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Chemical Structure| 479-91-4 Chemical Structure| 479-91-4

Structure of Vitexicarpin
CAS No.: 479-91-4

Chemical Structure| 479-91-4

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Casticin is a methoxyflavone compound derived from Vitex agnus-castus with antimitotic and anti-inflammatory activities. Casticin inhibits the activation of STAT3.

Synonyms: Casticin

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Product Details of Vitexicarpin

CAS No. :479-91-4
Formula : C19H18O8
M.W : 374.34
SMILES Code : O=C1C(OC)=C(C2=CC=C(OC)C(O)=C2)OC3=C1C(O)=C(OC)C(OC)=C3
Synonyms :
Casticin
MDL No. :MFCD00210481
InChI Key :PJQLSMYMOKWUJG-UHFFFAOYSA-N
Pubchem ID :5315263

Safety of Vitexicarpin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Vitexicarpin

JAK-STAT

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Human lung cancer A549 cells 20 µM 48 hours Induced DNA damage, showing smeared DNA Molecules. 2020 Jan 15;25(2):341
MC3T3-E1 cells 0, 1, 2 µM 7 and 21 days Cas had no significant effect on MC3T3-E1 cells. Int J Mol Med. 2023 May;51(5):43
Human lung cancer A549 cells 20 µM 0, 6, 12, 24, 48 hours Assess cell viability, results showed a time-dependent reduction in viable cell numbers Molecules. 2020 Jan 15;25(2):341
S18 cells 0, 1, 2, 4 µM 12 hours To evaluate the effect of Vitexicarpin on the clonogenic ability of S18 cells, results showed that Vitexicarpin significantly reduced the clonogenic activity of S18 cells Cancer Cell Int. 2019 Dec 21;19:348
Human lung cancer A549 cells 20 µM 12-48 hours Induced chromatin condensation, showing lighter DAPI staining and higher fluorescent intensity Molecules. 2020 Jan 15;25(2):341
Human lung cancer A549 cells 20 µM 24 and 48 hours Induced DNA damage, resulting in the development of comet tails Molecules. 2020 Jan 15;25(2):341
C666-1 cells 0, 2, 4, 8 µM 24 hours To evaluate the effect of Vitexicarpin on the cell cycle of C666-1 cells, results showed that Vitexicarpin caused accumulation of cells in the G2/M phase in a dose-dependent manner Cancer Cell Int. 2019 Dec 21;19:348
MC3T3-E1 pre-osteoblasts 1, 5, 10 µM 24 hours Vitex was not as highly toxic to normal cells as the known anti-osteosarcoma drug Methotrexate Int J Mol Sci. 2024 Mar 22;25(7):3582
C3H/10T1/2 mesenchymal stem cells (MSCs) 1, 5, 10 µM 24 hours Vitex was not as highly toxic to normal cells as the known anti-osteosarcoma drug Methotrexate Int J Mol Sci. 2024 Mar 22;25(7):3582
Human osteosarcoma SJSA1 cells 1, 5, 10 µM 24 hours Vitex significantly reduced the viability of SJSA1 cells to a greater extent than that of MG63 cells Int J Mol Sci. 2024 Mar 22;25(7):3582
Human osteosarcoma MG63 cells 1, 5, 10 µM 24 hours Vitex significantly reduced the viability of MG63 cells and induced apoptosis as evidenced by the appearance of cleaved-PARP, cleaved-caspase 3 Int J Mol Sci. 2024 Mar 22;25(7):3582
Human myeloma RPMI 8226 cells 5 µM 24 hours CTC significantly inhibited the survival and proliferation of RPMI 8226 cells with an IC50 value of 6 µM. Cancers (Basel). 2019 Feb 22;11(2):254
Human gastric cancer SNU16 cells 5 µM 24 hours CTC significantly inhibited the survival and proliferation of SNU16 cells with an IC50 value of 7 µM. Cancers (Basel). 2019 Feb 22;11(2):254
Human breast cancer MCF-7 cells 5 µM 24 hours CTC significantly inhibited the survival and proliferation of MCF-7 cells with an IC50 value of 8.5 µM. Cancers (Basel). 2019 Feb 22;11(2):254
BEAS-2B cells 5–20 µM 24 hours Casticin significantly reduced the levels of CCL5, MCP-1, IL-6, and IL-8 in TNF-α-stimulated BEAS-2B cells. In BEAS-2B cells stimulated with IL-4 and TNF-α, casticin significantly attenuated the levels of CCL11, CCL24, and CCL26. Front Pharmacol. 2018 Jun 14;9:635
4T1 cells 0.25 and 0.50 µM 24 hours To investigate the effects of Vitexicarpin on breast cancer cell migration and invasion, results showed that Vitexicarpin significantly inhibited the migration and invasion of 4T1 cells. Biosci Rep. 2018 Nov 30;38(6):BSR20180738
MDA-MB-231 cells 0.25 and 0.50 µM 24 hours To investigate the effects of Vitexicarpin on breast cancer cell migration and invasion, results showed that Vitexicarpin significantly inhibited the migration and invasion of MDA-MB-231 cells. Biosci Rep. 2018 Nov 30;38(6):BSR20180738
Hep G2 cells 3.0, 10.0, 30.0 µM 24 hours To investigate the inhibitory effect of Vitexicarpin on the growth of hepatocellular carcinoma cells, results showed that Vitexicarpin significantly inhibited the growth of Hep G2 cells with an IC50 of 13.6 μmol/L World J Gastroenterol. 2011 Oct 14;17(38):4298-307
PLC/PRF/5 cells 3.0, 10.0, 30.0 µM 24 hours To investigate the inhibitory effect of Vitexicarpin on the growth of hepatocellular carcinoma cells, results showed that Vitexicarpin significantly inhibited the growth of PLC/PRF/5 cells with an IC50 of 9.4 μmol/L World J Gastroenterol. 2011 Oct 14;17(38):4298-307
A375.S2 human melanoma cells 100-200 nM 24 hours To investigate the effect of Vitexicarpin on the migration and invasion of A375.S2 cells, results showed that Vitexicarpin significantly inhibited cell migration and invasion, and reduced the expression of MMP-2 and MMP-1. Molecules. 2016 Mar 19;21(3):384
NPC cell lines 5-8F 0, 1, 2, 4, 8 µM 24, 48, 72 hours To evaluate the effect of Vitexicarpin on the growth of NPC cells, results showed that Vitexicarpin decreased the viability of NPC cell lines in a concentration-dependent manner Cancer Cell Int. 2019 Dec 21;19:348
293T cells 0, 0.1, 0.5, 1, 4, 7, 10 µM 24, 48, 72 hours Evaluate cell viability, results showed that casticin did not significantly inhibit 293T cell viability. Cancer Cell Int. 2017 Jan 5;17:9
SGC996 cells 0, 0.1, 0.5, 1, 4, 7, 10 µM 24, 48, 72 hours Evaluate cell viability, results showed that casticin significantly inhibited gallbladder cancer cell proliferation in a dose- and time-dependent manner. Cancer Cell Int. 2017 Jan 5;17:9
NOZ cells 0, 0.1, 0.5, 1, 4, 7, 10 µM 24, 48, 72 hours Evaluate cell viability, results showed that casticin significantly inhibited gallbladder cancer cell proliferation in a dose- and time-dependent manner. Cancer Cell Int. 2017 Jan 5;17:9
Rat pituitary cells 0.01, 0.1, 1, 10 µM 48 hours To investigate the effects of Vitexicarpin on E2-stimulated pituitary cell proliferation and prolactin release. Results showed that Vitexicarpin significantly inhibited E2-induced pituitary cell proliferation and prolactin release. Acta Pharmacol Sin. 2010 Dec;31(12):1564-8
Human lung cancer A549 cells 0, 10, 20, 30, 40, 50 µM 48 hours Assess cell viability, results showed a concentration-dependent reduction in viable cell numbers Molecules. 2020 Jan 15;25(2):341
MCF-7 cells 25.8 µM 48 hours Evaluated antiproliferative potential, results showed IC50 value of FLV2 against MCF-7 cells was 25.8 μM Saudi Pharm J. 2022 Sep;30(9):1301-1314
HepG2 cells 23.9 µM 48 hours Evaluated antiproliferative potential, results showed IC50 value of FLV2 against HepG2 cells was 23.9 μM Saudi Pharm J. 2022 Sep;30(9):1301-1314
Bone marrow-derived macrophages (BMMs) 0, 0.5, 1, 1.5, 2 µM 5-7 days Cas inhibited RANKL-induced osteoclast differentiation in a concentration-dependent manner, with particularly pronounced effects at 2 µM. Int J Mol Med. 2023 May;51(5):43
MCF-7 cells 3.1 µM 6 days To evaluate the estrogen-like activity of Vitexicarpin on MCF-7 cells. Results showed that Vitexicarpin significantly increased MCF-7 cell proliferation at low concentrations, and this effect was completely attenuated by the ER antagonist ICI 182,780. Biomolecules. 2021 Jul 16;11(7):1033

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Balb/c mice Breast cancer lung metastasis model Intraperitoneal injection 10 mg/kg Once every 2 days for 4 weeks To investigate the effects of Vitexicarpin on breast cancer cell lung metastasis, results showed that Vitexicarpin significantly reduced the number of lung metastatic nodules. Biosci Rep. 2018 Nov 30;38(6):BSR20180738
Nude mice NOZ cell xenograft model Intraperitoneal injection 10, 20 mg/kg Every 2 days for 25 days Evaluate the anti-tumor effect of casticin in vivo, results showed that casticin inhibited tumor growth in a dose-dependent manner. Cancer Cell Int. 2017 Jan 5;17:9
Sprague Dawley (SD) rats Metoclopramide dihydrochloride-induced hyperprolactinemia (MIHP) model Intraperitoneal injection 10, 20, 40 mg/kg Once daily for 7 days To investigate the effects of Vitexicarpin on serum prolactin levels in hyperprolactinemic rats. Results showed that Vitexicarpin significantly reduced serum prolactin levels. Acta Pharmacol Sin. 2010 Dec;31(12):1564-8
Wistar rats Chronic obstructive pulmonary disease model Subcutaneous injection 10, 20, and 30 mg/kg Twice daily for 12 weeks CST significantly improved lung function, reduced white blood cells, neutrophils, and macrophages in BALF, restored plasma leptin and C-reactive protein levels, and inhibited the NF-?B and iNOS pathway. Drug Des Devel Ther. 2020 Nov 17;14:5019-5027
C57BL/6 female mice Ovariectomy (OVX)-induced osteoporosis model Intraperitoneal injection 2.5 mg/kg and 5 mg/kg Once every 2 days for 42 consecutive days Cas significantly reduced bone loss and osteoclast activity in ovariectomized mice by inhibiting the AKT/ERK and NF-κB signaling pathways. Int J Mol Med. 2023 May;51(5):43
Nude mice Xenograft mouse model Intraperitoneal injection 40 mg/kg Once daily for 12 days To evaluate the inhibitory effect of Vitexicarpin on tumour growth in vivo, results showed that Vitexicarpin significantly inhibited tumour growth Cancer Cell Int. 2019 Dec 21;19:348
Female BALB/c mice OVA-induced asthma model Intraperitoneal injection 5 or 10 mg/kg Administered 1 h before OVA challenge or methacholine inhalation, continued until the end of the experiment Casticin significantly reduced airway hyper-responsiveness (AHR), goblet cell hyperplasia, and oxidative responses in the lungs of asthmatic mice. Mechanistic studies revealed that casticin attenuated the levels of Th2 cytokine in bronchoalveolar lavage fluids and regulated the expression of Th2 cytokine and chemokine genes in the lung. Casticin also significantly regulated oxidative stress and reduced inflammation in the lungs of mice with asthma. Front Pharmacol. 2018 Jun 14;9:635

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.67mL

0.53mL

0.27mL

13.36mL

2.67mL

1.34mL

26.71mL

5.34mL

2.67mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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