不溶 |
折射率 | 1.5000 (estimate) |
酸度系数 | 7.87±0.20(Predicted) |
存储条件 | 2-8°C |
外观 | 粉末 |
颜色 | white to beige |
物化性质 | 易溶于苯、乙醚、氯仿、卤代烷烃等极性较低的有机溶剂,在丙酮、乙醇等亲水性有机溶剂中也有较好的溶解度,而在水中溶解度较小或几乎不溶 来源于睡莲科植物莲的干燥叶 |
MDL号 | MFCD01664592 |
体外研究 | Nuciferine is a partial agonist at DD 2 receptor with an activity (E max =67% of dopamine) similar to aripiprazole (E max =50% of dopamine). In line with its partial agonist activity, Nuciferine inhibited dopamine-induced activation of G i with a potency similar to clozapine (Nuciferine K B =62 nM; Clozapine K B =20 nM) as determined via Schild regression analysis. The natural product Nuciferine acts as an effective inhibitor of adult worm motility. Nuciferine is effective at inhibiting both basal and 5-HT evoked motility of adult schistosomes. Nuciferine inhibits Sm.5HTR L and schistosomule with 0.24±0.04 and 0.62±0.22 μM, respectively. |
体内研究 | In rodent models relevant to antipsychotic drug action, Nuciferine blocks head-twitch responses and discriminative stimulus effects of a 5-HT 2A agonist, substituted for clozapine discriminative stimulus, enhanced amphetamine induced locomotor activity, inhibited phencyclidine (PCP)-induced locomotor activity, and rescued PCP-induced disruption of prepulse inhibition without induction of catalepsy. In the presence of 1 or 3 mg/kg Nuciferine, cumulative PCP doses produce similar substitution to PCP alone. In the clozapine-trained animals, a dose-dependent substitution for 1.25 mg/kg clozapine is seen at 10 mg/kg Nuciferine (80.63% drug lever responding), with an ED 50 value of 5.42 mg/kg (95% CI 3.09-9.48 mg/kg) while the lower doses tested (0.1 mg/kg-3 mg/kg) fails to produce substitution for clozapine’s discriminative cue. In addition to a high percentage of responding on the clozapine-appropriate lever, 10 mg/kg Nuciferine also produces significant rate suppression as compared to vehicle control points (p<0.001). |
安全术语 | 24/25 - 避免与皮肤和眼睛接触。 |
危险品运输编号 | UN 1544PSN1 6.1 / PGIII |
海关编号 | 29389090 |
参考资料 展开查看 | 1. 梦杰 刘苏珍 周斌 崔小弟 陈振华.HPLC法同时测定荷叶中的荷叶碱、芦丁、槲皮素[J].中成药 2016 38(01):111-114. 2. 李梦杰 刘苏珍 周斌 等. RP-HPLC法同时测定荷叶颗粒中3种有效成分的含量[J]. 中国药房 2016(18期):2532-2534. 3. 吴鹏,李慧芬,张学兰,崔伟亮,王均秀.炒炭对荷叶主要化学成分转化机制的研究[J].中成药,2015,37(08):1767-1770. 4. 侯成波, 董月柳, 尹秀文,等. 荷叶多成分整体的肠渗透性研究[J]. 中国中药杂志, 2016, 41(07):1183-1187. 5. 李帆. 荷叶碱在青霉菌培养基中抑菌效果的研究[J]. 生物化工, 2018, 4(06):99-101. 6. 尹秀文, 侯成波, 陈江鹏,等. 采用在体单向肠灌流模型研究荷叶多成分整体的肠渗透性[J]. 中国中药杂志, 2017, 42(008):1525-1531. 7. 陈强,张华,沙玫,刘永静.一测多评法同时测定荷叶中4种生物碱含量[J].福建中医药,2020,51(06):29-32. 8. 郑艳艳,李莉,袁晓庆,孔方,刘言娟.响应面法优化蜗牛酶辅助超声提取荷叶总生物碱的工艺研究[J].安徽农业科学,2020,48(21):183-187. 9. Fugang Wang, Juan Cao, Xueqin Hou, Zhiyong Li & Xiaolan Qu (2018) Pharmacokinetics, tissue distribution, bioavailability, and excretion of nuciferine, an alkaloid from lotus, in rats by LC/MS/MS, Drug Development and Industrial Pharmacy, 44:9, 1557-1562, D 10. Chen, X., Zheng, X., Zhang, M. et al. Nuciferine alleviates LPS-induced mastitis in mice via suppressing the TLR4-NF-κB signaling pathway. Inflamm. Res. 67, 903–911 (2018). https://doi.org/10.1007/s00011-018-1183-2 11. Zhang, Lei, et al. "Direct coupling of thin-layer chromatography-bioautography with electrostatic field induced spray ionization-mass spectrometry for separation and identification of lipase inhibitors in lotus leaves." Analytica chimica acta 967 (2017): 5 12. Zhang, Lei, et al. "Direct coupling of thin-layer chromatography-bioautography with electrostatic field induced spray ionization-mass spectrometry for separation and identification of lipase inhibitors in lotus leaves." Analytica chimica acta 967 (2017): 5 13. [IF=6.558] Lei Zhang et al."Direct coupling of thin-layer chromatography-bioautography with electrostatic field induced spray ionization-mass spectrometry for separation and identification of lipase inhibitors in lotus leaves."Anal Chim Acta. 2017 May;967:52 14. [IF=5.279] Xianbao Deng et al."Analysis of Isoquinoline Alkaloid Composition and Wound-Induced Variation in Nelumbo Using HPLC-MS/MS."J Agr Food Chem. 2016;64(5):1130–1136 15. [IF=3.512] Thitirat Meelaph et al."Coregulation of Biosynthetic Genes and Transcription Factors for Aporphine-Type Alkaloid Production in Wounded Lotus Provides Insight into the Biosynthetic Pathway of Nuciferine."Acs Omega. 2018;3(8):8794–8802 16. [IF=3.225] Fugang Wang et al."Pharmacokinetics, tissue distribution, bioavailability, and excretion of nuciferine, an alkaloid from lotus, in rats by LC/MS/MS."Drug Dev Ind Pharm. 2018;44(9):1557-1562 17. [IF=3.174] Chen Xingxing et al."Nuciferine alleviates LPS-induced mastitis in mice via suppressing the TLR4-NF-κB signaling pathway."Inflamm Res. 2018 Dec;67(11):903-911 18. [IF=3] Zhang Pengyu et al."Discovery of novel antagonists on β2-adrenoceptor from natural products using a label-free cell phenotypic assay."N-S Arch Pharmacol. 2018 Dec;391(12):1411-1420 19. [IF=5.396] Zhen Shi et al."Nuciferine improves high-fat diet-induced obesity via reducing intestinal permeability by increasing autophagy and remodeling the gut microbiota."Food Funct. 2021 Jul;12(13):5850-5861 20. [IF=4.451] Haiyan Wen et al."Nuciferine attenuates the progression of osteoarthritis by targeting PI3K/Akt/NF-κB signaling pathway."J Funct Foods. 2021 Nov;86:104682 21. [IF=3.935] Peiliang Zhang et al."TLC-electrostatic field induced spray ionization-MS analysis of diverse structural skeletons and its coupling with TLC bioautography for characterization of lipase inhibitory components in American ginseng."J Pharmaceut Biomed. 2019 22. [IF=3.373] Na Zhang et al."TLC–MS identification of alkaloids in Leonuri Herba and Leonuri Fructus aided by a newly developed universal derivatisation reagent optimised by the response surface method."Phytochem Analysis. 2021 May;32(3):242-251 23. [IF=7.514] YueTong Yu et al."Identification and Quantification of Oligomeric Proanthocyanidins, Alkaloids, and Flavonoids in Lotus Seeds: A Potentially Rich Source of Bioactive Compounds."Food Chem. 2022 Jan;:132124 24. [IF=1.902] Yongjing Liu et al."Evaluation of Green and Efficient deep eutectic solvents as media for extracting Alkaloids from Lotus Leaf."Biomedical Chromatography. 2021 Dec 06 25. [IF=11.413] Xiliang Du et al."Nuciferine protects against high-fat diet-induced hepatic steatosis and insulin resistance via activating TFEB-mediated autophagy–lysosomal pathway."Acta Pharm Sin B. 2021 Dec;: 26. [IF=3.394] Chang Chen et al."Protective Effects of Nuciferine in Middle Cerebral Artery Occlusion Rats Based on Transcriptomics."Brain Sciences. 2022 May;12(5):572 27. [IF=7.491] Yeqing Ruan et al."Processing tactics for low-cost production of pure nuciferine from lotus leaf."ULTRASONICS SONOCHEMISTRY. 2022 May;86:106026 |
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