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Lespenefril is a novel and potent agent of antioxidant, antimicrobial and anti-inflammatory. It possesses a variety of bioactivities, including chemopreventive, antinociception, anti-inflammatory, anti-diabetic, and antitumor effects. Additionally, lepenefril stimulates the insulin signaling pathway.
| Targets |
Insulin Receptor
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|---|---|
| ln Vitro |
Kaempferitrin activates insulin signaling pathway. At 1–20 μM, kaempferitrin causes over 90% of matured 3T3–L1 adipocytes to survive; at 25 and 50 μM, the survival rates start to rapidly decline. The effects of 10 nM insulin are comparable to those of kaempferitrin (15 μM), which increases the tyrosine phosphorylation of the insulin receptor substrate 1 and the beta tyrosine phosphorylation of the insulin receptor. Additionally, wortmannin, a PI3-K inhibitor, can inhibit the stimulation of akt phosphorylation on ser473 caused by kaempferitrin (15 μM). At 15 μM, kaempferitrin potently induces GLUT4 translocation to the adipocyte membrane; wortmannin inhibits this. Furthermore, in mature 3T3-L1 adipocytes, kaempferitrin increases secreted adiponectin and total levels of Glu4 protein[1]. With IC50s of 45 ± 2.6 and 65 ± 2.6 μM, kaempferitrin is cytotoxic to human cancer cells like HeLa and MDA-MB231 cells, but has minimal toxic effects on non-tumorigenic cells. After treating HeLa cells for 24 and 48 hours, kaempferitrin (45 μM) causes the cells to undergo apoptosis and generate reactive oxygen species (ROS). Additionally, Kaempferitrin (45 μM) causes the expression of proteins linked to the intrinsic pathway of apoptosis, inhibits G1 arrest, and activates caspase 3 in HeLa cells[2].
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| ln Vivo |
Kaempferitrin (2.5, 10 and 25 mg/kg, i.p.) ignificantly reduces tumor weight by 37%, 81%, and 95%, and inhibits tumor growth by 40%, 87%, and 97%, respectively in nu/nu mice bearing HeLa tumor. In mice with tumors, kaempferitrin also reduces cell division and increases longevity[2].
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| Cell Assay |
The MTT assay is used to perform the viability assay. To achieve confluence, preconfluent 3T3-L1 preadipocytes are seeded. After confluence (day 0), kempferitrin is added in place of insulin, and three hours later, the compound's viability is assessed. On day eight, a second cell viability test is conducted. In the case of kaempferitrin plus insulin therapy, different kaempferitrin concentrations are administered concurrently with 0.2 nM insulin from day 0 to day 8. The control cells are those that were not treated with insulin or kaempferitrin from day 0 to day 8 of differentiation. At the conclusion of the 24 and 48-hour compound treatment periods, MTT cells are cultured for 3 hours in order to assess the viability of the matured 3T3-L1 cells treated with insulin or kaempferitrin. The survival rates are then computed and compared to those of the cells treated without insulin or kaempferitrin[1].
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| Animal Protocol |
The nu/nu mice receive a subcutaneous injection of 1.5 × 106 HeLa cells in their backs. Groups of five mice are given doses of either paclitaxel (PCX) at 1 mg/kg or cisplatin (CDDP) at 1 mg/kg intraperitoneally every day for 32 days, or 2.5 to 25 mg/kg of Kaempferitrin dissolved in 0.1 mL of 0.9% saline solution, four hours after the tumor is implanted. 0.1 mL of the vehicle solution was given to the animal control group. Tumor volume is calculated by multiplying length by width by height2. A vernier caliper is used to measure the size of tumors in millimeters. When the trials are over, the animals are slaughtered, and their tumors are removed and weighed[2].
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| References |
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| Molecular Formula |
C27H30O14
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|---|---|
| Molecular Weight |
578.52
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| Exact Mass |
578.16
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| Elemental Analysis |
C, 56.06; H, 5.23; O, 38.72
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| CAS # |
482-38-2
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| Related CAS # |
482-38-2
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| Appearance |
Solid powder
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| SMILES |
C[C@H]1[C@@H]([C@H]([C@H]([C@@H](O1)OC2=CC(=C3C(=C2)OC(=C(C3=O)O[C@H]4[C@@H]([C@@H]([C@H]([C@@H](O4)C)O)O)O)C5=CC=C(C=C5)O)O)O)O)O
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| InChi Key |
PUPKKEQDLNREIM-QNSQPKOQSA-N
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| InChi Code |
InChI=1S/C27H30O14/c1-9-17(30)20(33)22(35)26(37-9)39-13-7-14(29)16-15(8-13)40-24(11-3-5-12(28)6-4-11)25(19(16)32)41-27-23(36)21(34)18(31)10(2)38-27/h3-10,17-18,20-23,26-31,33-36H,1-2H3/t9-,10-,17-,18-,20+,21+,22+,23+,26-,27-/m0/s1
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| Chemical Name |
5-hydroxy-2-(4-hydroxyphenyl)-3,7-bis[[(2S,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxy]chromen-4-one
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| Synonyms |
BRN 0073958; Kaempferol 3,7-bisrhamnoside; Kaempferitrin
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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: 25~100 mg/mL (43.2~172.9 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.60 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 (3.60 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 (3.60 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7285 mL | 8.6427 mL | 17.2855 mL | |
| 5 mM | 0.3457 mL | 1.7285 mL | 3.4571 mL | |
| 10 mM | 0.1729 mL | 0.8643 mL | 1.7285 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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