2. Stem Cell/Wnt TGF-beta/Smad
  3. TGF-beta/Smad
  4. Phyllanthin

Phyllanthin is an effective oral anticancer agent. Phyllanthin inhibits MOLT-4 cell viability, increases apoptosis, inhibits cell migration and invasion. Phyllanthin exerts anti-fibrotic effects by down-regulating TGF signaling pathway via ALK5 and Smad2/3. Phyllanthin also has anti-inflammatory and antibacterial properties .

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Phyllanthin Chemical Structure

Phyllanthin Chemical Structure

CAS No. : 10351-88-9

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1 mg USD 60 In-stock
5 mg USD 150 In-stock
10 mg USD 220 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Phyllanthin:

Phyllanthin Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Phyllanthin is an effective oral anticancer agent. Phyllanthin inhibits MOLT-4 cell viability, increases apoptosis, inhibits cell migration and invasion. Phyllanthin exerts anti-fibrotic effects by down-regulating TGF signaling pathway via ALK5 and Smad2/3. Phyllanthin also has anti-inflammatory and antibacterial properties [1] [2] [3].

IC50 & Target

Inhibits TGF-β1 with inhibition constant of 33.15 mM.
In Vitro

Phyllanthin (1.56, 6.25 and 25μM; 2 h) inhibits LPS (HY-D1056) induced proinflammatory responses in U937 macrophages [4].
Phyllanthin (5-100 μM/mL; 24 h) inhibits cell growth with an IC 50 value of 25 µM/mL, and induces apoptosis in MOLT-4 leukemia cancer cells [3].
Phyllanthin is predicted to have strong activity against COVID-19 through inhibiting spike glycoprotein and main protease [7].

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

Phyllanthin Related Antibodies

Cell Viability Assay[3] [4]

Cell Line: U937 macrophages, MOLT-4 cells and normal MS‐5 cells
Concentration: 1.56, 3.12, 6.25, 12.5, and 25 μM (U937 macrophages);
5, 10, 25, 50, 75, and 100 μM/mL (MOLT-4 cells and normal MS‐5 cells)
Incubation Time: 24 h
Result: No effect on the viability of U937 macrophages and MS‐5 cells.
Reduced cell viability of MOLT-4 in a dose-dependent manner.

Western Blot Analysis[3] [4]

Cell Line: LPS (1 μg/mL) (HY- D1056) treated U937 macrophages for 30 min
Concentration: 1.56, 6.25, and 25 μM
Incubation Time: 2 h
Result: Inhibited phosphorylation levels of IKKα/β, p65 and IκBα in a concentration‐dependent manner.
Suppressed LPS‐stimulated activation of JNK, ERK, p38 and AKT in a concentration‐dependent manner.

Real Time qPCR[4]

Cell Line: LPS (1 μg/mL) (HY- D1056) treated U937 macrophages for 1 day
Concentration: 1.56, 6.25 and 25 μM
Incubation Time: 2 h
Result: Dose-dependently suppressed the increased TNF‐α mRNA level at concentrations of 1.25, 6.25 and 25 μM.
Significantly suppressed IL‐1β gene expression at concentrations of 6.25 and 25 μM.
In Vivo

Phyllanthin (10 mg/kg; oral administration; once a day; 30 days) has protective effects in carbon tetrachloride (HY-Y0298) induced hepatotoxicity and experimental liver fibrosis in mice [2].
Phyllanthin (30 mg/kg; oral administration; single dose) exerts anti-tumor effects in diethylnitrosamine (HY-N7434) induced liver carcinogenesis in rats [5].
Phyllanthin (20-100 mg/kg; oral administration; once a day; 14 days) inhibits cellular and humoral immune responses in Balb/C mice [6].

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

Animal Model: Carbon tetrachloride (HY-Y0298) treated Swiss strain female mice (32-35 g) [2]
Dosage: 10 mg/kg
Administration: Oral administration (p.o.); once a day; 30 days
Result: Normalized the level of liver marker enzymes (ALT and AST) and collagen content in hepatotoxicity and experimental liver fibrosis mice.
Restored normal liver architecture, reversed the formation of continuous fibrotic septa between the central and portal veins and nodules.
Reduced the levels of TGF-β1, ALK5, p-Smad2 and p-Smad3 in hepatotoxicity and experimental liver fibrosis mice.
Animal Model: Diethylnitrosamine (Cat. No. HY-N7434) treated male Wistar albino rats (210-230 g)[5]
Dosage: 30 mg/kg
Administration: Oral administration (p.o.); single dose
Result: Significantly reduced 8-OHdG levels and delayed the oxidative damage in diethylnitrosamine -induced liver cancer rats.
Significantly reduced liver tissue injury biomarkers (ALT, AST, GGT, ALP and LDH) levels and tumor markers (AFP and CEA).
Reduced cellular enlargement, nodules, and hyperplasiaenlargement in diethylnitrosamine-induced liver tissue.
Animal Model: Male Balb/C mice aged 6-8 weeks old (18-22 g) [6]
Dosage: 20 mg/kg, 40 mg/kg, and 100 mg/kg
Administration: Oral administration (p.o.); once a day; 14 days
Result: Dose-dependently inhibited CD11b/CD18 adhesion, the engulfment of E.coli by peritoneal macrophages molecules, NO and MPO release.
Dose-dependently inhibited T and B lymphocytes proliferation and down-regulated Th1 (IL-2 and IFN-γ) and Th2 (IL-4) cytokines.
Dose-dependently inhibited the sheep red blood cell (sRBC)-induced swelling rate of mice paw in delayed type hypersensitivity.
Significantly inhibited the serum levels of ceruloplasmin and lysozyme at higher doses (40 and 100 mg/kg).
Dose-dependently down-regulated anti-sRBC immunoglobulins (IgM and IgG) antibody titer.
Molecular Weight

418.52

Formula

C24H34O6
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

COC[C@@H](CC1=CC=C(OC)C(OC)=C1)[C@@H](COC)CC2=CC=C(OC)C(OC)=C2
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 : 62.5 mg/mL (149.34 mM; ultrasonic and warming and heat to 60°C; 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 2.3894 mL 11.9469 mL 23.8937 mL
5 mM 0.4779 mL 2.3894 mL 4.7787 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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  • Dilution Calculator

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

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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: ≥ 2.5 mg/mL (5.97 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 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.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (5.97 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: 99.96%

SDS (252 KB)

COA (264 KB) HNMR (194 KB) RP-HPLC (95 KB) MS (132 KB)

Handling Instructions (2659 KB)
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 2.3894 mL 11.9469 mL 23.8937 mL 59.7343 mL
5 mM 0.4779 mL 2.3894 mL 4.7787 mL 11.9469 mL
10 mM 0.2389 mL 1.1947 mL 2.3894 mL 5.9734 mL
15 mM 0.1593 mL 0.7965 mL 1.5929 mL 3.9823 mL
20 mM 0.1195 mL 0.5973 mL 1.1947 mL 2.9867 mL
25 mM 0.0956 mL 0.4779 mL 0.9557 mL 2.3894 mL
30 mM 0.0796 mL 0.3982 mL 0.7965 mL 1.9911 mL
40 mM 0.0597 mL 0.2987 mL 0.5973 mL 1.4934 mL
50 mM 0.0478 mL 0.2389 mL 0.4779 mL 1.1947 mL
60 mM 0.0398 mL 0.1991 mL 0.3982 mL 0.9956 mL
80 mM 0.0299 mL 0.1493 mL 0.2987 mL 0.7467 mL
100 mM 0.0239 mL 0.1195 mL 0.2389 mL 0.5973 mL
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Phyllanthin Related Classifications

Help & FAQs
  • 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.

Keywords:

Phyllanthin10351-88-9TGF-beta/SmadTransforming growth factor betabioactiveU937 macrophagesMOLT-4 leukemia cancer cellsMS‐5 cellsBalb/C miceMice model of hepatotoxicity and experimental liver fibrosisRat model of liver cancerInhibitorinhibitorinhibit

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