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]。