1. Apoptosis Autophagy NF-κB Anti-infection
  2. Apoptosis Autophagy Ferroptosis NF-κB Fungal
  3. Formosanin C

Formosanin C is a diosgenin saponin with multiple biological activities. Formosanin C possesses multiple anti-tumor mechanisms, including inducing apoptosis and autophagy, blocking the cell cycle, inhibiting metastasis and inducing ferroptosis. Formosanin C can inhibit the NF-κB signaling pathway to exert anti-inflammatory effects, and enhance the activity of immune cells. Formosanin C exhibits the inhibiting effect against C. albicans. Formosanin C can be used for the study of anti-inflammation, antifungal anti and anti-cancer (including lung cancer, liver cancer, breast cancer and colorectal cancer, etc.).

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

Formosanin C Chemical Structure

Formosanin C Chemical Structure

CAS No. : 50773-42-7

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Based on 4 publication(s) in Google Scholar

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Description

Formosanin C is a diosgenin saponin with multiple biological activities. Formosanin C possesses multiple anti-tumor mechanisms, including inducing apoptosis and autophagy, blocking the cell cycle, inhibiting metastasis and inducing ferroptosis. Formosanin C can inhibit the NF-κB signaling pathway to exert anti-inflammatory effects, and enhance the activity of immune cells. Formosanin C exhibits the inhibiting effect against C. albicans. Formosanin C can be used for the study of anti-inflammation, antifungal anti and anti-cancer (including lung cancer, liver cancer, breast cancer and colorectal cancer, etc.)[1][2][3][4][5][6].

In Vitro

Formosanin C (0-10 μM, 0-4 days) significantly enhances the proliferation response of GM-CFCs in human peripheral whole blood to PHA (Phytohemagglutinin) (HY-11107), and in mouse lymphocytes to Concanavalin A (HY-P2149), as well as in mouse granulocyte/macrophage progenitor cells[1].
. Formosanin C (24-72 h) inhibits HepG2, A549 and SW480 cells growth with IC50s of 13.62 μg/mL, 4.2 μM and 0.06 μM in 24 h, respectively[2][3].
. Formosanin C (5-10 μg/mL, 24-48 h) induces apoptosis of HepG2 cells in a concentration- and time-dependent manner[2].
. Formosanin C (0-8 μM, 24 h) suppresses the lung cancer A549 cells population through caspase activation-mediated apoptosis[3].
Formosanin C (0-5 μg/mL, 24 h) interferes with the cell cycle process by blocking HepG2 cells at the S phase[2].
. Formosanin C (4 μM, 0-72 h) can induce early stage autophagy progression, proceed to blockage of autophagic flux in A549 cells, increase mitochondrial membrane potential, block autophagy progression, and has no influence on CCCP (HY-100941)-induced mitophagy[3].
Formosanin C (2-4 μM, 24 h) suppresses the motility of lung cancer cells through EMT (Epithelial-Mesenchymal Transition) pathway[3].
Formosanin C (5 μM, 24 h) induces ferritinophagy and ferroptosis via a lipid ROS-dependent processin liver cancer HepG2 cells[4].
Formosanin C (0.625-5 μM, 24 h) blunts LPS (HY-D1056)-induced NO and PGE production in a dose-dependent manner, inhibits iNOS and COX-2 expression, and blocks LPS-upregulated mRNA expression and medium release of TNF-α, IL-1β, and IL-6 in macrophages[5].
Formosanin C exhibits the inhibiting effect against C. albicans (MlC =1 ug/mL, pH = 7) and inhibits biofilm formation (MlC = 25 ug/mL)[6].

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

Apoptosis Analysis[2]

Cell Line: HepG2 cells
Concentration: 5 and 10 μg/mL
Incubation Time: 24 and 48 h
Result: Observed karyorrhexis and karyopyknosis.
The nucleuses were broken into pieces at 48 h.
Observed a signal DNA ladder for advanced stage apoptosis and fragmentation for 48 h.

Cell Cycle Analysis[2]

Cell Line: HepG2 cells
Concentration: 0, 1, 3 and 5 μg/mL
Incubation Time: 24 h
Result: Resulted in a significant increase in the S phase and a decrease in the G2/M phase.

Western Blot Analysis[3]

Cell Line: A549 cells
Concentration: 2 and 4 μM
Incubation Time: 24 h
Result: Showed 71% suppression of cell migration at 4 μM.
Decreased the levels of N-cadherin and vimentin.

Western Blot Analysis[5]

Cell Line: macrophages
Concentration: 0.625, 1.25, 2.5 and 5 μg/mL
Incubation Time: 24 h
Result: Exhibited dose-dependent inhibition of iNOS and COX-2 protein expression.
Reduced the phosphorylation levels of IKK, IκBα and p65.
Did not affect the total protein expression of IKK, IκBα and p65.

Real Time qPCR[5]

Cell Line: macrophages
Concentration: 0.625, 1.25, 2.5 and 5 μg/mL
Incubation Time: 24 h
Result: Significantly inhibited the expression of iNOS and COX-2 mRNA induced by LPS.
Dose-dependently reduced the mRNA levels of TNF-α, IL-1β and IL-6.
In Vivo

Formosanin C (1-5 mg/kg, i,p., once daily for 2 days) significantly activates the activity of mouse NK cells and induces the production of interferon in C3H/He mice[1].
Formosanin C (1-5 mg/kg, i,p., once daily for 11 days or every other day for 13 days) significantly inhibited tumor growth in MH-134 cells induced mice xenograft model[1].

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

Animal Model: MH-134 hepatoma xenograft model established in C3H/HeN mice (male, 8 weeks old)[1]
Dosage: 1, 2.5 and 5 mg/kg
Administration: Intraperitoneal injection (i.p.), once daily for 11 days or every other day for 13 days
Result: Significantly inhibits tumor growth, with 2.5 mg/kg dose of the most effective.
Alleviated the toxicity caused by the high dose with alternate-day administration.
Molecular Weight

1015.18

Formula

C51H82O20

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@@]12[C@]3([H])[C@](O[C@]4(CC[C@@H](C)CO4)[C@H]3C)([H])C[C@@]1([H])[C@@]5([H])[C@]([C@@]6(C(C[C@@H](O[C@@]7([H])[C@@H]([C@H]([C@H](O[C@@]8([H])[C@@H]([C@@H]([C@@H](O[C@@]9([H])[C@@H]([C@@H]([C@@H](O)[C@H](C)O9)O)O)[C@H](C)O8)O)O)[C@@H](CO)O7)O)O[C@@]%10([H])[C@@H]([C@@H]([C@@H](O)[C@H](C)O%10)O)O)CC6)=CC5)C)([H])CC2

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (98.50 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 0.9850 mL 4.9252 mL 9.8505 mL
5 mM 0.1970 mL 0.9850 mL 1.9701 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.

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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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (2.46 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (2.46 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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: 99.28%

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 0.9850 mL 4.9252 mL 9.8505 mL 24.6262 mL
5 mM 0.1970 mL 0.9850 mL 1.9701 mL 4.9252 mL
10 mM 0.0985 mL 0.4925 mL 0.9850 mL 2.4626 mL
15 mM 0.0657 mL 0.3283 mL 0.6567 mL 1.6417 mL
20 mM 0.0493 mL 0.2463 mL 0.4925 mL 1.2313 mL
25 mM 0.0394 mL 0.1970 mL 0.3940 mL 0.9850 mL
30 mM 0.0328 mL 0.1642 mL 0.3283 mL 0.8209 mL
40 mM 0.0246 mL 0.1231 mL 0.2463 mL 0.6157 mL
50 mM 0.0197 mL 0.0985 mL 0.1970 mL 0.4925 mL
60 mM 0.0164 mL 0.0821 mL 0.1642 mL 0.4104 mL
80 mM 0.0123 mL 0.0616 mL 0.1231 mL 0.3078 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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Formosanin C
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