Betulin

製品コードS4754 バッチS475403

印刷

化学情報

Synonyms

betulinol, betuline, betulinic alcohol

Storage
(From the date of receipt)

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

化学式

C₃₀H₅₀O₂

分子量

442.72

CAS No.

473-98-3

Solubility (25°C)*

体外

DMSO (warmed with 50ºC water bath)

7 mg/mL (15.81 mM)

Water

Insoluble

Ethanol

Insoluble

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。	0.175mg/ml (0.40mM)	Taking the 1 mL working solution as an example, add 50 μL of 3.5 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。	0.175mg/ml (0.40mM)	Taking the 1 mL working solution as an example, add 50 μL of 3.5 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	Betulin (BE, betulinol, betuline, betulinic alcohol), also known as betulinol, betuline, or betulinic alcohol, is a pentacyclic lupane-type triterpenoid naturally distributed in many plants and displays a broad spectrum of biological and pharmacological properties such as anticancer and chemopreventive activity.
in vitro	Betulin significantly inhibits cell viability in cervix carcinoma HeLa cells, hepatoma HepG2 cells, lung adenocarcinoma A549 cells, and breast cancer MCF-7 cells with IC50 values ranging from 10 to 15 mg/mL. While this compound exhibits only moderate anticancer activity in other human cancer cells such as hepatoma SK-HEP-1 cells, prostate carcinoma PC-3, and lung carcinoma NCI-H460, with IC50 values ranging from 20 to 60 mg/mL, it shows minor growth inhibition in human erythroleukemia K562 cells (IC50>100 mg/mL). This compound does not directly trigger mitochondrial cytochrome c release in isolated mitochondria. Bax and Bak are rapidly translocated to the mitochondria 30 min after betulin treatment^[1]. In vitro, it inhibits LPS-induced tumor necrosis factor α (TNF-α) and (interleukin) IL-6 levels and up-regulates the level of IL-10. Also this chemical suppresses the phosphorylation of nuclear factor-kB (NF-kB) p65 protein in LPS-stimulated RAW 264.7 cells^[2].
in vivo	In vivo, Betulin alleviates LPS-induced acute lung injury. Treatment with this compound diminishes pro-inflammatory cytokines, myeloperoxidase activity and bacterial loads in lung tissue during gramnegative pneumonia. In HFD-fed apoE^−/− mice, this compound administration significantly reduces lesions in en face aortas and aortic sinuses. Furthermore, this compound administration significantly increases ABCA1 expression and suppresses macrophage positive areas in the aortic sinuses. Moreover, this compound administration improves plasma lipid profiles and enhances fecal cholesterol excretion in the mice^[3].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	K562, NCI-H460 and PC-3 cells
	濃度
	反応時間	48 h
	実験の流れ	Exponentially growing cells are seeded into a 96-well plate at 1×10⁴ cells/well in triplicate. After incubation for 24 h, cells are treated with increasing concentrations of betulin for 48 h. At the end of the treatment, 20 ml MTT (5 mg/mL) is added to each well, followed by an additional 4 h of incubation. The formazan grains formed by viable cells are solubilized with 200 mL DMSO, and the color intensity is measured at 550 nm with an ELISA reader.
動物実験	動物モデル	C57BL/6J male mice aged 8 weeks
	投薬量	4 or 8 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/20564340/
https://pubmed.ncbi.nlm.nih.gov/25173422/
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5057233/

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：

SREBP2 inhibitor betulin sensitizes hepatocellular carcinoma to lenvatinib by inhibiting the mTOR/IL-1β pathway [ Acta Biochim Biophys Sin -Shanghai), 2023, 55(9):1479-1486]	PubMed: 37434430
SREBP2 inhibitor betulin sensitizes hepatocellular carcinoma to lenvatinib by inhibiting the mTOR/IL-1β pathway [ Acta Biochim Biophys Sin (Shanghai), 2023, 55(9):1479-1486]	PubMed: 37434430
Pharmacological inhibition of fatty acid synthesis blocks SARS-CoV-2 replication [ Nat Metab, 2021, 10.1038/s42255-021-00479-4]	PubMed: 34580494
Organ-specific cholesterol metabolic aberration fuels liver metastasis of colorectal cancer [ Theranostics, 2021, 11(13):6560-6572]	PubMed: 33995676
Inhibition of SREBP-1 Activation by a Novel Small-Molecule Inhibitor Enhances the Sensitivity of Hepatocellular Carcinoma Tissue to Radiofrequency Ablation [ Front Oncol, 2021, 11:796152]	PubMed: 34900747

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。