Vitexicarpin, a natural product isolated and purified from the fruits of Vitex trifolia L. var. simplicifolia Cham., can significantly reduce vascular inflammation, through inhibition of ROS-NF-κB pathway in vascular endothelial cells, and may become a potential leading drug in the therapy of prostate carcinoma.
Vitexicarpin/蔓荆子黄素 细胞实验
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
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
Vitexicarpin/蔓荆子黄素 动物实验
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.
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