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| 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. |
| References |
[1]. Hu M, et al.Lycorine is a novel inhibitor of the growth and metastasis of hormone-refractory prostate cancer.Oncotarget. 2015 Jun 20;6(17):15348-61.
[2]. Zu-Guo Zheng, et al. Discovery of a Potent SCAP Degrader That Ameliorates HFD-induced Obesity, Hyperlipidemia and Insulin Resistance via an Autophagy-Independent Lysosomal Pathway. Autophagy. 2020 May 20;1-22. [3]. Liu, R. et al. Lycorine hydrochloride inhibits metastatic melanoma cell-dominant vasculogenic mimicry. Pigment cell & melanoma research 25, 630-638, doi:10.1111/j.1755-148X.2012.01036.x (2012). |
| Molecular Formula |
C16H17NO4
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|---|---|
| Molecular Weight |
287.3105
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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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| SMILES |
O([H])[C@]1([H])[C@]([H])(C([H])=C2C([H])([H])C([H])([H])N3C([H])([H])C4=C([H])C5=C(C([H])=C4[C@@]1([H])[C@]32[H])OC([H])([H])O5)O[H]
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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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