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475-83-2

中文名稱 荷葉堿
英文名稱 NUCIFERINE
CAS 475-83-2
分子式 C19H21NO2
分子量 295.38
MOL 文件 475-83-2.mol
更新日期 2024/12/20 18:41:59
475-83-2 結(jié)構(gòu)式 475-83-2 結(jié)構(gòu)式

基本信息

中文別名
何葉堿
荷葉堿
荷葉黃銅
G)喹啉
荷葉堿提取物
荷葉堿[葉]
天然荷葉提取物
荷葉堿(液相2)
荷葉堿(標準品)
荷葉提取物 荷葉堿
英文別名
6a
VLT 049
Nuciferi
nuciferin
NUCIFERINE
Sanjoinine
fettuccine
l-nuciferine
Sanjoinine E
(R)-Nuciferine
所屬類別
生物化工:中草藥成分

物理化學(xué)性質(zhì)

外觀性狀易溶于苯、乙醚、氯仿、鹵代烷烴等極性較低的有機溶劑,在丙酮、乙醇等親水性有機溶劑中也有較好的溶解度,而在水中溶解度較小或幾乎不溶 來源于睡蓮科植物蓮的干燥葉
熔點165.5°C
沸點437.06°C (rough estimate)
密度1.1156 (rough estimate)
折射率1.5000 (estimate)
儲存條件2-8°C
溶解度DMSO : 11.11 mg/mL (37.61 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble)
酸度系數(shù)(pKa)7.87±0.20(Predicted)
形態(tài)粉末
顏色白色至米色
旋光性 (optical activity)[α]/D -145 to -165°, c = 0.5 in ethanol
LogP2.357 (est)

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS06
警示詞危險
危險性描述H301
安全說明24/25
危險品運輸編號UN 1544PSN1 6.1 / PGIII
海關(guān)編碼29389090
毒性LD50 orl-rat: 280 mg/kg AIPTAK 197,261,72

應(yīng)用領(lǐng)域

用途1
清熱解暑,升發(fā)清陽,涼血止血。

常見問題列表

生物堿
荷葉堿是從睡蓮科植物蓮的干燥葉中提取的一種阿樸啡型生物堿,為荷葉中的主要降脂活性成分,以曬干粉碎的荷葉為原料,采用纖維素酶預(yù)處理、稀鹽酸浸提、超聲波輔助提取、氯仿萃取一系列方法提取而成。
中醫(yī)學(xué)認為,荷葉性味苦澀,平,歸肝、脾、胃、心經(jīng)。有清暑利濕、升發(fā)清陽、涼血止血等功效。荷葉的主要化學(xué)成分有荷葉堿、檸檬酸、草酸等,起主要減肥作用的是荷葉堿,藥理研究表明,荷葉具有利尿通便、通腸毒、降脂除油、清暑解熱等作用,能明顯降低血清中甘油三醇和膽固醇含量,具有調(diào)節(jié)血脂的保健作用。采用荷葉減肥不需要刻意節(jié)食,對人體無任何副作用。
生物活性
Nuciferine 是一種 5-HT2A,5-HT2C 和 5-HT2B 拮抗劑,IC50 分別為 478 nM,131 nM 和 1 μM;也是 5-HT7 的反向激動劑,IC50 為 150 nM。
靶點

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 )

體外研究

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.

體內(nèi)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).

圖譜信息

荷葉堿價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-N0049荷葉堿
Nuciferine
475-83-25mg500元
2024/11/08HY-N0049荷葉堿
Nuciferine
475-83-210mM * 1mLin DMSO550元
2024/11/08HY-N0049荷葉堿
Nuciferine
475-83-210mg700元
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