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| Targets |
p65; Autophagy
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| ln Vitro |
Neferine inhibits COX-2 expression and hypoxia-induced NF-B p65 nuclear translocation[1]. In cardiac fibroblasts, neferine inhibits the activation of TGF-1-Smad, ERK, and p38 MAPK signaling as well as the production of collagen that is caused by high glucose. In HG medium with varying concentrations of neferine (1, 2, or 5 μM), cardiac fibroblasts (CFs) are cultured. There are three different time points (24, 48, and 72 h) for CCK-8 assays. High glucose (30 mM) treatment significantly accelerates the proliferation of CFs in a time-dependent manner when compared to normal glucose (NG) and osmotic control (OC) treatments (P<0.05). When compared to vehicle treatment, neferine treatment at either 2 or 5 μM significantly reduces the HG-induced CF proliferation. Neferine does not, however, prevent the proliferation of CFs brought on by HG at 1 μM. Therefore, the remaining experiments employ 2 and 5 μM Neferine[2].
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| ln Vivo |
Low-dose (60 mg/kg/day, gavage) and high-dose (120 mg/kg/day, gavage) lisinine therapy can inhibit hyperglycemia-induced production of type I and III collagen and TGF-β1 proteins. Add[2]].
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| Cell Assay |
Cardiac fibroblasts (CFs) are extracted from the ventricular tissues of newborn mice. After starvation in serum-free medium for 24 h, CFs are incubated in DMEM containing 5.6 mM glucose (normal glucose; NG), 30 mM D-glucose (HG), 30 mM D-glucose plus 1 μM Neferine, 30 mM D-glucose plus 2 μM Neferine, 30 mM D-glucose plus 5 μM Neferine, and 5.6 mM glucose plus 27.5 mM mannose. Cells are removed after 24, 48, and 72 hours. The Cell-LightTM EdU assay and the Cell Counting Kit-8 (CCK-8) are used to measure cell proliferation[2].
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| Animal Protocol |
Mice: Male C57BL/6J mice that are eight weeks old are used. Streptozotocin dissolved in citrate buffer (pH 4.5) is injected intraperitoneally for five days straight to induce diabetes. Only citrate buffer is injected into control mice. An Accu-Check Active glucometer is used to measure the total blood sugar in mouse tail blood. Mice that had blood glucose levels greater than 18 mM were categorized as diabetic and used in this study. Four groups of eight animals each are created at random from the total number of animals. Three groups of diabetic mice are used: group 1, the diabetic control group (DM); group 2, which receives neferine at a dose of 60 mg/kg/day (DM-NL); and group 3, which receives neferine at a dose of 120 mg/kg/day (DM-NH). For 12 weeks, neferine is given by intragastric gavage twice per day. The normal and DM control groups receive equivalent amounts of normal sodium via gavage. At the conclusion of the 12-week treatment period, mice are anesthetized and sacrificed[2].
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| References |
[1]. Baskaran R, et al. Neferine prevents NF-κB translocation and protects muscle cells from oxidative stress and apoptosis induced by hypoxia. Biofactors. 2016 Jul 8;42(4):407-17.
[2]. Liu X, et al. Neferine inhibits proliferation and collagen synthesis induced by high glucose in cardiac fibroblasts and reduces cardiac fibrosis in diabetic mice. Oncotarget. 2016 Sep 20;7(38):61703-61715 |
| Molecular Formula |
C₃₈H₄₄N₂O₆
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|---|---|
| Molecular Weight |
624.77
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| Exact Mass |
624.32
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| Elemental Analysis |
C, 73.05; H, 7.10; N, 4.48; O, 15.36
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| CAS # |
2292-16-2
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| Related CAS # |
2292-16-2
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| Appearance |
Solid powder
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| SMILES |
CN1CCC2=CC(=C(C=C2[C@H]1CC3=CC=C(C=C3)OC)OC4=C(C=CC(=C4)C[C@@H]5C6=CC(=C(C=C6CCN5C)OC)OC)O)OC
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| InChi Key |
MIBATSHDJRIUJK-ROJLCIKYSA-N
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| InChi Code |
InChI=1S/C38H44N2O6/c1-39-15-14-27-21-36(44-5)38(23-30(27)31(39)17-24-7-10-28(42-3)11-8-24)46-34-19-25(9-12-33(34)41)18-32-29-22-37(45-6)35(43-4)20-26(29)13-16-40(32)2/h7-12,19-23,31-32,41H,13-18H2,1-6H3/t31-,32-/m1/s1
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| Chemical Name |
4-[[(1R)-6,7-dimethoxy-2-methyl-3,4-dihydro-1H-isoquinolin-1-yl]methyl]-2-[[(1R)-6-methoxy-1-[(4-methoxyphenyl)methyl]-2-methyl-3,4-dihydro-1H-isoquinolin-7-yl]oxy]phenol
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| Synonyms |
(-)-Neferine; Neferine; (R)-1,2-Dimethoxyaporphine
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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: 100~125 mg/mL (160.1~200.1 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.33 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 20.8 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: ≥ 2.08 mg/mL (3.33 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6006 mL | 8.0029 mL | 16.0059 mL | |
| 5 mM | 0.3201 mL | 1.6006 mL | 3.2012 mL | |
| 10 mM | 0.1601 mL | 0.8003 mL | 1.6006 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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