| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Targets |
Picropodophyllone acts as an inhibitor of microtubule assembly and DNA topoisomerase II, both critical targets in cancer therapy. It exhibits significant anticancer activity and has been shown to induce apoptosis in cancer cells through multiple mechanisms. As an aryltetralin lignan, it functions as a fungal inhibitor, suggesting additional antimicrobial targets. The compound's ability to interfere with microtubule dynamics and topoisomerase function makes it a valuable tool for studying cell division and DNA replication processes in both cancer and fungal cells.
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| ln Vitro |
Picropodophyllone exhibits antineoplastic activity against various cell lines, including P-388 (murine leukemia), A-549 (human lung carcinoma), and HT-29 (human colon carcinoma) with an IC50 of 12000.0 nM. It has been shown to induce apoptosis in cancer cells through several mechanisms. The compound also demonstrates significant antifungal activity against various fungal pathogens. These in vitro activities support its potential as a lead compound for both anticancer and antifungal drug development, although the relatively high IC50 value suggests moderate potency that may require optimization.
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| ln Vivo |
In vivo studies on Picropodophyllone have not been extensively documented in the available literature. The compound has been isolated from leaves of Podophyllum hexandrum and has antifungal activities. Its anticancer activity observed in vitro against multiple cell lines suggests potential in vivo efficacy that would require further investigation using appropriate animal models. As a research compound primarily used for laboratory studies, systematic in vivo pharmacokinetic and efficacy studies have not been fully reported.
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| Enzyme Assay |
For microtubule assembly inhibition assays, purified tubulin is incubated with Picropodophyllone at various concentrations, and microtubule polymerization is monitored spectrophotometrically at 350 nm. For DNA topoisomerase II inhibition, the enzyme is incubated with kinetoplast DNA and the compound, and decatenation activity is assessed by agarose gel electrophoresis. For antifungal activity testing, fungal cultures are grown in appropriate media and treated with Picropodophyllone, with minimum inhibitory concentration (MIC) determined by broth microdilution following CLSI guidelines.
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| Cell Assay |
Cancer cell lines including P-388 (murine leukemia), A-549 (human lung carcinoma), and HT-29 (human colon carcinoma) are cultured in appropriate media (e.g., RPMI 1640 with 10% FBS). Cells are seeded in 96-well plates and treated with Picropodophyllone at various concentrations for 48-72 hours. Cell viability is assessed using MTT or SRB assays, and IC50 values are calculated from dose-response curves. Apoptosis induction is evaluated by Annexin V-FITC/PI staining and flow cytometry, and cell cycle analysis is performed using propidium iodide staining.
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| Animal Protocol |
For in vivo anticancer efficacy studies, immunocompromised mice bearing tumor xenografts (e.g., A-549 lung carcinoma or HT-29 colon carcinoma) would be administered Picropodophyllone intraperitoneally or orally at various doses. Tumor volume would be measured twice weekly using calipers, and body weight monitored for toxicity. For antifungal efficacy, mouse models of systemic fungal infection would be employed, with survival and fungal burden in organs assessed. However, detailed in vivo protocols for Picropodophyllone have not been extensively reported in the literature.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Picropodophyllone have not been fully characterized in the available literature. As an aryltetralin lignan with a molecular weight of 412.39, it is expected to have moderate lipophilicity and may be absorbed after oral administration. Its metabolism likely involves hepatic cytochrome P450 enzymes, and elimination may occur via biliary excretion. Comprehensive pharmacokinetic studies including bioavailability, half-life, protein binding, and tissue distribution are needed to fully understand its ADME properties.
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| Toxicity/Toxicokinetics |
Picropodophyllone has not been fully validated for medical applications and is intended for research use only. It exhibits significant antifungal activity and antineoplastic activity against various cancer cell lines. The compound has been shown to induce apoptosis in cancer cells. As a natural product isolated from Podophyllum hexandrum, it is related to other podophyllotoxin derivatives with established anticancer activity. However, comprehensive toxicological studies including acute, subchronic, and chronic toxicity have not been documented.
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| References | |
| Additional Infomation |
Reports indicate that juniper contains matrine, and relevant data is available for reference.
Picropodophyllone is an aryltetralin lignan isolated from leaves of Podophyllum hexandrum. It functions as a fungal inhibitor and exhibits significant antifungal activity. The compound also demonstrates antineoplastic activity against P-388, A-549, and HT-29 cell lines with an IC50 of 12000.0 nM. Its mechanism involves inhibition of microtubule assembly and DNA topoisomerase II, leading to apoptosis induction in cancer cells. Picropodophyllone is currently in preclinical research stages and has not been approved for clinical use or received FDA approval. It is primarily used as a research tool for studying fungal pathogenesis and anticancer mechanisms. |
| Molecular Formula |
C22H20O8
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|---|---|
| Molecular Weight |
412.39
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| Exact Mass |
412.116
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| CAS # |
477-48-5
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| PubChem CID |
3083574
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| Appearance |
White to off-white solid powder
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| Boiling Point |
602.3±55.0 °C at 760 mmHg
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| Melting Point |
153-154 °C
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| LogP |
2.558
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
30
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| Complexity |
668
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| Defined Atom Stereocenter Count |
3
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| SMILES |
COC1=CC(=CC(=C1OC)OC)[C@H]2[C@H]3[C@H](COC3=O)C(=O)C4=CC5=C(C=C24)OCO5
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| InChi Key |
ISCQYPPCSYRZOT-MJXNMMHHSA-N
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| InChi Code |
InChI=1S/C22H20O8/c1-25-16-4-10(5-17(26-2)21(16)27-3)18-11-6-14-15(30-9-29-14)7-12(11)20(23)13-8-28-22(24)19(13)18/h4-7,13,18-19H,8-9H2,1-3H3/t13-,18+,19+/m0/s1
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| Chemical Name |
(5aR,8aS,9R)-9-(3,4,5-trimethoxyphenyl)-5a,6,8a,9-tetrahydro-[2]benzofuro[5,6-f][1,3]benzodioxole-5,8-dione
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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 mg/mL (242.49 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.06 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 (6.06 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 (6.06 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 | 2.4249 mL | 12.1244 mL | 24.2489 mL | |
| 5 mM | 0.4850 mL | 2.4249 mL | 4.8498 mL | |
| 10 mM | 0.2425 mL | 1.2124 mL | 2.4249 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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