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| 5mg |
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| Targets |
Podophyllotoxin glucoside targets topoisomerase II, an essential enzyme that manages DNA topology during replication. By inhibiting topoisomerase II, the compound prevents the relegation of DNA strands, leading to the accumulation of DNA breaks and ultimately triggering cell death. Its activity as a topoisomerase II inhibitor classifies it as an antineoplastic agent.
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| ln Vitro |
Podophyllotoxin glucoside has demonstrated anticancer activity against various cancer cell lines, including HeLa, KB, and GLC4. Its cytotoxicity is attributed to the inhibition of topoisomerase II, which interferes with DNA replication and leads to apoptosis. Studies show that it can effectively inhibit tumor cell growth and induce apoptosis, suggesting it is a potential active ingredient for anticancer therapy.
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| ln Vivo |
In vivo data for Podophyllotoxin glucoside is limited in the available literature. As a derivative of podophyllotoxin with anti-tumor effects, it is expected to exhibit anticancer activity in animal models. Its mechanism of action, involving the inhibition of topoisomerase II, is well-characterized. However, specific in vivo efficacy data and detailed animal model studies are not extensively detailed in the public domain.
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| Enzyme Assay |
The in vitro biochemical activity of Podophyllotoxin glucoside is typically assessed through assays measuring its inhibition of topoisomerase II. The compound is incubated with the enzyme and its DNA substrate. The inhibition of the enzyme's catalytic activity, which prevents DNA strand relegation, is then measured. This can be done by analyzing the accumulation of linear or cleaved DNA products via gel electrophoresis. The compound is dissolved in DMSO and diluted in the appropriate assay buffer.
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| Cell Assay |
In vitro cellular assays for Podophyllotoxin glucoside involve treating cancer cell lines, such as HeLa, KB, and GLC4, with the compound at various concentrations for 24-72 hours. Cell viability is then assessed using standard assays like MTT or CellTiter-Glo. The compound's effect on the cell cycle is analyzed via flow cytometry, and its ability to induce apoptosis is confirmed through methods like Annexin V/PI staining or caspase activity assays.
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| Animal Protocol |
In vivo animal studies for Podophyllotoxin glucoside, while not extensively documented, would typically involve administering the compound to mice bearing tumor xenografts derived from sensitive cancer cell lines. Tumor growth inhibition would be monitored, and the compound's pharmacokinetics and pharmacodynamics would be evaluated. The compound is typically formulated in a vehicle such as 10% DMSO, 40% PEG300, 5% Tween-80, and 45% saline for in vivo administration.
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| ADME/Pharmacokinetics |
Podophyllotoxin glucoside has a molecular weight of 576.55 g/mol and the formula C28H32O13. It is a solid, typically yellow in appearance, and is soluble in DMSO (40-50 mg/mL). It is recommended to store the powder at -20°C for up to 3 years and in solvent at -80°C for up to 1 year. Its density is 1.55 g/cm³.
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| Toxicity/Toxicokinetics |
As a naturally occurring compound and a derivative of podophyllotoxin, a known anticancer agent, it is generally considered to have potential toxicity. Podophyllotoxin and its derivatives can have significant side effects, including gastrointestinal issues and myelosuppression. Therefore, appropriate safety precautions are necessary when handling. As a research compound, standard preclinical toxicity assessments, including acute and repeated-dose studies, would be required to fully establish its safety profile.
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| References | |
| Additional Infomation |
Podophyllotoxin glucoside has been reported to be found in Podophyllum peltatum, Catharanthus flax, and other organisms with relevant data. Physiologically active prostaglandins are present in many tissues and organs. They are potent pressor substances and possess many other physiological activities.
Podophyllotoxin glucoside (CAS 16481-54-2) is a natural product found in plants such as *Podophyllum peltatum* and *Linum catharticum*. Its mechanism of action as an anticancer agent is through the inhibition of topoisomerase II. This is in contrast to its parent compound, podophyllotoxin, which primarily inhibits microtubule assembly. As a lignan compound, it is used in research for its potential in cancer therapy. This product is for research use only and is not for human therapeutic applications. |
| Molecular Formula |
C28H32O13
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|---|---|
| Molecular Weight |
576.54588
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| Exact Mass |
576.184
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| CAS # |
16481-54-2
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| PubChem CID |
161177
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
781.3±60.0 °C at 760 mmHg
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| Melting Point |
152-154℃
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| Flash Point |
258.2±26.4 °C
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| Vapour Pressure |
0.0±2.8 mmHg at 25°C
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| Index of Refraction |
1.660
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| LogP |
-0.66
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
41
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| Complexity |
907
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| Defined Atom Stereocenter Count |
9
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| SMILES |
COC1=CC(=CC(=C1OC)OC)[C@H]2[C@@H]3[C@H](COC3=O)[C@H](C4=CC5=C(C=C24)OCO5)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O
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| InChi Key |
NXVJTGLCCSFGAT-QNDDJFOYSA-N
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| InChi Code |
InChI=1S/C28H32O13/c1-34-17-4-11(5-18(35-2)26(17)36-3)20-12-6-15-16(39-10-38-15)7-13(12)25(14-9-37-27(33)21(14)20)41-28-24(32)23(31)22(30)19(8-29)40-28/h4-7,14,19-25,28-32H,8-10H2,1-3H3/t14-,19+,20+,21-,22+,23-,24+,25-,28-/m0/s1
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| Chemical Name |
(5R,5aR,8aR,9R)-5-[(2R,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-9-(3,4,5-trimethoxyphenyl)-5a,6,8a,9-tetrahydro-5H-[2]benzofuro[6,5-f][1,3]benzodioxol-8-one
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7345 mL | 8.6723 mL | 17.3445 mL | |
| 5 mM | 0.3469 mL | 1.7345 mL | 3.4689 mL | |
| 10 mM | 0.1734 mL | 0.8672 mL | 1.7345 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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