Ardisiacrispin A (Synonyms: Deglucocyclamin, LTS-4, Saxifragifolin B) |
カタログ番号GN10807
One-Click Copy Product Info
|
Ardisiacrispin Aは抗腫瘍活性を持つトリテルペンサポニン化合物である。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 23643-61-0
Sample solution is provided at 25 µL, 10mM.
Ardisiacrispin Aは抗腫瘍活性を持つトリテルペンサポニン化合物である[1-2]。Ardisiacrispin Aはカスパーゼ-8とカスパーゼ-9を活性化することで腫瘍細胞でアポトーシスを誘発し、微小管の構造を破壊することで癌細胞の増殖を阻害する。Ardisiacrispin Aは、抗腫瘍薬に関する研究に使える[3-4]。
In vitro（体外）実験で、Ardisiacrispin A（0–35μg/ml）でヒトメラノーマHTB-140細胞とヒト皮膚線維芽細胞（HSF）を1-10日間処理した。Ardisiacrispin Aは、細胞の生存率を著しく低下させ、細胞の増殖を時間と用量依存的に阻害し、細胞質空胞化とアクチン細胞骨格の崩壊を誘発し、同時に腫瘍細胞の運動能を阻害した[5]。Ardisiacrispin A（0–50μg/ml）でA549ヒト肺癌細胞を24時間処理した。Ardisiacrispin Aはアポトーシスを著しく誘発し、細胞の増殖を阻害した[6]。
In vivo（体内）実験で、Ardisiacrispin A（2mg/kg）をSprague-Dawleyラットに単回静脈内注射した。Ardisiacrispin Aは速やかに、雄SDラットで非常に高いピーク血漿濃度（Cmaxは約15054ng/mL）に達したものの、消失の速度は中等から速い速度で、血漿中半減期（t1/2）は約2.2時間であった[7]。
References:
[1] Podolak I, Janeczko Z, Galanty A, et al. A triterpene saponin from Lysimachia thyrsiflora L. Acta Pol Pharm. 2007 Jan-Feb;64(1):39-43.
[2] Jansakul C, Baumann H, Kenne L, et al. Ardisiacrispin A and B, two utero-contracting saponins from Ardisia crispa. Planta Med. 1987 Oct;53(5):405-9.
[3] Tao HH, Zhou YQ, Wei X, et al. Anti-inflammatory activity of a new lactone isolated from the leaves of Ardisia crenata Sims. Chem Biodivers. 2024 Jan;21(1):e202300983.
[4] Chen L, Weng Q, Li F, et al. Pharmacokinetics and Bioavailability Study of Tubeimoside I in ICR Mice by UPLC-MS/MS. J Anal Methods Chem. 2018 Jul 5;2018:9074893.
[5] Galanty A, Michalik M, Sedek L, et al. The influence of LTS-4, a saponoside from Lysimachia thyrsiflora L., on human skin fibroblasts and human melanoma cells. Cell Mol Biol Lett. 2008;13(4):585-98.
[6] Lee YG, Kim TH, Kwon JE, et al. Cytotoxic Effects of Ardisiacrispin A from Labisia pumila on A549 Human Lung Cancer Cells. Life (Basel). 2024 Feb 18;14(2):276.
[7] Fang B, Bao S, Wang S, et al. Pharmacokinetic study of ardisiacrispin A in rat plasma after intravenous administration by UPLC-MS/MS. Biomed Chromatogr. 2017 Mar;31(3).
| 細胞実験[1]: | |
細胞株 | ヒト皮膚線維芽細胞（HSF）とヒトメラノーマHTB-140細胞 |
準備方法 | 37°C、5% CO₂で、10%のウシ胎児血清を添加したDulbecco's改変Eagle's培地（DMEM）でHSFとHTB-140細胞を培養した。濃度が0から35μg/mlのArdisiacrispin Aで細胞を1-10日間インキュベートした。 |
反応条件 | 0から35μg/ml；1-10日間 |
アプリケーション | Ardisiacrispin Aは、時間と用量依存的に、両方の細胞種の生存率を低下させ、増殖を阻害し、メラノーマ細胞に対する効果はより著しかった。Ardisiacrispin Aは形態学的な変化（細胞質空胞化とアクチン細胞骨格の崩壊）を誘発した。また、LTS-4はメラノーマHTB-140細胞の運動活性をも著しく阻害した。 |
| 動物実験 [2]: | |
動物モデル | 雄のSprague-Dawley（SD）ラット |
準備方法 | 実験の前に、ラットを12時間絶食させ、水を自由に摂取させた。尾静脈を通じて、Ardisiacrispin A（2mg/kg）を単回静脈内注射した。投与後、予め指定された時点（0.0333、0.15、0.5、1、1.5、2、3、4、6、8）で、血液サンプル（0.3mL）を尾静脈からヘパリン処理した採血管に採取した。 |
投与形態 | 2mg/kg；静脈内注射；単回注射 |
アプリケーション | 投与後、Ardisiacrispin Aは中程度の消失半減期（t1/2 ~2.2時間）と高いピーク血漿濃度（Cmax ~15054ng/mL）を示した。 |
References: | |
| Cas No. | 23643-61-0 | SDF | |
| 同義語 | Deglucocyclamin, LTS-4, Saxifragifolin B | ||
| Canonical SMILES | CC1(C2CCC3(C(C2(CCC1OC4C(C(C(CO4)OC5C(C(C(C(O5)CO)O)O)OC6C(C(C(CO6)O)O)O)O)OC7C(C(C(C(O7)CO)O)O)O)C)CCC89C3(CC(C1(C8CC(CC1)(C)C=O)CO9)O)C)C)C | ||
| Formula | C52H84O22 | M.Wt | 1061.22 |
| 溶解度 | 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. |
||
| 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 | 942.3 μL | 4.7116 mL | 9.4231 mL |
| 5 mM | 188.5 μL | 942.3 μL | 1.8846 mL |
| 10 mM | 94.2 μL | 471.2 μL | 942.3 μL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)