Ardisiacrispin A是一种三萜皂苷类化合物，具有抗肿瘤活性。
Cas No.:23643-61-0
Sample solution is provided at 25 µL, 10mM.
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Ardisiacrispin A is a triterpenoid saponin compound with antitumor activity[1-2]. Ardisiacrispin A induces apoptosis in tumor cells by activating caspase-8 and caspase-9, and inhibits cancer cell proliferation by disrupting microtubule structure. Ardisiacrispin A can be used in research related to antitumor drugs[3-4].
In vitro, Ardisiacrispin A (0–35μg/ml) was used to treat human melanoma HTB-140 cells and human skin fibroblasts (HSFs) for 1–10 days. Ardisiacrispin A significantly reduced cell viability, inhibited cell proliferation in a time- and dose-dependent manner, and induced cytoplasmic vacuolization and actin cytoskeleton disintegration, while also inhibiting the motility of tumor cells[5]. Ardisiacrispin A (0–50μg/ml) was used to treat A549 human lung cancer cells for 24 hours. Ardisiacrispin A significantly induced apoptosis and inhibited cell proliferation[6].
In vivo, Ardisiacrispin A (2mg/kg) was administered as a single intravenous injection to Sprague-Dawley rats. Ardisiacrispin A rapidly reached a very high peak plasma concentration (Cmax approximately 15054ng/mL) in male SD rats, but was eliminated at a moderate to fast rate, with a plasma half-life (t1/2) of about 2.2 hours[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).
Ardisiacrispin A是一种三萜皂苷类化合物，具有抗肿瘤活性[1-2]。Ardisiacrispin A通过活化caspase-8和caspase-9诱导肿瘤细胞凋亡，并通过破坏微管结构抑制癌细胞增殖。Ardisiacrispin A可用于抗肿瘤药物的相关研究[3-4]。
在体外，Ardisiacrispin A（0–35μg/ml）处理人类黑色素瘤HTB-140细胞和人类皮肤成纤维细胞（HSFs）1–10天。Ardisiacrispin A以时间和剂量依赖性的方式显著降低细胞活力、抑制细胞增殖，并引起细胞质空泡化、肌动蛋白细胞骨架解体，同时对肿瘤细胞的运动性产生抑制作用[5]。Ardisiacrispin A（0-50μg/ml）处理A549人类肺癌细胞24小时，显著诱导细胞凋亡，同时抑制细胞增殖[6]。
在体内，Ardisiacrispin A（2mg/kg）单次静脉注射给予Sprague-Dawley大鼠。Ardisiacrispin A在雄性SD大鼠体内迅速达到很高的血药峰值浓度（Cmax约为15054ng/mL），但消除速度中等偏快，血浆半衰期（t1/2）约为2.2小时[7]。
| Cell experiment [1]: | |
Cell lines | Human skin fibroblasts (HSFs) and human melanoma HTB-140 cells |
Preparation Method | HSFs and HTB-140 cells were maintained in Dulbecco's Modified Eagle's medium (DMEM) supplemented with 10% fetal calf serum (FCS) at 37°C, 5% CO₂. Cells were incubated with Ardisiacrispin A at concentrations ranging from 0 to 35μg/ml for periods from 1 to 10 days. |
Reaction Conditions | 0 to 35μg/ml; 1 to 10 days. |
Applications | Ardisiacrispin A decreased the viability and inhibited the proliferation of both cell types in a time- and dose-dependent manner, with a more pronounced effect on melanoma cells. Ardisiacrispin A induced morphological changes, including cytoplasm vacuolization and actin cytoskeleton disintegration. LTS-4 also significantly inhibited the motile activity of melanoma HTB-140 cells. |
| Animal experiment [2]: | |
Animal models | Male Sprague-Dawley (SD) rats |
Preparation Method | Rats were fasted for 12 hours with free access to water prior to the experiment. A single dose of Ardisiacrispin A (2mg/kg) was administered intravenously via the tail vein. Blood samples (0.3mL) were collected from the tail vein into heparinized tubes at predetermined time points (0.0333, 0.15, 0.5, 1, 1.5, 2, 3, 4, 6, 8h) post-dose. |
Dosage form | 2mg/kg; i.v.; single injection. |
Applications | Ardisiacrispin A exhibited a moderate elimination half-life (t1/2 ~2.2h) and a high peak plasma concentration (Cmax ~15054ng/mL) following administration. |
References: | |
| Cas No. | 23643-61-0 | SDF | |
| 别名 | 百两金素,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 | ||
| 分子式 | C52H84O22 | 分子量 | 1061.22 |
| 溶解度 | 储存条件 | Store at -20°C,protect from light | |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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2.
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