Ardisiacrispin B is a natural triterpenoid saponin compound isolated from the traditional Chinese medicinal plant Ardisia [1]. Ardisiacrispin B exhibits cytotoxic effects in multifactorial drug-resistant cancer cells via ferroptosis and apoptotic cell death [2]. Ardisiacrispin B has anticancer, anti-inflammatory and antioxidant effects [3-4].
In CCRF-CEM cells, Ardisiacrispin B (0.005-6.4μM; 72h) induced apoptosis in CCRF-CEM cells via activation of inititator caspases 8 and 9 and effector caspase 3/7, alteration of MMP and increase in ROS production [2]. In RAW264.7 cells, Ardisiacrispin B (0.125μM, 0.5μM, 2μM; 24h) has a good anti-inflammatory effect on LPS-induced RAW264.7 cells, strongly inhibits the release of NO, TNF-α and IL-1β in cells, and significantly inhibits the expression of PI3K, P-PI3K, AKT and P-AKT [5]. In A549 cells, Ardisiacrispin B (2.5μM, 5μM, 10μM, 20μM,50μM; 48h) displayed moderate cytotoxicity against A549 with an IC50 value of 8.7μM [6].
In sprague dawley rats, Ardisiacrispin B (50mg/kg; ig; twice a day for 3 consecutive days) is converted into water-soluble components in the body mainly through metabolic processes such as oxidation, dehydration, and glycoside conjugation [5].
References:
[1]. Jansakul C, Baumann H, Kenne L, et al. Ardisiacrispin A and B, two utero-contracting saponins from Ardisia crispa. Planta medica. 1987 Oct; 53(05): 405-409.
[2]. Mbaveng AT, Ndontsa BL, Kuete V, et al. A naturally occuring triterpene saponin ardisiacrispin B displayed cytotoxic effects in multi-factorial drug resistant cancer cells via ferroptotic and apoptotic cell death. Phytomedicine. 2018 Apr 1; 43: 78-85.
[3]. Tao HH, Zhou YQ, Wei X, et al. Anti‐inflammatory activity of a new lactone isolated from the leaves of Ardisia crenata Sims. Chemistry & Biodiversity. 2024 Jan; 21(1): e202300983.
[4]. Xie Q, Shama R, Yu J, et al. Ethnobotanical study of Zhuang medicinal herbs of Ardisia: variety systematization, traditional uses, phytochemistry, pharmacology, clinical application, and toxicity. Journal of Pharmacy and Pharmacology. 2024 Apr 1; 76(4): 327-353.
[5]. Zhou W, Yang G, Wen Y, et al. Metabolites-based network pharmacology to preliminarily verify in vitro anti-inflammatory effect of Ardisiacrispin B. International Journal of Molecular Sciences. 2023 Dec 2; 24(23): 17059.
[6]. Dai LM, Huang RZ, Zhang B, et al. Cytotoxic triterpenoid saponins from Lysimachia foenum-graecum. Phytochemistry. 2017 Apr 1; 136: 165-174.
Ardisiacrispin B是从传统中药植物紫金牛属植物中分离得到的天然三萜皂苷化合物 [1]。Ardisiacrispin B通过诱导铁死亡和凋亡性细胞死亡，在多因素耐药癌细胞中表现出细胞毒作用 [2]。Ardisiacrispin B具有抗癌、抗炎和抗氧化作用 [3-4]。
在CCRF-CEM细胞中，Ardisiacrispin B（0.005-6.4μM；72h）通过激活启动子caspase 8和9 以及效应子caspase 3/7、改变MMP和增加ROS生成，诱导CCRF-CEM细胞凋亡 [2]。在RAW264.7细胞中，Ardisiacrispin B（0.125μM、0.5μM、2μM；24h）对LPS诱导的RAW264.7细胞具有良好的抗炎作用，强效抑制细胞内NO、TNF-α和IL-1β的释放，并显著抑制PI3K、P-PI3K、AKT和P-AKT的表达 [5]。在A549细胞中，Ardisiacrispin B（2.5μM、5μM、10μM、20μM、50μM；48h）对A549细胞表现出中等细胞毒性，IC50值为8.7μM [6]。
在sprague dawley大鼠中，Ardisiacrispin B（50mg/kg；ig；每天2次，连续3天）在体内主要通过氧化、脱水、糖苷结合等代谢过程转化为水溶性成分 [5]。