| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
| ln Vitro |
Lycorine has a minor effect on PNT1A cell proliferation, as well as a cyclic inhibitory effect on cell proliferation on the four PCa cell lines mentioned above, with an IC50 range of 5 μM to 10 μM [1]. In order to control or safeguard SREBF in the endoplasmic reticulum, SCAP (SREBF molecular chaperone), an endoplasmic reticulum-to-Golgi transporter, transforms structurally by creating a complex with INSIG1 (insulin-inducible gene) 1)[2]. In a dose- and time-dependent way, Lycorine (5-40 μM; 16) considerably reduces SREBF activity (up to -70%) without having overt effects in cells. Lycorine (10-20 μM; 2-16 hours). Cytotoxicity [2]. decreases in HL-7702 cells the amounts of mature SREBF1 and SREBF2 proteins [2]. ABCG5 and ABCG8 are two NR1H3 target genes that are not affected by lycorine (20 μM; 16 hours) or NR1H3 transcription activation. Sterol Forwarding activity for NR1H3 is activated [1]. Treatment with lycorine (0-25 μM; 48 hours) markedly and dose-dependently suppressed the expression of vascular endothelial (VE)-cadherin and marginally decreased the expression of Sema4D in C8161 cells. The VE-cadherin protein level in C8161 cells was dramatically lowered by the expression of the other 6 genes after 48 hours of treatment with Lycorine (0-25 μM) [3].
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| ln Vivo |
Lycorine (facial; 15 mg/kg, 30 mg/kg; once daily) attenuates fat coupling and depletion therapy and enhances fat stratification and oxidation of grafts and precursor and mature SREBF in mice [2].
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| Cell Assay |
Cell viability assay [2]
Cell Types: HL-7702/SRE- Luc. Cell Tested Concentrations: 16 hrs (hours) Incubation Duration: 5 μM; 10 μM; 20 μM; 40 μM Experimental Results: No cytotoxicity to HL-7702 cells. Western Blot Analysis[2] Cell Types: HL-7702/SRE-Luc Cell Tested Concentrations: 2 hour, 4 hrs (hours), 8 hrs (hours), 12 hrs (hours), 16 hrs (hours) Incubation Duration: 10 μM; 20 μM Experimental Results: p-SREBF1, m-SREBF1, p-SREBF2 and p-SREBF1 protein expression diminished. RT-PCR[3] Cell Types:C8161 Cell Tested Concentrations: 0 μM, 1.56 μM, 3.13 μM, 6.25 μM, 12.5 μM, 25 μM Incubation Duration: 48 hrs (hours) Experimental Results: Dramatically inhibited the expression of VE-cadherin in a dose-dependent manner, and also slightly diminished C8161 Expression of Sema4D in cells. |
| Animal Protocol |
Animal/Disease Models: C57BL/6J mice fed high-fat diet (HFD) [2]
Doses: 15 mg/kg, 30 mg/kg Route of Administration: oral; one time/day Experimental Results: Improved high-fat diet-induced hypertensive disorders in mice Lipidemia, hepatic steatosis, and insulin resistance. |
| ADME/Pharmacokinetics |
Metabolism / Metabolites
Paraoxygenase (PON1) is a key enzyme in organophosphate metabolism. PON1 can inactivate certain organophosphates through hydrolysis. PON1 hydrolyzes active metabolites from various organophosphate pesticides and nerve agents (such as soman, sarin, and VX). The existence of PON1 polymorphism leads to differences in the enzyme activity level and catalytic efficiency of this esterase, which in turn suggests that different individuals may be more susceptible to the toxic effects of organophosphate exposure. |
| Toxicity/Toxicokinetics |
Toxicity Summary
Lycorine is a cholinesterase, or acetylcholinesterase (AChE) inhibitor. Cholinesterase inhibitors (or "anticholinesterases") inhibit the activity of acetylcholinesterase. Because acetylcholinesterase plays a vital physiological role, chemicals that interfere with its activity are potent neurotoxins; even low doses can cause excessive salivation and lacrimation, followed by muscle spasms and ultimately death. Neurotoxins and substances in many pesticides have been shown to exert their effects by binding to serine residues at the active site of acetylcholinesterase, thereby completely inhibiting the enzyme's activity. Acetylcholinesterase breaks down the neurotransmitter acetylcholine, which is released at the neuromuscular junction, causing muscle or organ relaxation. The mechanism of action of acetylcholinesterase inhibitors is to allow acetylcholine to accumulate and exert its sustained effect, ensuring the continuous transmission of nerve impulses and preventing muscle contraction from ceasing. The most common acetylcholinesterase inhibitors are phosphorus-containing compounds designed to bind to the enzyme's active site. Its structural requirements include a phosphorus atom with two lipophilic groups, a leaving group (such as a halogen or thiocyanate group), and a terminal oxygen atom. |
| References |
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| Additional Infomation |
Lycorine is an indolithidine alkaloid with the structure 3,12-disehydrogalantan, substituted with hydroxyl groups at positions 2 and 9 and with a methylenedioxy group at position 10. It was isolated from Crinum asiaticum and has been shown to possess antimalarial activity. Lycorine functions as a protein synthesis inhibitor, antimalarial drug, plant metabolite, and anticoronavirus agent. It is derived from the hydride of galantan. Lycorine has been reported to be found in Crinum moorei, Clivia nobilis, and several other organisms with relevant data. Lycorine is a toxic crystalline alkaloid found in various Amaryllidaceae plants, such as cultivated shrub lilies (Clivia miniata), lycoris, and narcissus. Ingestion of certain doses of lycorine can be highly toxic and even fatal. Symptoms of lycorine poisoning include vomiting, diarrhea, and convulsions. A definition of lycorine can be found at mercksource.com. Nevertheless, it is still sometimes used for medicinal purposes, which is one of the reasons why some groups harvest the very popular Clivia miniata.
See also: Lycorine hydrochloride (note moved to). |
| Molecular Formula |
C16H17NO4
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|---|---|
| Molecular Weight |
287.3105
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| Exact Mass |
287.115
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| CAS # |
476-28-8
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| Related CAS # |
Lycorine hydrochloride monohydrate;6150-58-9;Lycorine hydrochloride;2188-68-3
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| PubChem CID |
72378
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
477.4±45.0 °C at 760 mmHg
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| Melting Point |
253-255ºC (dec.)
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| Flash Point |
242.5±28.7 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.733
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| LogP |
0.77
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
21
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| Complexity |
481
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C1CN2CC3=CC4=C(C=C3[C@H]5[C@H]2C1=C[C@@H]([C@H]5O)O)OCO4
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| InChi Key |
XGVJWXAYKUHDOO-DANNLKNASA-N
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| InChi Code |
InChI=1S/C16H17NO4/c18-11-3-8-1-2-17-6-9-4-12-13(21-7-20-12)5-10(9)14(15(8)17)16(11)19/h3-5,11,14-16,18-19H,1-2,6-7H2/t11-,14-,15+,16+/m0/s1
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| Chemical Name |
(1S,17S,18S,19S)-5,7-dioxa-12-azapentacyclo[10.6.1.02,10.04,8.015,19]nonadeca-2,4(8),9,15-tetraene-17,18-diol
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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 : ~25 mg/mL (~87.01 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.70 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.70 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.70 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 25 mg/mL (87.01 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 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 |
*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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