Nuciferine
(Synonyms: 荷叶碱) 目录号 : GN10607
Nuciferine是从荷叶中提取的主要生物活性成分，可作为5-HT2A、5-HT2C和5-HT2B受体拮抗剂，IC50值分别为0.478μM、0.131μM和1μM。
Cas No.:475-83-2
Sample solution is provided at 25 µL, 10mM.
Nuciferine, a main bioactive component obtained from the lotus leaf, is an antagonist at 5-HT2A, 5-HT2C, and 5-HT2B receptors, with the IC50 values of 0.478μM, 0.131μM, and 1μM, respectively[1]. Nuciferine can reduce blood lipids by inhibiting cholesterol synthesis and cholesterol esterase activity, and increasing the expression of low-density lipoprotein receptor[2]. Nuciferine has been widely used to reduce serum uric acid levels, improve renal function, and as a key anti-inflammatory compound in mouse models of hyperuricemia[3].
In vitro, Nuciferine treatment for 72 hours significantly inhibited the proliferation of HepG2 cells and HCCLM3 cells, with IC50 values of 67.97μM and 61.88μM, respectively[4]. Treatment of 3T3-L1 preadipocytes with 20μM Nuciferine for 72 hours significantly inhibited cell proliferation, reduced intracellular lipid accumulation, decreased triglyceride content, and down-regulated the expression of lipid metabolism-related genes[5]. Treatment of chondrocytes with 25μM Nuciferine for 24h significantly reduced IL-1β-induced iNOS, PEG2 and IL-6 levels in mouse chondrocytes, significantly reduced IL-1β-induced degradation of extracellular matrix, without affecting cell viability[6].
In vivo, Nuciferine treatment (400mg/kg/day) via oral administration for 42 days resulted in a significant reduction in both plasma and hepatic triglyceride concentrations and a significant increase in hepatic glycogen content in male broiler chickens[7]. Intraperitoneal injection of Nuciferine (20mg/kg) every 2 days for 2 weeks significantly suppressed the volume and weight of the suppressed tumor in the xenograft tumor mouse models[8].
References:
[1] Farrell M S, McCorvy J D, Huang X P, et al. In vitro and in vivo characterization of the alkaloid nuciferine[J]. PLoS One, 2016, 11(3): e0150602.
[2] Huang X, Hao N, Chen G, et al. Chemistry and biology of nuciferine[J]. Industrial Crops and Products, 2022, 179: 114694.
[3] Wang M X, Liu Y L, Yang Y, et al. Nuciferine restores potassium oxonate-induced hyperuricemia and kidney inflammation in mice[J]. European Journal of Pharmacology, 2015, 747: 59-70.
[4] Li T, Wang W, Zhu M, et al. The antineoplastic effects of nuciferine on hepatocellular carcinoma are associated with suppression of the HER2-AKT/ERK1/2 signaling pathway[J]. Discover Oncology, 2025, 16(1): 822.
[5] Xu H, Wang L, Yan K, et al. Nuciferine inhibited the differentiation and lipid accumulation of 3T3-L1 preadipocytes by regulating the expression of lipogenic genes and adipokines[J]. Frontiers in Pharmacology, 2021, 12: 632236.
[6] Peng M, Shen G, Tu Q, et al. Nuciferine ameliorates osteoarthritis: An in vitro and in vivo study[J]. International Immunopharmacology, 2024, 142: 113098.
[7] Zhou Y, Chen Z, Lin Q, et al. Nuciferine reduced fat deposition by controlling triglyceride and cholesterol concentration in broiler chickens[J]. Poultry Science, 2020, 99(12): 7101-7108.
[8] Xie J R, Chen X J, Zhou G. Nuciferine inhibits oral squamous cell carcinoma partially through suppressing the STAT3 signaling pathway[J]. International Journal of Molecular Sciences, 2023, 24(19): 14532.
Nuciferine是从荷叶中提取的主要生物活性成分，可作为5-HT2A、5-HT2C和5-HT2B受体拮抗剂，IC50值分别为0.478μM、0.131μM和1μM[1]。Nuciferine通过抑制胆固醇合成和胆固醇酯酶活性，并增加低密度脂蛋白受体表达来降低血脂[2]。Nuciferine广泛用于高尿酸血症小鼠模型中以降低血清尿酸水平、改善肾功能，并作为关键抗炎化合物[3]。
在体外，Nuciferine处理72小时可显著抑制HepG2和HCCLM3细胞增殖，IC50值分别为67.97μM和61.88μM[4]。20μM的Nuciferine处理3T3-L1前脂肪细胞72小时能显著抑制细胞增殖、减少细胞内脂质积累、降低甘油三酯含量，并下调脂代谢相关基因表达[5]。25μM的Nuciferine处理小鼠软骨细胞24小时可显著降低IL-1β诱导的iNOS、PEG2和IL-6水平，显著抑制IL-1β诱导的细胞外基质降解，不影响细胞活力[6]。
在体内，雄性肉鸡经口服Nuciferine（400mg/kg/day，持续42天）后，血浆和肝脏甘油三酯浓度显著降低，肝糖原含量显著增加[7]。异种移植瘤小鼠模型经腹腔注射Nuciferine（20mg/kg，每2天一次，持续2周）后，肿瘤体积和肿瘤重量均被显著抑制[8]。
| Cell experiment [1]: | |
Cell lines | HepG2 cells |
Preparation Method | HepG2 cells were cultured in a complete medium consisting of DMEM, fetal bovine serum (10%), and penicillin/streptomycin (1%) in an incubator with standard temperature (37 °C), humidity, and carbon dioxide content (5%). HepG2 cells were cultured in 96-well plates at a density of 6×103 cells/well and then incubated for 24h to allow adherence. After treatment of HepG2 cells with PBS solution (negative control), 5-fluorouracil (positive control), or Nuciferine at specific concentrations (0, 25, 50, 100, and 200μM) for 72h, the viability of HepG2 cells was assessed by the addition of MTT reagent (20µL/ well) and incubation (4h). For relative quantitative analysis, the medium containing MTT was aspirated, and the formazan formed in the cells was dissolved in 150µL DMSO. Finally, optical density values at 490nm were obtained using a microplate reader. |
Reaction Conditions | 0, 25, 50, 100, and 200μM; 72h |
Applications | Nuciferine significantly inhibited the proliferation of HepG2 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | BALB/c nude mice |
Preparation Method | Five-week-old female BALB/c nude mice were used to establish the xenograft tumor model, and 5 ×107 CAL27 cells were implanted subcutaneously into 6 nude mice in each group. After 10 days, Nuciferine (20mg/kg; dissolved in a solution containing 2% DMSO, 40% PEG400, 5% Tween-80, and 53% saline) and colivelin (1mg/kg; dissolved in saline) were administered intraperitoneally every 2 days. After 14 days of drug administration, mice were euthanized using an overdose of anesthetic and subsequently photographed. The length (L) and width (W) of the tumor were measured using a vernier caliper, and the tumor volume (V) was calculated according to the formula V = L × W2 × 0.5. |
Dosage form | 20mg/kg; every 2 days for 14 days; i.p. |
Applications | Nuciferine treatment significantly suppressed tumor volume and weight in the xenograft tumor mouse models. |
References: | |
| Cas No. | 475-83-2 | SDF | |
| 别名 | 荷叶碱 | ||
| 化学名 | (6aR)-1,2-dimethoxy-6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline | ||
| Canonical SMILES | CN1CCC2=CC(=C(C3=C2C1CC4=CC=CC=C43)OC)OC | ||
| 分子式 | C19H21NO2 | 分子量 | 295.38 |
| 溶解度 | ≥ 14.75mg/mL in DMSO with gentle warming | 储存条件 | Store at -20°C,protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.3855 mL | 16.9273 mL | 33.8547 mL |
| 5 mM | 0.6771 mL | 3.3855 mL | 6.7709 mL |
| 10 mM | 0.3385 mL | 1.6927 mL | 3.3855 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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