Roemerine
(Synonyms: 莲碱,(-)-Roemerine) 目录号 : GC63175
An aporphine alkaloid with diverse biological activities
Cas No.:548-08-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Remerin is an aporphine alkaloid that has been found in N. nucifera and has diverse biological activities.1,2,3,4 It selectively binds to the serotonin (5-HT) receptor subtype 5-HT2A over 5-HT1A and dopamine D1 and D2 receptors (Kis = 0.0621, 1.17, 1.4, and 22.6 ?M, respectively).2 Remerin is active against C. albicans as well as chloroquine-resistant and -sensitive strains of P. falciparum with IC50 values of 4.5, 0.4, and 0.2 ?g/ml, respectively.1 It enhances cytotoxicity induced by vinblastine in multidrug-resistant KB-V1 oral epidermoid carcinoma cells.3 Remerin (20 mg/kg) improves survival in a mouse model of sepsis induced by methicillin-resistant S. aureus (MRSA).4
1.Agnihotri, V.K., ElSohly, H.N., Khan, S.I., et al.Constituents of Nelumbo nucifera leaves and their antimalarial and antifungal activityPhytochem. Lett.1(2)89-93(2008) 2.Munusamy, V., B.K., Y., Buckle, M.J.C., et al.Structure-based identification of aporphines with selective 5-HT2A receptor-binding activityChem. Biol. Drug Des.81(2)250-256(2012) 3.You, M., Wickramaratne, D.B.M., Silva, G.L., et al.(?)-Roemerine, an aporphine alkaloid from Annona senegalensis that reverses the multidrug-resistance phenotype with cultured cellsJ. Nat. Prod.58(4)598-604(1995) 4.Yin, S., Rao, G., Wang, J., et al.Roemerine improves the survival rate of septicemic BALB/c mice by increasing the cell membrane permeability of Staphylococcus aureusPLoS One10(11)e0143863(2015)
| Cas No. | 548-08-3 | SDF | |
| 别名 | 莲碱,(-)-Roemerine | ||
| 分子式 | C18H17NO2 | 分子量 | 279.33 |
| 溶解度 | 储存条件 | ||
| 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 | 3.58 mL | 17.9 mL | 35.7999 mL |
| 5 mM | 0.716 mL | 3.58 mL | 7.16 mL |
| 10 mM | 0.358 mL | 1.79 mL | 3.58 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。
Neuroactivity of the naturally occurring aporphine alkaloid, Roemerine
Nat Prod Res 2021 Dec;35(24):6147-6152.PMID:33025828DOI:10.1080/14786419.2020.1830395.
Roemerine is a naturally occurring aporphine alkaloid. In this study, we screened a conformer library of Food and Drug Administration (FDA)-approved drugs to identify similar drugs that can assist in identifying the biological targets of Roemerine. To assess the neuroactivity in vitro, we measured the levels of cell metabolites, Brain-Derived Neurotrophic Factor (BDNF) and serotonin (5-HT) in SH-SY5Y cell line. By means of structure-based virtual screening, we identified five drugs that are similar to Roemerine; mirtazapine, atomoxetine, epinastine, diphenhydramine and orphenadrine. GC-MS metabolomics study revealed that Roemerine has a high impact on alanine-aspartate-glutamate pathway in cell lysate and cultured medium. Additionally, Roemerine increased intercellular 5-HT level and intracellular BDNF protein expression at 10 µM. In conclusion, Roemerine - a major alkaloid in antidepressant-like effect possessing plants (P. lacerum and P. syriacum) - has a neuronal activity through increasing BDNF protein expression and affecting serotonergic and glutamatergic systems in SH-SY5Y cell line.
Roemerine Improves the Survival Rate of Septicemic BALB/c Mice by Increasing the Cell Membrane Permeability of Staphylococcus aureus
PLoS One 2015 Nov 25;10(11):e0143863.PMID:26606133DOI:10.1371/journal.pone.0143863.
Staphylococcus aureus is one of the most frequently occurring hospital- and community-associated pathogenic bacteria featuring high morbidity and mortality. The occurrence of methicillin-resistant S. aureus (MRSA) has increased persistently over the years. Therefore, developing novel anti-MRSA drugs to circumvent drug resistance of S. aureus is highly important. Roemerine, an aporphine alkaloid, has previously been reported to exhibit antibacterial activity. The present study aimed to investigate whether Roemerine can maintain these activities against S.aureus in vivo and further explore the underlying mechanism. We found that Roemerine is effective in vitro against four S. aureus strains as well as in vivo against MRSA insepticemic BALB/c mice. Furthermore, Roemerine was found to increase cell membrane permeability in a concentration-dependent manner. These findings suggest that Roemerine may be developed as a promising compound for treating S. aureus, especially methicillin-resistant strains of these bacteria.
An LC-ESI-MS/MS method for the simultaneous determination of pronuciferine and Roemerine in some Papaver species
J Chromatogr B Analyt Technol Biomed Life Sci 2018 Oct 1;1096:223-227.PMID:30189375DOI:10.1016/j.jchromb.2018.08.020.
Papaver species, well known for their alkaloids, have been used for the treatment of several diseases, such as inflammation, diarrhea, depression, and sleep disorders in certain parts of Anatolia. In this study, four Papaver species (P. lacerum, P. syriacum, P. glaucum and P. rhoeas) were collected from different localities of Turkey. Methanolic extracts were prepared from the aerial parts of the plants. A rapid analytical method was developed for the simultaneously quantitative analysis of two alkaloids, pronuciferine and Roemerine, using liquid chromatography tandem mass spectrometry. Multiple reaction monitoring in the positive ionization mode was used for detection. Pronuciferine and Roemerine were analyzed on a C18 column (2.1 × 50 mm, 3 μm) with the mobile phase run in the gradient mode with 0.1% formic acid in water (A) and 0.1% formic acid in acetonitrile at a flow rate of 0.3 mL/min. The transitions 312.1→283.1 m/z and 280.0→249.0 m/z were used to monitor pronuciferine and Roemerine, respectively. The assay was linear in the concentration range of 0.01 μg/mL to 1 μg/mL (r = 0.996 for Roemerine, r = 0.998 for pronuciferine). The validation studies revealed that the method was linear, sensitive, accurate, precise, selective, repeatable, robust, and rugged. Finally, the developed method was applied to quantify pronuciferine and Roemerine in the selected species. The amounts of pronuciferine and Roemerine were respectively found as 8.5 to 48 μg/g and 4.4 to 43,000 μg/g.
[Anti-prostate cancer effect of Roemerine: An experimental study]
Zhonghua Nan Ke Xue 2017 Jan;23(1):27-33.PMID:29658233doi
Objective: To investigate the anti-prostate cancer (PCa) effect of Roemerine in vitro and in vivo in the mouse model of PCa. Methods: We detected the effects of Roemerine on the proliferation, apoptosis and migration of PCa cells DU145, LNCaP, PC-3 and 22RV1, screened out the sensitive cell line and constructed a tumor-bearing model in mice for verification of the antitumor efficacy of Roemerine in vivo. Results: Roemerine inhibited the proliferation and migration of the DU145, LNCaP, PC-3 and 22RV1 cells and induced their apoptosis in different degrees, particularly those of the LNCaP cells. The average tumor weight was less in the Roemerine intervention group (［1.99±0.95］ g) than in the control (［2.95±1.04］ g), the least in the high-dose Roemerine (30 mg/kg) plus paclitaxel intervention group (［0.90±0.16］ g). The mean heart, liver, and kidney indexes were markedly lower in the Roemerine (0.58±0.06, 6.20±0.42 and 1.49±0.33) than in the paclitaxel group (0.66±0.04, 6.99±0.72 and 1.95±0.34), while the mean spleen and thymus indexes were remarkably higher in the former (0.54±0.11 and 0.06±0.01) than in the latter (0.41±0.09 and 0.05±0.01). Pathological staining showed a lower degree of malignancy and metastasis in both the Roemerine and the Roemerine + paclitaxel intervention group than in the control, as well as a lower degree of visceral injury in the Roemerine and Roemerine + paclitaxel groups than in the paclitaxel group. Conclusions: Roemerine has some anti-PCa effect and alleviates adverse reactions in paclitaxel combination administration.
Synthesis and evaluation of nuciferine and Roemerine enantiomers as 5-HT2 and α1 receptor antagonists
Medchemcomm 2018 Feb 26;9(3):576-582.PMID:30108948DOI:10.1039/c7md00629b.
In this study, the (S)-enantiomers of the aporphine alkaloids, nuciferine and Roemerine, were prepared via a synthetic route involving catalytic asymmetric hydrogenation and both stereoisomers were evaluated in vitro for functional activity at human 5-HT2 and adrenergic α1 receptor subtypes using a transforming growth factor-α shedding assay. Both enantiomers of each of the compounds were found to act as antagonists at 5-HT2 and α1 receptors. (R)-roemerine was the most potent compound at 5-HT2A and 5-HT2C receptors (pKb = 7.8-7.9) with good selectivity compared to (S)-roemerine at these two receptors and compared to its activity at 5-HT2B, α1A, α1B and α1D receptors.