GLPBio

Withaferin A

Catalog No.: GC17309Purity:>98.00%Synonyms: NSC 101088, NSC 273757
COASDSData Sheet
Withaferin A ist ein aus Withania somnifera isoliertes Steroidlacton, das die NF-kB-Aktivierung hemmt und auf Vimentin abzielt, mit starken entzÜndungshemmenden und krebsbekÄmpfenden AktivitÄten.

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Withaferin A
Cas No.: 5119-48-2
10mM (in 1mL DMSO)In Stock
$232.00
1
1mgIn Stock
$104.00
1
5mgIn Stock
$224.00
1
10mgIn Stock
$368.00
1
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    618, 1017–1023 (2023)
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    610, 366–372 (2022)
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    187(9):2288-2304 (2024)
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    183(7):1867-1883 (2020)
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Beschreibung (Description)

Withaferin A is a steroidal lactone generally obtained from Withania somnifera (L.) Dunal, commonly known as Ashwagandha[1]. Withaferin A can inhibits NF-κB at a very low concentration in endothelial cells[2] and exhibits a broad spectrum of biological activities, including antioxidant, anti-inflammatory, antibacterial, antistress, cardioprotective, neuroprotective, and anticancer activities[3]. Withaferin A is commonly utilized in cancer research due to its anticancer activities against various cancer cell lines and preclinical cancer models, achieved by modulating the expression and activity of different oncogenic proteins[4].

Withaferin A potently inhibited cell proliferation in human MPM cells, treatment with Withaferin A at 5µM for 72h significantly inhibit cell growth[5]. In MCF-7 cells, treatment with Withaferin A at 2.5µM for 24h can increase in the level of total as well as S15 phosphorylated p53, which has been implicated in apoptosis induction[6].

Withaferin A (4mg/kg; 14d; i.p.) treatment can inhibits Isoproterenol-induced myocardial fibrosis in mice and significantly reduce heart necrosis[7]. Treatment with Withaferin A (4mg/kg; 10d; i.p.) significantly reduced murine solid tumour growth and improved survival rate of tumour bearing mice[8].

References:
[1]. Paul S, Chakraborty S, Anand U, et al. Withania somnifera (L.) Dunal (Ashwagandha): A comprehensive review on ethnopharmacology, pharmacotherapeutics, biomedicinal and toxicological aspects. Biomed Pharmacother. 2021 Nov;143:112175. doi: 10.1016/j.biopha.2021.112175. Epub 2021 Sep 27. PMID: 34649336.
[2]. Mohan R, Hammers HJ, Bargagna-Mohan P, et al. Withaferin A is a potent inhibitor of angiogenesis. Angiogenesis. 2004;7(2):115-22. doi: 10.1007/s10456-004-1026-3. PMID: 15516832.
[3]Tewari D, Chander V, Dhyani A, et al. Withania somnifera (L.) Dunal: Phytochemistry, structure-activity relationship, and anticancer potential. Phytomedicine. 2022 Apr;98:153949. doi: 10.1016/j.phymed.2022.153949. Epub 2022 Jan 19. PMID: 35151215.
[4]. Kumar S, Mathew SO, Aharwal RP, et al. Withaferin A: A Pleiotropic Anticancer Agent from the Indian Medicinal Plant Withania somnifera (L.) Dunal. Pharmaceuticals (Basel). 2023 Jan 22;16(2):160. doi: 10.3390/ph16020160. PMID: 37259311; PMCID: PMC9966696.
[5]. Yang H, Wang Y, Cheryan VT, et al. Withaferin A inhibits the proteasome activity in mesothelioma in vitro and in vivo. PLoS One. 2012;7(8):e41214. doi: 10.1371/journal.pone.0041214. Epub 2012 Aug 17. PMID: 22912669; PMCID: PMC3422308.
[6]. Hahm ER, Lee J, Huang Y, et al. Withaferin a suppresses estrogen receptor-α expression in human breast cancer cells. Mol Carcinog. 2011 Aug;50(8):614-24. doi: 10.1002/mc.20760. Epub 2011 Mar 22. PMID: 21432907; PMCID: PMC3129407.
[7]. Challa AA, Vukmirovic M, Blackmon J, et al. Withaferin-A reduces type I collagen expression in vitro and inhibits development of myocardial fibrosis in vivo. PLoS One. 2012;7(8):e42989. doi: 10.1371/journal.pone.0042989. Epub 2012 Aug 10. PMID: 22900077; PMCID: PMC3416765.
[8]. Abeesh P, Vishnu WK, Guruvayoorappan C. Preparation and characterization of withaferin A loaded pegylated nanoliposomal formulation with high loading efficacy: In vitro and in vivo anti-tumour study. Mater Sci Eng C Mater Biol Appl. 2021 Sep;128:112335. doi: 10.1016/j.msec.2021.112335. Epub 2021 Jul 27. Erratum in: Mater Sci Eng C Mater Biol Appl. 2021 Nov;130:112432. doi: 10.1016/j.msec.2021.112432. PMID: 34474886.

Protokoll (Protocol)

Cell experiment [1]:

Cell lines

 MPM

Preparation Method

 MPM cells were treated with 5µM dose of Withaferin A for 72h. Then viable/live cells were determined by MTT assay to evaluate cell proliferation.

Reaction Conditions

 5µM; 72h

Applications

 Withaferin A treatment inhibits MPM cell proliferation.
Animal experiment [2]:

Animal models

 129 Svev male mice

Preparation Method

 Isoproterenol (50mg/kg) was injected subcutaneously into 129 Svev male mice for 2 consecutive days, while Withaferin A (4mg/kg) was administered intraperitoneally daily for 14 days. 24h after the last injection, hearts were removed, weighed, fixed and processed for histopathologic analysis.

Dosage form

 4mg/kg; 14d; i.p.

Applications

 Withaferin A was greatly reduced Isoproterenol-induced heart necrosis compared to animals treated with Isoproterenol alone.

References:
[1]. Yang H, Wang Y, Cheryan VT, et al. Withaferin A inhibits the proteasome activity in mesothelioma in vitro and in vivo. PLoS One. 2012;7(8):e41214. doi: 10.1371/journal.pone.0041214. Epub 2012 Aug 17. PMID: 22912669; PMCID: PMC3422308.
[2]. Challa AA, Vukmirovic M, Blackmon J, et al. Withaferin-A reduces type I collagen expression in vitro and inhibits development of myocardial fibrosis in vivo. PLoS One. 2012;7(8):e42989. doi: 10.1371/journal.pone.0042989. Epub 2012 Aug 10. PMID: 22900077; PMCID: PMC3416765.

Produktdokumente (Product Documents)

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Chemische Eigenschaften (Chemical Properties)

CAS-Nr.
5119-48-2
Synonyme
NSC 101088, NSC 273757
Chemischer Name
(4S,4aR,5aR,6aS,6bS,9R,9aS,11aS,11bR)-4-hydroxy-9-((S)-1-((R)-5-(hydroxymethyl)-4-methyl-6-oxo-3,6-dihydro-2H-pyran-2-yl)ethyl)-9a,11b-dimethyl-5a,6,6a,6b,7,8,9,9a,10,11,11a,11b-dodecahydrocyclopenta[1,2]phenanthro[8a,9-b]oxiren-1(4H)-one
SMILES
O[C@@H](C=C1)[C@@]23O[C@@H]2C[C@@H]([C@H]4[C@@]5(C)[C@@H]([C@H](C)[C@@H](CC(C)=C6CO)OC6=O)CC4)[C@H](CC5)[C@]3(C1=O)C
Summenformel
C28H38O6
Molekulargewicht
470.6
Löslichkeit
DMF: 5 mg/ml, DMSO:50mg/ml, DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml
Lagerung
4°C, protect from light
Allgemeine Hinweise
Wählen Sie anhand der Löslichkeitsdaten des Produkts ein geeignetes Lösungsmittel. Aliquotieren Sie die Stammlösung nach der Herstellung, um wiederholte Gefrier-Auftau-Zyklen zu vermeiden.
Verwenden Sie Stammlösungen bei Lagerung bei -80°C innerhalb von 6 Monaten bzw. bei -20°C innerhalb von 1 Monat.
Zur Verbesserung der Löslichkeit das Röhrchen auf 37°C erwärmen und für eine angemessene Dauer beschallen.
Versandbedingungen
Evaluierungsmuster werden mit Kühlakkus versandt. Andere verfügbare Größen werden bei Raumtemperatur oder auf Anfrage mit Kühlakkus versandt.

Rechner (Calculators)Molarität / Verdünnung / Molekulargewicht / Einheitenumrechnung / In-vivo-Formulierung / Löslichkeit

g/mol

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