1. Anti-infection Cell Cycle/DNA Damage Apoptosis
  2. Fungal Bacterial Topoisomerase Apoptosis
  3. Podocarpusflavone A

Podocarpusflavone A is a biflavonoid present in the leaves of Podocarpus henkelii, with anti-tumor, topoisomerase I inhibitory, antibacterial and antifungal activities. Podocarpusflavone A exhibits antibacterial activity against Enterococcus faecalis and Pseudomonas aeruginosa. Podocarpusflavone A shows weak activity against fungal pathogens. Podocarpusflavone A targets topoisomerase I and induces cell cycle arrest and apoptosis in MCF-7 cells. Podocarpusflavone A can be used for studies on cancer, bacterial and fungal infections.

For research use only. We do not sell to patients.

Podocarpusflavone A

Podocarpusflavone A Chemical Structure

CAS No. : 22136-74-9

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Description

Podocarpusflavone A is a biflavonoid present in the leaves of Podocarpus henkelii, with anti-tumor, topoisomerase I inhibitory, antibacterial and antifungal activities. Podocarpusflavone A exhibits antibacterial activity against Enterococcus faecalis and Pseudomonas aeruginosa. Podocarpusflavone A shows weak activity against fungal pathogens. Podocarpusflavone A targets topoisomerase I and induces cell cycle arrest and apoptosis in MCF-7 cells. Podocarpusflavone A can be used for studies on cancer, bacterial and fungal infections[1].

IC50 & Target[2]

Topoisomerase I

65.98 μg/mL (IC50)

Cellular Effect
Cell Line Type Value Description References
A549 IC50
1.6 μg/mL
Compound: 2
Cytotoxicity against A549 cells
Cytotoxicity against A549 cells
[PMID: 17027271]
B16 IC50
1.6 μg/mL
Compound: 2
Cytotoxicity against B16 cells
Cytotoxicity against B16 cells
[PMID: 17027271]
BGC-823 IC50
1.6 μg/mL
Compound: 2
Cytotoxicity against BGC823 cells
Cytotoxicity against BGC823 cells
[PMID: 17027271]
BHK-21 IC50
0.75 μM
Compound: 12
Cytotoxicity against hamster BHK-21 cells assessed as reduction in cell viability incubated for 24 hrs by Celltiter assay
Cytotoxicity against hamster BHK-21 cells assessed as reduction in cell viability incubated for 24 hrs by Celltiter assay
[PMID: 34274831]
Bel-7402 IC50
1.6 μg/mL
Compound: 2
Cytotoxicity against BEL-7402 cells
Cytotoxicity against BEL-7402 cells
[PMID: 17027271]
DU-145 IC50
1.6 μg/mL
Compound: 2
Cytotoxicity against DU145 cells
Cytotoxicity against DU145 cells
[PMID: 17027271]
HT-29 IC50
1.6 μg/mL
Compound: 2
Cytotoxicity against HT29 cells
Cytotoxicity against HT29 cells
[PMID: 17027271]
HT-29 IC50
7.9 μM
Compound: Podocarpusflavone A
Antiproliferative activity against human HT-29 cells assessed as decrease in cell viability after 24 hrs by CCK8 assay
Antiproliferative activity against human HT-29 cells assessed as decrease in cell viability after 24 hrs by CCK8 assay
[PMID: 30108705]
L6 IC50
0.75 μM
Compound: 12
Cytotoxicity against African green monkey COS-7 cells assessed as reduction in cell viability incubated for 24 hrs by Celltiter assay
Cytotoxicity against African green monkey COS-7 cells assessed as reduction in cell viability incubated for 24 hrs by Celltiter assay
[PMID: 34274831]
MCF7 IC50
1.6 μg/mL
Compound: 2
Cytotoxicity against MCF7 cells
Cytotoxicity against MCF7 cells
[PMID: 17027271]
MCF7 IC50
35.1 μM
Compound: 5
Cytotoxicity against human MCF7 cells measured after 24 hrs by MTT assay
Cytotoxicity against human MCF7 cells measured after 24 hrs by MTT assay
[PMID: 34875389]
MDA-MB-231 IC50
1.6 μg/mL
Compound: 2
Cytotoxicity against MDA-MB-231 cells
Cytotoxicity against MDA-MB-231 cells
[PMID: 17027271]
PC-3 GI50
> 100 μM
Compound: 17
Growth inhibition of human PC3 cells by colorimetric MTT assay
Growth inhibition of human PC3 cells by colorimetric MTT assay
[PMID: 25736997]
SGC-7901 IC50
1.6 μg/mL
Compound: 2
Cytotoxicity against SGC7901 cells
Cytotoxicity against SGC7901 cells
[PMID: 17027271]
In Vitro

Podocarpusflavone A (PFA) (Serial two-fold dilutions from an initial 1 mg/mL; 12-24 h) shows broad-spectrum bactericidal activity against Enterococcus faecalis and Pseudomonas aeruginosa (MIC = 60 μg/mL), with weaker activity against Staphylococcus aureus (MIC = 130 μg/mL) and Escherichia coli (MIC = 250 μg/mL)[1].
Podocarpusflavone A (Serial two-fold dilutions from an initial 1 mg/mL; 24-48 h) exhibits weak antifungal activity against Candida albicans and Aspergillus fumigatus (MIC = 250 μg/mL) and Cryptococcus neoformans (MIC = 130 μg/mL) at 24 h and 48 h incubation[1].
Podocarpusflavone A (CC50 threshold of 1000 μg/mL; MIC values as measured in antibacterial and antifungal assays) has favorable selective antimicrobial activity (SI > 15) against Enterococcus faecalis and Pseudomonas aeruginosa, with lower selectivity against other tested bacterial and fungal pathogens[1].
Podocarpusflavone A (PF) (1-40 µM; 72 h) shows potent antiproliferative activity against KB, MCF-7, DLD and HEp-2 tumor cell lines with ED50 values of 4.67 µg/mL, 15.17 µg/mL, 4.95 µg/mL and 10.87 µg/mL[2].

Podocarpusflavone A (20-40 µg/mL; 24 h) induces cell cycle arrest at sub-G1/S phase and triggers apoptosis in MCF-7 cells[2].
Podocarpusflavone A shows moderate Topoisomerase I inhibitory activity with an IC50 value of 65.98 µg/mL[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[2]

Cell Line: MCF-7 cells
Concentration: 20, 40 µg/mL
Incubation Time: 24 h
Result: Induced cell cycle arrest at sub-G1/S phase in MCF-7 cells.

Apoptosis Analysis[2]

Cell Line: MCF-7 cells
Concentration: 20, 40 µg/mL
Incubation Time: 24 h
Result: Induced apoptosis in MCF-7 cells.
Molecular Weight

552.48

Formula

C31H20O10

CAS No.
Appearance

Solid

Color

Light yellow to green yellow

SMILES

O=C1C=C(C2=CC=C(OC)C=C2)OC3=C(C4=CC(C5=CC(C6=C(O)C=C(O)C=C6O5)=O)=CC=C4O)C(O)=CC(O)=C13

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (90.50 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8100 mL 9.0501 mL 18.1002 mL
5 mM 0.3620 mL 1.8100 mL 3.6200 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.25 mg/mL (2.26 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.62%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8100 mL 9.0501 mL 18.1002 mL 45.2505 mL
5 mM 0.3620 mL 1.8100 mL 3.6200 mL 9.0501 mL
10 mM 0.1810 mL 0.9050 mL 1.8100 mL 4.5251 mL
15 mM 0.1207 mL 0.6033 mL 1.2067 mL 3.0167 mL
20 mM 0.0905 mL 0.4525 mL 0.9050 mL 2.2625 mL
25 mM 0.0724 mL 0.3620 mL 0.7240 mL 1.8100 mL
30 mM 0.0603 mL 0.3017 mL 0.6033 mL 1.5084 mL
40 mM 0.0453 mL 0.2263 mL 0.4525 mL 1.1313 mL
50 mM 0.0362 mL 0.1810 mL 0.3620 mL 0.9050 mL
60 mM 0.0302 mL 0.1508 mL 0.3017 mL 0.7542 mL
80 mM 0.0226 mL 0.1131 mL 0.2263 mL 0.5656 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Podocarpusflavone A
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