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Purity: ≥98%
Puerarin (Kakonein), a naturally occuring isoflavone isolated from the root of Radix puerariae, is a 5-HT2C receptor and benzodiazepine site antagonist. Puerarin (Kakonein), an isoflavone that binds to the benzodiazepine site and the 5-HT2C receptor is present in the root of Radix puerariae. In China, pulmonary ailments are treated clinically with pulmonaria. Puerarin has been shown in another study to have anti-cancer qualities. Puerarin, at a dose-dependent 25 μM, inhibits the growth of HT-29 cells by increasing bax and decreasing c-myc and bcl-2.
| Targets |
5-HT2C Receptor
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| ln Vitro |
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| Enzyme Assay |
Puerarin (7,4'-dihydroxy-8-C-glucosylisoflavone) is the most abundant isoflavone-C-glucoside extracted from Radix puerariae, and it has been used for various medicinal purposes in traditional oriental medicine for thousands of years. In the present study, the ability of the puerarin to modulate inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2) and C reactive protein (CRP) expression and induce changes in the nuclear factor κB (NF-κB) pathway in RAW264.7 macrophage cells was examined. The protein and mRNA levels of lipopolysaccharide (LPS)-induced iNOS, COX-2 and CRP were determined in RAW246.7 macrophage cells. Inhibitor κB (I-κB) phosphorylation and p65NF-κB expression in RAW246.7 macrophage cells were also detected under our experimental conditions. The results indicated that puerarin inhibited the expression of LPS-induced iNOS, COX-2 and CRP proteins and also suppressed their mRNAs from RT-PCR experiments in RAW264.7 cells. Subsequently, we determined that the inhibition of iNOS, COX-2 and CRP expression was due to a dose-dependent inhibition of phosphorylation and degradation of I-κB, which resulted in the reduction of p65NF-κB nuclear translocation. These data suggested that the effect of puerarin-mediated inhibition of LPS-induced iNOS, COX-2 and CRP expression is attributed to suppressed NF-κB activation at the transcriptional level [4].
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| Cell Assay |
RAW264.7 cells are kept at subconfluence in a humidified environment that is 95% air and 5% CO2 and is kept at 37°C. Dulbecco's Modified Eagle's Medium, enhanced with 10% fetal bovine serum, penicillin (100 units/mL), and streptomycin (100 μg/mL), is the medium utilized for routine subculture. Following puerarin treatment, the cells' viability is assessed using the MTT assay. The cells are incubated at 37°C with MTT (0.05 mg/mL) for 4 hours, after which the supernatants are removed for nitrite determination. The optical density is then measured at 540 nm. Puerarin is present in concentrations of 10, 20, 40, and 100 μM.
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| References |
[1]. Pharmacol Biochem Behav. 2003 Jun;75(3):619-25. [4]. Pharmacol Rep. 2011;63(3):781-9. |
| Molecular Formula |
C21H20O9
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| Molecular Weight |
416.38
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| Exact Mass |
416.11
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| Elemental Analysis |
C, 60.58; H, 4.84; O, 34.58
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| CAS # |
3681-99-0
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| Related CAS # |
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| Appearance |
White to off-white solid powder
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| SMILES |
C1=CC(=CC=C1C2=COC3=C(C2=O)C=CC(=C3[C@H]4[C@@H]([C@H]([C@@H]([C@H](O4)CO)O)O)O)O)O
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| InChi Key |
HKEAFJYKMMKDOR-VPRICQMDSA-N
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| InChi Code |
InChI=1S/C21H20O9/c22-7-14-17(26)18(27)19(28)21(30-14)15-13(24)6-5-11-16(25)12(8-29-20(11)15)9-1-3-10(23)4-2-9/h1-6,8,14,17-19,21-24,26-28H,7H2/t14-,17-,18+,19-,21+/m1/s1
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| Chemical Name |
7-hydroxy-3-(4-hydroxyphenyl)-8-[(2S,3R,4R,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]chromen-4-one
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3 mg/mL (7.20 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 30.0 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: ≥ 3 mg/mL (7.20 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 30.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: 3 mg/mL (7.20 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Solubility in Formulation 4: 20 mg/mL (48.03 mM) in 20% SBE-β-CD in Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. 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. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4017 mL | 12.0083 mL | 24.0165 mL | |
| 5 mM | 0.4803 mL | 2.4017 mL | 4.8033 mL | |
| 10 mM | 0.2402 mL | 1.2008 mL | 2.4017 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03676296 | Completed | Drug: Puerarin Drug: Placebo |
Cardiovascular Disease Risk Factors | The University of Hong Kong | September 5, 2018 | Phase 2 |
| NCT02254655 | Completed | Drug: Puerarin injection 400 mg Drug: Control |
Rheumatoid Arthritis | Chengdu PLA General Hospital | November 2013 | Phase 2 |
| NCT00854724 | Completed | Drug: Puerarin, Placebo | Alcohol Abuse | Mclean Hospital | February 2009 | Phase 2 |
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