Lycoramine
(Synonyms: 二氢加兰他敏) 目录号 : GC64557
Lycoramine 是一种从 Lycoris radiate 中分离出的加兰他敏的二氢衍生物。Lycoramine 是一种有效的乙酰胆碱酯酶 (AChE) 抑制剂。
Cas No.:21133-52-8
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
Lycoramine, a dihydro-derivative of galanthamine, is isolated from Lycoris radiate. Lycoramine is a potent acetylcholinesterase (AChE) inhibitor[1][2].
[1]. Yuan Y, et, al. Online acetylcholinesterase inhibition evaluation by high-performance liquid chromatography-mass spectrometry hyphenated with an immobilized enzyme reactor. J Chromatogr A. 2020 Jan 4; 1609:460506.
[2]. IRWIN RL, et, al. Cholinesterase inhibition by galanthamine and lycoramine. Biochem Pharmacol. 1960 May; 3:147-8.
| Cas No. | 21133-52-8 | SDF | Download SDF |
| 别名 | 二氢加兰他敏 | ||
| 分子式 | C17H23NO3 | 分子量 | 289.37 |
| 溶解度 | DMSO : 100 mg/mL (345.58 mM; Need ultrasonic) | 储存条件 | 4°C, protect from light |
| 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 | 3.4558 mL | 17.2789 mL | 34.5578 mL |
| 5 mM | 0.6912 mL | 3.4558 mL | 6.9116 mL |
| 10 mM | 0.3456 mL | 1.7279 mL | 3.4558 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。
Evaluation of the Therapeutic Effect of Lycoramine on Alzheimer's Disease in Mouse Model
Curr Med Chem 2021;28(17):3449-3473.PMID:33200692DOI:10.2174/0929867327999201116193126.
Background: Alzheimer's disease is one of the leading health problems characterized by the accumulation of Aβ and hyperphosphorylated tau that account for the senile plaque formations causing extensive cognitive decline. Many of the clinical diagnoses of Alzheimer's disease are made in the late stages, when the pathological changes have already progressed. Objective: The objective of this study is to evaluate the promising therapeutic effects of a natural compound, Lycoramine, which has been shown to have therapeutic potential in several studies and to understand its mechanism of action on the molecular level via differential protein expression analyses. Methods: Lycoramine and galantamine, an FDA approved drug used in the treatment of mild to moderate AD, were administered to 12 month-old 5xFAD mice. Effects of the compounds were investigated by Morris water maze, immunohistochemistry and label- free differential protein expression analyses. Results: Here we demonstrated the reversal of cognitive decline via behavioral testing and the clearance of Aβ plaques. Proteomics analysis provided in-depth information on the statistically significant protein perturbations in the cortex, hippocampus and cerebellum sections to hypothesize the possible clearance mechanisms of the plaque formation and the molecular mechanism of the reversal of cognitive decline in a transgenic mouse model. Bioinformatics analyses showed altered molecular pathways that can be linked with the reversal of cognitive decline observed after Lycoramine administration but not with galantamine. Conclusion: Lycoramine shows therapeutic potential to halt and reverse cognitive decline at the late stages of disease progression, and holds great promise for the treatment of Alzheimer's disease.
Total Syntheses of Galanthamine and Lycoramine via a Palladium-Catalyzed Cascade Cyclization and Late-Stage Reorganization of the Cyclized Skeleton
Org Lett 2021 Dec 17;23(24):9659-9663.PMID:34874174DOI:10.1021/acs.orglett.1c03943.
Herein, we report the highly efficient total syntheses of galanthamine and Lycoramine from a common tetracyclic intermediate. This concise synthetic route features a two-phase strategy, which includes the early-stage rapid construction of a tetracyclic skeleton followed by the late-stage selective reorganization of the tetracyclic skeleton. Key to the success of this strategy are a palladium-catalyzed carbonylative cascade annulation, a DDQ-mediated intramolecular regioselective oxidative lactamization, as well as a BF3·Et2O-promoted reorganization of the bridged tetracyclic skeleton.
Total Synthesis of Galanthamine and Lycoramine Featuring an Early-Stage C-C and a Late-Stage Dehydrogenation via C-H Activation
Org Lett 2020 Feb 21;22(4):1244-1248.PMID:31904968DOI:10.1021/acs.orglett.9b04337.
Herein, we report a novel strategy toward galanthamine and Lycoramine. The concise synthesis was enabled by a Rh-catalyzed gram-scale C-C activation for the tetracyclic carbon framework and a regioselective Pd-catalyzed C-H activation for double-bond introduction. An aqueous-phase Beckmann rearrangement was performed for nitrogen atom insertion. Galanthamine and Lycoramine were completed in 11 and 10 steps, respectively.
Alkaloid accumulation in different parts and ages of Lycoris chinensis
Z Naturforsch C J Biosci 2010 Jul-Aug;65(7-8):458-62.PMID:20737914DOI:10.1515/znc-2010-7-807.
The galanthamine, lycorine, and Lycoramine content of Lycoris chinensis was researched during development from young to old plants, i.e. in seeds, ten-day-old seedlings, three-month-old seedlings, one-year-old seedlings, and perennial seedlings. Notably the alkaloid level reduced to its lowest content 10 days after seed germinating. Then the accumulation of galanthamine tended to increase with age, reaching a higher value in perennial seedlings. The production pattern of lycorine and Lycoramine was found similar to that of galanthamine. Different plant organs were also evaluated for their galanthamine, lycorine, and Lycoramine contents. Mature seeds had the highest content of galanthamine (671.33 microg/g DW). Kernels, seed capsules, and root-hairs were the main repository sites for galanthamine, lycorine, and Lycoramine. The leaves were the least productive organs.
Alkaloids of Lycoris guangxiensis1
Planta Med 1987 Jun;53(3):259-61.PMID:17269013DOI:10.1055/s-2006-962697.
A new alkaloid, N-allylnorgalanthamine ( 1), was isolated from the bulbs of LYCORIS GUANGXIENSIS Y. Hsu et Q. J. Fan (Amaryllidaceae). Additionally, seven known alkaloids, lycorine, narwedine, galanthamine, Lycoramine, crinine, norgalanthamine, and pseudolycorine were also obtained. The structure of 1 was established through the interpretation of spectral data.