Lupeol

製品コードS3614 バッチS361403

印刷

化学情報

Synonyms

(3β,13ξ)-Lup-20(29)-en-3-ol, Clerodol, Monogynol B, Fagarasterol, Farganasterol

Storage
(From the date of receipt)

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

化学式

C₃₀H₅₀O

分子量

426.72

CAS No.

545-47-1

Solubility (25°C)*

体外

DMSO

3 mg/mL (7.03 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。	0.150mg/ml (0.35mM)	Taking the 1 mL working solution as an example, add 50 μL of 3 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。	0.150mg/ml (0.35mM)	Taking the 1 mL working solution as an example, add 50 μL of 3 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	Lupeol (Clerodol, Monogynol B, Fagarasterol, Farganasterol) is a significant lupane-type triterpene represented in the plant, fungi and animal kingdoms with anticancer, antiprotozoal, chemopreventive and anti-inflammatory properties.
in vitro	Lupeol is a multi-target agent with immense anti-inflammatory potential targeting key molecular pathways which involve nuclear factor kappa B (NFκB), cFLIP, Fas, Kras, phosphatidylinositol-3-kinase (PI3K)/Akt and Wnt/β-catenin in a variety of cells. This compound can induce apoptosis of human promyelotic HL-60 leukemia cells and induce the formation of hypodiploid nuclei and fragmentation of DNA in a dose and time dependent manner. It induces death of cancer cell lines of various histopathological origins, including T-lymphoblastic leukemia CEM (IC50 = 50 μM), breast carcinoma MCF-7 (IC50 = 50 μM), lung carcinoma A-549 (IC50 = 50 μM), multiple myeloma RPMI 8226 (IC50 = 50 μM), cervical carcinoma HeLa (IC50 = 37 μM), and malignant melanoma G361 (IC50 = 50 μM) when treated for 72 h. This agent also inhibits the proliferation of the ERα-negative breast cancer cells MDA-MB-231. This chemical (50-30 μg/ml) exhibits anti-angiogenic property in an in vitro tube formation model of human umbilical venous endothelial cells. It inhibits the PI3K/Akt, NFκB signaling network, and decreases the activity of Ras protein (GTP-bound Ras) in pancreatic cancer cells. The compound modulates the microtubule assembly and the protein level of its regulatory molecules such as Stathmin and Survivin in prostate cancer cells thus causing G2/M cell cycle arrest^[1]. It has been shown to act as a potent inhibitor of protein kinases and serine proteases and inhibit the activity of DNA topoisomerase II, a target for anticancer chemotherapy^[2].
in vivo	Topical application of Lupeol decreases myeloperoxidase levels thus causing reduction in cell infiltration into inflamed tissues in mice. Oral administration of this compound (12.5-200 mg/kg) results in the significant reduction in CD4+ T and CD8+ T cell counts and the level of cytokines (IL-2, IFN-gamma and IL-4) in arthritic mice. Its administration causes a significant reduction in cellularity and eosinophil levels in the broncho-alveolar fluid. It also exerts its wound healing effect by decreasing the level of monocytes and docking with GSK3β protein. For cancer, this agent significantly inhibits the NFκB translocation and its DNA binding activity in a mouse model of skin tumorigenesis. It inhibits growth of highly metastatic tumors of human melanoma origin by modulating ratio of Bcl-2 and Bax protein levels in vitro and in vivo. Thus, this compound itself being non-toxic to normal cells could be used as a chemopreventive as well chemotherapeutic agent against skin cancer. It has been shown to inhibit the generation of ROS and restore the depleted antioxidant levels within prostatic tissue of androgen pretreated mice. This chemical is a non-toxic but highly potent chemopreventive and chemotherapeutic agent^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	LNCaP cells
	濃度	20 μM
	反応時間	48 h
	実験の流れ	Microarray analysis: LNCaP cells were treated with subtoxic dose (20 μM) of Lupeol. After 48 h of incubation, cells were harvested and RNA was isolated by using RNeasy kit. Next, 4 μg of RNA was enzymatically converted into complementary RNA, labeled and hybridized with the microarrays followed by detection with the chemiluminescent reagents and X-ray film.
動物実験	動物モデル	CD-1 mice
	投薬量	1 or 2 mg/0.2 ml acetone/animal, w/v
	投与方法	topical

参考

https://pubmed.ncbi.nlm.nih.gov/19464787/
https://pubmed.ncbi.nlm.nih.gov/15122342/
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2722146/

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：

Lupeol, an androgen receptor inhibitor, enhances the chemosensitivity of prostate cancer stem cells to antiandrogen enzalutamide-based therapy [ Toxicol Appl Pharmacol, 2023, 478:116699]	PubMed: 37777120
Antiandrogen enzalutamide induced genetic, cellular, and hepatic damages: amelioration by triterpene Lupeol [ Drug Chem Toxicol, 2022, 1-12]	PubMed: 35188013

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。