荷叶碱

中文名称:

荷叶碱

中文同义词:

7-四氢-4H-二苯并(DE;G)喹啉;荷叶碱(液相2);NUCIFERINE 荷叶碱;天然荷叶提取物;2-二甲氧基-6-甲基-5;荷叶黄铜;荷叶碱, 来源于荷叶

英文名称:

NUCIFERINE

英文同义词:

(-)-nucipherine;(r)-1,2-dimethoxyaporphine;1,2-dimethoxy-6a-beta-aporphin;6a;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;satis indigotica fort Extract;Lotus Leaf Extract Nuciferin

CAS号:

475-83-2

分子式:

C19H21NO2

分子量:

295.38

EINECS号:

相关类别:

提取物;分析标准品;植物提取物;中药对照品;标准品;对照品,标准品;标准品-中药标准品;对照品;植提标准品;医药原料;中药标准品;植物提取物原料;阿朴啡型生物碱;精细化工;分析对照品;标准品-对照品;其他原料;生物碱;原料;标准品 -中药标准品;天然植物提取物;Miscellaneous Natural Products;chemical reagent;pharmaceutical intermediate;phytochemical;reference standards from Chinese medicinal herbs (TCM).;standardized herbal extract;分析试剂-标准品;标准品，对照品;医药、农药及染料中间体;化工原料;含量产品

Mol文件:

475-83-2.mol

熔点 

165.5°C

沸点 

437.06°C (rough estimate)

密度 

1.1156 (rough estimate)

折射率 

1.5000 (estimate)

储存条件 

2-8°C

形态

powder

酸度系数(pKa)

7.87±0.20(Predicted)

颜色

white to beige

旋光性 (optical activity)

[α]/D -145 to -165°, c = 0.5 in ethanol

生物碱

荷叶碱是从睡莲科植物莲的干燥叶中提取的一种阿朴啡型生物碱，为荷叶中的主要降脂活性成分，以晒干粉碎的荷叶为原料，采用纤维素酶预处理、稀盐酸浸提、超声波辅助提取、氯仿萃取一系列方法提取而成。 中医学认为，荷叶性味苦涩，平，归肝、脾、胃、心经。有清暑利湿、升发清阳、凉血止血等功效。荷叶的主要化学成分有荷叶碱、柠檬酸、草酸等，起主要减肥作用的是荷叶碱，药理研究表明，荷叶具有利尿通便、通肠毒、降脂除油、清暑解热等作用，能明显降低血清中甘油三醇和胆固醇含量，具有调节血脂的保健作用。采用荷叶减肥不需要刻意节食，对人体无任何副作用。

生物活性

Nuciferine 是一种 5-HT2A，5-HT2C 和 5-HT2B 拮抗剂，IC50 分别为 478 nM，131 nM 和 1 μM；也是 5-HT7 的反向激动剂，IC50 为 150 nM。

靶点

5-HT 2C Receptor 131 nM (IC 50 ) 5-HT 7 Receptor 150 nM (IC 50 ) 5-HT 2A Receptor 478 nM (IC 50 ) 5-HT 2B Receptor 1 μM (IC 50 ) 5-HT 6 Receptor 700 nM (EC 50 ) 5-HT 1A Receptor 3.2 μM (EC 50 ) D 2 Receptor 64 nM (EC 50 ) D 4 Receptor 2 μM (EC 50 ) D 5 Receptor 2.6 μM (EC 50 )

5-HT 2C Receptor 131 nM (IC 50 )

5-HT 7 Receptor 150 nM (IC 50 )

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).

化学性质 

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

用途 

用于含量测定/鉴定/药理实验等 药理药效:具有减肥降脂的作用。

用途 

清热解暑，升发清阳，凉血止血。

安全说明 

24/25

危险品运输编号 

UN 1544PSN1 6.1 / PGIII

海关编码 

29389090

毒性

LD50 orl-rat: 280 mg/kg AIPTAK 197,261,72