Cinobufotalin (Synonyms: NSC 90326) |
カタログ番号GC32757
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Cinobufotalinは、複数の生物学的活性を持つステロイドグリコシドである。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1108-68-5
Sample solution is provided at 25 µL, 10mM.
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Cinobufotalinは、複数の生物学的活性を持つステロイドグリコシドである[1]。Cinobufotalinはヒキガエルの分泌物から抽出される心態式ステロイドである[2]。Cinobufotalinは心態、利尿薬、止血薬として使用されており、抗腫瘍活性も患っている[3]。
体外では、Cinobufotalin（0.1、1、5、10μM）の治療は24-72時間で用量依存的にSK-OV-3、CRL-1978とCRL-11731細胞の増殖、遷移と浸潤を阻害する[4]。 Cinobufotalin（40、60、80nm）の24-48Hの治療はHEPG2、SMMC-7721とSNU-368細胞に作用し、上皮マーカー（E-Cadherin）を上方修正し、間葉系マーカー（N-Cadherin，Snail，Snail，Snail，Slug和Zeb1和Zeb1）を下方修正する[5]。
体内ではCinobufotalin（1，5mg/kg）で1週間腹腔内注射によりA549細胞異種移植鼠を治療に与え、それは腫瘍の成長率を著しく阻害し、生存率を増加できる[6]。 Cinobufotalin（5mg/kg）は復興内注射によってH22肝がん鼠を治療することで顕著に腫瘍の成長を阻害し、鼠の免疫機能を増加し、Cinobufotalinの化学療法作用を高める[7]。
References:
[1] El-Seedi H R, Yosri N, El-Aarag B, et al. Chemistry and the potential antiviral, anticancer, and anti-inflammatory activities of cardiotonic steroids derived from toads[J]. Molecules, 2022, 27(19): 6586.
[2] Cheng C, Wang J, Chen J, et al. New therapeutic aspects of steroidal cardiac glycosides: the anticancer properties of Huachansu and its main active constituent Bufalin[J]. Cancer Cell International, 2019, 19: 1-27.
[3] Liu Q, Shu L, Wen Y, et al. Cinobufagin and cinobufotalin from Traditional Chinese Medicine and chemical synthesis[J]. Authorea Preprints, 2023.
[4] Afroze S H, Peddaboina C, MCDOWELL A B, et al. Differential effects of in vitro treatment with cinobufotalin on three types of ovarian cancer cells[J]. Anticancer Research, 2018, 38(10): 5717-5724.
[5] Li W, Pei S, Zhang X, et al. Cinobufotalin inhibits the epithelial-mesenchymal transition of hepatocellular carcinoma cells through down-regulate β-catenin in vitro and in vivo[J]. European Journal of Pharmacology, 2022, 922: 174886.
[6] Kai S, Lu J, Hui P, et al. Pre-clinical evaluation of cinobufotalin as a potential anti-lung cancer agent[J]. Biochemical and biophysical research communications, 2014, 452(3): 768-774.
[7] Wang P P, Wang Y H, Wang L S, et al. Anti-tumor effect and its related mechanisms of cinobufotalin combined with cisplatin on H22 liver cancer mice[J]. Zhongguo Zhong yao za zhi= Zhongguo Zhongyao Zazhi= China Journal of Chinese Materia Medica, 2020, 45(16): 3945-3951.
| 細胞実験[1]: | |
細胞株 | SK-OV-3、CRL-1978、CRL-11731 細胞 |
準備方法 | 細胞培養物を、24、48、および72Hの間、Cinobufotalin（0.1、1、5、10μm）で処理する。細胞の増殖、遷移、および浸潤は、それぞれセルチター、サイトセレクト、およびフルオロブロックアッセイを使用して測定する。 |
反応条件 | 0.1, 1, 5, 10μM; 24, 48, 72時間 |
アプリケーション | Cinobufotalinの治療は用量依存的にSK-OV-3、CRL-1978とCRL-11731細胞の増殖、遷移と浸潤を阻害する。 |
| 動物実験 [2]: | |
動物モデル | 雄のヌード鼠 |
準備方法 | A549細胞をヌードマウスの右腿に皮下注射し、腫瘍が平均体積200〜300mm3に達したときに治療が開始される。動物は、各グループ10の鼠を持つ3つのグループにランダム化される。（a）車両。 （b）Cinobufotalin1.0mg/kg; （c）5.0mg/kgのCinobufotalin。Cinobufotalinを1日2回腹腔内（i.p.）に1週間注射する。鼠は治療に関連する毒性/死亡率について毎日検査され、腫瘍は週に1回キャリパーで最大5週間測定する。 |
投与形態 | 1.0、5.0mg/kg 1日2回1週間。 i.p. |
アプリケーション | Cinobufotalinは鼠のA549異種移植片の成長を顕著に阻害する。 |
References: | |
| Cas No. | 1108-68-5 | SDF | |
| 同義語 | NSC 90326 | ||
| Canonical SMILES | C[C@]([C@@H](C(C=C1)=COC1=O)[C@H]2OC(C)=O)(CC[C@@]3([H])[C@@]4([H])CC[C@@]5(O)[C@@]3(CC[C@H](O)C5)C)[C@@]64[C@@H]2O6 | ||
| Formula | C26H34O7 | M.Wt | 458.54 |
| 溶解度 | DMSO : ≥ 35 mg/mL (76.33 mM) | Storage | Store at -20°C,protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.1808 mL | 10.9042 mL | 21.8083 mL |
| 5 mM | 436.2 μL | 2.1808 mL | 4.3617 mL |
| 10 mM | 218.1 μL | 1.0904 mL | 2.1808 mL |
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 24 reference(s) in Google Scholar.)