Laurolitsine
(Synonyms: 去甲异波尔定,(+)-Norboldine) 目录号 : GC39010
Laurolitsine ((+)-Norboldine) 是从 Peumus boldus Molina 叶子中分离得到的一种生物碱。
Cas No.:5890-18-6
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
Laurolitsine ((+)-Norboldine) is an alkaloid isolated from the leaves of Peumus boldus Molina[1].
[1]. Teng CM, et al. Antiplatelet effects of some aporphine and phenanthrene alkaloids in rabbits and man. J Pharm Pharmacol. 1997 Jul;49(7):706-11.
| Cas No. | 5890-18-6 | SDF | |
| 别名 | 去甲异波尔定,(+)-Norboldine | ||
| Canonical SMILES | OC1=C(OC)C2=C3C(CCN[C@@]3([H])CC4=CC(O)=C(OC)C=C24)=C1 | ||
| 分子式 | C18H19NO4 | 分子量 | 313.35 |
| 溶解度 | Soluble in DMSO | 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 | 3.1913 mL | 15.9566 mL | 31.9132 mL |
| 5 mM | 0.6383 mL | 3.1913 mL | 6.3826 mL |
| 10 mM | 0.3191 mL | 1.5957 mL | 3.1913 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。
Laurolitsine ameliorates type 2 diabetes by regulating the hepatic LKB1-AMPK pathway and gut microbiota
Phytomedicine 2022 Nov;106:154423.PMID:36075181DOI:10.1016/j.phymed.2022.154423.
Background: Type 2 diabetes mellitus (DM) is a highly prevalent chronic metabolic disease. Effective antidiabetic drugs are needed to improve and expand the available treatments. Using the ob/ob diabetic mouse model, we previously demonstrated that the alkaloid-rich extract from Litsea glutinosa bark (CG) has potent antidiabetic effects and that Laurolitsine (LL) is the richest alkaloid in CG. Purpose: We conducted a systematic investigation of the antidiabetic effects and potential mechanisms of LL in vitro and in vivo. Methods: The antidiabetic effects of LL and its mechanisms of action were explored in HL-7702 hepatocytes in vitro and in db/db mice in vivo by a series of experiments, including cellular toxicity analysis, glucose consumption analysis, serum/liver biochemical analysis, pathological examinations, Western blots, RNA-seq analysis, and gut microbiota analysis. Results: LL stimulated glucose consumption and activated AMP-activated protein kinase (AMPK) without inducing lactic acid production or cytotoxicity in vitro. LL had potent antidiabetic effects with hypoglycemic activity in vivo. It improved insulin resistance, glucose tolerance and lipid metabolism; protected liver, renal and pancreatic functions; and promoted weight loss in db/db mice. Transcriptomic analysis suggested that the antidiabetic effects of LL involved the regulation of mitochondrial oxidative phosphorylation. We further demonstrated that LL effectively activated the hepatic liver kinase B1 (LKB1)/AMPK pathway by regulating the ADP/ATP ratio. Simultaneously, LL significantly modulated the gut microbial community, specifically decreasing the abundances of Mucispirillum schaedleri and Anaerotruncus_sp_G3_2012, which might also contribute to its antidiabetic effects. Conclusion: These results suggest that LL is a promising antidiabetic drug candidate that may improve glucolipid metabolism via modulation of the hepatic LKB1/AMPK pathway and the gut microbiota.
Study on the pharmacokinetics, tissue distribution and excretion of Laurolitsine from Litsea glutinosa in Sprague-Dawley rats
Pharm Biol 2021 Dec;59(1):884-892.PMID:34219593DOI:10.1080/13880209.2021.1944221.
Context: Laurolitsine is an aporphine alkaloid and exhibits potent antihyperglycemic and antihyperlipidemic effects in ob/ob mice. Objective: To investigate the pharmacokinetics, tissue distribution and excretion of Laurolitsine. Materials and methods: A LC-MS/MS method was established and validated to determine Laurolitsine concentrations in the biological matrix of rats (plasma, tissue homogenate, urine and faeces). 10 Sprague-Dawley (SD) rats were used for plasma exposure study: 5 rats were injected with 2.0 mg/kg of Laurolitsine via the tail vein, and the other 5 rats were administered Laurolitsine (10.0 mg/kg) by gavage. 25 SD rats used for tissue distribution study and 5 SD rats for urine and faeces excretion study: rats administered Laurolitsine (10.0 mg/kg) by gavage. After administered, serial blood, tissue, urine and faeces were collected. Analytical quantification was performed by a previous LC-MS/MS method. The pharmacokinetics, bioavailability, tissue distribution and excretion of Laurolitsine were described. Results: The pharmacokinetic parameters of oral and intravenous administration with Tmax were 0.47 and 0.083 h, t1/2 were 3.73 and 1.67 h, respectively. Oral bioavailability was as low as 18.17%. Laurolitsine was found at a high concentration in the gastrointestinal tract, liver, lungs and kidneys (26 015.33, 905.12, 442.32 and 214.99 ng/g at 0.5 h, respectively) and low excretion to parent Laurolitsine in urine and faeces (0.03 and 1.20% in 36 h, respectively). Conclusions: This study established a simple, rapid and accurate LC-MS/MS method to determine Laurolitsine in different rat samples and successful application in a pharmacokinetic study.
Variation of the alkaloid content of Peumus boldus (boldo)
Fitoterapia 2018 Jun;127:179-185.PMID:29454020DOI:10.1016/j.fitote.2018.02.020.
Eighteen alkaloids were detected in the bark, leaves, wood and roots of Peumus boldus, including traces of secoboldine, N-methylsecoboldine (boldine methine), glaucine and norreticuline, not reported previously as constituents of this species. Using appropriate standards, we quantified thirteen of them by UHPLC-MS/MS. Boldine was dominant in the bark, and Laurolitsine in wood and roots. The alkaloid composition of the leaves, determined for 130 individually identified trees, classified by age and sex, was highly variable, where N-methyllaurotetanine, laurotetanine, coclaurine and in some cases isocorydine predominated, but not boldine.
Aporphine alkaloids with in vitro antiplasmodial activity from the leaves of Phoebe tavoyana
J Asian Nat Prod Res 2020 Jan;22(1):52-60.PMID:30897964DOI:10.1080/10286020.2018.1553958.
One new aporphine named tavoyanine A (1), along with four known aporphines laetanine (2), roemerine (3), Laurolitsine (4), and boldine (5), and one morphinandienone type sebiferine (6) were isolated from the leaves of Phoebe tavoyana (Meissn.) Hook f. (Lauraceae). The isolation was achieved by chromatographic techniques, and the structural elucidation was performed via spectral methods. This paper also reports the antiplasmodial activity of roemerine (3), Laurolitsine (4), boldine (5), and sebiferine (6). The results showed that 3-6 have a potent inhibitory activity against the growth of Plasmodium falciparum 3D7 clone, with IC50 values of 0.89, 1.49, 1.65, and 2.76 µg/ml, respectively.
Phytoconstituents from ten natural herbs as potent inhibitors of main protease enzyme of SARS-COV-2: In silico study
Phytomed Plus 2021 Nov;1(4):100083.PMID:35403086DOI:10.1016/j.phyplu.2021.100083.
Background: Lack of treatment of novel Coronavirus disease led to the search of specific antivirals that are capable to inhibit the replication of the virus. The plant kingdom has demonstrated to be an important source of new molecules with antiviral potential. Purpose: The present study aims to utilize various computational tools to identify the most eligible drug candidate that have capabilities to halt the replication of SARS-COV-2 virus by inhibiting Main protease (Mpro) enzyme. Methods: We have selected plants whose extracts have inhibitory potential against previously discovered coronaviruses. Their phytoconstituents were surveyed and a library of 100 molecules was prepared. Then, computational tools such as molecular docking, ADMET and molecular dynamic simulations were utilized to screen the compounds and evaluate them against Mpro enzyme. Results: All the phytoconstituents showed good binding affinities towards Mpro enzyme. Among them Laurolitsine possesses the highest binding affinity i.e. -294.1533 kcal/mol. On ADMET analysis of best three ligands were simulated for 1.2 ns, then the stable ligand among them was further simulated for 20 ns. Results revealed that no conformational changes were observed in the Laurolitsine w.r.t. protein residues and low RMSD value suggested that the Laurolitsine-protein complex was stable for 20 ns. Conclusion: Laurolitsine, an active constituent of roots of Lindera aggregata, was found to be having good ADMET profile and have capabilities to halt the activity of the enzyme. Therefore, this makes Laurolitsine a good drug candidate for the treatment of COVID-19.