Neferine
(Synonyms: 甲基莲心碱; (-)-Neferine) 目录号 : GN10103
Neferine (NEF)是一种从传统中药莲子心分离出来的天然双苄基异喹啉生物碱。Neferine具有多种药理特性。
Cas No.:2292-16-2
Sample solution is provided at 25 µL, 10mM.
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Neferine (NEF) is a natural bisbenzylisoquinoline alkaloid separated from the traditional Chinese medicine Nelumbinis plumula. Neferine has a variety of pharmacological properties[1].
In vitro, Neferine (1, 3 and 10μM; 20min) inhibited the expression of cytokines and chemokines in TNF-α/IFN-γ-stimulated human keratinocyte (HaCaT) cells, and Neferine reduced the phosphorylation of MAPK and the NF-κB signaling pathway[2]. Neferine (12.5 or 25μM; 24h) enhanced the AMPK and ACC phosphorylation in OA-stimulated HepG2 cells [3].
In vivo, Neferine significantly alleviated DNCB-induced skin barrier damage, scratching responses, and epidermal hyperplasia in mice. And Neferine significantly decreased transepidermal water loss (TEWL), erythema, blood flow, and ear thickness and increased surface skin hydration[2]. Neferine (5mg/kg/day or 10mg/kg/day; 4 weeks; i.p.) treatment mitigated hepatic lipid deposition, inflammatory cell infiltration as well as hepatic fibrosis[3]. Neferine (20mg/kg; 30 days; i.p.) inhibits tumorigenesis and induces ferroptosis in nude mice[4].
References:
[1] Marthandam Asokan S, Mariappan R, Muthusamy S, Velmurugan BK. Pharmacological benefits of neferine - A comprehensive review. Life Sci. 2018 Apr 15;199:60-70.
[2] Yang CC, Hung YL, Ko WC, Tsai YJ, Chang JF, Liang CW, Chang DC, Hung CF. Effect of Neferine on DNCB-Induced Atopic Dermatitis in HaCaT Cells and BALB/c Mice. Int J Mol Sci. 2021 Jul 30;22(15):8237.
[3] Wang MY, Zhang SS, An MF, Xia YF, Fan MS, Sun ZR, Zhang LJ, Zhao YL, Sheng J, Wang XJ. Neferine ameliorates nonalcoholic steatohepatitis through regulating AMPK pathway. Phytomedicine. 2023 Jun;114:154798.
[4] Li S, Zhang Y, Zhang J, Yu B, Wang W, Jia B, Chang J, Liu J. Neferine Exerts Ferroptosis-Inducing Effect and Antitumor Effect on Thyroid Cancer through Nrf2/HO-1/NQO1 Inhibition. J Oncol. 2022 Jun 27;2022:7933775.
Neferine (NEF)是一种从传统中药莲子心分离出来的天然双苄基异喹啉生物碱。Neferine具有多种药理特性[1]。
在体外，Neferine (1, 3和10μM; 20min)抑制了TNF-α/IFN-γ刺激的人角质形成细胞（HaCaT）中细胞因子和趋化因子的表达，并降低了丝裂原活化蛋白激酶(MAPK)的磷酸化以及核因子κB(NF-κB)信号通路[2]。Neferine (12.5或25μM; 24h)增强了油酸(OA)刺激的HepG2细胞中AMPK和ACC的磷酸化[3]。
在体内，Neferine (3mg/kg和10mg/kg; 15天; 腹腔注射)显著减轻了DNCB诱导的小鼠皮肤屏障损伤、搔抓反应和表皮增生。Neferine显著降低了经表皮失水（TEWL）、红斑、血流和耳厚度，并增加了皮肤表面的水合度[2]。Neferine (5mg/kg/天或10mg/kg/天; 4周; 腹腔注射)治疗减轻了肝脏脂肪沉积、炎性细胞浸润以及肝纤维化[3]。Neferine (20mg/kg; 30天; 腹腔注射)在裸鼠中抑制肿瘤形成并诱导铁死亡[4]。
| Cell experiment [1]: | |
Cell lines | HepG2 cells |
Preparation Method | HepG2 cells were plated on glass coverslips in 12-well plates and treated with OA (0.5mM) for 24h in the absence or presence of Neferine (12.5 or 25µM). The cells were harvested and rinsed twice with phosphate-buffered saline (PBS). The cells were then fixed with 4% paraformaldehyde at room temperature for 20min. The cells were rinsed with PBS 2-3 times at room temperature for 5min and stained with Oil Red O working solution (60% Oil Red O dye and 40% distilled water) at room temperature for 20min. The cells were observed under a light microscope. |
Reaction Conditions | 12.5 or 25µM; 24h |
Applications | Neferine (12.5 or 25μM; 24h) enhanced the AMPK and ACC phosphorylation in OA-stimulated HepG2 cells. |
| Animal experiment [2]: | |
Animal models | 4-week-old BALB/c nude mice |
Preparation Method | Ten nude mice were subcutaneously inoculated with a total of 2 × 10⁶ IHH-4 cells and then randomly divided into two groups: a control group and a Neferine 20mg/kg group. Mice in the Neferine 20mg/kg group were intraperitoneally injected with 20mg/kg Neferine, while those in the control group were given the same amount of dimethyl sulfoxide (DMSO). The tumor volume and mouse body weight were monitored every five days. After 30 days of consecutive monitoring, the mice were euthanized via intraperitoneal injection of sodium pentobarbital (100mg/kg), and the tumor samples were removed, weighed, and stored for subsequent examination. The tumor volume was calculated using the following formula: volume = 1/2 × length × width. |
Dosage form | 20mg/kg; 30 days; i.p. |
Applications | Neferine (20mg/kg; 30 days; i.p.) inhibits tumorigenesis and induces ferroptosis in nude mice. |
References: | |
| Cas No. | 2292-16-2 | SDF | |
| 别名 | 甲基莲心碱; (-)-Neferine | ||
| 化学名 | 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 | ||
| Canonical SMILES | CN1CCC2=CC(=C(C=C2C1CC3=CC=C(C=C3)OC)OC4=C(C=CC(=C4)CC5C6=CC(=C(C=C6CCN5C)OC)OC)O)OC | ||
| 分子式 | C38H44N2O6 | 分子量 | 624.77 |
| 溶解度 | DMSO : 125 mg/mL (200.07 mM; Need ultrasonic) | 储存条件 | 4°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 | 1.6006 mL | 8.0029 mL | 16.0059 mL |
| 5 mM | 0.3201 mL | 1.6006 mL | 3.2012 mL |
| 10 mM | 0.1601 mL | 0.8003 mL | 1.6006 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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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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