Polyphyllin VI
(Synonyms: 重楼皂苷VI) 目录号 : GN10249
Polyphyllin VI是一种具有口服活性的天然皂苷,主要通过诱导细胞周期阻滞、细胞凋亡和细胞焦亡发挥抗癌作用。
Cas No.:55916-51-3
Sample solution is provided at 25 µL, 10mM.
Polyphyllin VI is an orally active natural saponin that exerts anticancer effects primarily by inducing cell-cycle arrest, apoptosis, and pyroptosis[1][2]. Polyphyllin VI is commonly used in cancer-mechanism studies, especially those focused on cell-death pathways and their associated signaling cascades[3].
In vitro, treatment of glioma cells with Polyphyllin VI (0-8μM; 12-48h) dose-dependently inhibits cell proliferation, blocks cycle at G2/M, suppresses migration, and induces apoptosis and autophagy[4]. Polyphyllin VI (0-30μM; 48h) inhibits U2OS osteosarcoma proliferation, triggers G2/M arrest, collapses mitochondrial membrane potential, and simultaneously evokes caspase-mediated apoptosis[5].
In vivo, Polyphyllin VI (5mg/kg/day; i.p.; 14 days) reversed bleomycin-induced pulmonary fibrosis in C57BL/6J mice, reduced collagen deposition, suppressed α-SMA and vimentin expression, and restored E-cadherin levels[6]. Polyphyllin VI (10mg/kg/day; i.p.; 10 days) increased NLRP3 inflammasome activation and caspase-1-mediated pyroptosis in A549 tumor xenografts of athymic nude mice[7].
References:
[1] Lin Z, Liu Y, Li F, et al. Anti-lung Cancer Effects of Polyphyllin VI and VII Potentially Correlate with Apoptosis In Vitro and In Vivo. Phytother Res. 2015;29(10):1568-1576.
[2] Liu Y, Dong X, Wang W, et al. Molecular Mechanisms of Apoptosis in HepaRG Cell Line Induced by Polyphyllin VI via the Fas Death Pathway and Mitochondrial-Dependent Pathway. Toxins (Basel). 2018;10(5):201.
[3] Wang Y, Huang X, Xian B, et al. Machine learning and bioinformatics-based insights into the potential targets of saponins in Paris polyphylla smith against non-small cell lung cancer. Front Genet. 2022;13:1005896.
[4] Liu W, Chai Y, Hu L, et al. Polyphyllin VI Induces Apoptosis and Autophagy via Reactive Oxygen Species Mediated JNK and P38 Activation in Glioma. Onco Targets Ther. 2020;13:2275-2288.
[5] Yuan YL, Jiang N, Li ZY, et al. Polyphyllin VI induces apoptosis and autophagy in human osteosarcoma cells by modulation of ROS/JNK activation. Drug Des Devel Ther. 2019;13:3091-3103.
[6] Xie Y, Gan C, Liu H, et al. Polyphyllin VI Ameliorates Pulmonary Fibrosis by Suppressing the MAPK/ERK and PI3K/AKT Signaling Pathways via Upregulating DUSP6. Phytother Res. 2024;38(12):5930-5948.
[7] Teng JF, Mei QB, Zhou XG, et al. Polyphyllin VI Induces Caspase-1-Mediated Pyroptosis via the Induction of ROS/NF-κB/NLRP3/GSDMD Signal Axis in Non-Small Cell Lung Cancer. Cancers (Basel). 2020;12(1):193.
Polyphyllin VI是一种具有口服活性的天然皂苷,主要通过诱导细胞周期阻滞、细胞凋亡和细胞焦亡发挥抗癌作用[1][2]。Polyphyllin VI常用于癌症机制研究,特别是细胞死亡途径及其相关信号通路的研究[3]。
体外实验中,Polyphyllin VI(0-8μM;12-48h)可剂量依赖性地抑制胶质瘤细胞增殖,阻滞细胞周期于G2/M期,抑制细胞迁移,并诱导细胞凋亡和自噬[4]。 Polyphyllin VI(0–30μM;48h)可抑制U2OS骨肉瘤细胞增殖,诱导G2/M期阻滞,破坏线粒体膜电位,并同时引发caspase介导的细胞凋亡[5]。
体内实验中,Polyphyllin VI(5mg/kg/天;腹腔注射;连续14天)可逆转博来霉素诱导的C57BL/6J小鼠肺纤维化,减少胶原沉积,抑制α-SMA和波形蛋白表达,并恢复E-钙黏蛋白水平[6]。Polyphyllin VI(10mg/kg/天;腹腔注射;连续10天)可增强A549荷瘤裸鼠肿瘤组织中NLRP3炎症小体的激活,并诱导caspase-1介导的细胞焦亡[7]。
| Cell experiment [1]: | |
Cell lines | Glioma Cell lines U87, LN229, U251, and U343 |
Preparation Method | Glioma Cell lines U87, LN229, U251, and U343 were cultured in DMEM medium supplemented with 10% FBS and maintained in an incubator at 37°C, and 5% CO2. Approximately 2000 glioma cells were re-suspended in 100µL of complete medium and cultured in 6-well plates for 24 hrs. The cells were treated with varying concentrations of Polyphyllin VI (0, 2, 4, 6, and 8µM) followed by a 12, 24 and 48 hrs incubation. Thereafter, the cells were treated with the WST-8 reagent from CCK-8 for 2 hrs, then their viability assayed by detecting the absorbance at OD 450nm. Cell apoptosis was analyzed using the Annexin V-FITC Kit. Cell cycle distribution was detected by flow cytometry. Transwell assay was carried out to determine the role of Polyphyllin VI on the invasive ability of glioma cells. |
Reaction Conditions | 0-8μM; 12-48h |
Applications | Polyphyllin VI (0-8μM; 12-48h) dose-dependently inhibits cell proliferation, suppresses migration, and induces apoptosis in glioma cells. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice |
Preparation Method | C57BL/6 mice were first anesthetized with 5mg/mL pentobarbital sodium. Then, 100μL of normal saline containing BLM sulfate(2mg/kg) was directly injected into the trachea of C57BL/6J mice. For the therapeutic experiment, the mice were randomly categorized into two groups on the seventh day following BLM modeling: the BLM+solvent (dimethyl sulfoxide: polyethylene glycol 400: normal saline=5:45:50) group and the BLM+Polyphyllin VI (5mg/kg/day) group. All mice were injected intraperitoneally with PPVI for 14 days, during which the mice's weight was measured every 3 days. Then the mice were sacrificed for tissue sample collection, and the weight of the lungs was recorded. Histopathological and immunohistochemical (IHC) tests were conducted on a lung excised from the left and soaked in 4% paraformaldehyde. |
Dosage form | 5mg/kg/day; i.p.; 14 days |
Applications | Polyphyllin VI reversed bleomycin-induced pulmonary fibrosis in C57BL/6J mice, reduced collagen deposition, suppressed α-SMA and vimentin expression, and restored E-cadherin levels. |
References: | |
| Cas No. | 55916-51-3 | SDF | |
| 别名 | 重楼皂苷VI | ||
| 化学名 | Chonglou saponin VI | ||
| Canonical SMILES | O[C@@H]([C@@H](O)[C@H]1O)[C@]([H])(O[C@H]2[C@@](O[C@H]3CC4=CC[C@]([C@](C[C@@](O[C@]5(OC6)CC[C@H]6C)([H])[C@]7(O)[C@@H]5C)([H])[C@@]7(CC8)C)([H])[C@@]8([H])[C@]4(CC3)C)([H])O[C@H](CO)[C@@H](O)[C@@H]2O)C[C@@H]1C | ||
| 分子式 | C39H62O13 | 分子量 | 738.91 |
| 溶解度 | ≥ 73.9mg/mL in EtOH with gentle warming | 储存条件 | Store at -20℃ |
| 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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1 mg | 5 mg | 10 mg |
| 1 mM | 1.3533 mL | 6.7667 mL | 13.5334 mL |
| 5 mM | 270.7 μL | 1.3533 mL | 2.7067 mL |
| 10 mM | 135.3 μL | 676.7 μL | 1.3533 mL |
| 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 | |||
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| % DMSO % % Tween 80 % saline | ||||||||||
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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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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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