Palmatine
(Synonyms: 黄藤素) 目录号 : GC39127
An alkaloid with diverse biological activities
Cas No.:3486-67-7
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
Palmatine is an alkaloid that has been found in C. rhizoma and has diverse biological activities.1,2,3,4,5 It inhibits acetylcholinesterase (AChE) and butyrylcholinesterase (BChE; IC50s = 0.51 and 6.84 ?M, respectively).1 Palmatine (20, 40, and 80 ?M) reduces Zika virus infection of Vero cells in a concentration-dependent manner.2 In vivo, palmatine (50 and 100 mg/kg) reduces colonic myeloperoxidase (MPO) activity and IL-10, IL-1β, IL-6, and TNF-α levels, as well as protects mucosal integrity in a mouse model of colitis induced by dextran sulfate .3 It reduces stomach ulcer area in a rat model of acetic acid-induced gastric ulcers.4 Palmatine (10 and 20 mg/kg) reduces the number of small intestine and colon tumors in the ApcMin+/- mouse model of multiple intestinal neoplasia.5
1.Jung, H.A., Min, B.S., Yokozawa, T., et al.Anti-Alzheimer and antioxidant activities of Coptidis Rhizoma alkaloidsBiol. Pharm. Bull.32(8)1433-1438(2009) 2.Ho, Y.-J., Lu, J.-W., Huang, Y.-L., et al.Palmatine inhibits Zika virus infection by disrupting virus binding, entry, and stabilityBiochem. Biophys. Res. Commun.518(4)732-738(2019) 3.Zhang, X.-J., Yuan, Z.-W., Qu, C., et al.Palmatine ameliorated murine colitis by suppressing tryptophan metabolism and regulating gut microbiotaPharmacol. Res.13734-46(2018) 4.Wang, L., Wang, X., Zhang, S.-L., et al.Gastroprotective effect of palmatine against acetic acid-induced gastric ulcers in ratsJ. Nat. Med.71(1)257-264(2016) 5.Ma, W.-K., Li, H., Dong, C.-L., et al.Palmatine from Mahonia bealei attenuates gut tumorigenesis in ApcMin/+ mice via inhibition of inflammatory cytokinesMol. Med. Rep.14(1)491-498(2016)
| Cas No. | 3486-67-7 | SDF | |
| 别名 | 黄藤素 | ||
| Canonical SMILES | COC1=C(OC)C2=C[N+]3=C(C4=CC(OC)=C(OC)C=C4CC3)C=C2C=C1 | ||
| 分子式 | C21H22NO4+ | 分子量 | 352.4 |
| 溶解度 | DMSO : 70mg/mL | 储存条件 | Store at -20°C |
| 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 | 2.8377 mL | 14.1884 mL | 28.3768 mL |
| 5 mM | 0.5675 mL | 2.8377 mL | 5.6754 mL |
| 10 mM | 0.2838 mL | 1.4188 mL | 2.8377 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。
Palmatine: A review of its pharmacology, toxicity and pharmacokinetics
Biochimie 2019 Jul;162:176-184.PMID:31051209DOI:10.1016/j.biochi.2019.04.008.
Palmatine is a natural isoquinoline alkaloid and has been widely used in pharmaceutical field. The purpose of this review is to provide the latest and comprehensive information on the pharmacology, toxicity and pharmacokinetics of Palmatine in the past, to explore the therapeutic potential of this compound and look for ways to reduce toxicity. Information on Palmatine was collected from the internet database PubMed, Elsevier, ResearchGate, Web of Science, Wiley Online Library and Europe PMC using a combination of keywords including "pharmacology", "toxicology", "pharmacokinetics". All studies of this genus were included in this review until March 2019. Palmatine has a wide spectrum of pharmacological effects, including anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, anti-bacterial, anti-viral and regulating blood lipids. However, Palmatine has obvious DNA toxicity, and has a complex effect on metabolic enzymes in the liver. Pharmacokinetic studies have demonstrated that glucuronidation and sulfation are the main metabolic pathways of Palmatine. Palmatine can be used in many diseases. Future research directions include: how the concentration of Palmatine affects pharmacological effects and toxicity; the mechanism of synergy between Palmatine and other protoberberine alkaloid; Structural modification of Palmatine is one of the key methods to enhance pharmacological activity and reduce activity.
Palmatine attenuated dextran sulfate sodium (DSS)-induced colitis via promoting mitophagy-mediated NLRP3 inflammasome inactivation
Mol Immunol 2019 Jan;105:76-85.PMID:30496979DOI:10.1016/j.molimm.2018.10.015.
Activation of NLRP3 inflammasomes is crucial in the pathological process of Ulcerative colitis (UC), which could be negatively regulated by PINK1/Parkin-driven mitophagy. Palmatine is a herb derived isoquinoline alkaloid with potent anti-inflammatory and anti-bacteria activities. In present study, we evaluated the effect of Palmatine on dextran sulfate sodium (DSS)-induced mice colitis and examined whether its effect is exerted by promoting mitophagy-mediated NLRP3 inflammasome inactivation. The result showed that Palmatine (40, 100 mg/kg) significantly prevented bodyweight loss and colonic shortening in DSS mice, and reduced the disease activity index and histopathologic score. The levels of MPO, IL-1β, TNF-α and the number of F4/80+ cells in colon of DSS mice were remarkably decreased by Palmatine. Moreover, Palmatine suppressed NLRP3 inflammasomes activation, but enhanced the expression of the mitophagy-related proteins involving LC3, PINK1 and Parkin in colonic tissue of DSS mice. These effects was consistent with the in vitro data revealing that Palmatine inhibited the activation of NLRP3 inflammasomes, while promoted the expression and mitochondrial recruitment of PINK1 and Parkin in THP-1 cell differentiated macrophages. Furthermore, the effect of Palmatine on THP-1 cells was neutralized by a mitophagy inhibitor Cyclosporin A (CsA) and PINK1-siRNA. In parallel, CsA significantly attenuated the therapeutic effect of Palmatine in DSS mice, illustrating that the anti-colitis effect of Palmatine is closely related to mitophagy. Taken together, the current results demonstrated that Palmatine protected mice against DSS-induced colitis by facilitating PINK1/Parkin-driven mitophagy and thus inactivating NLRP3 inflammasomes in macrophage.
Palmatine as an Agent Against Metabolic Syndrome and Its Related Complications: A Review
Drug Des Devel Ther 2020 Nov 17;14:4963-4974.PMID:33235437DOI:10.2147/DDDT.S280520.
Palmatine is a naturally occurring isoquinoline alkaloid with various pharmacological properties. Given its antioxidant and anti-inflammatory properties, Palmatine may be able to impede the effects of metabolic syndrome (MetS) and its related diseases triggered by inflammation and oxidative stress. This review summarises the existing literature about the effects of Palmatine supplementation on MetS and its complications. The evidence shows that Palmatine could protect against MetS, and cardiovascular diseases, osteoporosis and osteoarthritis, which might be associated with MetS. These protective effects are mediated by the antioxidant and anti-inflammatory properties of Palmatine. Although preclinical experiments have demonstrated the efficacy of Palmatine against MetS and its related diseases, no human clinical trials have been performed to validate these effects. This research gap should be bridged to validate the efficacy and safety of Palmatine supplementation in protecting humans against MetS and its related diseases.
Palmatine: A review of pharmacological properties and pharmacokinetics
Phytother Res 2020 Jan;34(1):33-50.PMID:31496018DOI:10.1002/ptr.6504.
The aim of this review is to collect together the results of the numerous studies over the last two decades on the pharmacological properties of Palmatine published in scientific databases like Scopus and PubMed, which are scattered across different publications. Palmatine, an isoquinoline alkaloid from the class of protoberberines, is a yellow compound present in the extracts from different representatives of Berberidaceae, Papaveraceae, Ranunculaceae, and Menispermaceae. It has been extensively used in traditional medicine of Asia in the treatment of jaundice, liver-related diseases, hypertension, inflammation, and dysentery. New findings describe its possible applications in the treatment of civilization diseases like central nervous system-related problems. This review intends to let this alkaloid come out from the shade of a more frequently described alkaloid: berberine. The toxicity, pharmacokinetics, and biological activities of this protoberberine alkaloid will be developed in this work.
Palmatine Protects Against MSU-Induced Gouty Arthritis via Regulating the NF-κB/NLRP3 and Nrf2 Pathways
Drug Des Devel Ther 2022 Jul 2;16:2119-2132.PMID:35812134DOI:10.2147/DDDT.S356307.
Purpose: Gouty arthritis could be triggered by the deposition of monosodium uric acid (MSU) crystals. Palmatine (PAL), a protoberberine alkaloid, has been proven to possess compelling health-beneficial activities. In this study, we aimed to explore the effect of PAL on LPS plus MSU crystal-stimulated gouty arthritis in vitro and in vivo. Methods: PMA-differentiated THP-1 macrophages were primed with LPS and then stimulated with MSU crystal in the presence or absence of PAL. The expression of pro-inflammatory cytokines and oxidative stress-related biomarkers and signal pathway key targets were determined by ELISA kit, Western blot, immunohistochemistry and qRT-PCR, respectively. In addition, the anti-inflammatory and antioxidant activities of PAL on MSU-induced arthritis mice were also evaluated. Results: The results indicated that PAL (20, 40 and 80 μM) dose-dependently decreased the mRNA expression and levels of pro-inflammatory cytokines (interleukin-1beta (IL-1β), IL-6, IL-18 and tumor necrosis factor alpha (TNF-α)). The levels of superoxide dismutase (SOD) and glutathione (GSH) were remarkably enhanced, while the level of malondialdehyde (MDA) was reduced. Western blot analysis revealed that PAL appreciably inhibited NF-κB/NLRP3 signaling pathways through inhibiting the phosphorylation of p-65 and IκBα, blocking the expression of NLRP3, ASC, IL-1β and Caspase-1, as well as enhancing the antioxidant protein expression of Nrf2 and HO-1. In vivo, PAL attenuated MSU-induced inflammation in gouty arthritis, as evidenced by mitigating the joint swelling, and decreasing the productions of IL-1β, IL-6, IL-18, TNF-α and MDA, while enhancing the levels of SOD and GSH. Moreover, PAL further attenuated the infiltration of neutrophils into joint synovitis. Conclusion: PAL protected against MSU-induced inflammation and oxidative stress via regulating the NF-κB/NLRP3 and Nrf2 pathways. PAL may represent a potential candidate for the treatment of gouty arthritis.