Phyllanthin
Based on 1 publication(s) in Google Scholar
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 .
For research use only. We do not sell to patients.
- Purity: 99.97%
- CAS No.: 10351-88-9
- Formula: C24H34O6
- Molecular Weight:418.52
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications Citing Use of MedChemExpress (MCE) Phyllanthin
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Biological Activity
Inhibits TGF-β1 with inhibition constant of 33.15 mM.
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.
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Cell Line:U937 macrophages, MOLT-4 cells and normal MS‐5 cells
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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
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Result:No effect on the viability of U937 macrophages and MS‐5 cells.
Reduced cell viability of MOLT-4 in a dose-dependent manner.
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Cell Line:LPS (1 μg/mL) (HY- D1056) treated U937 macrophages for 30 min
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Concentration:1.56, 6.25, and 25 μM
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Incubation Time:2 h
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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.
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Cell Line:LPS (1 μg/mL) (HY- D1056) treated U937 macrophages for 1 day
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Concentration:1.56, 6.25 and 25 μM
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Incubation Time:2 h
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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.
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.
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Animal Model:Carbon tetrachloride (HY-Y0298) treated Swiss strain female mice (32-35 g) [2]
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Dosage:10 mg/kg
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Administration:Oral administration (p.o.); once a day; 30 days
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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.
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Animal Model:Diethylnitrosamine (Cat. No. HY-N7434) treated male Wistar albino rats (210-230 g)[5]
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Dosage:30 mg/kg
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Administration:Oral administration (p.o.); single dose
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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.
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Animal Model:Male Balb/C mice aged 6-8 weeks old (18-22 g) [6]
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Dosage:20 mg/kg, 40 mg/kg, and 100 mg/kg
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Administration:Oral administration (p.o.); once a day; 14 days
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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.
Chemical Information
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CAS No. 10351-88-9
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Appearance Solid
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Molecular Weight 418.52
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Formula C24H34O6
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Color White to off-white
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SMILES
COC[C@@H](CC1=CC=C(OC)C(OC)=C1)[C@@H](COC)CC2=CC=C(OC)C(OC)=C2
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (287 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Hassanein EHM, et al. The promising antioxidant effects of lignans: Nrf2 activation comes into view. Naunyn Schmiedebergs Arch Pharmacol. 2024 Sep;397(9):6439-6458. [Content Brief]
[2]. Krithika R, et al. Mechanism of protective effect of phyllanthin against carbon tetrachloride-induced hepatotoxicity and experimental liver fibrosis in mice. Toxicol Mech Methods. 2015;25(9):708-17. [Content Brief]
[3]. Wang H, et al. Phyllanthin inhibits MOLT-4 leukemic cancer cell growth and induces apoptosis through the inhibition of AKT and JNK signaling pathway. J Biochem Mol Toxicol. 2021 Jun;35(6):1-10. [Content Brief]
[4]. Harikrishnan H, et al. Phyllanthin from Phyllanthus amarus inhibits LPS-induced proinflammatory responses in U937 macrophages via downregulation of NF-κB/MAPK/PI3K-Akt signaling pathways. Phytother Res. 2018 Dec;32(12):2510-2519. [Content Brief]
[5]. You Y, et al. Phyllanthin prevents diethylnitrosamine (DEN) induced liver carcinogenesis in rats and induces apoptotic cell death in HepG2 cells. Biomed Pharmacother. 2021 May;137:111335. [Content Brief]
[6]. Ilangkovan M, et al. Phyllanthin from Phyllanthus amarus inhibits cellular and humoral immune responses in Balb/C mice. Phytomedicine. 2016 Nov 15;23(12):1441-1450. [Content Brief]
[7]. Marhaeny HD, et al. Phyllanthin and hypophyllanthin, the isolated compounds of Phyllanthus niruri inhibit protein receptor of corona virus (COVID-19) through in silico approach. J Basic Clin Physiol Pharmacol. 2021 Jun 25;32(4):809-815. [Content Brief]
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 |