Parthenolide |
Catalog No.GN10357
One-Click Copy Product Info
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Parthenolide is an NF-κB inhibitor with IC50 values for Eca109, KYSE-510, SiHa and MCF-7 cells of approximately 10.3, 13.3, 8.42 and 9.54µM at 48h respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 20554-84-1
Sample solution is provided at 25 µL, 10mM.
Parthenolide is an NF-κB inhibitor with IC50 values for Eca109, KYSE-510, SiHa and MCF-7 cells of approximately 10.3, 13.3, 8.42 and 9.54µM at 48h respectively[1][2]. Parthenolide, a sesquiterpene lactone derived from the plant Tanacetum parthenium, is recognized for its multifaceted biological activities, including anti-inflammatory, anti-tumor, and anti-viral properties. Parthenolide holds promise as a stable anti-inflammatory therapeutic and is currently under investigation in cancer clinical trials[3][4].
In vitro, Parthenolide (0, 5, 10, 20μM) treated human esophageal cancer Eca109 cells for 48h suppressed cell proliferation and migration by downregulating expression of NF-κB and VEGF in Eca109 cells[1]. Parthenolide (0.5, 1.0 and 5.0μM) exerted anti-inflammatory effect on lipopolysaccharide (LPS)-activated mouse macrophages by dose-dependently reducing IL-12 production through the downregulation of NFκB-mediated activation and binding to the p40-κB site[5]. After being applied to Vero cells infected with HSV-1 at a concentration of 2.5µg/mL for 24 hours, Parthenolide exhibited antiviral activity by disrupting cellular pathways crucial for effective virus replication. This was achieved by enhancing the expression of both caspase-8 and caspase-9, and by diminishing the accumulation of the NF-κB p65 subunit within the cell nucleus[6].
In vivo, 4mg/kg Parthenolide was intraperitoneal injected three times a week in human esophageal cancer cells bering mice for 4 weeks and exhibited anti-tumor-growth and anti-angiogenesis effect by negatively regulating the NF-κB/AP-1 pathway[1]. Parthenolide(10mg/kg)was administered by intraperitoneal (i.p.) injection and relieved colon inflammation in mice model by regulating Treg/Th17 balance in a gut-microbe dependent manner, mainly through the increased microbiota-derived SCFAs production[7]. Parthenolide exerted a protective effect from the liver injury after biliary duct ligation (BDL) in Phb1 KO mice. By intraperitoneal administered at a dose of 3mg/kg, 24 hours and 1 hour before BDL, or twice a week over a two-week period, Parthenolide effectively normalized the elevated levels of HDAC4 protein that resulted from the absence of Phb1[8].
References:
[1] Tian B.,Xiao YH,Ma JL,et al.Parthenolide Inhibits Angiogenesis in Esophageal Squamous Cell Carcinoma Through Suppression of VEGF.Onco Targets Ther.2020 Jul 29;13:7447–7458.
[2] Al-Fatlawi A.A., Atheer A Al-Fatlawi A.A., Irshad M, Rahisuddin, Ahmad A.Effect of parthenolide on growth and apoptosis regulatory genes of human cancer cell lines.Pharm Biol. 2015 Jan;53(1):104-9.
[3] Wang MT, Qiyan Li QY.Parthenolide could become a promising and stable drug with anti-inflammatory effects.Nat Prod Res. 2015;29(12):1092-101.
[4] Ghantous A, Sinjab A,Herceg Z,Darwiche N.Parthenolide: from plant shoots to cancer roots.Drug Discov Today.2013 Sep;18(17-18):894-905
[5] Kang BY,Chung SW,Kim TS.Inhibition of interleukin-12 production in lipopolysaccharide-activated mouse macrophages by parthenolide, a predominant sesquiterpene lactone in Tanacetum parthenium: involvement of nuclear factor-kappaB.Immunol Lett.2001 Jul 2;77(3):159-63.
[6] Benassi-Zanqueta E.,Marques C.F.,Nocchi S.R.,et al. Parthenolide Influences Herpes simplex virus 1 Replication in vitro.Intervirology. 2018;61(1):14-22.
[7] Liu YJ,Tang B,Wang FC,et al.Parthenolide ameliorates colon inflammation through regulating Treg/Th17 balance in a gut microbiota-dependent manner.Theranostics. 2020 Apr 6;10(12):5225-5241
[8] Barbier-Torres L.,Beraza N., Fernández-Tussy P.,et al.Histone deacetylase 4 promotes cholestatic liver injury in the absence of prohibitin-1.Hepatology.2015 Oct;62(4):1237-48.
| Cell experiment [1]: | |
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Cell lines |
SiHa and MCF-7 cells |
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Preparation Method |
Both SiHa and MCF-7 cells were treated with various concentrations of Parthenolide ranging between 3.5 and 21µM for 24 and 48h time points before MTT assay and LDH assay were performed. SiHa and MCF-7 cells were treated with different concentrations (4.5–11.5µM) of Parthenolide for 48h before mRNA expression of apoptosis regulatory genes were examined. |
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Reaction Conditions |
3.5–21µM; 24h and 48h |
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Applications |
Parthenolide inhibited the growth of MCF-7 and SiHa cancerous cells by upregulating caspase-3, -6, and -9 genes and causing DNA fragmentation as the consequence of apoptosis. |
| Animal experiment [2]: | |
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Animal models |
Female BALB/c nude mice |
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Preparation Method |
Eca109 cells were digested with trypsin to yield a single cell suspension containing 1×107 cells/mL in PBS. At a dose of 100µL per mice, the cell suspension was subcutaneously injected to the right side of each 4-week-old female BALB/c nude mice. The two groups generated by random selection were injected intraperitoneally with DMSO and Parthenolide (4mg/kg) three times a week, respectively. The body weight and tumor volume of the mice were measured every 2 days. |
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Dosage form |
4mg/kg; i.p.; 3 times/week |
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Applications |
Parthenolide suppressed tumor growth and tumor angiogenesis in human esophageal cancer Eca109 cells subcutaneous xenograft tumor model by inhibiting expression of NF-κB, AP-1, and VEGF. |
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References: |
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| Cas No. | 20554-84-1 | SDF | |
| Chemical Name | (1aR,7aS,10aS,10bS,E)-1a,5-dimethyl-8-methylene-2,3,6,7,7a,8,10a,10b-octahydrooxireno[2',3':9,10]cyclodeca[1,2-b]furan-9(1aH)-one | ||
| Canonical SMILES | C[C@@]12CC/C=C(C)/CC[C@@H]3[C@H](OC(C3=C)=O)[C@@H]1O2 | ||
| Formula | C15H20O3 | M.Wt | 248.32 |
| Solubility | ≥ 9.2mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.0271 mL | 20.1353 mL | 40.2706 mL |
| 5 mM | 805.4 μL | 4.0271 mL | 8.0541 mL |
| 10 mM | 402.7 μL | 2.0135 mL | 4.0271 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)