甲基莲心碱结构式
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常用名 | 甲基莲心碱 | 英文名 | Neferine |
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CAS号 | 2292-16-2 | 分子量 | 624.766 | |
密度 | 1.2±0.1 g/cm3 | 沸点 | 710.9±60.0 °C at 760 mmHg | |
分子式 | C38H44N2O6 | 熔点 | N/A | |
MSDS | 中文版 美版 | 闪点 | 383.8±32.9 °C |
甲基莲心碱用途Neferine 是一种双苄基异喹啉类生物碱。Neferine 强效抑制 NF-κB 激活。 |
中文名 | 甲基莲心碱 |
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英文名 | 4-[[(1R)-6,7-dimethoxy-2-methyl-3,4-dihydro-1H-isoquinolin-1-yl]methyl]-2-[[(1R)-6-methoxy-1-[(4-methoxyphenyl)methyl]-2-methyl-3,4-dihydro-1H-isoquinolin-7-yl]oxy]phenol |
中文别名 | 荷花碱 |
英文别名 | 更多 |
描述 | Neferine 是一种双苄基异喹啉类生物碱。Neferine 强效抑制 NF-κB 激活。 |
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相关类别 | |
靶点 |
p65 Autophagy |
体外研究 | Neferine down调节缺氧诱导的NF-κBp65核转位和COX-2表达[1]。 Neferine减少高葡萄糖诱导的胶原蛋白生成并抑制心脏成纤维细胞中TGF-β1-Smad,ERK和p38 MAPK信号传导的激活。在具有不同浓度的Neferine(1,2或5μM)的HG培养基中培养心脏成纤维细胞(CF)。 CCK-8测定在不同时间点(24,48和72小时)进行。与正常葡萄糖(NG)和渗透控制(OC)处理相比,高葡萄糖(30mM)处理以时间依赖性方式显着增加CFs的增殖(P <0.05)。与媒介物处理相比,通过2或5μM的Neferine处理,高葡萄糖(HG)诱导的CF增殖显着减弱。然而,1μM的Neferine不抑制HG诱导的CF增殖。因此,在剩余的实验中使用2和5μM的甲基莲心碱[2]。 |
体内研究 | 低剂量(60 mg/kg /天灌胃)和高剂量(120 mg/kg /天灌胃)的甲基莲心碱治疗可降低高血糖诱导的I,III和TGF-β1蛋白表达增加[2] ]。 |
细胞实验 | 从新生小鼠心室组织分离心脏成纤维细胞(CF)。在无血清培养基中饥饿24小时后,将CFs在含有5.6mM葡萄糖(正常葡萄糖; NG),30mM D-葡萄糖(HG),30mM D-葡萄糖加1μMNeferine,30mM D-的DMEM中孵育。葡萄糖加2μMNeferine,30mM D-葡萄糖加5μMNeferine,和5.6mM葡萄糖加27.5mM甘露糖。在24小时,48小时和72小时收获细胞。用Cell Counting Kit-8(CCK-8)和Cell-LightTM EdU测定[2]测量细胞增殖。 |
动物实验 | 小鼠[2]使用8周龄的C57BL / 6J雄性小鼠。通过腹膜内注射溶解在柠檬酸盐缓冲液(pH4.5)中的链脲佐菌素以60mg / kg体重诱导糖尿。5天。对照小鼠仅注射柠檬酸盐缓冲液。用Accu-Check Active血糖仪检测小鼠尾血中的全血葡萄糖。血糖浓度高于18mM的小鼠被认为是糖尿病动物并用于本研究。将动物随机分成四组,每组八只动物。糖尿病小鼠分为三组:第1组,糖尿病对照组(DM);第2组,以60mg / kg /天的剂量接受甲基莲心碱(DM-NL);和组3,其以120mg / kg /天(DM-NH)的剂量接受Neferine。每天通过胃内灌胃给予Neferine两次,持续12周。通过管饲法向正:虳M对照组施用等量的正常钠。在12周治疗结束时将小鼠麻醉并处死[2]。 |
参考文献 |
[1]. Baskaran R, et al. Neferine prevents NF-κB translocation and protects muscle cells from oxidative stress and apoptosis induced by hypoxia. Biofactors. 2016 Jul 8;42(4):407-17. [2]. Liu X, et al. Neferine inhibits proliferation and collagen synthesis induced by high glucose in cardiac fibroblasts and reduces cardiac fibrosis in diabetic mice. Oncotarget. 2016 Sep 20;7(38):61703-61715. |
密度 | 1.2±0.1 g/cm3 |
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沸点 | 710.9±60.0 °C at 760 mmHg |
分子式 | C38H44N2O6 |
分子量 | 624.766 |
闪点 | 383.8±32.9 °C |
精确质量 | 624.319946 |
PSA | 72.86000 |
LogP | 5.49 |
外观性状 | white to beige |
蒸汽压 | 0.0±2.4 mmHg at 25°C |
折射率 | 1.601 |
储存条件 | 2-8°C |
水溶解性 | DMSO: >15mg/mL |
:β (欧洲) | C |
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危险品运输编码 | NONH for all modes of transport |
RTECS号 | SM9495000 |
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Anti-amnesic activity of neferine with antioxidant and anti-inflammatory capacities, as well as inhibition of ChEs and BACE1.
Life Sci. 87(13-14) , 420-30, (2010) the multifunctional potential of neferine derived from the embryo of Nelumbo nucifera seeds for the age-related neurodegenerative disorders, in vivo anti-amnesic activities and in vitro cholinesterase... |
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Blockade of HERG K+ channel by isoquinoline alkaloid neferine in the stable transfected HEK293 cells.
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Neferine |
4-{[(1R)-6,7-Dimethoxy-2-methyl-1,2,3,4-tetrahydro-1-isoquinolinyl]methyl}-2-{[(1R)-6-methoxy-1-(4-methoxybenzyl)-2-methyl-1,2,3,4-tetrahydro-7-isoquinolinyl]oxy}phenol |
4-{[(1r)-6,7-dimethoxy-2-methyl-1,2,3,4-tetrahydroisoquinolin-1-yl]methyl}-2-{[(1r)-6-methoxy-1-(4-methoxybenzyl)-2-methyl-1,2,3,4-tetrahydroisoquinolin-7-yl]oxy}phenol |
Phenol, 4-[[(1R)-1,2,3,4-tetrahydro-6,7-dimethoxy-2-methyl-1-isoquinolinyl]methyl]-2-[[(1R)-1,2,3,4-tetrahydro-6-methoxy-1-[(4-methoxyphenyl)methyl]-2-methyl-7-isoquinolinyl]oxy]- |
Neferin |
Phenol,4-((1,2,3,4-tetrahydro-6,7-dimethoxy-2-methyl-1-isoquinolinyl)methyl)-2-((1,2,3,4-tetrahydro-6-methoxy-1-((4-methoxyphenyl)methyl)-2-methyl-7-isoquinolinyl)oxy) |