Apigenin

N. catalogoS2262 Lotto:S226206

Stampa

Dati tecnici

Formula

C15H10O5

Peso molecolare 270.24 Numero CAS 520-36-5
Solubilità (25°C)* In vitro DMSO 54 mg/mL (199.82 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Aggiungere i solventi al prodotto singolarmente e in ordine.)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml significa leggermente solubile o insolubile.
* Si prega di notare che Selleck testa la solubilità di tutti i composti internamente e la solubilità effettiva può differire leggermente dai valori pubblicati. Ciò è normale ed è dovuto a leggere variazioni da lotto a lotto.
* Spedizione a temperatura ambiente (I test di stabilità mostrano che questo prodotto può essere spedito senza alcuna misura di raffreddamento.)

Preparazione delle soluzioni stock

Attività biologica

Descrizione Apigenin è un potente inibitore di P450 per CYP2C9 con Ki di 2 μM.
Target
CYP2C9
2 μM(Ki)
In vitro Apigenin inhibits PKC by competing with adenosine triphosphate (ATP). This compound also reduces the level of TPA-stimulated phosphorylation of cellular proteins and inhibits TPA-induced c-jun and c-fos expression. It exhibits the reverting effect on the transformed morphology of v-H-ras transformed NIH3T3 cells. It has been shown to possess anti-mutagenic properties in a setting of nitropyrene-induced genotoxicity in Chinese hamster ovary cells. This chemical suppresses of LPS-induced cyclooxygenase-2 and nitric oxide synthase-2 activity and expression in mouse macrophages. It has been reported to inhibit protein kinase C activity, mitogen-activated protein kinase (MAPK), transformation of C3HI mouse embryonic fibroblasts and downstream oncogenes in v-Ha-ras-transformed NIH3T3 cells. This compound blocks peroxisome proliferation-regulated kinase (ERK), a MAPK in isolated hepatocytes. It has further been shown to down-regulate the expression of the Na+/Ca2+-exchanger, a protein important for calcium extrusion in neonatal rat cardiac myocytes. It induces a reversible G2/M and G0/G1 arrest by inhibiting p34 (cdc2) kinase activity, accompanied by increased p53 protein stability in epidermal cells and fibroblasts. It is also effective in inhibiting TNFα-induced intracellular adhesion molecule-1 upregulation in cultured human endothelial cells. It inhibits the expression of HIF-1α and VEGF via the PI3K/Akt/p70S6K1 and HDM2/p53 pathways in human ovarian cancer cells. It inhibits differentiation by suppressing MAPK signal transduction and reducing API transcription factor level in human keratinocytes. This compound also inhibits proliferating of human keratinocytes.
In vivo Apigenin down-regulates production of IL-4 in ovalbumin-immunized BALB/C mice. This compound inhibits melanoma lung metastases by impairing interaction of tumor cells with endothelium. It is shown to cause a significant increase in uterine weight and overall uterine concentration of estrogen receptor (ER)-α in female mice (64) and also suppresses prostate and breast cancer cell growth through estrogen receptor β1. This chemical suppresses the levels of IGF-I in prostate tumor xenografts and increases levels of IGFBP-3, a binding protein that sequesters IGF-I in vascular circulation. This compound (12.5 mg/kg) increases cell proliferation in the dentate gyrus of hippocampus of adult mice.
Caratteristiche Molto più potente di kaempferol e myricetina nell'inibizione di CT-L.

Protocollo (da riferimento)

Saggio cellulare:

[5]
  • Linee cellulari

    WI-38, T-24, HT-1376 and PC-3 cells

  • Concentrazioni

    0, 1, 5, 10, 20, 30, 40, and 50 μg/ml

  • Tempo di incubazione

    24 h

  • Metodo

    To measure the effect of apigenin on cell viability, the WI-38, T-24, HT-1376 and PC-3 cells were seeded in 24-well plates (1 × 105 cells/well) for 16-18 h. The cells were then treated with or without various concentrations (0, 1, 5, 10, 20, 30, 40, and 50 μg/ml) of this compound for 24 h. Each treatment was repeated 3 times. After the exposure period, the medium was removed and followed by washing the cells with PBS. The medium was then changed and incubated with 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution (5 mg/ml)/well for 4 h. The medium was removed, and formazan was solubilised in isopropanol and measured spectrophotometrically at 563 nm. The percentage of viable cells was estimated by comparing them with the untreated control cells.
Studio sugli animali:

[6]
  • Modelli animali

    heterozygous C57BL/TGN TRAMP mice

  • Dosaggi

    20 and 50 μg/mouse/day

  • Somministrazione

    p.o.

Riferimenti

  • https://pubmed.ncbi.nlm.nih.gov/9589348/
  • https://pubmed.ncbi.nlm.nih.gov/20306120/
  • https://pubmed.ncbi.nlm.nih.gov/17493651/
  • https://pubmed.ncbi.nlm.nih.gov/19441930/
  • https://pubmed.ncbi.nlm.nih.gov/25859163/
  • https://pubmed.ncbi.nlm.nih.gov/24067903/

Convalida del prodotto da parte del cliente

<p>Western blotting confirmed that both GLUT-1 (A) and p-Akt (B) were expressed in Hep-2 cells in different apigenin and cisplatin concentration.</p>

, , Int J Clin Exp Pathol, 2014, 7(7):3938-3.

SKH-1 mice were subjected to UVB radiation (1000 J/m2 daily, 5 days), or topical apigenin (Api, 5 μmol, in 200 μl vehicle, DMSO: acetone 1:9) was applied 1 h prior to each UVB exposure. Mice were also sham-irradiated and treated with apigenin, and the control group of mice was subjected to sham irradiation and vehicle. 24 h after the final UVB exposure, the mice were euthanized, dorsal skin was harvested, fixed in formalin and paraffin-embedded. (A) Representative Hematoxylin and Eosin (H&E) staining of skin sections (scale bar, 100 μm). (B) Quantitation of epidermal thickness (mean ± SD), *, P < 0.001; **, P< 0.0001. Three sections per mouse and 3 mice per group were evaluated.

Dati da [ , , Cell Signal, 2016, 28(5):460-468 ]

The effects of apigenin and GLUT-1 AS-ODNs on xenograft apoptosis (the second experiment), observed an under optical microscope (magnification, ×400), and the percentage of apoptotic cells in 100 cells per field was counted and used to calculate the mean apoptosis index (AI). AI, apoptotic index.

Dati da [ , , Oncol Rep, 2015, 34(4):1805-14 ]

GLUT-1 mRNA expression levels were significantly reduced in the ACC-2 human adenoid cystic carcinoma cells following treatment with increasing doses of apigenin (P<0.05), as determined by reverse transcription-quantitative polymerase chain reaction. Following treatment with 10 µM apigenin, the expression levels of GLUT-1 mRNA did not vary significantly with increasing treatment duration (P>0.05). Following treatment with 40 and 160 µM apigenin, the expression levels of GLUT-1 mRNA were significantly reduced with increasing treatment duration. *P<0.05 vs. control. GLUT-1, glucose transporter-1.

Dati da [ , , Mol Med Rep, 2015, 12(5):6461-6 ]

Selleck's Apigenin È stato citato da 39 Pubblicazioni

Apigenin promotes remodeling of peripheral and skeletal adipocytes in response to β3-AR and TLR4 activation [ Frontiers in Endocrinology, October 17, 2025, 1633584] PubMed: 41180186
Apigenin inhibits proliferation of human chondrosarcoma cells via cell cycle arrest and mitochondrial apoptosis induced by ROS generation-an in vitro and in vivo study [ International Journal of Clinical and Experimental Medicine, March 30, 2018, 1615-1631]
Synergism Antiproliferative Effects of Apigenin and Naringenin in NSCLC Cells [ Molecules, June 23, 2023, 4947] PubMed: 37446609
Apigenin induces apoptosis and counteracts cisplatin-induced chemoresistance via Mcl-1 in ovarian cancer cells [ Experimental and Therapeutic Medicine, June 11, 2020, 1329-1336] PubMed: 32742367
Apigenin inhibits lipid metabolism of hepatocellular carcinoma cells by targeting the histone demethylase KDM1A [ Phytomedicine, 2024, 135:156024] PubMed: 39341125
The Effects of Resveratrol and Apigenin on Jejunal Oxidative Injury in Ducks and on Immortalized Duck Intestinal Epithelial Cells Exposed to H2O2 [ Antioxidants (Basel), 2024, 13(5)611] PubMed: 38790716
Viscoelastic high-molecular-weight hyaluronic acid hydrogels support rapid glioblastoma cell invasion with leader-follower dynamics [ bioRxiv, 2024, 2024.04.04.588167] PubMed: 38617333
Connexin43 is associated with the progression of clear cell renal carcinoma and is regulated by tangeretin to sygergize with tyrosine kinase inhibitors [ Transl Oncol, 2023, 35:101712] PubMed: 37354638
Synergism Antiproliferative Effects of Apigenin and Naringenin in NSCLC Cells [ Molecules, 2023, 28(13)4947] PubMed: 37446609
Nao Tan Qing ameliorates Alzheimer's disease-like pathology by regulating glycolipid metabolism and neuroinflammation: A network pharmacology analysis and biological validation [ Pharmacol Res, 2022, 185:106489] PubMed: 36228869

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