Corypalmine
(Synonyms: D-四氢药根碱,Discretinine) 目录号 : GC35732
Corypalmine ((R)-(+)-Corypalmine), an alkaloid isolated from Stephania cepharantha, is an inhibitor of prolyl endopeptidase/oligopeptidase (PREP/POP) with IC50 of 128.0 μM.
Cas No.:27313-86-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Corypalmine ((R)-(+)-Corypalmine), an alkaloid isolated from Stephania cepharantha, is an inhibitor of prolyl endopeptidase/oligopeptidase (PREP/POP) with IC50 of 128.0 μM.
[1] Li He, et al. Zhongguo Zhong Yao Za Zhi. 2010 May;35(10):1272-5. [2] Lucie Cahlíková, et al. Fitoterapia. 2015 Jun;103:192-6.
| Cas No. | 27313-86-6 | SDF | |
| 别名 | D-四氢药根碱,Discretinine | ||
| Canonical SMILES | OC1=C(OC)C=C2C(CCN3CC4=C(OC)C(OC)=CC=C4CC32)=C1 | ||
| 分子式 | C20H23NO4 | 分子量 | 341.4 |
| 溶解度 | DMSO : 33.33 mg/mL (97.63 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 | 2.9291 mL | 14.6456 mL | 29.2912 mL |
| 5 mM | 0.5858 mL | 2.9291 mL | 5.8582 mL |
| 10 mM | 0.2929 mL | 1.4646 mL | 2.9291 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。
Determination of Corypalmine in mouse blood by UPLC-MS/MS and its application to a pharmacokinetic study
Biomed Chromatogr 2018 Aug;32(8):e4255.PMID:29633295DOI:10.1002/bmc.4255.
In this work, a selective and sensitive ultra-performance liquid chromatography tandem mass spectrometry method was established and validated for determination of Corypalmine in mouse blood after oral or intravenous administration. A UPLC BEH C18 column was used to separate Corypalmine and berberrubine (internal standard) at 40°C. The mobile phase was composed of acetonitrile and 10 mmol/L ammonium acetate (containing 0.1% formic acid) at a flow rate of 0.4 mL/min, and the total run time was 4.0 min. Electrospray ionization in positive ion mode was applied; target fragment ions m/z 342.2 → 178.0 for Corypalmine and m/z 322.1 → 307.0 for berberrubine were identified with multiple reaction monitoring mode. The linear range was 1-1000 ng/mL (r > 0.995) and the lower limit of quantification for Corypalmine in plasma was 1.0 ng/mL. The intra- and inter-day precisions were both <14%. The range of accuracy in this method was 97.5-109.0%. Mean recovery was >69.6%, and the matrix effect was 96.8-107.6%. Based on its high sensitivity, specificity and reliability, this method was successfully applied to study the pharmacokinetic parameters of Corypalmine in mouse by oral and intravenous administration, and finally, the bioavailability of Corypalmine was identified at 4.6%.
[Alkaloids in stems and leaves of Stephania cepharantha]
Zhongguo Zhong Yao Za Zhi 2010 May;35(10):1272-5.PMID:20707195DOI:10.4268/cjcmm20101011.
Objective: To study the alkaloids in the stems and leaves of Stephania cepharantha. Method: The dried stems and leaves of S. cepharantha were percolated with 95% ethanol and the solvent was removed by rotary evaporation to give a concentrate, and the concentrate was extracted by petroleum ether and chloroform. Column chromatograghy on MCI CHP 20P, silica gel, Rp-18, Sephadex LH-20 and polyamide were applied for the isolation and purification of the chloroform fraction. The structures were elucidated by their physicochemical properties and spectral data. Result: Eleven alkaloids were obtained and identified as lysicamine (1), tetrahadropalmatine (2), palmatine (3), isocorydione (4), corydalmine (5), Corypalmine (6), sinoracutine (7), sinoacutine (8), cepharamine (9), isocorydine (10) and corydine (11). Conclusion: Compounds 2-7 were isolated from S. cepharantha for the first time, and compound 7 was isolated from the genus Stephania for the first time, compound 4 was isolated from the Menispermaceae family for the first time.
Isoquinoline alkaloids as prolyl oligopeptidase inhibitors
Fitoterapia 2015 Jun;103:192-6.PMID:25863351DOI:10.1016/j.fitote.2015.04.004.
Prolyl oligopeptidase is a cytosolic serine peptidase that hydrolyses proline-containing peptides at the carboxy terminus of proline residues. It has been associated with schizophrenia, bipolar affective disorder, and related neuropsychiatric disorders and therefore may have important clinical implications. Thirty-one isoquinoline alkaloids of various structural types, previously isolated in our laboratory, were screened for their ability to inhibit prolyl oligopeptidase. Promising results have been showed by alkaloids californidine (IC50=55.6±3.5 μM), dihydrosanquinarine (IC50=99.1±7.6 μM), Corypalmine (IC50=128.0±10.5 μM) and N-methyllaurotetanine (IC50=135.0±11.7 μM).
Cytotoxicity and bacterial membrane destabilization induced by Annona squamosa L. extracts
An Acad Bras Cienc 2017;89(3 Suppl):2053-2073.PMID:28813096DOI:10.1590/0001-3765201720150702.
This study aimed to further investigate the cytotoxicity against tumor cell lines and several bacterial strains of Annona squamosa and its mode of action. Methanol extracts of A. squamosa leaves (ASL) and seeds (ASS) were used. ASL showed significant antibacterial activity against S. aureus, K. pneumoniae and E. faecalis with MIC values of 78, 78 and 39 µg/mL respectively. Moreover, ASL exhibited significant biofilm disruption, rapid time dependent kinetics of bacterial killing, increased membrane permeability and significantly reduced the cell numbers and viability. Regarding the cytotoxicity against tumor cell lines, ASS was more active against Jurkat and MCF-7 cells, with CI50 1.1 and 2.1 µg/mL, respectively. ASL showed promising activity against Jurkat and HL60, with CI50 4.2 and 6.4 µg/mL, respectively. Both extracts showed lower activity against VERO cells and reduced the clonogenic survival at higher concentrations (IC90) to MCF-7 and HCT-116 lineages. The alkaloids anonaine, asimilobine, Corypalmine, liriodenine nornuciferine and reticuline were identified in extracts by UPLC-ESI-MS/MS analysis. This study reinforced that A. squamosa presents a remarkable phytomedicinal potential and revealed that its antimicrobial mechanism of action is related to bacterial membrane destabilization.
7,7-Dimethylaporphine alkaloids from the stem of Guatteriopsis friesiana
J Nat Prod 2009 Aug;72(8):1516-9.PMID:19639965DOI:10.1021/np800788n.
Phytochemical investigation of a methanolic extract of the stem of Guatteriopsis friesiana afforded two new 7,7-dimethylaporphine alkaloids, 6,6a-dihydrodemethoxyguadiscine (1) and guatteriopsiscine (3), together with demethoxyguadiscine (2), liriodenine (4), Corypalmine (5), and coreximine (6). Their structures were elucidated on the basis of spectroscopic methods (UV, IR, EIMS, HRESIMS, 1D/2D NMR). The absolute configurations of 1 and 3 were determined from the circular dichroism curves. The presence of 7,7-dimethylaporphine alkaloids in this species is important for the chemotaxonomy of Guatteriopsis. Antimicrobial activity of compounds 1-5 was investigated, and 4 showed activity against Rhodococcus equi, with a MIC value of 10 microg x mL(-1).