Periplocin
(Synonyms: 杠柳毒苷) 目录号 : GC44600
Periplocin是从Periploca sepium分离的强心苷类化合物，具有抗增殖活性。
Cas No.:13137-64-9
Sample solution is provided at 25 µL, 10mM.
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Periplocin is one of the cardenolides isolated from Periploca sepium, with anti-proliferative activities[1]. Periplocin can increase the caspase-3, -8, and -9 enzyme activities and decrease PI3K/Akt/mTOR activity to trigger apoptosis[2]. Periplocin has been widely used as an anticancer agent in cellular and animal models to inhibit cancer progression[3].
In vitro, Periplocin treatment significantly inhibited the proliferation of Muc-Myx2a, Muc-Myx2b and T60 cells with IC50 values of 0.25µM, 0.30µM, and 0.10µM, respectively[4]. Periplocin treatment at 50µM for 24 hours significantly activated RIP3/MLKL signaling pathway and induced necroptosis in TPC-1 cells[5]. Treatment of SK-HEP-1 cells with 500nM Periplocin for 48 hours significantly induced cell cycle arrest and apoptosis, accompanied by the inhibition of AKT/NF-κB signaling pathway[6].
In vivo, Periplocin treatment via intraperitoneal injection at a dose of 15mg/kg/day for 14 days notably reduced tumor growth in A549 cell-xenograft mice and decreased Ki67 expression in the tumor tissues[7]. Daily intraperitoneal injection of Periplocin at a dose of 5mg/kg for 8 weeks reduced bone loss in ovariectomy-induced osteoporotic mice[8].
References:
[1] Lohberger B, Wagner S, Wohlmuther J, et al. Periplocin, the most anti-proliferative constituent of Periploca sepium, specifically kills liposarcoma cells by death receptor mediated apoptosis[J]. Phytomedicine, 2018, 51: 162-170.
[2] Liu X, Liu J, Yan B, et al. Study of the PI3K/Akt/mTOR signaling pathway in vitro and molecular docking analysis of periplocin inhibits cell cycle progression and induces apoptosis in MDA‐MB‐231[J]. Environmental Toxicology, 2024, 39(1): 444-456.
[3] Bae E S, Byun W S, Ock C W, et al. Periplocin exerts antitumor activity by regulating Nrf2-mediated signaling pathway in gemcitabine-resistant pancreatic cancer cells[J]. Biomedicine & Pharmacotherapy, 2023, 157: 114039.
[4] Lohberger B, Bernhart E, Stuendl N, et al. Periplocin mediates TRAIL-induced apoptosis and cell cycle arrest in human myxofibrosarcoma cells via the ERK/p38/JNK pathway[J]. Phytomedicine, 2020, 76: 153262.
[5] Ding L, Wen F, Zeng L, et al. Periplocin induces necroptosis in papillary thyroid carcinoma through DR4 mediated RIPK3 and MLKL signaling[J]. Scientific Reports, 2025, 15(1): 20383.
[6] Lin J P, Huang M H, Sun Z T, et al. Periplocin inhibits hepatocellular carcinoma progression and reduces the recruitment of MDSCs through AKT/NF-κB pathway[J]. Life Sciences, 2023, 324: 121715.
[7] Wang J, Zhu Y, Song J, et al. Periplocin potentiates ferroptotic cell death in non-small cell lung cancer by inducing the degradation of Nrf2[J]. Cancer Cell International, 2025, 25(1): 294.
[8] Zhang X, Sun Z, Zhang Y, et al. Periplocin targets low density lipoprotein receptor-related protein 4 to attenuate osteoclastogenesis and protect against osteoporosis[J]. Biochemical Pharmacology, 2023, 211: 115516.
Periplocin是从Periploca sepium分离的强心苷类化合物，具有抗增殖活性[1]。Periplocin可通过增强caspase-3、-8、-9酶活性并抑制PI3K/Akt/mTOR通路进而诱导细胞凋亡[2]。Periplocin已作为抗癌剂广泛应用于细胞和动物模型中抑制癌症进展[3]。
在体外，Periplocin处理48小时能显著抑制Muc-Myx2a、Muc-Myx2b和T60细胞增殖，IC50值分别为0.25µM、0.30µM和0.10µM[4]。使用50µM的Periplocin处理TPC-1细胞24小时，可显著激活RIP3/MLKL信号通路并诱导坏死性凋亡[5]。用500nM的Periplocin处理SK-HEP-1细胞48小时，能显著诱导细胞周期阻滞和凋亡，同时抑制AKT/NF-κB信号通路[6]。
在体内，每日腹腔注射15mg/kg/day剂量的Periplocin连续14天，可显著抑制A549细胞移植瘤小鼠的肿瘤生长，并降低肿瘤组织中Ki67的表达[7]。每日腹腔注射5mg/kg剂量的Periplocin持续8周，能减轻卵巢切除诱导的骨质疏松小鼠的骨量丢失[8]。
| Cell experiment [1]: | |
Cell lines | TPC-1 cells |
Preparation Method | TPC-1 cells were cultured in DMEM medium supplemented with 10% fetal bovine serum, 100U/ml penicillin, and 100U/ml streptomycin. The culture conditions were 37℃ and 5% CO2 in a humidified incubator. TPC-1 cells were seeded in 96-well plates at a density of 2000 cells per well and treated with various concentrations of Periplocin (62.5nM, 125nM, 250nM, and 500nM) for 48h, CCK-8 reagent was added, and absorbance was measured at 450nm. |
Reaction Conditions | 62.5nM, 125nM, 250nM, and 500nM; 48h |
Applications | Periplocin treatment significantly inhibited the viability of TPC-1 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Female nude mice |
Preparation Method | Six-week-old female nude mice were raised in a standard sterile environment, and 1×106 A549 cells were suspended in 100µl PBS and injected subcutaneously into the mice. When the tumor volume reached approximately 50mm3, the mice were randomly divided into three groups and received intraperitoneal injection of vehicle (5% DMSO, 10% ethanol, and 85% saline), Periplocin (15mg/kg/day), or imidazole ketone erastin (IKE) (40mg/kg/day) for two weeks. The tumor size was measured using a vernier caliper every two days. And calculate the tumor volume via the formula: (length×width2)×(1/2). |
Dosage form | 15mg/kg/day for 14 days; i.p. |
Applications | Periplocin treatment markedly reduced tumor growth in A549 cell-xenograft mice. |
References: | |
| Cas No. | 13137-64-9 | SDF | |
| 别名 | 杠柳毒苷 | ||
| Canonical SMILES | C[C@@]12[C@@](CC[C@@H]2C(CO3)=CC3=O)(O)[C@]4([H])CC[C@]5(O)C[C@@H](O[C@]6([H])O[C@H](C)[C@@H](O[C@@]7([H])[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O7)[C@@H](OC)C6)CC[C@]5(C)[C@@]4([H])CC1 | ||
| 分子式 | C36H56O13 | 分子量 | 696.8 |
| 溶解度 | DMF: 10 mg/ml,DMSO: 10 mg/ml,DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml | 储存条件 | 4°C, protect from light |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.4351 mL | 7.1757 mL | 14.3513 mL |
| 5 mM | 287 μL | 1.4351 mL | 2.8703 mL |
| 10 mM | 143.5 μL | 717.6 μL | 1.4351 mL |
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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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2.
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