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Ardisiacrispin B Sale

(Synonyms: 百两金皂苷B) 目录号 : GC65163

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 。

Ardisiacrispin B Chemical Structure

Cas No.:112766-96-8

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Sample solution is provided at 25 µL, 10mM.

Description

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]

实验参考方法

Cell experiment [1]:

Cell lines

CCRF-CEM cells

Preparation Method

Leukemia CCRF-CEM cells were maintained in RPMI 1640 medium supplemented with 10% fetal calf serum in a humidified 5% CO2 atmosphere at 37℃. The cytotoxicity of Ardisiacrispin B and the reference drug doxorubicin (positive control) were evaluated. Dimethyl sulfoxide (DMSO) was used to solubilize the samples and tested as a negative control. The highest concentration of DMSO was less than 0.1%. The concentration range of ardisiacrispin B tested in CCRF-CEM was 0.005-6.4μM.

Reaction Conditions

0.005-6.4μM; 72h

Applications

Ardisiacrispin B 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.

Animal experiment [2]:

Animal models

Sprague dawley rats

Preparation Method

Twenty SPF-grade male sprague dawley rats weighing 200 ± 20g (8-10 weeks old). Once the rats entered the animal house, they were managed in packs of five per cage, fed with standard chow, and provided with fresh, purified water that was replaced daily. The animal house was well lit with a 12-hour day/night cycle, well ventilated, and maintained at a room temperature of 22 ± 2℃ and a relative humidity of 15–60%, and it required regular disinfection. Prior to the experiment, rats were adaptively reared in the laboratory for 7 days. These animals were randomly divided into a blank control group and an Ardisiacrispin B administrated group. The blank control group was gavaged water, and the Ardisiacrispin B administered group was gavaged with 50mg/kg of Ardisiacrispin B aqueous solution (concentration of 6mg/mL), twice a day for 3 consecutive days.

Dosage form

50mg/kg; ig; twice a day for 3 consecutive days

Applications

Ardisiacrispin B is converted into water-soluble components in the body mainly through metabolic processes such as oxidation, dehydration, and glycoside conjugation.

References:
[1]. 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.
[2]. 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.

化学性质

Cas No. 112766-96-8 SDF Download SDF
别名 百两金皂苷B
分子式 C53H86O22 分子量 1075.24
溶解度 DMSO: 100 mg/mL 储存条件 Store at -20°C, away from moisture and light
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1 mg 5 mg 10 mg
1 mM 0.93 mL 4.6501 mL 9.3002 mL
5 mM 0.186 mL 0.93 mL 1.86 mL
10 mM 0.093 mL 0.465 mL 0.93 mL
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