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| 1g |
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| Other Sizes |
| Targets |
Palmatine hydroxide targets multiple biological pathways and molecules. The compound has been shown to interact with various enzymes, receptors, and transcription factors. Palmatine inhibits acetylcholinesterase, which may contribute to its neuroprotective effects. The compound also modulates inflammatory pathways by inhibiting the production of pro-inflammatory cytokines and downregulating NF-κB signaling. Palmatine has been shown to induce apoptosis in cancer cells through various mechanisms including mitochondrial dysfunction, ROS generation, and activation of caspases. The compound also exhibits antimicrobial activity by disrupting bacterial cell membranes and inhibiting bacterial enzymes. Palmatine has been shown to activate AMPK, which may contribute to its metabolic effects. The compound's ability to interact with multiple targets makes it a promising candidate for various therapeutic applications.
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| ln Vitro |
Palmatin (0-100 μM; 42 h) diminishes the viral titers of DENV-2 and YFV with EC50 values of 26.4 μM and 7.3 μM, respectively, and suppresses WNV with an EC50 value of 3.6 μM [3]. The growth of colon cancer cells is inhibited by palmatin (0-1128 μM; 24-72 hours) [5]. By means of mitochondria-related pathways, palmatin (0-704 μM; 24 hours) can cause AURKA protein levels to drop, G2/M phase arrest, and death in colon cancer cells [5].
In vitro, palmatine hydroxide has demonstrated various biological activities including anti-inflammatory, antimicrobial, antiviral, anticancer, and neuroprotective effects. The compound inhibits the production of pro-inflammatory cytokines such as TNF-α, IL-1β, and IL-6 in activated immune cells. Palmatine has been shown to induce apoptosis in various cancer cell lines through mechanisms involving ROS generation, mitochondrial dysfunction, and activation of caspases. The compound exhibits antimicrobial activity against various bacteria and fungi by disrupting cell membranes and inhibiting essential enzymes. Palmatine has demonstrated antiviral activity against various viruses including influenza virus and hepatitis B virus. The compound also exhibits neuroprotective effects by reducing oxidative stress and inhibiting acetylcholinesterase activity. Palmatine has been shown to modulate various signaling pathways including NF-κB, MAPK, and PI3K/Akt pathways. |
| ln Vivo |
Oral palmatine (50 or 100 mg/kg; taken once daily for 7 days) reduces the infiltration of inflammatory cells and ameliorates colitis caused by dextran sulfate sodium (DSS) [1]. In mice, fulminant liver failure induced by lipopolysaccharide and D-galactosamine can be lessened by intraperitoneal injection of palmatin (0-200 mg/kg) once [2]. In mice, palmatine (0–1 mg/kg; i.p.; 10 days) exhibits memory-improving effects [4]. The growth of HCT-116 xenografts in mice is effectively inhibited by palmatine (33.75–135 mg/kg; oral; once daily for 26 days) [5].
In vivo, palmatine hydroxide has been studied in various animal models for its therapeutic potential. The compound has demonstrated anti-inflammatory effects in models of acute and chronic inflammation, reducing the production of inflammatory mediators and alleviating tissue damage. Palmatine has shown antidepressant-like effects in animal models of depression, possibly through modulation of neurotransmitter systems. The compound has demonstrated neuroprotective effects in models of neurodegenerative diseases, reducing oxidative stress and improving cognitive function. Palmatine has shown antihyperglycemic effects in diabetic animal models, improving glucose metabolism and insulin sensitivity. The compound has also demonstrated hepatoprotective effects in models of liver injury. Palmatine's multiple pharmacological activities make it a promising candidate for the treatment of various diseases. However, the compound is primarily used as a research tool and is not approved for clinical use. |
| Enzyme Assay |
In vitro assays for palmatine hydroxide typically involve measuring its effects on various biological targets. For enzyme inhibition assays, palmatine is dissolved in appropriate buffers and tested against enzymes such as acetylcholinesterase, cyclooxygenases, or lipoxygenases. For cell-based assays, the compound is dissolved in DMSO and diluted in cell culture medium at concentrations ranging from 1-100 μM. Cells are treated with palmatine for 24-72 hours, and various endpoints are measured. Anti-inflammatory activity is assessed by measuring the production of inflammatory mediators in activated immune cells. Anticancer activity is assessed by measuring cell viability, apoptosis, and cell cycle progression. Antimicrobial activity is assessed by measuring the minimum inhibitory concentration against various pathogens. The compound is typically stored at room temperature and protected from light.
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| Cell Assay |
Cell proliferation assay[5]
Cell Types: HCT-116, SW480, HT-29 Tested Concentrations: 0, 88, 176, 352 and 704 μM (HCT-116, SW480); 0, 141, 282, 564 and 1128 μM (HT -29) Incubation Duration: 24, 48 and 72 hrs (hours) Experimental Results: Cell viability diminished in a dose-dependent manner. Western Blot Analysis[5] Cell Types: HCT-116, SW480, HT-29 Tested Concentrations: 100 nM for HCT-116, 500 nM for SW480 and HT-29 Incubation Duration: 24, 48 and 72 hrs (hours) Experimental Results: Pro-apoptotic markers substances, such as P53/P73, Caspase3 and Caspase9. AURKA protein levels are diminished. Cytochrome increases. c In the cytoplasm, both Bcl2 and Bcl-xl were diminished in a dose-dependent manner. Cell cycle analysis[5] Cell Types: HCT-116, SW480 Tested Concentrations: 88, 176, 352 and 704 μM Incubation Duration: 24, 48 and 72 hrs (hours) Experimental Results: Induced G2/M phase arrest in a dose-dependent manner. Apoptosis analysis [5] Cell Types: HCT-116, SW480 Tested Concentrations: 88, 176, 352 and 704 μM Incubation Duration: 24, 48 and 72 h Experimental Results: Apoptosis was induced in a dose-depen In vitro cell-based assays using palmatine hydroxide are conducted in various cell lines including cancer cells, immune cells, and neuronal cells. Cells are seeded in multi-well plates and treated with palmatine at concentrations ranging from 1-100 μM for 24-72 hours. Cell viability is assessed using MTT or CCK-8 assays. Apoptosis is measured using annexin V/PI staining or caspase activity assays. Inflammatory cytokine production is measured by ELISA or qPCR. ROS levels are measured using fluorescent probes such as DCFH-DA. For mechanistic studies, cells are harvested for Western blot analysis to measure the expression of proteins involved in apoptosis, inflammation, and signaling pathways. The compound is typically dissolved in DMSO and diluted in cell culture medium, with the final DMSO concentration kept below 0.1%. The compound's effects are concentration-dependent. |
| Animal Protocol |
Animal/Disease Models: DSS-induced colitis BALB/c mouse model (8 weeks old) [1]
Doses: 50 or 100 mg/kg Route of Administration: Orally, daily, for 7 days Experimental Results: Improved DSS-induced colitis It also prevents the infiltration of inflammatory cells in colitis; Dramatically extends the length of the colon; and Dramatically inhibits colonic MPO activity. Reduce the levels of colon inflammatory cytokines (TNF-α, IFN-γ, IL-1β, IL-6, IL-4 and IL-10); protect mucosal integrity by regulating TJs proteins and apoptotic proteins; restore DSS-induced Reduction of TJ proteins ZO-1, ZO-2 and Claudin-1; 100 mg/kg dose diminished Bax expression and enhanced Bcl-2 expression, preventing epithelial cell apoptosis and improving intestinal integrity. Preventing changes in intestinal microbiota in mice with DSS-induced colitis. Animal/Disease Models: Male ICR mouse (20-22 g), D-galactosamine/lipopolysaccharide (GalN/LPS)-induced fulminant liver failure model [2] Doses: 25, 50, 100 or 200 mg/kg given Medication: intraperitonealinj In vivo animal experiments with palmatine hydroxide are conducted in various disease models including inflammation, depression, diabetes, and neurodegenerative diseases. The compound is typically administered orally, intraperitoneally, or intravenously at doses ranging from 1-50 mg/kg depending on the study. In models of inflammation, palmatine is administered before or after induction of inflammation, and inflammatory markers are measured in tissues and serum. In models of depression, palmatine is administered daily for several weeks, and behavioral tests are performed to assess antidepressant-like effects. In diabetic models, blood glucose levels and insulin sensitivity are measured. In neurodegenerative models, cognitive function and oxidative stress markers are assessed. Tissue samples are collected for histopathological examination and biochemical analysis. The compound is formulated in appropriate vehicles such as saline, DMSO, or PEG for administration. |
| ADME/Pharmacokinetics |
Palmatine hydroxide has a molecular weight of approximately 367.42 g/mol and the formula C21H22NO4·OH. The compound is a yellow crystalline powder that is soluble in water and organic solvents. The compound's pharmacokinetic properties have been studied in preclinical research. After oral administration, palmatine is absorbed from the gastrointestinal tract and distributed to various tissues. The compound undergoes metabolism in the liver and is excreted primarily in urine and feces. The compound's half-life in plasma is typically 2-4 hours depending on the species. For long-term storage, the compound is kept at room temperature and protected from light. The compound's stability in solution should be assessed for specific applications. The compound is intended for research use only and is not approved for clinical use.
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| Toxicity/Toxicokinetics |
The toxicity of palmatine hydroxide has been evaluated in preclinical studies. In animal models, the compound is generally well-tolerated at therapeutic doses (1-50 mg/kg), with no significant adverse effects reported. At higher doses, the compound may cause gastrointestinal disturbances and hepatotoxicity. The compound's toxicity is dose-dependent, and the therapeutic window should be determined for specific applications. Standard toxicology studies include acute toxicity testing to determine the maximum tolerated dose, as well as repeated-dose toxicity studies to assess the effects of chronic administration. Histopathological examination of major organs is performed to identify any target organ toxicity. The compound is intended for research use only and is not approved for clinical use. Safety data sheets recommend standard handling procedures for research chemicals. The compound should be handled in a well-ventilated area.
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| References |
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| Additional Infomation |
Palmatine hydroxide (CAS 131-04-4) is a protoberberine alkaloid found in various plants including Phellodendron amurense, Coptis chinensis, and Fibraurea recisa. It has the molecular formula C21H22NO4·OH and a molecular weight of approximately 367.42 g/mol. Palmatine is a quaternary ammonium salt that is structurally related to berberine. The compound has been studied for its various pharmacological activities including anti-inflammatory, antimicrobial, antiviral, anticancer, and neuroprotective effects. Palmatine has been used in traditional Chinese medicine for the treatment of various conditions. The compound is a yellow crystalline powder that is soluble in water and organic solvents. Palmatine inhibits acetylcholinesterase and modulates inflammatory pathways by inhibiting NF-κB signaling. The compound induces apoptosis in cancer cells and exhibits antimicrobial activity. Palmatine has demonstrated anti-inflammatory, antidepressant, neuroprotective, and antihyperglycemic effects in animal models. The compound is intended for research use only and is not approved for clinical use. It is typically stored at room temperature and protected from light.
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| Molecular Formula |
C21H22NO4+.HO-
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| Molecular Weight |
369.41102
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| Exact Mass |
369.158
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| CAS # |
131-04-4
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| Related CAS # |
Palmatine chloride;10605-02-4;Palmatine;3486-67-7
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| PubChem CID |
200119
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.208
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
27
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| Complexity |
475
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
FQXRAAFEBRSBND-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C21H22NO4.H2O/c1-23-18-6-5-13-9-17-15-11-20(25-3)19(24-2)10-14(15)7-8-22(17)12-16(13)21(18)26-4;/h5-6,9-12H,7-8H2,1-4H3;1H2/q+1;/p-1
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| Chemical Name |
2,3,9,10-tetramethoxy-5,6-dihydroisoquinolino[2,1-b]isoquinolin-7-ium;hydroxide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~15.62 mg/mL (~42.28 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7070 mL | 13.5351 mL | 27.0702 mL | |
| 5 mM | 0.5414 mL | 2.7070 mL | 5.4140 mL | |
| 10 mM | 0.2707 mL | 1.3535 mL | 2.7070 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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