Lycorine
(Synonyms: 石蒜碱) 目录号 : GC38967
An alkaloid with diverse biological activities
Cas No.:476-28-8
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Lycorine is an alkaloid that has been found in Amaryllidaceae and has diverse biological activities.1,2,3,4 It is active against P. falciparum (IC50 = 1.026 ?g/ml).1 Lycorine inhibits severe acute respiratory syndrome coronavirus (SARS-CoV) viral infection in Vero cells (EC50 = 15.7 ?M).2 It inhibits migration of A549 non-small cell lung cancer (NSCLC) and U373 MG glioblastoma cells when used at a concentration of 5 ?M.3 Lycorine (0.4 mg/kg) increases survival and reduces virus-induced paralysis in a mouse model of enterovirus 71 infection.4
1.Sener, B., Orhan, I., and Satayavivad, J.Antimalarial activity screening of some alkaloids and the plant extracts from AmaryllidaceaePhytother. Res.17(10)1220-1223(2003) 2.Li, S.-Y., Chen, C., Zhang, H.-Q., et al.Identification of natural compounds with antiviral activities against SARS-associated coronavirusAntiviral Res.67(1)18-23(2005) 3.Lamoral-Theys, D., Andolfi, A., Van Goietsenoven, G., et al.Lycorine, the main phenanthridine Amaryllidaceae alkaloid, exhibits significant antitumor activity in cancer cells that display resistance to proapoptotic stimuli: An investigation of structure-activity relationship and mechanistic insightJ. Med. Chem.52(20)6244-6256(2009) 4.Liu, J., Yang, Y., Xu, Y., et al.Lycorine reduces mortality of human enterovirus 71-infected mice by inhibiting virus replicationVirol. J.8483(2011)
| Cas No. | 476-28-8 | SDF | |
| 别名 | 石蒜碱 | ||
| Canonical SMILES | O[C@@H]1[C@@H](O)C=C(CC2)[C@@]3([H])N2CC4=C([C@@]31[H])C=C(OCO5)C5=C4 | ||
| 分子式 | C16H17NO4 | 分子量 | 287.31 |
| 溶解度 | DMSO: 25 mg/mL (87.01 mM) | 储存条件 | Store at -20°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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.4806 mL | 17.4028 mL | 34.8056 mL |
| 5 mM | 0.6961 mL | 3.4806 mL | 6.9611 mL |
| 10 mM | 0.3481 mL | 1.7403 mL | 3.4806 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。
Lycorine ameliorates bleomycin-induced pulmonary fibrosis via inhibiting NLRP3 inflammasome activation and pyroptosis
Pharmacol Res 2020 Aug;158:104884.PMID:32428667DOI:10.1016/j.phrs.2020.104884.
Idiopathic pulmonary fibrosis (IPF) is a chronic and irreversible lung disease with limited therapeutic strategies. Lycorine (LYC), an alkaloid isolated from Amaryllidaceae family plants, exhibits effective anti-inflammatory, antiviral, and anti-tumor activities. In this study, we attempted to determine the effect of LYC on bleomycin (BLM)-induced IPF and NLRP3 inflammasome activation. Our results demonstrated that the LYC treatment ameliorated BLM-induced pulmonary fibrosis and inflammation in mice. LYC inhibited active Caspase-1 expression and lactate dehydrogenase (LDH) release during BLM-induced acute lung injury (ALI) in mice. Furthermore, our in vitro assay showed that LYC inhibited LPS/Nigericin- or LPS/ATP-induced NACHT, LRP and PYD domains-containing protein 3 (NLRP3) inflammasome activation, and pyroptosis in bone marrow-derived macrophages (BMDMs). Mechanically, LYC could disturb the interaction of NLRP3 with apoptosis-associated speck-like protein containing a CARD (ASC) by targeting the pyrin domain (PYD) on Leu9, Leu50, and Thr53. Our findings indicate that LYC ameliorated BLM-induced pulmonary fibrosis by inhibiting NLRP3 inflammasome activation and pyroptosis through targeting the PYD domain of ASC. Thus, LYC might be a potential therapeutic agent for pulmonary inflammation and fibrosis.
Lycorine improves peripheral nerve function by promoting Schwann cell autophagy via AMPK pathway activation and MMP9 downregulation in diabetic peripheral neuropathy
Pharmacol Res 2022 Jan;175:105985.PMID:34863821DOI:10.1016/j.phrs.2021.105985.
Diabetic peripheral neuropathy (DPN) is the most common complication of diabetes mellitus and no effective therapy is approved. Here, Lycorine, a natural alkaloid, was identified as a potential drug for DPN by the bioinformatics analysis of GEO datasets and Connectivity Map database. Lycorine administration improved peripheral nerve function and autophagy-associated proteins of diabetic mice. Again, in vitro high glucose-cultured rat Schwann cells (RSC96) showed enhanced autophagosome marker LC3-II with the treatment of Lycorine. Additionally, beclin-1 and Atg3 were decreased in high glucose-stimulated RSC96 cells, which were reversed by Lycorine treatment. Furthermore, DPN-associated differentially expressed genes (DEGs) from GEO datasets and lycorine-drug targets from PubChem and PharmMapper were visually analyzed and revealed that MMP9 was both DPN-associated DEGs and lycorine-drug target. Functional enrichment analysis of MMP9-relevant genes showed that cell energy metabolism was involved. Moreover, Lycorine reduced high glucose-enhanced MMP9 expression in RSC96 cells. Overexpression of MMP9 attenuated lycorine-induced the expression of beclin-1, Atg3 and LC3-II in high glucose-cultured RSC96 cells. In addition, AMPK pathway activation was confirmed in lycorine-treated high glucose-cultured RSC96 cells. Then AMPK pathway inhibition attenuated lycorine-reduced MMP9 expression in high glucose-treated RSC96 cells. Molecular docking analysis revealed that Lycorine bound the domain of AMPK containing Thr 172 site, which affected AMPK (Thr 172) phosphorylation. Finally, AMPK pathway activation and MMP9 downregulation were also revealed in the sciatic nerves of diabetic mice administrated with Lycorine. Taken together, Lycorine was advised to promote Schwann cell autophagy via AMPK pathway activation and MMP9 downregulation-induced LC3-II transformation in diabetic peripheral neuropathy.
Lycorine and organ protection: Review of its potential effects and molecular mechanisms
Phytomedicine 2022 Sep;104:154266.PMID:35752077DOI:10.1016/j.phymed.2022.154266.
Background: Multiorgan dysfunction, especially sepsis-related multiorgan damage, remains a major cause of high mortality in the late stages of infection and a great clinical challenge. In recent years, natural drugs have received widespread attention because of their low cost, wide sources, high efficacy, low toxicity, and limited side effects. Lycorine, a natural compound extracted from Amaryllidaceae, exhibits multiple pharmacological activities, including in the regulation of autophagy and the induction of cancer cell apoptosis, and has anti-inflammatory, antifungal, antiviral, antimalarial, and antitumor activities. However, studies on Lycorine have mainly focused on its antitumor properties, and research on its use for organ protection, especially in sepsis-related organ injury, is relatively limited. Purpose: To review and discuss the effects and mechanisms of Lycorine in the treatment of multi-organ dysfunction, especially sepsis. Methods: Literature searches in electronic databases, such as Web of Science, Science Direct, PubMed, Google Scholar, and Scopus, were performed using 'Lycorine', 'Amaryllidaceae', 'Pharmacology', 'Pharmacokinetics', 'Anti-inflammation', 'Autophagy', 'Apoptosis', 'Anti-microbial and anti-parasitic', 'Antitumor', 'Organ protection', and 'Sepsis' as keywords, the correlated literature was extracted and conducted from the databases mentioned above. Results: By summarizing the progress made in existing research, we found that the general effects of Lycorine involve the regulation of autophagy and the induction of cancer cell apoptosis, and anti-inflammatory, antifungal, antiviral, antimalarial, and antitumor effects; through these pathways, the compound can ameliorate organ damage. In addition, Lycorine was found to have an important effect on organ damage in sepsis. Conclusion: Lycorine is a promising natural organ protective agent. This review will provide a new theoretical basis for the treatment of organ protection, especially in sepsis.
Lycorine: A prospective natural lead for anticancer drug discovery
Biomed Pharmacother 2018 Nov;107:615-624.PMID:30114645DOI:10.1016/j.biopha.2018.07.147.
Nature is the most abundant source for novel drug discovery. Lycorine is a natural alkaloid with immense therapeutic potential. Lycorine is active in a very low concentration and with high specificity against a number of cancers both in vivo and in vitro and against various drug-resistant cancer cells. This review summarized the therapeutic effect and the anticancer mechanisms of Lycorine. At the same time, we have discussed the pharmacology and comparative structure-activity relationship for the anticancer activity of this compound. The researches outlined in this paper serve as a foundation to explain Lycorine as an important lead compound for new generation anticancer drug design and provide the principle for the development of biological strategies to utilize Lycorine in the treatment of cancers.
Lycorine hydrochloride inhibits cell proliferation and induces apoptosis through promoting FBXW7-MCL1 axis in gastric cancer
J Exp Clin Cancer Res 2020 Oct 30;39(1):230.PMID:33126914DOI:10.1186/s13046-020-01743-3.
Background: Lycorine hydrochloride (LH), an alkaloid extracted from the bulb of the Lycoris radiata, is considered to have anti-viral, anti-malarial, and anti-tumorous effects. At present, the underlying mechanisms of LH in gastric cancer remain unclear. MCL1, an anti-apoptotic protein of BCL2 family, is closely related to drug resistance of tumor. Therefore, MCL1 is considered as a potential target for cancer treatment. Methods: The effect of LH on gastric cancer was assessed in vitro (by MTT, BrdU, western blotting…) and in vivo (by immunohistochemistry). Results: In this study, we showed that LH has an anti-tumorous effect by down-regulating MCL1 in gastric cancer. Besides, we unveiled that LH reduced the protein stability of MCL1 by up-regulating ubiquitin E3 ligase FBXW7, arrested cell cycle at S phase and triggered apoptosis of gastric cancer cells. Meanwhile, we also demonstrated that LH could induce apoptosis of the BCL2-drug-resistant-cell-lines. Moreover, PDX (Patient-Derived tumor xenograft) model experiment proved that LH combined with HA14-1 (inhibitor of BCL2), had a more significant therapeutic effect on gastric cancer. Conclusions: The efficacy showed in our data suggests that Lycorine hydrochloride is a promising anti-tumor compound for gastric cancer.