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Merck
CN

B0189

Casticin

from Vitex trifolia, ≥98% (HPLC)

Synonym(s):

Casticine, Quercetagetin 3,6,7,4′-tetramethyl ether, Vitexicarpin

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About This Item

Empirical Formula (Hill Notation):
C19H18O8
CAS Number:
Molecular Weight:
374.34
UNSPSC Code:
12352200
NACRES:
NA.25
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InChI

1S/C19H18O8/c1-23-11-6-5-9(7-10(11)20)17-19(26-4)16(22)14-12(27-17)8-13(24-2)18(25-3)15(14)21/h5-8,20-21H,1-4H3

InChI key

PJQLSMYMOKWUJG-UHFFFAOYSA-N

biological source

Vitex trifolia

assay

≥98% (HPLC)

form

powder

solubility

ethanol: 1 mg/mL, clear, colorless to light yellow

application(s)

metabolomics
vitamins, nutraceuticals, and natural products

storage temp.

2-8°C

General description

Casticin is one of the flavonoids present in the traditional Chinese medicine Inula japonica Thunb. It is a polymethyl compound with three rings, a catechol moiety at ortho position, one double bond, two hydroxyl groups, and four methoxy groups. It has been isolated from the fruits, seeds, and leaves of various Vitex species.

Application

Casticin from Vitex trifolia is used to study its mechanisms of action as an antiiflammatory and anticancer agent via processes such as TRAIL-induced apoptosis, cell cycle arrest, ROS generation, and glutathione (GSH) depletion.

Biochem/physiol Actions

Casticin has anticancer, pro-apoptotic, anti-proliferative, anti-asthmatic, and anti-angiogenic properties. In addition, it exhibits anti-inflammatory behavior by means of its inhibitory effect on lipoxygenases and T- & B-lymphocytes. Due to its oestrogenic activity, it is being used to manage Premenstrual syndrome in women. It is also reported to mitigate rheumatoid arthritis and liver fibrosis manifestations.
Tubulin-binding anticancer flavonoid. Casticin induces apoptosis in cancer cells.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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Flavonoids from the aerial parts of Inula japonica
Qin J, et al.
Chinese Journal of Natural Medicines, 8, 257-259 (2010)
Lihua He et al.
Oncology reports, 29(1), 103-108 (2012-10-16)
Casticin, a polymethoxyflavone, has been reported to exert anticancer activities. The objectives of this study were to examine the molecular mechanisms by which casticin induces the growth inhibition and cell cycle arrest in human hepatocellular carcinoma (HCC) cells. The HCC
Chiara Righeschi et al.
Cancer genomics & proteomics, 9(3), 143-151 (2012-05-18)
Natural polyphenols play an important role in tumor inhibition. We used a doxorubicin-sensitive acute T-lymphoblastic leukemia cell line (CCRF-CEM) and its multidrug-resistant subline (CEM/ADR5000) to evaluate the activity of 15 plant polyphenols isolated in our laboratory (hypericin and pseudohypericin, verbascoside
Jun Yang et al.
World journal of gastroenterology, 17(38), 4298-4307 (2011-11-18)
To investigate the apoptotic activities of casticin in hepatocellular carcinoma (HCC) cells and its molecular mechanisms. PLC/PRF/5 and Hep G2 cell lines were cultured in vitro and the inhibitory effect of casticin on the growth of cells was detected by
Khadidja Haïdara et al.
Cancer letters, 242(2), 180-190 (2006-01-03)
We studied the mechanism of anti-tumor activity of the flavonoid Casticin, derived from Achillea millefolium. Casticin anti-tumor activity results in cell growth arrest in G2/M and in apoptotic death. As a tubulin-binding agent (TBA), Casticin induces p21, which in turn

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