Veratramine
(Synonyms: 黎芦碱; NSC17821; NSC23880) 目录号 : GC37895
Veratramine是一种脂溶性生物碱,存在于多种百合科植物中。
Cas No.:60-70-8
Sample solution is provided at 25 µL, 10mM.
Veratramine, a lipid-soluble alkaloid, is found in a variety of plants of the lily family [1]. Veratramine can reduce blood pressure, antagonize sodium ion channels and function as an analgesic [2]. Veratramine is widely used as an anti-cancer agent to inhibit the vitality of cancer cells in various cell models[3].
In vitro, Veratramine treatment for 24 hours can significantly inhibited cell proliferation of A172 cells, HS-683 cells, and T98G cells, with IC50 values of 88.81μM, 77.82μM, and 87.12μM, respectively[4]. The 10μM Veratramine treatment of Vero-E6 cells for 2 hours significantly reduced the PEDV-nucleocapsid (N) protein after α-coronavirus porcine epidemic diarrhea virus (PEDV) infection and inhibited the PI3K/Akt activity induced by PEDV[5]. Treatment with 20μM Veratramine for 60 minutes significantly inhibited EGF-induced activator protein-1 (AP-1) transcriptional activation and EGF-induced transformation of JB6 P+ cells[6].
In vivo, Veratramine treatment via daily tail vein injection at 50μg/kg/day for 4 weeks alleviated neuropathic pain in the diabetic rat model and reduced spinal cord and sciatic nerve damage[7]. Veratramine treatment (2mg/kg; 3 times a week) via tail vein injection for 4 weeks significantly inhibited subcutaneous tumor growth of liver cancer cells in the xenograft model of mice, with a low systemic toxicity[8].
References:
[1] Seale J T, McDougal O M. Veratrum parviflorum: an underexplored source for bioactive steroidal alkaloids[J]. Molecules, 2022, 27(16): 5349.
[2] Dirks M L, Seale J T, Collins J M, et al. Veratrum californicum alkaloids[J]. Molecules, 2021, 26(19): 5934.
[3] Tang J, Li H L, Shen Y H, et al. Antitumor and antiplatelet activity of alkaloids from veratrum dahuricum[J]. Phytotherapy Research, 2010, 24(6): 821-826.
[4] Kim D, Kwon W, Park S, et al. Anticancer effects of veratramine via the phosphatidylinositol-3-kinase/serine-threonine kinase/mechanistic target of rapamycin and its downstream signaling pathways in human glioblastoma cell lines[J]. Life Sciences, 2022, 288: 120170.
[5] Chen H, Zhao P, Zhang C, et al. Veratramine inhibits porcine epidemic diarrhea virus entry through macropinocytosis by suppressing PI3K/Akt pathway[J]. Virus Research, 2024, 339: 199260.
[6] Bai F, Liu K, Li H, et al. Veratramine modulates AP-1-dependent gene transcription by directly binding to programmable DNA[J]. Nucleic acids research, 2018, 46(2): 546-557.
[7] Zhang Y, Ye G, Chen Y, et al. Veratramine ameliorates pain symptoms in rats with diabetic peripheral neuropathy by inhibiting activation of the SIGMAR1-NMDAR pathway[J]. Pharmaceutical Biology, 2022, 60(1): 2145-2154.
[8] Yin L, Xia Y, Xu P, et al. Veratramine suppresses human HepG2 liver cancer cell growth in vitro and in vivo by inducing autophagic cell death[J]. Oncology Reports, 2020, 44(2): 477-486.
Veratramine是一种脂溶性生物碱,存在于多种百合科植物中[1]。Veratramine具有降压、钠离子通道拮抗和镇痛作用[2]。Veratramine作为抗癌剂广泛应用于多种细胞模型中抑制癌细胞活力[3]。
在体外,Veratramine处理24小时可显著抑制A172、HS-683和T98G细胞增殖,IC50值分别为88.81μM、77.82μM和87.12μM[4]。10μM的Veratramine处理Vero-E6细胞2小时能显著降低α-冠状病毒猪流行性腹泻病毒(PEDV)感染后的PEDV-核衣壳(N)蛋白水平,并抑制PEDV诱导的PI3K/Akt活性[5]。20μM的Veratramine处理60分钟可显著抑制EGF诱导的激活蛋白-1(AP-1)转录激活及JB6 P+细胞转化[6]。
在体内,糖尿病大鼠模型每日尾静脉注射Veratramine(50μg/kg/day;持续4周)可缓解神经病理性疼痛并减轻脊髓和坐骨神经损伤[7]。肝细胞癌异种移植瘤小鼠每周三次尾静脉注射Veratramine(2mg/kg;持续4周)能显著抑制皮下肿瘤生长,且全身毒性较低[8]。
Cell experiment [1]: | |
Cell lines | A172 cells |
Preparation Method | A172 cells were cultured in RPMI-1640 medium containing 10% FBS, penicillin (100units/ml) and streptomycin (100units/ml), and were placed in a humidified incubator at 37°C and 5% CO2. A172 cells (1×103 cells per well) were seeded in 96-well plates and cultured for 24 hours. Then, the cells were treated with different concentrations of Veratramine (0, 10, 25, and 50µM) for 24, 48 and 72 hours. 10µl of CCK-8 solution was added to each well and the cells were further cultured for 4 hours. The absorbance was measured at 450nm using an enzyme reader. |
Reaction Conditions | 0, 10, 25, and 50µM; 24, 48 and 72h |
Applications | Veratramine treatment significantly inhibited A172 cell proliferation in a time- and dose-dependent manner. |
Animal experiment [2]: | |
Animal models | Female BALB/c mice |
Preparation Method | The liver cancer xenograft model was established by subcutaneous injection of human HepG2 cells (1×106 cells suspended in 0.1ml PBS for each mouse) into the armpits of female BALB/c mice (6–8 weeks old). Once the tumors reached a volume of approximately 75-100mm3, the mice were randomly divided into two groups, with five mice per group, a PBS group and Veratramine group. PBS (200µl) or Veratramine (2mg/kg) were injected into the mice via the tail vein. The mice were treated three times a week for 4 weeks. During the treatment, the weights of the mice and the volume of the tumors were measured every week. The volume of the tumors was calculated according to the following formula: V = 0.5 × length × width2. Three days after the last treatment, the mice were sacrificed. Subcutaneous tumors from the mice were excised and weighed. |
Dosage form | 2mg/kg; three times a week for 4 weeks; tail vein injection |
Applications | Veratramine treatment inhibited the subcutaneous tumor growth in mice. |
References: |
Cas No. | 60-70-8 | SDF | |
别名 | 黎芦碱; NSC17821; NSC23880 | ||
Canonical SMILES | O[C@H]1[C@H]([C@H](C2=C(C)C3=C(C=C2)[C@]4([H])CC=C(C[C@@H](O)CC5)[C@@]5(C)[C@@]4([H])C3)C)NC[C@@H](C)C1 | ||
分子式 | C27H39NO2 | 分子量 | 409.6 |
溶解度 | DMSO: ≥ 100 mg/mL (244.14 mM) | 储存条件 | Store at -20°C,protect from light |
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1 mg | 5 mg | 10 mg |
1 mM | 2.4414 mL | 12.207 mL | 24.4141 mL |
5 mM | 488.3 μL | 2.4414 mL | 4.8828 mL |
10 mM | 244.1 μL | 1.2207 mL | 2.4414 mL |
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