Narciclasine
(Synonyms: 水仙环素; Lycoricidinol) 目录号 : GC12491
Narciclasine是一种具有抗有丝分裂和促凋亡活性的植物生长调节剂。
Cas No.:29477-83-6
Sample solution is provided at 25 µL, 10mM.
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Narciclasine is a plant growth regulator with antimitotic activity and pro-apoptotic property [1]. Narciclasine can interact with the ribosomal 60S subunit and inhibit peptide bond formation by preventing the 3' end of the donor substrate from binding to the peptidyl transferase center, thereby reducing protein synthesis [2]. Narciclasine has been widely used to induce mitochondrial membrane potential depolarization and eliminate pathogenic parasites[3].
In vitro, Narciclasine treatment for 48 hours significantly inhibited the viability of HCT116, MDA-MB-231, and HT-29 cells with IC50 values of 0.108µM, 0.0495µM, and 1.205µM, respectively[4]. Treatment of SCC-47 cells with 100nM of Narciclasine for 24 hours resulted in decreased expression of the mesenchymal markers N-cadherin and β-catenin and inhibited cell migration and invasion[5]. Treatment of BCG-823 cells with 1µM of Narciclasine for 24 hours inhibited the proliferation of BCG-823 cells, inhibited the levels of p-AKT and p-mTOR, and promoted apoptosis and autophagy[6].
In vivo, Narciclasine treatment via oral administration at a dose of 1mg/kg/week for seven weeks attenuated high-fat diet-induced obesity in mice, reduced fat mass accumulation, and enhanced mitochondrial respiration and fatty acid oxidation in skeletal muscle[7]. Daily intraperitoneal injection of Narciclasine (1mg/kg/day) for 14 days reduced VEGF-induced angiogenesis in mice[8]. Subcutaneous administration of Narciclasine (1mg/kg) 12h prior to intraperitoneal injection of zymosan A attenuated inflammation and blocked leukocyte adhesion and transendothelial migration in a mouse model of zymosan-induced peritonitis[9].
References:
[1] Ingrassia L, Lefranc F, Dewelle J, et al. Structure− activity relationship analysis of novel derivatives of narciclasine (an Amaryllidaceae isocarbostyril derivative) as potential anticancer agents[J]. Journal of medicinal chemistry, 2009, 52(4): 1100-1114.
[2] Nair J J, van Staden J. Insight to the antifungal properties of Amaryllidaceae constituents[J]. Phytomedicine, 2020, 73: 152753.
[3] Gomes K S, Costa-Silva T A, Borges W S, et al. Antiparasitic Activity of Narciclasine and Evaluation of Its Effects on Plasma Membrane and Mitochondria of Trypanosoma cruzi[J]. ACS omega, 2025, 10(3): 3025-3032.
[4] Wang M, Liang L, Wang R, et al. Narciclasine, a novel topoisomerase I inhibitor, exhibited potent anti-cancer activity against cancer cells[J]. Natural Products and Bioprospecting, 2023, 13(1): 27.
[5] Shieu M K, Ho H Y, Lin C C, et al. Narciclasine suppresses oral cancer metastasis by modulating cathepsin B and extracellular signal–related kinase pathways[J]. Biomedicine & Pharmacotherapy, 2023, 158: 114159.
[6] Yuan Y, He X, Li X, et al. Narciclasine induces autophagy-mediated apoptosis in gastric cancer cells through the Akt/mTOR signaling pathway[J]. BMC Pharmacology and Toxicology, 2021, 22(1): 70.
[7] Julien S G, Kim S Y, Brunmeir R, et al. Narciclasine attenuates diet-induced obesity by promoting oxidative metabolism in skeletal muscle[J]. PLoS biology, 2017, 15(2): e1002597.
[8] Bräutigam J, Bischoff I, Schürmann C, et al. Narciclasine inhibits angiogenic processes by activation of Rho kinase and by downregulation of the VEGF receptor 2[J]. Journal of Molecular and Cellular Cardiology, 2019, 135: 97-108.
[9] Stark A, Schwenk R, Wack G, et al. Narciclasine exerts anti‐inflammatory actions by blocking leukocyte–endothelial cell interactions and down‐regulation of the endothelial TNF receptor 1[J]. The FASEB Journal, 2019, 33(8): 8771-8781.
Narciclasine是一种具有抗有丝分裂和促凋亡活性的植物生长调节剂[1]。Narciclasine可通过与核糖体60S亚基相互作用，抑制肽键形成从而减少蛋白质合成[2]。Narciclasine已广泛应用于诱导线粒体膜电位去极化以及清除致病性寄生虫[3]。
在体外，Narciclasine处理48小时能显著抑制HCT116、MDA-MB-231和HT-29细胞活力，IC50值分别为0.108µM、0.0495µM和1.205µM[4]。使用100nM的Narciclasine处理SCC-47细胞24小时，可降低间充质标志物N-钙黏蛋白和β-catenin的表达，并抑制细胞迁移和侵袭[5]。用1µM的Narciclasine处理BCG-823细胞24小时，能抑制细胞增殖，降低p-AKT和p-mTOR水平，并促进细胞凋亡和自噬[6]。
在体内，每周口服1mg/kg/week剂量的Narciclasine连续七周，可减轻高脂饮食诱导的小鼠肥胖，减少脂肪堆积，并增强骨骼肌线粒体呼吸和脂肪酸氧化[7]。每日腹腔注射1mg/kg/day剂量的Narciclasine连续14天，能抑制VEGF诱导的小鼠血管生成[8]。在zymosan A诱导的小鼠腹膜炎模型中，腹腔注射zymosan A前12小时皮下注射1mg/kg剂量的Narciclasine，可减轻炎症反应并阻断白细胞黏附和跨内皮迁移[9]。
| Cell experiment [1]: | |
Cell lines | H1299 cells |
Preparation Method | H1299 cells were cultured in RPMI 1640 medium supplemented with 10% fetal bovine serum (FBS) and 1% penicillin/streptomycin. The cells were cultured in a humidified incubator at 37℃ with 5% CO2. Cells suspended in 100µl/ well medium were seeded in 96-well plates at a density of 5400 cells per well and cultured for 24 hours. Cells were treated with different concentrations of Narciclasine (0, 50, 100, 200, 400, 800, 1000, 1200, and 1400nM) for 48 hours. 20µl of MTT solution (5mg/ml) was added to each well, and the culture was continued for 4 hours at 37°C. The supernatant was discarded, 100µl DMSO was added to each well to dissolve methylene dye, and the absorbance at 570nm was measured. |
Reaction Conditions | 0, 50, 100, 200, 400, 800, 1000, 1200, and 1400nM; 48h |
Applications | Narciclasine treatment inhibited the cell viability of H1299 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | C57BL/6J mice |
Preparation Method | Eight-week-old male C57BL/6J mice were housed in a 12h light/12h dark cycle with free access to water. The mice were divided into two groups: fed with a normal diet (NCD) and a high-fat diet (HFD). NCD and HFD mice were treated with Narciclasine (1mg/kg/week) or vehicle by gavage once a week for 7 weeks starting from 10 weeks of age. Body weight and visceral and subcutaneous fat were analyzed. |
Dosage form | 1mg/kg/week for 7 weeks; p.o. |
Applications | Narciclasine treatment significantly reduced HFD-induced weight gain and, promoted the reduction of visceral and subcutaneous fat in mice. |
References: | |
| Cas No. | 29477-83-6 | SDF | |
| 别名 | 水仙环素; Lycoricidinol | ||
| 化学名 | (2S,3R,4S,4aR)-2,3,4,7-tetrahydroxy-3,4,4a,5-tetrahydro-2H-[1,3]dioxolo[4,5-j]phenanthridin-6-one | ||
| Canonical SMILES | C1OC2=C(O1)C(=C3C(=C2)C4=CC(C(C(C4NC3=O)O)O)O)O | ||
| 分子式 | C14H13NO7 | 分子量 | 307.26 |
| 溶解度 | ≥ 14.7mg/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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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.2546 mL | 16.2729 mL | 32.5457 mL |
| 5 mM | 650.9 μL | 3.2546 mL | 6.5091 mL |
| 10 mM | 325.5 μL | 1.6273 mL | 3.2546 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.50%
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