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Sophocarpine monohydrate, a natural product found in Sophora alopecuroides, has a wide range of pharmacological effects (anti-viral, anti-tumor, anti-inflammatory). Sophocarpine exerts anti-cachectic effects by inhibiting TNF-α and IL-6 production in both RAW264.7 cells and murine primary macrophages. Sophocarpine also shows antivirus activity by inhibiting HHV-6 replication in Molt-3 cells. In addition, Sophocarpine is a potent blocker of HERG K+ channels with an IC50 of about 200 mM.
| Targets |
PI3K/AKT signaling pathway; natural alkaloid
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|---|---|
| ln Vitro |
Sophocarpine is one of the major ingredients of Sophorae flavescentis which could inhibits many kinds of cancers. However, the effect of sophocarpine on gastric cancer (GC) and the mechanism involved remain unknown. The present study aims to explore the effects of the sophocarpine on the proliferation and apoptosis of GC cells and elucidates the relevant molecular mechanisms. After treatment with sophocarpine, GC cells were evaluated on their proliferation, autophagy, cell cycle progress and apoptosis. The protein levels of LC3-I, LC3-II, Beclin, p62, PTEN, PI3K, p53, Bax, Bcl-2, AKT and p-AKT were detected by western blot. Sophocarpine inhibited the proliferation of GC cells both in vitro and in vivo dose-dependently. Sophocarpine not only caused cell apoptosis and cell cycle arrest in G0/G1 phase but also induced cell autophagy. Moreover, sophocarpine dose-dependently suppressed PI3K/AKT signaling pathway and activated apoptosis in gastric cancer cells. Thus, sophocarpine significantly inhibited the growth of GC cells through multiple mechanisms such as induction of autophagy, activation of cell apoptosis and down-regulation of cell survival signaling pathway [1].
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| Toxicity/Toxicokinetics |
rat LD50 oral 196 mg/kg Zhongguo Yaoxue Zazhi. Chinese Pharmacuetical Journal., 27(201), 1992
rat LD50 intraperitoneal 124 mg/kg Zhongguo Yaoxue Zazhi. Chinese Pharmacuetical Journal., 27(201), 1992 mouse LD50 oral 242 mg/kg BEHAVIORAL: TREMOR; BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD Zhongcaoyao. Chinese Traditional and Herbal Medicine., 11(555), 1980 mouse LD50 intravenous 72 mg/kg Zhongguo Yaoxue Zazhi. Chinese Pharmacuetical Journal., 27(201), 1992 mouse LD50 intramuscular 92410 ug/kg BEHAVIORAL: TREMOR; BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD Zhongcaoyao. Chinese Traditional and Herbal Medicine., 11(555), 1980 |
| References | |
| Additional Infomation |
Sophocarpine is an alkaloid.
Sophocarpine has been reported in Daphniphyllum oldhamii, Daphniphyllum pentandrum, and other organisms with data available. |
| Molecular Formula |
C15H22N2O
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|---|---|
| Molecular Weight |
246.3480
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| Exact Mass |
246.173
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| Elemental Analysis |
C, 73.13; H, 9.00; N, 11.37; O, 6.49
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| CAS # |
6483-15-4
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| Related CAS # |
Sophocarpine monohydrate; 145572-44-7
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| PubChem CID |
115269
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
425.4±45.0 °C at 760 mmHg
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| Flash Point |
194.0±21.1 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.603
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| LogP |
1.37
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
18
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| Complexity |
392
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| Defined Atom Stereocenter Count |
4
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| SMILES |
O=C1C([H])=C([H])C([H])([H])[C@]2([H])[C@@]3([H])C([H])([H])C([H])([H])C([H])([H])N4C([H])([H])C([H])([H])C([H])([H])[C@@]([H])(C([H])([H])N21)[C@]43[H]
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| InChi Key |
AAGFPTSOPGCENQ-JLNYLFASSA-N
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| InChi Code |
InChI=1S/C15H22N2O/c18-14-7-1-6-13-12-5-3-9-16-8-2-4-11(15(12)16)10-17(13)14/h1,7,11-13,15H,2-6,8-10H2/t11-,12+,13+,15-/m0/s1
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| Chemical Name |
(1R,2R,9S,17S)-7,13-diazatetracyclo[7.7.1.02,7.013,17]heptadec-4-en-6-one
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| Synonyms |
(-)-Sophocarpine; Sophocarpine
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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 : ~50 mg/mL (~202.96 mM)
H2O : ~10 mg/mL (~40.59 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.44 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 (8.44 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 20.8 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: ≥ 2.08 mg/mL (8.44 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: 10 mg/mL (40.59 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0593 mL | 20.2963 mL | 40.5927 mL | |
| 5 mM | 0.8119 mL | 4.0593 mL | 8.1185 mL | |
| 10 mM | 0.4059 mL | 2.0296 mL | 4.0593 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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