Neferine

製品コードS5144 バッチS514402

印刷

化学情報

Synonyms

(R)-1,2-Dimethoxyaporphine

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₃₈H₄₄N₂O₆

分子量

624.77

CAS No.

2292-16-2

Solubility (25°C)*

体外

DMSO

100 mg/mL (160.05 mM)

Ethanol

100 mg/mL (160.05 mM)

Water

˂1 mg/mL

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	5mg/ml (8.00mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.71mg/ml (1.14mM)	Taking the 1 mL working solution as an example, add 50 μL of 14.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	ハスの天然成分であるNeferine ((R)-1,2-Dimethoxyaporphine)は、抗腫瘍効果があります。Neferineは腎臓がん細胞にアポトーシスを誘発します。Neferineは、筋細胞におけるAkt/mTOR経路とNrf2の活性化を介して、オートファジーを抑制します。NeferineはNF-κBの活性化を強く阻害します。Neferineは、抗糖尿病、抗老化、抗微生物、抗血栓、抗不整脈、抗炎症、さらには抗HIVなど、多くの治療効果を持っています。
in vitro	Neferine induces reactive oxygen species mediated caspase-dependent apoptosis in liver and lung cancer cells, reverses the multidrug resistance in human breast cancer cells (MCF-7/ADM), human hepatocarcinoma (HepG2/ADR) and human gastric carcinoma cells (SGC7901/VCR). This compound enhances the cytotoxic potential of cisplatin in A549 cells and augments cisplatin inducecd Sub-G1 accumulation. It inhibits the migration and invasion of human lung cancer cells and lowers the antioxidant enzyme activities. This chemical sensitizes the lung cancer cells to cisplatin and induces apoptosis through G1 cell cycle arrest, upstream ROS production, depletion of cellular antioxidant pool, reduction of mitochondrial membrane potential (ΔΨm) with increased expression of Bax, Bad, Bak, down regulates the expression of Bcl2, release of cytochrome c, cleaved caspase-9, cleaved caspase-3 and PARP.
in vivo	Neferine has an antifibrosis effect on CCl4-induced hepatic fibrosis in mice, possibly partly due to the decreased expression of TGF-β1 in the liver. The plasma concentration-time curves of this compound (10, 20 and 50 mg/kg, i.g.) shows double absorption peaks with the first peak at 10 min and the second peak at 1 h. The t^β_1/2 are 15.6 h, 22.9 h and 35.5 h, for each of these doses, respectively. This compound distributes rapidly into different organ systems, with the highest concentrations found in the liver, followed by the lung, kidney and heart at doses of 10 or 20 mg/kg. At 50 mg/kg dose, concentrations of the kidney and lung are higher than those of others. Moreover, this compound is mainly metabolized in the liver and converted partially by CYP2D6 to liensinine, isoliensinine, desmethyl-liensinine and desmethyl-isoliensinine.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	A549 cells
	濃度	1-30μM
	反応時間	12h, 24h, 48h and 72h
	実験の流れ	The cells are seeded at a density of 1x10⁴ cells/well, and were allowed to attach for overnight in a CO2 incubator. Cells are then treated with different concentrations of cisplatin/neferine and incubated for different time periods (12h, 24h, 48h and 72h). After the treatment period, 20 μl of MTT reagent (5mg/ml) in 100 μl medium is added and incubated at 37°C for 4 h after aspirating the medium with this compound and cisplatin. Then the media with MTT is flicked off, the purple formazan crystals are dissolved in 200 μl of DMSO and the absorbance is recorded with a microquant plate reader at 570 nm.
動物実験	動物モデル	Adult male Kunming mice
	投薬量	5, 10, 20 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/28214344/
https://pubmed.ncbi.nlm.nih.gov/25800905/
https://pubmed.ncbi.nlm.nih.gov/17654697/

https://pubmed.ncbi.nlm.nih.gov/27041079/

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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Lotus Sprout Extract Induces Selective Melanosomal Autophagy and Reduces Pigmentation [ J Cosmet Dermatol, 2024, 10.1111/jocd.16587]	PubMed: 39305105
PGE2 activates EP4 in subchondral bone osteoclasts to regulate osteoarthritis [ Bone Res, 2022, 10(1):27]	PubMed: 35260562
Identification of a group of bisbenzylisoquinoline (BBIQ) compounds as ferroptosis inhibitors [ Cell Death Dis, 2022, 13(11):1000]	PubMed: 36435804
Swine acute diarrhea syndrome coronavirus induces autophagy to promote its replication via the Akt/mTOR pathway [ iScience, 2022, 25(11):105394]	PubMed: 36281226
Neferine induces apoptosis by modulating the ROS‑mediated JNK pathway in esophageal squamous cell carcinoma [ Oncol Rep, 2020, 44(3):1116-1126]	PubMed: 32705225

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。