荷叶碱性质、用途与生产工艺
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。
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。
|
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
)
|
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.
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。
荷叶碱
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