Cepharanthine
(Synonyms: 千金藤碱) 目录号 : GN10113
Cepharanthine是一种双苄基异喹啉生物碱，具有强效抗病毒活性，对SARS-CoV-2和HIV-1的EC50值分别为0.15µM和0.026µM。
Cas No.:481-49-2
Sample solution is provided at 25 µL, 10mM.
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Cepharanthine, a bisbenzylisoquinoline alkaloid, has potent antiviral activity with the EC50 values of 0.15µM and 0.026µM for SARS-CoV-2 and HIV-1, respectively[1]. Cepharanthine effectively reversed most of the dysregulated genes and pathways in virus-infected cells, including endoplasmic reticulum (ER) stress/unfolded protein response and heat shock factor 1 (HSF1)-mediated heat shock response[2]. Cepharanthine has been widely used as an anti-inflammatory agent to reduce the levels of TNF-α, IL-1β and IL-6 in cellular and animal models[3].
In vitro, Cepharanthine treatment for 48 hours significantly inhibited the proliferation of Eca109 cells with an IC50 value of 6.20 ± 0.17μM[4]. Treatment with 20μM Cepharanthine for 24 hours significantly inhibited the viability of HT1376 cells, reduced the migration and invasion of cells, and activated the Rap1 signaling pathway in the cells[5]. Pretreatment with 10μM Cepharanthine for 1h significantly inhibited lipopolysaccharide-induced NO production and iNOS and COX-2 expression in RAW264.7 cells[6].
In vivo, Cepharanthine (20mg/kg) administered intraperitoneally once every two days for 24 days significantly suppressed tumor weight and volume in a mouse model of hepatocellular carcinoma and reduced Ki67 expression in tumor tissues[7]. Cepharanthine treatment at a dose of 15mg/kg once weekly via intraperitoneal injection for 12 weeks significantly ameliorated cartilage degeneration and prevented osteoarthritis (OA) in a mouse OA model[8].
References:
[1] Liu K, Hong B, Wang S, et al. Pharmacological activity of cepharanthine[J]. Molecules, 2023, 28(13): 5019.
[2] Shi L, Wang S, Zhang S, et al. Research progress on pharmacological effects and mechanisms of cepharanthine and its derivatives[J]. Naunyn-Schmiedeberg's Archives of Pharmacology, 2023, 396(11): 2843-2860.
[3] Liang D, Li Q, Du L, et al. Pharmacological effects and clinical prospects of cepharanthine[J]. Molecules, 2022, 27(24): 8933.
[4] Zhou P, Zhang R, Wang Y, et al. Cepharanthine hydrochloride reverses the mdr1 (P-glycoprotein)-mediated esophageal squamous cell carcinoma cell cisplatin resistance through JNK and p53 signals[J]. Oncotarget, 2017, 8(67): 111144.
[5] Chen B, Chen L, Yang J, et al. Cepharanthine inhibits migration, invasion, and EMT of bladder cancer cells by activating the Rap1 signaling pathway in vitro[J]. American journal of translational research, 2024, 16(5): 1602.
[6] Paudel K R, Karki R, Kim D W. Cepharanthine inhibits in vitro VSMC proliferation and migration and vascular inflammatory responses mediated by RAW264. 7[J]. Toxicology in vitro, 2016, 34: 16-25.
[7] Feng F, Pan L, Wu J, et al. Cepharanthine inhibits hepatocellular carcinoma cell growth and proliferation by regulating amino acid metabolism and suppresses tumorigenesis in vivo[J]. International journal of biological sciences, 2021, 17(15): 4340.
[8] Yao M, Zhang C, Ni L, et al. Cepharanthine ameliorates chondrocytic inflammation and osteoarthritis via regulating the MAPK/NF-κB-Autophagy pathway[J]. Frontiers in Pharmacology, 2022, 13: 854239.
Cepharanthine是一种双苄基异喹啉生物碱，具有强效抗病毒活性，对SARS-CoV-2和HIV-1的EC50值分别为0.15µM和0.026µM[1]。Cepharanthine能有效逆转病毒感染的细胞中大多数失调基因和通路，包括内质网（ER）应激/未折叠蛋白反应和热休克因子1（HSF1）介导的热休克反应[2]。Cepharanthine作为抗炎剂广泛被应用于细胞和动物模型，可降低TNF-α、IL-1β和IL-6水平[3]。
在体外，Cepharanthine处理48小时可显著抑制Eca109细胞增殖，IC50值为6.20 ± 0.17μM[4]。20μM的Cepharanthine处理HT1376细胞24小时能显著抑制细胞活力，减少细胞的迁移和侵袭，并激活Rap1信号通路[5]。10μM的Cepharanthine预处理RAW264.7细胞1小时可显著抑制脂多糖诱导的NO产生及iNOS和COX-2表达[5]。
在体内，肝细胞癌小鼠模型每两天腹腔注射Cepharanthine（20mg/kg；持续24天）能显著抑制肿瘤重量和体积，并降低肿瘤组织中Ki67表达[7]。骨关节炎小鼠模型每周腹腔注射15mg/kg剂量的Cepharanthine（持续12周）可显著改善软骨退化并预防骨关节炎进展[8]。
| Cell experiment [1]: | |
Cell lines | HT1376 cells |
Preparation Method | HT1376 cells were cultured in Roswell Park Memorial Institute-1640 medium supplemented with 10% fetal bovine serum (FBS) from a Chinese company and 1% antibiotics containing 100U/mL penicillin G and 100μg/mL streptomycin. Subsequently, cells were cultured under specific conditions maintained at 37°C, 5% CO2, and 70% to 80% humidity. HT1376 cells were seeded in 96-well plates at a density of 5000 cells per well. After cell attachment, cells were treated with different concentrations (0, 5, 10, 15, 20, 25, and 30μM) of Cepharanthine (dissolved in dimethyl sulfoxide) for 24h. After washing with PBS, the cells were treated with CCK-8 reagent and incubated with complete medium for 2h at 37°C to determine the absorbance at 450nm. |
Reaction Conditions | 0, 5, 10, 15, 20, 25, and 30μM; 24h |
Applications | Cepharanthine treatment reduced the cell viability of HT1376 cells in a concentration-dependent manner. |
| Animal experiment [2]: | |
Animal models | Female nude mice |
Preparation Method | Twenty female nude mice were maintained under standard conditions, and each nude mouse was subcutaneously injected with 2×106 Hep3B cells in the right axilla. When the tumor diameter was between 5-8mm, the mice were randomly divided into control group, a positive control group (cisplatin; 5mg/kg), and treatment group (Cepharanthine; 20mg/kg), with 5 mice in each group. The drug was injected intraperitoneally every 2 days, and the longest (L) and longitudinal (R) axes of the tumor were recorded. The tumor volume (V) was calculated according to the following formula: V=0.5×L×R2. After 24 days of treatment, the nude mice were sacrificed, and tumor tissues were collected and fixed overnight in 4% paraformaldehyde for subsequent immunohistochemical experiments. |
Dosage form | 20mg/kg every two days for 24 days; i.p. |
Applications | Cepharanthine treatment significantly inhibited tumor weight and volume in mice, and decreased Ki67 expression in tumor tissues. |
References: | |
| Cas No. | 481-49-2 | SDF | |
| 别名 | 千金藤碱 | ||
| Canonical SMILES | CN1CCC2=CC3=C(C4=C2C1CC5=CC=C(C=C5)OC6=C(C=CC(=C6)CC7C8=CC(=C(C=C8CCN7C)OC)O4)OC)OCO3 | ||
| 分子式 | C37H38N2O6 | 分子量 | 606.71 |
| 溶解度 | ≥ 21.9mg/mL in DMSO | 储存条件 | Store at -20°C |
| 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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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6482 mL | 8.2412 mL | 16.4823 mL |
| 5 mM | 329.6 μL | 1.6482 mL | 3.2965 mL |
| 10 mM | 164.8 μL | 824.1 μL | 1.6482 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
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，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
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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